Babu Joseph Mavunkel

US Patent:

6340685, Jan 22, 2002

Filed:

Mar 24, 1999

Appl. No.:

09/275176

Inventors:

Babu J. Mavunkel - Sunnyvale CA
John A. Lewicki - Los Gatos CA
David Y. Liu - Palo Alto CA
George F. Schreiner - Los Altos Hills CA
John J. Perumattam - Los Altos CA

Assignee:

Scios, Inc. - Sunnyvale CA

International Classification:

A61K 31496

US Classification:

514253, 544367, 544370, 544373

Abstract:

A compound of the formula: and the pharmaceutically acceptable salts thereof, wherein each of Z and Z is independently CR or N; where each R is independently H or is alkyl (1-6C) optionally including one or more heteroatoms selected from O, S and N and optionally substituted by one or more of halo, OR, SR, NR , RCO, COOR, CONR , OOCR, or NROCR where R is H or alkyl (1-6C), or by CN or O, or by an aliphatic or aromatic 5 or 6 membered ring optionally containing 1-2 N heteroatoms; or two R taken together form a bridge optionally containing a heteroatom; R is âwherein X is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two 6 taken together may form an alkyene (2-3C) bridge; n is 0 or 2; Z is CH or N; X is CH, CH or an isostere thereof; and Ar consists of one or two phenyl moieties directly coupled to X optionally substituted by halo, nitro, alkyl (1-6C), alkenyl (1-6C), CN or CF , or by RCO, COOR, CONR , NR , OR, SR, OOCR or NROCR wherein R is H or alkyl (1-6C) or by phenyl, itself optionally substituted by the foregoing substituents; R is H, or alkyl (1-6C) optionally including one heteroatom which is O, S or N, and optionally substituted by one or more of halo, OR, SR, NR , RCO, COOR, CONR , OOCR, or NROCR where R is H or alkyl (1-6C), or by CN or O, or by an aliphatic or aromatic 5 or 6 membered ring optionally containing 1-2 N heteroatoms; R is H, halo, NO , alkyl (1-6C), alkenyl (1-6C), CN, OR, SR, NR , RCO, COOR, CONR , OOCR, or NROCR where R is H or alkyl (1-6C).

US Patent:

6410540, Jun 25, 2002

Filed:

Aug 27, 1999

Appl. No.:

09/385494

Inventors:

R. Richard Goehring - Pipersville PA
Gregory R. Luedtke - Sunnyvale CA
Babu J. Mavunkel - Sunnyvale CA
Sarvajit Chakravarty - Sunnyvale CA
Sundeep Dugar - Bridgewater NJ
George F. Schreiner - Los Altos Hills CA
David Y. Liu - Palo Alto CA
John A. Lewicki - Los Gatos CA

Assignee:

Scios, Inc. - Sunnyvale CA

International Classification:

A61K 3150

US Classification:

51425213, 51425409, 514330

Abstract:

The invention is directed to methods to treat conditions mediated by p38-kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein Z is N or CR , R is a noninterfering substituent, each of X and X is a linker, Ar and Ar are identical or different, and represent optionally substituted C1-C20 hydrocarbyl residues wherein at least one of Ar and Ar is an optionally substituted aryl group, with the proviso that when X is CH or an isostere thereof, X is CO or an isostere thereof, and Ar is optionally substituted phenyl, Ar is other than an optionally substituted indolyl, benzimidazolyl or benzotriazolyl substituent, and wherein said optionally substituted phenyl is not an optionally substituted indolyl, benzimidazolyl, or benzotriazolyl, Y is a noninterfering substituent, wherein n is an integer from 0-4, and wherein m is an integer from 0-4 and 1 is an integer from 0-3.

US Patent:

6448257, Sep 10, 2002

Filed:

Mar 24, 2000

Appl. No.:

09/535316

Inventors:

Babu J. Mavunkel - Sunnyvale CA
David Y. Liu - Palo Alto CA
George F. Schreiner - Los Altos Hills CA
John A. Lewicki - Los Gatos CA

Assignee:

Scios, Inc. - Sunnyvale CA

International Classification:

A61K 31437

US Classification:

514292, 546 89

Abstract:

Compounds of the formula: wherein the dotted line represents an optional bond; and the pharmaceutically acceptable salts thereof, wherein X is an alkyl bridge optionally containing an O, S, or N heteroatom that forms an aliphatic 5-7 membered ring and is optionally substituted by one or more of halo, OR, SR, NR , RCO, COOR, CONR , OOCR, or NROCR where R is H or alkyl (1-6C), or by one or more CN or O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R is âwherein X is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two Y taken together may form an alkylene (2-3C) bridge; n is 0-4; Z is CH or N; X is CH or CHR where R is H or alkyl (1-6C), or an isostere thereof; and Ar, R and R are as defined in the specification. These compounds are selective inhibitors of p38 kinase.

US Patent:

6541477, Apr 1, 2003

Filed:

Feb 28, 2001

Appl. No.:

09/796997

Inventors:

R. Richard Goehring - Pipersville PA
Babu J. Mavunkel - Sunnyvale CA
David Y. Liu - Palo Alto CA
George F. Schreiner - Los Altos Hills CA
Gregory Leudtke - Sunnyvale CA
John A. Lewicki - Los Gatos CA

Assignee:

Scios, Inc. - Sunnyvale CA

International Classification:

A61K 31495

US Classification:

51425213, 5142541, 514330

Abstract:

The invention is directed to methods for treating conditions mediated by by P38 kinase using compounds of the formula wherein Ar and Ph are limited to specific embodiments or wherein the compound of formula (3) is a compound set forth in FIGS. A- T.

US Patent:

6589954, Jul 8, 2003

Filed:

May 21, 1999

Appl. No.:

09/316761

Inventors:

Babu J. Mavunkel - Sunnyvale CA
David Y. Liu - Palo Alto CA
George F. Schreiner - Los Altos Hills CA
John A. Lewicki - Los Gatos CA
John J. Perumattam - Los Altos CA

Assignee:

Scios, Inc. - Sunnyvale CA

International Classification:

A61K 31495

US Classification:

514253, 544367, 544373

Abstract:

Indoles, benzimidazoles and benztriazoles which are substituted at the 5 or 6 position with a substituent comprising an aromatic moiety linked through a piperazine ring to said indole, benzimidazole or benztriazole are useful in treating cardiac conditions associated with heart failure and in treating conditions characterized by proinflammation.

US Patent:

6696443, Feb 24, 2004

Filed:

Nov 20, 2001

Appl. No.:

09/990184

Inventors:

Babu Mavunkel - Sunnyvale CA
Sundeep Dugar - San Jose CA
Gregory Luedtke - Sunnyvale CA
Xuefei Tan - Sunnyvale CA
Glenn McEnroe - San Mataeo CA

Assignee:

Scios, Inc. - Fremont CA

International Classification:

C07D40106

US Classification:

514241, 544180, 544182, 544236, 544238, 544257, 544279, 544333, 544350, 546114, 546115, 546121, 546122, 546139, 546194, 546199, 546208, 546202, 546209, 546211, 546212, 546214, 514242, 514248, 51425203, 51425505, 5142593, 5142592, 51425941, 514256, 514300, 514301, 514302, 514314, 514318, 514319, 514320, 514321, 514322, 514323, 514324, 514326

Abstract:

Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38- kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38- kinase activity.

US Patent:

6864260, Mar 8, 2005

Filed:

May 28, 2002

Appl. No.:

10/157048

Inventors:

Babu J. Mavunkel - Sunnyvale CA, US
Sarvajit Chakravarty - Sunnyvale CA, US
John J. Perumattam - Los Altos CA, US
Sundeep Dugar - San Jose CA, US
Qing Lu - Foster City CA, US
Xi Liang - Mountain View CA, US

Assignee:

Scios, Inc. - Fremont CA

International Classification:

A61K031/495
C07D403/06

US Classification:

514253, 544367, 544370, 544373

Abstract:

The invention is directed to methods to inhibit p-α kinase using compounds which contain a phenyl group linked through a piperazine ring to a substituted indole.

US Patent:

6867209, Mar 15, 2005

Filed:

May 19, 2000

Appl. No.:

09/575060

Inventors:

Babu J. Mavunkel - Sunnyvale CA, US
Sarvajit Chakravarty - Sunnyvale CA, US
John J. Perumattam - Los Altos CA, US
Sundeep Dugar - San Jose CA, US
Qing Lu - Foster City CA, US
Xi Liang - Mountain View CA, US

Assignee:

Scios, Inc. - Freemont CA

International Classification:

A61K031/495
C07D241/04

US Classification:

514253, 514183, 5142328, 5142352, 5142358, 540481, 544121, 544142, 544363, 544396

Abstract:

The invention is directed to methods to inhibit p38-α kinase using compounds of the formula.