Joel K Kawakami

US Patent:

20030144310, Jul 31, 2003

Filed:

Sep 24, 2002

Appl. No.:

10/253288

Inventors:

Lakmal Boteju - Cedar Grove NJ, US
Michael Konkel - Garfield NJ, US
Joel Kawakami - Newfoundland NJ, US
John Wetzel - Fairlawn NJ, US

International Classification:

A61K031/505
A61K031/445
A61K031/4164
A61K031/40
C07D239/42
C07D223/16
C07D213/53
A61K031/18

US Classification:

514/275000, 514/317000, 514/357000, 514/408000, 514/401000, 514/605000, 544/330000, 546/229000, 546/332000, 548/354100, 548/566000, 564/095000

Abstract:

This invention provides a compound having the structure: wherein R1 is straight chained or branched C1-C7 alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7 alkenyl or alkynyl; C3-C7 cycloalkyl, monofluorocycloalkyl, or polyfluorocycloalkyl; C5-C7 cycloalkenyl; naphthyl; arylalkyl, heteroarylalkyl, phenyl or heteroaryl, wherein the arylalkyl, heteroarylalkyl, phenyl or heteroaryl is unsubstituted or substituted with one or more of the following substituents: halogen, hydroxy, C1-C6 alkoxy, aryloxy, straight chained or branched C2-C6 alkyl, aryl, heteroaryl, nitro, cyano, C1-C6 alkylthio, substituted or unsubstituted arylalkyl or heteroarylalkyl, —C( Y)R7, —C( Y)OR7, —N(R7), —C( Y)NR7, —NR7C( Y)R7 or —N(R7)C( Y)N(R7), wherein Y is O or S; wherein R7 is independently H, straight chained or branched C1-C7 alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7 alkenyl or alkynyl; C3-C7 cycloalkyl, monofluorocycloalkyl, or polyfluorocycloalkyl; C5-C7 cycloalkenyl; wherein R2 is —(CH)—NH—C( NH)—NH; —(CH)n—C( NH)—NH; —(CH)—N(R7); or -J; wherein n is an integer between 1 and 6, and wherein J is any of the following structures: wherein each of R3 and R4 is independently H, straight chained or branched C1-C7 alkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7 alkenyl or alkynyl; C3-C7 cycloalkyl, monofluorocycloalkyl, or polyfluorocycloalkyl; or C5-C7 cycloalkenyl; wherein R5 is —OR8 or —N(R8); wherein each R8 is independently H, straight chained or branched C1-C7 alkyl, alkoxyalkyl, alkylthioalkyl, monofluoroalkyl or polyfluoroalkyl; straight chained or branched C2-C7 alkenyl or alkynyl; C3-C7 cycloalkyl, monofluorocycloalkyl, or polyfluorocycloalkyl; C5-C7 cycloalkenyl; wherein R6 is arylalkyl, heteroarylalkyl, aryl or heteroaryl, each optionally substituted with one or more of the following substituents: halogen, hydroxy, C1-C6 alkoxy, aryloxy, straight chained or branched C1-C6 alkyl, aryl, heteroaryl, nitro, cyano, C1-C6 alkylthio, substituted or unsubstituted arylalkyl or heteroarylalkyl, —C( Y)R7, —C( Y)OR7, —N(R7), —C( Y)NR7, —NR7C( Y)R7 or —N(R7)C( Y)N(R7), or a pharmaceutically acceptable salt thereof. This invention also provides a method of treating a lower urinary tract disorder in a subject in need of such treatment comprising administering to the subject an effective amount of any of the aforementioned compounds.

US Patent:

20030176314, Sep 18, 2003

Filed:

Sep 24, 2002

Appl. No.:

10/253237

Inventors:

Carlos Forray - Paramus NJ, US
Joel Kawakami - Newfoundland NJ, US
Michael Konkel - Garfield NJ, US
Lakmal Boteju - Cedar Grove NJ, US
John Wetzel - Fairlawn NJ, US
Stewart Noble - Lake Forest IL, US
Honghe Wan - Kearny NJ, US

International Classification:

A61K031/00

US Classification:

514/001000

Abstract:

This invention provides methods of treating pain, urinary incontinence and other abnormalities mediated by a NPFF receptor, which comprises administering to a subject a therapeutically effective amount of a chemical compound which acts at the NPFF1 receptor, the NPFF2 receptor, or at both the NPFF1 and NPFF2 receptors.

US Patent:

20090048301, Feb 19, 2009

Filed:

Jul 9, 2004

Appl. No.:

10/564267

Inventors:

Xiaoling Chen - Brooklyn NY, US
Hai-Ying He - Brooklyn NY, US
Joel Kawakami - Honolulu HI, US
Alexander Kiselyov - San Diego CA, US
Xiaohu Ouyang - Flushing NY, US
Vatee Pattaropong - New Madrid MO, US
Evgueni Piatnitski - King of Prussia PA, US
Maria Carolina Tuma - Jersey City NJ, US
John Kincaid - San Diego CA, US

Assignee:

IMCLONE SYSTEMS INCORPORATED - New York NY

International Classification:

A61K 31/444
C07D 401/04
A61K 31/4439
C07D 401/14
A61P 35/00

US Classification:

514333, 5462724, 514340, 514338, 546256

Abstract:

The present invention relates to heterocyclic compounds that have anticancer activity, and pharmaceutical compositions that contain such compounds, methods of treating diseases and conditions in mammals using such compounds and composition and methods for their manufacture.

US Patent:

20090318438, Dec 24, 2009

Filed:

Sep 25, 2008

Appl. No.:

12/286132

Inventors:

Xiaoling Chen - Brooklyn NY, US
Hai-Ying He - Brooklyn NY, US
Joel Kawakami - Honolulu HI, US
Alexander Kiselyov - San Diego CA, US
Xiaohu Ouyang - Flushing NY, US
Vatee Pattaropong - New Madrid MO, US
Evgueni Piatnitski - King of Prussia PA, US
Maria Carolina Tuma - Jersey City NJ, US
John Kincaid - San Diego CA, US

International Classification:

A61K 31/5377
A61K 31/444
C07D 401/04
A61K 31/496
C07D 413/14
A61P 35/00
C07D 405/00
C07D 401/14
A61K 31/4439

US Classification:

5142338, 514340, 514333, 514338, 546256, 5462724, 51425505

Abstract:

The present invention relates to heterocyclic compounds that have anticancer activity, and pharmaceutical compositions that contain such compounds, methods of treating diseases and conditions in mammals using such compounds and composition and methods for their manufacture.

US Patent:

20030139431, Jul 24, 2003

Filed:

Sep 21, 2002

Appl. No.:

10/253946

Inventors:

Joel Kawakami - Newfoundland NJ, US
John Wetzel - Fairlawn NJ, US
Lakmal Boteju - Cedar Grove NJ, US
Michael Konkel - Garfield NJ, US
Honghe Wan - Kearny NJ, US
Stewart Noble - Lake Forest IL, US

International Classification:

A61K031/517
A61K031/47

US Classification:

514/266400, 514/313000

Abstract:

This invention provides compounds having the structure: wherein X=CH, C(CH) or N; each of R, R, R, Rand Ris independently H, C-Cstraight chained or branched alkyl, C-Cstraight chained or branched alkenyl, C-Cstraight chained or branched alkynyl, C-Ccycloalkyl, substituted or unsubstituted aryl, hydroxy, halogenated ether, nitro, amino, halogen, —CN, —C( Z)R, —C( Z)OR, —C( Z)N(R), —N(R)—C( Z)R, —N(R)—C( Z)N(R), —OC( Z)R, —C( Z)OR—ORor —SR; wherein Z is O or S; and wherein Ris C-Cstraight chained or branched alkyl, aryl, (CH)Q, C-Calkenyl, C-Ccycloalkyl, C-Ccycloalkenyl, wherein Q is OR, SR, N(R)or aryl, wherein Ris H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, wherein Rand Rand the carbons to which they are attached form a fused aryl, heteroaryl, C-Ccyclic alkyl or heterocyclic alkyl ring; or wherein Rand Rand the carbons to which they are attached form a fused aryl, heteroaryl, cyclic alkyl or heterocyclic alkyl ring; and wherein each alkyl, alkenyl, alkynyl and alkoxy group is optionally substituted with a substituent independently selected from R, where Ris 1) hydroxy, 2) C-Calkoxy, 3) halogen, 4) nitro, 5) amino, 6) CF, or 7) carboxy, and each cycloalkyl group is optionally substituted with a substituent independently selected from R, where Ris 1) a group selected from R, 2) C-Calkyl, 3) C-Calkenyl, 4) C-Calkynyl or 5) cyclic C-Calkyl, and each aryl is optionally substituted with R. This invention also provides methods of treating pain, urge incontinence; as well as methods of preparing the compounds.