IP Library › Granted Patent US 9,827,238
Granted Patent B2
US 9,827,238 · App. 15/209,205 · Granted Nov 28, 2017

Drug treatment of overactive bladder

Inventor: Michael E. DiSanto (Burlington, NJ)
Assignee: Blebbicorp, LLC
A61K31/4745A45C5/03A45C5/14A45C9/00A61K45/06H03L1/026H04B1/16
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Quick Facts
Patent No.
US 9,827,238
App. No.
15/209,205
Granted
Nov 28, 2017
Kind
B2
Abstract

Provided are methods of treating an overactive bladder in a patient which include: administering a Myosin II ATPase inhibitor compound; or administering an X group and Y group substituted (3a-hydroxy-1-phenyl-1,2,3,3a-tetrahydro-4H-pyrollo[2,3b] quinolin-4-one) compound of Formula 1 or administering an X group and Y group substituted (3a-hydroxy-1-phenyl-1,2,3,3a-tetrahydro-4H-pyrollo[2,3b] quinolin-4-one) compound of Formula II; or administering pharmaceutically-acceptable salts, racemic mixtures, enantiomers, or prodrugs of said compounds, useful in their active form as inhibitors of Myosin II ATPase related to over-active bladder. Optionally the compounds are administered intervesicularly into the bladder. Also provided are pharmaceutical compositions comprising said compounds useful in their active form, as methods of treating a patient suffering from an over-active bladder related to inhibition of Myosin II ATPase. These pharmaceutical compositions also may contain one or more other compounds useful in their active form, as methods of treating a patient suffering from an over-active bladder.

Claims (105)

1. A Myosin II ATPase inhibitor compound of Formula (I) or a pharmaceutically-acceptable salt, a racemic mixture, or an enantiomer thereof, comprising:

wherein an X is selected from the group consisting of hydrogen, hydroxy, fluoro, chloro, bromo, iodo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, methoxy, methyl, nitro, (C 1-6 )alkoxy, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, acetoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetamido, carb(C 1-6 )alkoxy, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, cyclopropyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, acetonyl, phenyl, benzyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the X is optionally substituted at a carbon atom with a substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, thio, (C 1-6 )alkoxy, methylthio, thiomethyl, C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, carbamyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, amino, methylamino, acetonyl, aminomethyl, amino (C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, (C 4-10 )aryl, acetoxy, phenyl, napthyl, (C 1-6 )alkylamino(C 1-6 )alkyl, benzyl, (C 1-6 )alkylaminoketo, carb(C 1-6 )alkoxy, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, acetamido, and (C 4-8 )heteroaryl, and

wherein the X is optionally substituted at a primary nitrogen atom or at a secondary nitrogen atom with a substituent Q selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, phenyl, benzyl, napthyl, (C 4-7 )cycloalkenyl, (C 4-8 )heterocyclic, (C 4-10 )aryl, (C 4-10 )haloaryl, and (C 4-8 )heteroaryl; and

wherein a Y is selected from the group consisting of fluoro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, methoxy, methythio, (C 1-6 )alkoxy, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, fluoromethyl, iodo, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, acetamido, (C 1-6 )alkylaminoketo, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the Y is optionally substituted at a carbon atom with a substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, (C 1-6 ) alkoxy, methylthio, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, carbamyl, fluoromethyl, amino, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino [(C 1-6 )alkyl] 2 , acetoxy, (C 1-6 )alkylamino, carb(C 1-6 )alkoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetonyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, phenyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, napthyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, acetamido, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, benzyl, and (C 4-8 )heteroaryl, and

wherein the Y is optionally substituted at a primary nitrogen atom or at a secondary nitrogen atom with a substituent T selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, phenyl, napthyl, (C 4-7 )cycloalkenyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, (C 4-8 )heteroaryl, and benzyl.

2. The compound of Formula (I) according to claim 1 ,

wherein the X is selected from the group consisting of hydrogen, fluoro, chloro, bromo, iodo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, methyl, nitro, (C 1-6 )alkoxy, carbamyl, chloromethyl, fluoromethyl, (C 1-6 )haloalkyl, amino, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, acetoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, acetonyl, phenyl, benzyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein the Y is selected from the group consisting of fluoro, bromo, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, acetamido, (C 1-6 )alkylaminoketo, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl.

3. The compound of Formula (I) according to claim 1 ,

wherein the X is selected from the group consisting of hydrogen, (C 1-6 )alkyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, (C 4-10 )aryl, and (C 4-8 )heteroaryl,

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, carboxy, carbethoxy, acetyl, and (C 1-6 )alkyl, and

wherein the X is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent Q selected from the group consisting of (C 1-6 )alkyl, cyclopropyl, phenyl, and benzyl; and

wherein the Y is selected from the group consisting of fluoro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, amino(C 1-6 )alkyl, (C 1-6 )alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, acetoxy, carb(C 1-6 )alkoxy, acetonyl, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the Y is optionally substituted at the carbon atom with the substituent Z selected from the group consisting of hydroxy, fluoro, chloro, bromo, iodo, nitro, carboxy, carbethoxy, acetyl, and (C 1-6 )alkyl, and

wherein the Y is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent T selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl.

4. The compound of Formula (I) according to claim 1 ,

wherein the X is selected from the group consisting of hydrogen, (C 1-6 )alkyl, and amino,

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of hydroxy, fluoro, chloro, and bromo, and

wherein the X is optionally substituted at the primary nitrogen atom with the substituent Q selected from the group consisting of methyl, (C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-10 )aryl, and (C 4-8 )heterocyclic; and

wherein the Y is selected from the group consisting of fluoro, bromo, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl, and

wherein the Y is optionally substituted at the carbon atom with the substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 1-6 ) alkoxy, methylthio, thio, thiomethyl, (C 1-6 )alkylthio, chloromethyl, trifluoromethyl, (C 3-7 )cycloalkyl, and (C 4-8 )heterocyclic.

5. The compound of Formula (I) according to claim 1 ,

wherein the X is selected from the group consisting of hydrogen, (C 1-6 )alkyl, (C 1-6 )alkoxy, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, phenyl, benzyl, and napthyl, and

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, carboxy, amino, amino(C 1-6 )alkyl, (C 1-6 )alkylamino, phenyl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein the Y is selected from the group consisting of fluoro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, fluoromethyl, iodo, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, acetamido, (C 1-6 )alkylaminoketo, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the Y is optionally substituted at the carbon atom with the substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, (C 1-6 ) alkoxy, methylthio, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, carbamyl, fluoromethyl, amino, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , acetoxy, (C 1-6 )alkylamino, carb(C 1-6 )alkoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetonyl, phenyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, napthyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, and acetamido, and

wherein the Y is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent T selected from the group consisting of (C 1-6 )alkyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, phenyl, napthyl, (C 4-10 )aryl, and (C 4-10 )haloaryl.

6. The compound of Formula (I) according to claim 1 ,

wherein the X is selected from the group consisting of hydrogen, (C 1-6 )alkyl, methoxy, nitro, (C 1-6 )haloalkyl, amino(C 1-6 )alkyl, and (C 1-6 )alkylamino,

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of (C 1-6 )haloalkoxy, acetonyl, amino(C 1-6 )alkyl, (C 1-6 )alkylamino, (C 4-10 )aryl, acetoxy, (C 3-7 )cycloalkyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and acetamido, and

wherein the X is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent Q selected from the group consisting of (C 1-6 )alkyl, cyclopropyl, and (C 4-8 )heterocyclic; and

wherein the Y is selected from the group consisting of fluoro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-10 )aryl, napthyl, and (C 4-8 )heteroaryl,

wherein the Y is optionally substituted at the carbon atom with the substituent Z selected from the group consisting of (C 3-7 )cycloalkyl, and benzyl, and

wherein the Y is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with a substituent T selected from the group consisting of (C 1-6 )alkyl, cyclopropyl, (C 3-7 )cycloalkyl, and (C 4-8 )heterocyclic.

7. The compound of Formula (I) according to claim 1 ,

wherein the X is selected from the group consisting of hydrogen, carboxy, acetyl, (C 1-6 )alkyl, methyl, amino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, cyclopropyl, (C 3-7 )cycloalkyl, phenyl, benzyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, and amino; and

wherein the Y is selected from the group consisting of fluoro, bromo, (C 2-6 )alkyl, trifluoromethyl, cyclopropyl, (C 3-7 )cycloalkyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the Y is optionally substituted at the carbon atom with the substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, nitro, and carboxy, and

wherein the Y is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent T selected from the group consisting of (C 1-6 )alkyl, cyclopropyl, (C 4-8 )heterocyclic, (C 4-8 )heteroaryl, and benzyl.

8. A Myosin II ATPase inhibitor compound of Formula (I) or a pharmaceutically-acceptable salt, a racemic mixture, or an enantiomer thereof, comprising:

wherein an X is selected from the group consisting of fluoro, chloro, iodo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, acetoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetamido, carb(C 1-6 )alkoxy, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, cyclopropyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, acetonyl, phenyl, benzyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the X is optionally substituted at a carbon atom with a substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, methoxy, chloromethyl, carbamyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, amino, methylamino, acetonyl, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, (C 4-10 )aryl, acetoxy, phenyl, napthyl, (C 1-6 )alkylamino(C 1-6 )alkyl, benzyl, (C 1-6 )alkylaminoketo, carb(C 1-6 )alkoxy, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, acetamido, and (C 4-8 )heteroaryl, and

wherein the X is optionally substituted at a primary nitrogen atom or at a secondary nitrogen atom with a substituent Q selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, phenyl, benzyl, napthyl, (C 4-8 )heterocyclic, (C 4-10 )aryl, (C 4-10 )haloaryl, and (C 4-8 )heteroaryl; and

wherein a Y is selected from the group consisting of hydrogen, hydroxy, fluoro, chloro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, fluoromethyl, iodo, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, acetamido, (C 1-6 )alkylaminoketo, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, nitro, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the Y is optionally substituted at a carbon atom with a substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, (C 1-6 ) alkoxy, methylthio, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, carbamyl, fluoromethyl, amino, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , acetoxy, (C 1-6 )alkylamino, carb(C 1-6 )alkoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetonyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, phenyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, napthyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, acetamido, (C 3-7 )cycloalkyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, benzyl, and (C 4-8 )heteroaryl, and

wherein the Y is optionally substituted at a primary nitrogen atom or at a secondary nitrogen atom with a substituent T selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, phenyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, (C 4-8 )heteroaryl, and benzyl.

9. The compound of Formula (I) according to claim 8 ,

wherein the X is selected from the group consisting of fluoro, chloro, iodo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, acetoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetamido, carb(C 1-6 )alkoxy, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, cyclopropyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, acetonyl, and phenyl, and

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, methoxy, chloromethyl, carbamyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carb(C 1-6 )alkoxy, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, acetamido, and (C 4-8 )heteroaryl; and

wherein a Y is selected from the group consisting of hydrogen, hydroxy, fluoro, chloro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, fluoromethyl, iodo, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, acetamido, (C 1-6 )alkylaminoketo, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, nitro, (C 3-7 )cycloalkyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the Y is optionally substituted at a carbon atom with the substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, (C 1-6 ) alkoxy, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carb(C 1-6 )alkoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, acetonyl, phenyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, napthyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 ) alkoxy(C 1-6 )alkyl, acetamido, (C 3-7 )cycloalkyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, benzyl, and (C 4-8 )heteroaryl, and

wherein the Y is optionally substituted at a primary nitrogen atom or at a secondary nitrogen atom with a substituent T selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, phenyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, (C 4-8 )heteroaryl, and benzyl.

10. The compound of Formula (I) according to claim 8 ,

wherein an X is selected from the group consisting of (C 2-6 )alkyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, (C 1-6 )alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, cyclopropyl, phenyl, benzyl, (C 3-7 )cycloalkyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, (C 4-10 )aryl, acetoxy, phenyl, napthyl, benzyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, acetamido, and (C 4-8 )heteroaryl, and

wherein the X is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent Q selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 1-6 )haloalkyl; and

wherein the Y is selected from the group consisting of hydrogen, hydroxy, fluoro, chloro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, fluoromethyl, iodo, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, (C 1-6 )alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, acetamido, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, and nitro,

wherein the Y is optionally substituted at the carbon atom with the substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, (C 1-6 ) alkoxy, methylthio, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, phenyl, (C 3-7 )cycloalkyl, (C 4-10 )aryl, benzyl, and (C 4-8 )heteroaryl, and

wherein the Y is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with a substituent T selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 3-7 )cycloalkyl, phenyl, napthyl, (C 4-10 )aryl, and benzyl.

11. The compound of Formula (I) according to claim 8 ,

wherein the X is selected from the group consisting of fluoro, chloro, iodo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, and (C 1-6 )haloalkyl; and

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, chloromethyl, carbamyl, fluoromethyl, and trifluoromethyl; and

wherein the Y is selected from the group consisting of hydrogen, (C 1-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, (C 1-6 )haloalkyl, methylamino, aminomethyl, amino(C 1-6 )alkyl, (C 1-6 )alkylamino, cyclopropyl, nitro, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein the Y is optionally substituted at the carbon atom with the substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, nitro, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, (C 1-6 ) alkoxy, methylthio, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, aminomethyl, amino(C 1-6 )alkyl, acetoxy, (C 1-6 )alkylamino, carb(C 1-6 )alkoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetonyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, phenyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, napthyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, and acetamido; and

wherein the Y is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent T selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 3-7 )cycloalkyl, phenyl, napthyl, (C 4-10 )aryl, (C 4-8 )heterocyclic, and benzyl.

12. The compound of Formula (I) according to claim 8 ,

wherein the X is selected from the group consisting of fluoro, chloro, (C 2-6 )alkyl, chloromethyl, fluoromethyl, trifluoromethyl, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, acetoxy, acetamido, cyclopropyl, phenyl, benzyl, (C 3-7 )cycloalkyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein the Y is selected from the group consisting of hydrogen, hydroxy, fluoro, chloro, bromo, cyano, carboxy, acetyl, (C 1-6 )alkyl, methoxy, cyclopropyl, (C 1-6 )alkanoyl, nitro, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, C 4-8 )heterocyclic, and (C 4-8 )heteroaryl.

13. The compound of Formula (I) according to claim 8 ,

wherein the X is selected from the group consisting of fluoro, chloro, iodo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, acetonyl, phenyl, benzyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, phenyl, napthyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein the Y is selected from the group consisting of hydrogen, hydroxy, fluoro, chloro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, nitro, (C 3-7 )cycloalkyl, phenyl, (C 4-0 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein the Y is optionally substituted at the carbon atom with the substituent Z selected from the group consisting of hydroxy, fluoro, chloro, bromo, iodo, carboxy, methylthio, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, amino, (C 1-6 )haloalkyl, phenyl, napthyl, (C 4-10 )aryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein the Y is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent T selected from the group consisting of (C 1-6 )alkyl, cyclopropyl, and (C 3-7 )cycloalkyl.

14. The compound of Formula (I) according to claim 8 ,

wherein an X is selected from the group consisting of fluoro, carboxy, (C 2-6 )alkyl, fluoromethyl, amino(C 1-6 )alkyl, cyclopropyl, (C 3-7 )cycloalkyl, (C 4-10 )aryl, and (C 4-8 )heteroaryl,

wherein the X is optionally substituted at the carbon atom with the substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, and (C 1-6 )alkyl, and

wherein the X is optionally substituted at the primary nitrogen atom or at the secondary nitrogen atom with the substituent Q selected from the group consisting of (C 1-6 )alkyl, and (C 3-7 )cycloalkyl; and

wherein a Y is selected from the group consisting of hydrogen, hydroxy, fluoro, chloro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, methoxy, (C 1-6 )haloalkyl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl, and

wherein the Y is optionally substituted at a carbon atom with a substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, and bromo.

15. A Myosin II ATPase inhibitor compound of Formula (I) or a pharmaceutically-acceptable salt, a racemic mixture, or an enantiomer thereof, comprising:

wherein an X is selected from the group consisting of hydroxy, fluoro, chloro, bromo, iodo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, methoxy, methyl, nitro, (C 1-6 )alkoxy, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, acetoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetamido, carb(C 1-6 )alkoxy, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, cyclopropyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, acetonyl, phenyl, benzyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the X is optionally substituted at a carbon atom with a substituent W selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, methoxy, thio, (C 1-6 )alkoxy, methylthio, thiomethyl, C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, carbamyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, amino, amino(C 1-6 )alkyl, (C 4-10 )aryl, acetoxy, phenyl, napthyl, (C 1-6 )alkylamino(C 1-6 )alkyl, benzyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 3-7 )cycloalkyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, acetamido, and (C 4-8 )heteroaryl, and

wherein the X is optionally substituted at a primary nitrogen atom or at a secondary nitrogen atom with a substituent Q selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, phenyl, benzyl, napthyl, (C 4-8 )heterocyclic, (C 4-10 )aryl, (C 4-10 )haloaryl, and (C 4-8 )heteroaryl; and

wherein a Y is selected from the group consisting of hydroxy, fluoro, chloro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, fluoromethyl, iodo, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, acetamido, (C 1-6 )alkylaminoketo, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, nitro, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl,

wherein the Y is optionally substituted at a carbon atom with a substituent Z selected from the group consisting of methyl, hydroxy, fluoro, chloro, bromo, iodo, nitro, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, methoxy, (C 1-6 ) alkoxy, methylthio, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, carbamyl, fluoromethyl, amino, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , acetoxy, (C 1-6 )alkylamino, carb(C 1-6 )alkoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetonyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, phenyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, napthyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, acetamido, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, benzyl, and (C 4-8 )heteroaryl, and

wherein the Y is optionally substituted at a primary nitrogen atom or at a secondary nitrogen atom with a substituent T selected from the group consisting of methyl, (C 1-6 )alkyl, cyclopropyl, (C 1-6 )haloalkyl, (C 3-7 )cycloalkyl, phenyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, (C 4-8 )heteroaryl, and benzyl.

16. The compound of Formula (I) according to claim 15 ,

wherein an X is selected from the group consisting of hydroxy, fluoro, chloro, bromo, iodo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, methoxy, methyl, nitro, (C 1-6 )alkoxy, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, acetoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetamido, carb(C 1-6 )alkoxy, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, cyclopropyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, acetonyl, phenyl, benzyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein a Y is selected from the group consisting of hydroxy, fluoro, chloro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, methoxy, methythio, (C 1-6 )alkoxy, thio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, chloromethyl, fluoromethyl, iodo, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 ) alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, nitro, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl.

17. The compound of Formula (I) according to claim 15 ,

wherein an X is selected from the group consisting of hydroxy, fluoro, chloro, bromo, iodo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, methoxy, methyl, nitro, (C 1-6 )alkoxy, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, methylamino, amino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, acetoxy, (C 1-6 )alkylamino(C 1-6 )alkyl, acetamido, carb(C 1-6 )alkoxy, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, cyclopropyl, (C 1-6 )hydroxyalkyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, acetonyl, phenyl, benzyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, and (C 1-6 )alkoxy(C 1-6 )alkyl; and

wherein a Y is selected from the group consisting of fluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, (C 1-6 )alkylaminoketo, acetoxy, carb(C 1-6 )alkoxy, cyclopropyl, (C 1-6 )alkyl-C(═O)—O—(C 1-6 )alkyl, (C 1-6 )alkyl-O—C(═O)—(C 1-6 )alkyl, (C 1-6 )hydroxyalkyl, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, nitro, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl.

18. The compound of Formula (I) according to claim 15 ,

wherein an X is selected from the group consisting of hydroxy, fluoro, chloro, bromo, iodo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, (C 2-6 )alkenyl, (C 2-6 )alkynl, methoxy, methyl, nitro, (C 1-6 )alkoxy, thio, methylthio, thiomethyl, (C 1-6 )alkylthio, thio(C 1-6 )alkyl, carbamyl, chloromethyl, fluoromethyl, trifluoromethyl, (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, acetoxy, carb(C 1-6 )alkoxy, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, and napthyl; and

wherein a Y is selected from the group consisting of (C 1-6 )haloalkyl, (C 1-6 )haloalkoxy, carbamyl, amino, methylamino, aminomethyl, amino(C 1-6 )alkyl, amino[(C 1-6 )alkyl] 2 , (C 1-6 )alkylamino, (C 1-6 )alkylamino(C 1-6 )alkyl, carb(C 1-6 )alkoxy, acetonyl, (C 1-6 )alkylcarboxy, (C 1-6 )alkanoyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, nitro, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl.

19. The compound of Formula (I) according to claim 15 ,

wherein an X is selected from the group consisting of hydroxy, fluoro, chloro, bromo, iodo, cyano, carboxy, carbethoxy, acetyl, (C 1-6 )alkyl, phenyl, benzyl, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, napthyl, (C 4-10 )aryl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl; and

wherein a Y is selected from the group consisting of hydroxy, fluoro, chloro, bromo, cyano, carboxy, carbethoxy, acetyl, (C 2-6 )alkyl, methoxy, (C 1-6 )alkyl-keto-(C 1-6 )alkyl, (C 1-6 )alkoxy(C 1-6 )alkyl, nitro, (C 3-7 )cycloalkyl, (C 4-7 )cycloalkenyl, phenyl, (C 4-10 )aryl, napthyl, benzyl, (C 4-10 )haloaryl, (C 4-8 )heterocyclic, and (C 4-8 )heteroaryl.

20. The compound of Formula (I) according to claim 15 ,

wherein an X is selected from the group consisting of fluoro, bromo, (C 1-6 )alkyl, phenyl, benzyl, (C 3-7 )cycloalkyl, (C 4-10 )aryl, (C 4-10 )haloaryl, and (C 4-8 )heterocyclic; and

wherein a Y is selected from the group consisting of hydroxy, fluoro, bromo, cyano, carboxy, nitro, (C 3-7 )cycloalkyl, (C 4-10 )aryl, napthyl, benzyl, and (C 4-8 )heteroaryl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 12, 2016
From: DISANTO, MICHAEL E., MR.
To: BLEBBICORP, LLC
Reel/Frame 039697/0443 →
Continuity (2)
Continuation 14118448 · Jan 27, 2014
Related Publication 20170020861A1 · Jan 26, 2017