IP Library Granted Patent US 7,781,617
Granted Patent B2
US 7,781,617 · App. 11/631,128 · Granted Aug 24, 2010

Effective use method of medicaments and method of preventing expression of side effect

Assignee: Kyorin Pharmaceutical Co., Ltd
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Quick Facts
Patent No.
US 7,781,617
App. No.
11/631,128
Granted
Aug 24, 2010
Kind
B2
Abstract

A medicine which effectively functions as an immunosuppressant or anti-inflammatory agent and is effective in diminishing the occurrence of side effects. The medicine comprises a combination of: a diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure and having the function of diminishing lymphocytes circulating through the periphery; and an immunosuppressant and/or an anti-inflammatory agent.

Claims (26)

1. A medicament for preventing rejection response in organ or cell transplantation, comprising a diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure having an activity of reducing lymphocytes circulating peripherally, wherein the compound is represented by formula (1):

wherein:

R 1 represents a halogen atom, trihalomethyl group, hydroxy group, lower alkyl group having 1 to 7 carbon atoms, optionally substituted phenyl group, aralkyl group, lower alkoxy group having 1 to 4 carbon atoms, trifluoromethyloxy group, phenoxy group, cyclohexylmethyloxy group, optionally substituted aralkyloxy group, pyridylmethyloxy group, cinnamyloxy group, naphthylmethyloxy group, phenoxymethyl group, hydroxymethyl group, hydroxyethyl group, lower alkylthio group having 1 to 4 carbon atoms, lower alkylsulfinyl group having 1 to 4 carbon atoms, lower alkylsulfonyl group having 1 to 4 carbon atoms, benzylthio group, acetyl group, nitro group or cyano group,

R 2 represents a hydrogen atom, halogen atom, trihalomethyl group, lower alkoxy group having 1 to 4 carbon atoms, lower alkyl group having 1 to 7 carbon atoms, phenethyl group or benzyloxy group,

R 3 represents a hydrogen atom, halogen atom, trifluoromethyl group, lower alkoxy group having 1 to 4 carbon atoms, hydroxy group, benzyloxy group, lower alkyl group having 1 to 7 carbon atoms, phenyl group, lower alkoxymethyl group having 1 to 4 carbon atoms, or lower alkylthio group having 1 to 4 carbon atoms,

X represents O, S, SO or SO 2 , and

n represents an integer of 1 to 4,

or its pharmaceutically acceptable salt or hydrate,

in combination with an immunosuppressive agent and/or anti-inflammatory agent.

2. The medicament according to claim 1 , wherein the compound represented by the formula (1) is 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol.

3. The medicament according to claim 1 , wherein the compound represented by the formula (1) is 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol hydrochloride.

4. The medicament according to claim 3 , wherein the immunosuppressive agent is a calcineurin inhibitor.

5. The medicament according to claim 4 , wherein the calcineurin inhibitor is cyclosporin A or tacrolimus.

6. A method for preventing rejection response in organ or cell transplantation, comprising administering to a subject in need thereof a therapeutically effective amount of a medicament comprising a diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure having an activity of reducing lymphocytes circulating peripherally, wherein the compound is represented by formula (1):

wherein:

R 1 represents a halogen atom, trihalomethyl group, hydroxy group, lower alkyl group having 1 to 7 carbon atoms, optionally substituted phenyl group, aralkyl group, lower alkoxy group having 1 to 4 carbon atoms, trifluoromethyloxy group, phenoxy group, cyclohexylmethyloxy group, optionally substituted aralkyloxy group, pyridylmethyloxy group, cinnamyloxy group, naphthylmethyloxy group, phenoxymethyl group, hydroxymethyl group, hydroxyethyl group, lower alkylthio group having 1 to 4 carbon atoms, lower alkylsulfinyl group having 1 to 4 carbon atoms, lower alkylsulfonyl group having 1 to 4 carbon atoms, benzylthio group, acetyl group, nitro group or cyano group,

R 2 represents a hydrogen atom, halogen atom, trihalomethyl group, lower alkoxy group having 1 to 4 carbon atoms, lower alkyl group having 1 to 7 carbon atoms, phenethyl group or benzyloxy group,

R 3 represents a hydrogen atom, halogen atom, trifluoromethyl group, lower alkoxy group having 1 to 4 carbon atoms, hydroxy group, benzyloxy group, lower alkyl group having 1 to 7 carbon atoms, phenyl group, lower alkoxymethyl group having 1 to 4 carbon atoms, or lower alkylthio group having 1 to 4 carbon atoms,

X represents O, S, SO or SO 2 , and

n represents an integer of 1 to 4,

or its pharmaceutically acceptable salt or hydrate,

in combination with an immunosuppressive agent andlor anti-inflammatory agent.

7. The method according to claim 6 , wherein the compound represented by formula (1) is 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol.

8. The method according to claim 6 , wherein the compound represented by formula (1) is 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol hydrochloride.

9. The method according to claim 8 , wherein the immunosuppressive agent is a calcineurin inhibitor.

10. The method according to claim 9 , wherein the calcineurin inhibitor is cyclosporin A or tacrolimus.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 21, 2021
From: KYORIN PHARMACEUTICAL CO., LTD
To: PRIOTHERA LIMITED
Reel/Frame 055994/0605 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 20, 2007
From: KUDOU, SHINJI; KURIYAMA, KAZUHIKO; YASUE, TOKUTAROU
To: KYORIN PHARMACEUTICAL CO., LTD.
Reel/Frame 018984/0557 →
Priority Claims (2)
JP 2004-209591 · Jul 16, 2004 · national
JP 2005-056875 · Mar 2, 2005 · national
Continuity (1)
Related Publication 20080032923A1 · Feb 7, 2008