IP Library › Patent Application 18717086

Patent Application

App. No. 18/717,086

COMPOUNDS FOR THE TREATMENT OF CANCER

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App. No.: 18/717,086

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Abstract

The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, useful for the treatment of cancer. The present disclosure also relates to pharmaceutical composition of the novel compound and method of treating benign or malignant disease of the breast or reproductive tract, prostate cancer, or endometrial cancer using the same.

Claims (652)

1 . A compound of formula (I)

wherein;

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

Z is selected from ═O, ═N—OH, —O-alkyl, —O-haloalkyl, —NH—OH or —O-alkyl-OH wherein the bond between the Z substituent attached to carbon can be single or double bond depend on the substituent selected;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

wherein R 3 is selected from NH 2 , NHR 4 , or NR 5 R 6 ; R 4 is selected from group comprising optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; R 5 and R 6 are selected independently from group comprising optionally substituted alkyl, aryl, heteroaryl, heterocycloalkyl, cycloalkyl; or R 5 and R 6 are taken together along with the nitrogen to which they are attached to form a three to seven membered heterocyclic ring and may optionally be substituted at a substitutable position with one or more R 7 radicals, wherein the one or more R 7 radicals are independently selected at each occurrence from the group consisting of optionally substituted alkyl, alkylcarbonyl, formyl, halo, haloalkyl, alkylphosphate, phosphate, oxo, cyano, nitro, amino, hydroxyalkylamino, alkoxy, alkoxycarbonyl, carboxyalkyl, hydroxyalkyl, alkenyl, alkynyl, alkylthio, cycloalkyl, aryl, heteroaryl, aralkyl, heterocycloalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, alkoxyalkyl;

ii)

wherein R 8 is selected from group comprising optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl; or —CR 9 R 10 ; where R 9 and R 10 are taken together along with the carbon to which they are attached to form a three to seven membered saturated, partially unsaturated or unsaturated heterocyclic ring in which up to 4 carbon atoms are replaced by heteroatoms chosen from the group consisting of O, S or N and may optionally be substituted at a substitutable position with one or more R 11 radicals, wherein one or more R 11 radicals are independently selected at each occurrence from the group consisting of optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylcarbonyl, formyl, halo, alkylphosphate, phosphate, cyano, nitro, alkoxy, amino, alkoxycarbonyl, alkenyl, alkynyl, alkylthio arylcarbonyl;

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

wherein R 17 is selected from optionally substituted bicyclic compounds, spirocyclic compounds or bridged bicyclic compounds; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

2 . A compound of formula (I-A)

wherein;

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

Z is selected from ═O, ═N—OH, —O-alkyl, O-haloalkyl, —NH—OH or —O-alkyl-OH wherein the bond between the Z substituent attached to carbon can be single or double bond depend on the substituent selected;

pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

3 . The compound according to claim 1 comprising the compound (II) represented by following formulae:

wherein;

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

4 . The compound according to claim 1 comprising the compound (III) represented by following formulae:

wherein X and A has the same meaning as given in compound of formula (II); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

5 . The compound according to claim 1 comprising the compound (IV) represented by following formulae:

wherein Y and A has the same meaning as given in compound of formula (II); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

6 . The compound according to claim 1 comprising the compound (V) represented by following formulae:

wherein;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

7 . The compound according to claim 1 comprising the compound (VI) represented by following formulae:

wherein;

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

8 . The compound according to claim 1 comprising the compound (VII) represented by following formulae:

wherein X and A has the same meaning as given in compound of formula (VI); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

9 . The compound according to claim 1 comprising the compound (VIII) represented by following formulae:

wherein Y and A has the same meaning as given in compound of formula (VI); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

10 . The compound according to claim 1 comprising the compound (IX) represented by following formulae:

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 3 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

11 . The compound according to claim 1 comprising the compound (X) represented by following formulae:

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 3 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

12 . The compound according to claim 1 comprising the compound (XI) represented by following formulae:

wherein X and A has the same meaning as given in compound of formula (X); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

13 . The compound according to claim 1 comprising the compound (XII) represented by following formulae:

wherein Y and A has the same meaning as given in compound of formula (X); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

14 . The compound according to claim 1 comprising the compound (XIII) represented by following formulae:

wherein;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

wherein R 8 is selected from group comprising optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl; or —CR 9 R 10 ; where R 9 and R 10 are taken together along with the carbon to which they are attached to form a three to seven membered saturated, partially unsaturated or unsaturated heterocyclic ring in which up to 4 carbon atoms are replaced by heteroatoms chosen from the group consisting of O, S or N and may optionally be substituted at a substitutable position with one or more Ru radicals, wherein one or more Ru radicals are independently selected at each occurrence from the group consisting of optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylcarbonyl, formyl, halo, alkylphosphate, phosphate, cyano, nitro, alkoxy, amino, alkoxycarbonyl, alkenyl, alkynyl, alkylthio arylcarbonyl;

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

15 . The compound according to claim 1 comprising the compound (XIV) represented by following formulae:

wherein;

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

16 . The compound according to claim 1 comprising the compound (XV) represented by following formulae:

wherein X and A has the same meaning as given in compound of formula (XIV); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

17 . The compound according to claim 1 comprising the compound (XVI) represented by following formulae:

wherein Y and A has the same meaning as given in compound of formula (XIV); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

18 . The compound according to claim 1 comprising the compound (XVII) represented by following formulae:

wherein;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

wherein R 8 is selected from group comprising optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl; or —CR 9 R 10 ; where R 9 and R 10 are taken together along with the carbon to which they are attached to form a three to seven membered saturated, partially unsaturated or unsaturated heterocyclic ring in which up to 4 carbon atoms are replaced by heteroatoms chosen from the group consisting of O, S or N and may optionally be substituted at a substitutable position with one or more Ru radicals, wherein one or more Ru radicals are independently selected at each occurrence from the group consisting of optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylcarbonyl, formyl, halo, alkylphosphate, phosphate, cyano, nitro, alkoxy, amino, alkoxycarbonyl, alkenyl, alkynyl, alkylthio arylcarbonyl;

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

19 . The compound according to claim 1 comprising the compound (XVIII) represented by following formulae:

wherein;

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 3 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

20 . The compound according to claim 1 comprising the compound (XIX) represented by following formulae:

wherein X and A has the same meaning as given in compound of formula (XVIII); pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

21 . The compound according to claim 1 comprising the compound (XX) represented by following formulae:

wherein Y and A has the same meaning as given in compound of formula XVIII; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

22 . The compound according to claim 1 comprising the compound (XXI) represented by following formulae:

wherein;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

23 . The compound according to claim 1 comprising the compound (XXII) represented by following formulae:

wherein;

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

24 . The compound according to claim 1 comprising the compound (XXIII) represented by following formulae:

wherein X and A has the same meaning as given in compound of formula XXII; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

25 . The compound according to claim 1 comprising the compound (XXIV) represented by following formulae:

wherein Y and A has the same meaning as given in compound of formula XXII; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

26 . The compound according to claim 1 comprising the compound (XXV) represented by following formulae:

wherein;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

wherein R 8 is selected from group comprising optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl; or —CR 9 R 10 ; where R 9 and R 10 are taken together along with the carbon to which they are attached to form a three to seven membered saturated, partially unsaturated or unsaturated heterocyclic ring in which up to 4 carbon atoms are replaced by heteroatoms chosen from the group consisting of O, S or N and may optionally be substituted at a substitutable position with one or more R 1 radicals, wherein one or more R 1 radicals are independently selected at each occurrence from the group consisting of optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylcarbonyl, formyl, halo, alkylphosphate, phosphate, cyano, nitro, alkoxy, amino, alkoxycarbonyl, alkenyl, alkynyl, alkylthio arylcarbonyl;

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 5 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

27 . The compound according to claim 1 comprising the compound (XXVI) represented by following formulae:

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

a is selected from carbon or nitrogen;

Q is selected from group consisting of optionally substituted alkyl, alkylcarbonyl, formyl, halo, haloalkyl, alkylphosphate, phosphate, oxo, cyano, nitro, amino, alkoxy, alkoxycarbonyl, carboxyalkyl, hydroxyalkyl, alkenyl, alkynyl, alkylthio, cycloalkyl, aryl, heteroaryl, aralkyl, heterocycloalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, alkoxyalkyl;

pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

28 . The compound according to claim 1 comprising the compound (XXVII) represented by following formulae:

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

wherein R 5 and R 6 are taken together along with the nitrogen to which they are attached to form a three to seven membered saturated, partially unsaturated or unsaturated heterocyclic ring and substituted at a substitutable position with one or more R 7 radicals, wherein the one or more R 7 radicals are independently selected at each occurrence from the group consisting of substituted alkyl, alkylcarbonyl, formyl, halo, haloalkyl, alkylphosphate, phosphate, phosphonyl, oxo, cyano, nitro, amino, alkoxy, alkoxycarbonyl, carboxyalkyl, hydroxyalkyl, alkenyl, alkynyl, alkylthio, cycloalkyl, aryl, heteroaryl, aralkyl, heterocycloalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, alkoxyalkyl and; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof. In one embodiment, one or more substitution on radical R 7 is further substituted with one or more substitution selected from group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, amino, alkylamino, acyl, acyloxy, acylamino, aminocarbonyl, alkoxycarbonyl, alkoxyalkyloxy, alkoxycarbonyloxy, carbamate, sulfinyl, sulfonyl, alkoxy, sulfanyl, halogen, carboxy, trihalomethyl, cyano, hydroxy, mercapto, nitro, phosphate, alkylphosphate; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

29 . The compound according to claim 1 comprising the compound (XVIII) represented by following formulae:

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

S is selected from O, C, or N; and

wherein R 7 is selected from group consisting of optionally substituted alkyl, alkylcarbonyl, formyl, halo, haloalkyl, alkylphosphate, phosphate, oxo, cyano, nitro, amino, alkoxy, alkoxycarbonyl, carboxyalkyl, hydroxyalkyl, alkenyl, alkynyl, alkylthio, cycloalkyl, aryl, heteroaryl, aralkyl, heterocycloalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, alkoxyalkyl;

pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

30 . The compound according to claim 1 comprising the compound (XXIX) represented by following formulae:

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

R 4′ is selected from group Hydrogen and optionally substituted alkyl.

R 4 is selected from group comprising optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

31 . The compound according to claim 30 comprising optionally substituted substituents on R 4 and R 4 ′ is selected from the group consisting of radicals such as C1-C8-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, amino, alkylamino, dialkylamino acyl, acyloxy, acylamino, aminocarbonyl, alkoxycarbonyl, alkoxyalkyloxy, alkoxycarbonyloxy, carbamate, sulfinyl, sulfonyl, alkoxy, sulfanyl, halogen, carboxy, haloalkyl, cyano, hydroxy, mercapto, nitro, phosphate, oxo, alkylphosphate.

32 . The compound according to claim 1 comprising the compound (XXX) represented by following formulae:

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

d is selected from carbon or nitrogen; wherein R 15 and R 16 together forms a optionally substituted carbocyclic or heterocyclic structure;

m and n can be independently 1 to 3;

pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

33 . The compound according to claim 32 , the formula XXX is optionally substituted with substituents selected from group consisting of alkyl, alkylcarbonyl, formyl, halo, haloalkyl, alkylphosphate, phosphate, oxo, cyano, nitro, amino, alkoxy, alkoxycarbonyl, carboxyalkyl, hydroxyalkyl, alkenyl, alkynyl, alkylthio, cycloalkyl, aryl, heteroaryl, aralkyl, heterocycloalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, alkoxyalkyl.

34 . The compound according to claim 1 comprising the compound (XXXI) represented by following formulae:

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

D is selected from optionally substituted bicyclic compound, spirocyclic compound or bridged bicyclic compounds, wherein the attachment of the bicyclic compound, spirocyclic compound or bridged bicyclic compounds is through either carbon or nitrogen atom; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

35 . The compound according to claim 1 , wherein the compound is selected from the group comprising of

Com-

pound

No.

Structures

100

101

102

103

104

105

106

107

108

109

110

111

112

113

114

115

116

117

118

119

120

121

122

123

124

125

126

127

128

129

130

131

132

133

134

135

136

137

138

139

140

141

142

143

144

145

146

147

148

149

150

151

152

153

154

155

156

157

158

159

160

161

162

163

164

165

166

167

168

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170

171

172

173

174

175

176

177

178

179

180

181

182

183

184

185

186

187

188

189

190

191

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193

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198

199

200

201

202

203

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205

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207

208

209

210

211

212

213

214

215

216

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218

219

220

221

222

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224

225

226

227

228

229

230

231

232

233

234

235

236

237

238

239

240

241

242

243

244

245

246

247

248

249

250

36 . A pharmaceutical composition comprising a compound of formula (I) of claim 1 or a compound (I-A) of claim 2 ; enantiomers, diastereomers, racemates, pharmaceutically acceptable salts or solvates thereof, and a pharmaceutically acceptable excipients.

37 . (canceled)

38 . A method of treating a benign or malignant diseases of the breast or reproductive tract, comprising administration of a compound of formula (I)

wherein;

X is halogen or hydrogen;

Y is alkyl, —O-alkyl or hydrogen;

A is selected from

or —O—R 2 , wherein R 1 is selected from hydrogen or alkyl; R 2 is selected independently from group consisting of

ii)

wherein R 8 is selected from group comprising optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl; or —CR 9 R 10 ; where R 9 and R 10 are taken together along with the carbon to which they are attached to form a three to seven membered saturated, partially unsaturated or unsaturated heterocyclic ring in which up to 4 carbon atoms are replaced by heteroatoms chosen from the group consisting of O, S or N and may optionally be substituted at a substitutable position with one or more Ru radicals, wherein one or more Ru radicals are independently selected at each occurrence from the group consisting of optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylcarbonyl, formyl, halo, alkylphosphate, phosphate, cyano, nitro, alkoxy, amino, alkoxycarbonyl, alkenyl, alkynyl, alkylthio arylcarbonyl;

iii)

wherein each R 12 is selected independently from hydrogen; optionally substituted optionally substituted alkyl, aryl, acyl, heterocycloalkyl or heteroaryl;

iv)

wherein each R 13 is selected independently from hydrogen; optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

v) amino acids, wherein the amino acid is linked via ester linkage at the point of attachment;

vi)

wherein R 14 is

wherein m and p are independently selected from 0 to 5, n refers to degree of polymerization and is selected from 1 to 250 and Z is optionally substituted alkyl or cycloalkyl;

vii)

wherein R 15 is selected from group comprising of optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;

viii)

wherein R 16 is selected from group comprising of hydrogen; optionally substituted alkyl, aryl, acyl, heteroaryl; and X is optionally substituted heterocycloalkyl;

ix)

39 .- 80 . (canceled)

81 . The pharmaceutical composition according to claim 36 , comprising at least one formula of compound selected from formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI, formula XII, formula XIII, formula XIV, formula XV, formula XVI, formula XVII, formula XVIII, formula XIX, formula XX, formula XXI, formula XXII, formula XXIII, formula XXIV, formula XXV, formula XXVI, formula XXVII, formula XXVIII, formula XXIX, formula XXX and formula XXXI pharmaceutically acceptable salts, enantiomers, diastereomers, racemates or solvates thereof; and at least one pharmaceutically acceptable excipient.

82 . The method of treating cancer according to claim 38 , comprising administering at least one formula of compound selected from formula II, formula III, formula IV, formula V, formula VI, formula VII, formula VIII, formula IX, formula X, formula XI, formula XII, formula XIII, formula XIV, formula XV, formula XVI, formula XVII, formula XVIII, formula XIX, formula XX, formula XXI, formula XXII, formula XXIII, formula XXIV, formula XXV, formula XXVI, formula XXVII, formula XXVIII, formula XXIX, formula XXX and formula XXXI; pharmaceutically acceptable salts, enantiomers, diastereomers, racemates, or solvates thereof.

Assignments (2)

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 14, 2025

From: SHIVANKA RESEARCH, LLC

To: AMNEAL PHARMACEUTICALS LLC

Reel/Frame 071115/0600 →

ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 9, 2024

From: PUROHIT, PARVA YOGESHCHANDRA; GOSWAMI, VISHALGIRI GUNVANTGIRI; MEHTA, CHIRAG CHIMANLAL; BARMADE, MAHESH ANGADRAO; SANGLE, GANESH VISHWANATH; UNADKAT, VISHAL BHARATBHAI; VARIYA, KETAN GORDHANBHAI; PANDYA, HETA NISHIL

To: SHIVANKA RESEARCH LLC

Reel/Frame 067939/0767 →