Kevin T Moriarty

US Patent:

6756378, Jun 29, 2004

Filed:

Dec 28, 2001

Appl. No.:

10/034585

Inventors:

John J. Baldwin - Gwynedd Valley PA
Edward McDonald - Reigate, GB
Kevin Joseph Moriarty - Norristown PA
Christopher Ronald Sarko - New Milford CT
Nobuo Machinaga - Tokyo, JP
Atsushi Nakayama - Tokyo, JP
Jun Chiba - Tokyo, JP
Shin Iimura - Tokyo, JP
Yoshiyuki Yoneda - Tokyo, JP

Assignee:

Pharmacopeia Drug Discovery, Inc. - Cranbury NJ
Daiichi Pharmaceutical Co., Ltd. - Tokyo

International Classification:

C07D20712

US Classification:

51425401, 514326, 514343, 514382, 514412, 514423, 544372, 546208, 5462791, 548251, 548452, 548453, 548540

Abstract:

Compounds that selectively inhibit the binding of ligands to 41 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are pharmaceutical compositions, methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion, which involve compounds of Formula I.

US Patent:

6800645, Oct 5, 2004

Filed:

Jul 7, 2000

Appl. No.:

09/612530

Inventors:

Paul Joseph Cox - Dagenham, GB
Shelley Bower - Dagenham, GB
David John Aldous - Dagenham, GB
Peter Charles Astles - Dagenham, GB
Daniel Gerard McGarry - King of Prussia PA
Christopher Hulme - Phoenixville PA
John Robinson Regan - Larchmont NY
Fu-Chih Huang - North Wales PA
Stevan Wakefield Djuric - Libertyville IL
Kevin Joseph Moriarty - Norristown PA
Rose Mappilakunnel Mathew - Phoenixville PA
Gregory Bernard Poli - Perkasie PA

Assignee:

Aventis Pharma Limited - Kent

International Classification:

A61K 3147

US Classification:

514314, 514308, 514309, 514312, 514313, 546169, 546140, 546141, 546146, 546153, 546156, 546158, 546159, 546165, 546166

Abstract:

This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; R represents hydrogen or a straight- or branched-chain alkyl group of 1 to about 4 carbon atoms, optionally substituted by hydroxy or one or more halogen atoms, or when Z represents a direct bond R may also represent a lower alkenyl or lower alkynyl group, or a formyl group; R represents hydrogen, alkenyl, alkoxy, alkyl, alkylsulphinyl, alkylsulphonyl, alkylthio, aryl, arylalkyloxy, arylalkylsulphinyl, arylalkylsulphonyl, arylalkylthio, aryloxy, arylsulphinyl, arylsulphonyl, arylthio, cyano, cycloalkenyl, cycloalkenyloxy, cycloalkyl, cycloalkyloxy, heteroaryl, heteroarylalkyloxy, heteroaryloxy, hydroxy, âSO NR R , âNR SO R , âNR R , âC( O)R , âC( O)C( O)R , âC( O)NR R , âC( O)OR , âO(C O)NR R , or âNR C( O)R ; R represents âC( Z)âN(R )R , âC( Z)âCHR R , âC( Z)âR , âCR C(R )(CH ) âR , âC(R ) C(R )R , âC(R )(R )C(R )(R )R , âC(R )(R )CH(R )(CH ) âR , âR , âV( Z)âR , âC(R ) NâOC( O)R , âC( O)âN(R )OR , âCâCâR , âCH âC( Z)âR , âC( Z)âC( Z)R , âCH âNHR , âCH âZR , âCH âSOR , âCH âSO R , âCF âOR , âNHâCH R , âZâCH R , âSOâCH R , âSO âCH R , âOâCF R , âOâC( Z)R , âN NâR , âNHâSO R , âSO âNR R , âCZâCZâNHR , âNHâCOâOR , âOâCOâNHR , âNHâCOâNHR , âR , âCX CX R , âC( NOR ), â(CH ) R , âCH âCOâNH(CH ) R , âCH âNHâCO(CH ) R , âCH âCOâCH R , âC( NR )âNH(CH ) R , âC(X ) Nâ(CH ) R or âCH(X )âCH R ; A represents a direct bond, or a straight or branched C alkylene chain optionally substituted by hydroxyl, alkoxy, oxo, cycloalkyl, aryl or heteroaryl, or A represents a straight or branched C alkenylene or C alkynylene chain; Z represents a direct bond, an oxygen or sulphur atom or NH; n and m each represent zero or 1, provided that n is 1 when m is zero and n is zero when m is 1; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.

US Patent:

6906067, Jun 14, 2005

Filed:

Jun 26, 2001

Appl. No.:

09/891750

Inventors:

Kevin Joseph Moriarty - Norristown PA, US
Yvonne Shimshock - Hillsborough NJ, US
Gulzar Ahmed - Yardley PA, US
Junjun Wu - Malden MA, US
James Wen - Dayton NJ, US
Wei Li - Acton MA, US
Shawn David Erickson - Leonia NJ, US
Jeffrey John Letourneau - East Windsor NJ, US
Edward McDonald - Banstead, GB
Katerina Leftheris - Skillman NJ, US
Stephen T. Wrobleski - Whitehouse Station NJ, US
Zahid Hussain - Monmouth Junction NJ, US
Ian Henderson - Hopewell NJ, US
Axel Metzger - East Windsor NJ, US
John J. Baldwin - Gwynedd Valley PA, US
Alaric J. Dyckman - Lawrenceville NJ, US

Assignee:

Bristol-Myers Squibb Company - Princeton NJ
Pharmaceopeia, Inc. - Cranbury NJ

International Classification:

C07D251/40
C07D251/48
C07D251/52
A61K031/53
A61P035/00

US Classification:

514241, 544197, 544198, 544208, 544209, 544213, 544217, 544218

Abstract:

N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.

US Patent:

7179819, Feb 20, 2007

Filed:

Feb 26, 2004

Appl. No.:

10/787905

Inventors:

John J. Baldwin - Gwynedd Valley PA, US
Edward McDonald - Surrey, GB
Kevin Joseph Moriarty - Norristown PA, US
Christopher Ronald Sarko - New Milford CT, US
Nobuo Machinaga - Tokyo, JP
Atsushi Nakayama - Tokyo, JP
Jun Chiba - Tokyo, JP
Iimura Shin - Tokyo, JP
Yoshiyuki Yoneda - Tokyo, JP

Assignee:

Daiichi Pharmaceutical Co., Ltd. - Tokyo
Pharmacopeia Drug Discovery, Inc. - Cranbury NJ

International Classification:

C07D 277/04
A61K 31/425
C07D 207/12

US Classification:

514326, 514365, 546209, 548200

Abstract:

Compounds that selectively inhibit the binding of ligands to α4β1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I:.

US Patent:

7479495, Jan 20, 2009

Filed:

Jun 2, 2005

Appl. No.:

11/143430

Inventors:

Kevin Joseph Moriarty - Norristown PA, US
Yvonne Shimshock - Hillsborough NJ, US
Gulzar Ahmed - Yardley PA, US
Junjun Wu - Malden MA, US
James Wen - Dayton NJ, US
Wei Li - Acton MA, US
Shawn David Erickson - Leonia NJ, US
Jeffrey John Letourneau - East Windsor NJ, US
Edward McDonald - Banstead, GB
Katerina Leftheris - Skillman NJ, US
Stephen T. Wrobleski - Whitehouse Station NJ, US
Zahid Hussain - Monmouth Junction NJ, US
Ian Henderson - Hopewell NJ, US
Axel Metzger - East Windsor NJ, US
John J. Baldwin - Gwynedd Valley PA, US
Alaric J. Dyckman - Lawrenceville NJ, US

Assignee:

Pharmacopeia, Inc. - Cranbury NJ
Bristol-Myers Squibb Company - Princeton NJ

International Classification:

C07D 239/32
C07D 239/48
C07D 239/50
C07D 401/04
C07D 401/12
C07D 403/04
C07D 403/12
A61K 31/505
A61K 31/506
A61P 19/02
A61P 35/00

US Classification:

514269, 514272, 514273, 514275, 544317, 544320, 544321, 544323, 544326

Abstract:

N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I:Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.

US Patent:

20020065270, May 30, 2002

Filed:

Dec 22, 2000

Appl. No.:

09/747195

Inventors:

Kevin Moriarty - Norristown PA, US
Yvonne Shimshock - Hillsborough NJ, US
Gulzar Ahmed - Yardley PA, US
Junjun Wu - Malden MA, US
James Wen - Dayton NJ, US
Wei Li - Acton MA, US
Shawn Erickson - Leonia NJ, US
Jeffrey Letourneau - East Windsor NJ, US
Edward McDonald - Surrey, GB
Katerina Leftheris - Skillman NJ, US
Stephen Wrobleski - Whitehouse Station NJ, US

International Classification:

A61K031/551
A61K031/53
A61K031/506
A61K031/4439
C07D251/42
C07D243/06

US Classification:

514/218000, 514/245000, 514/256000, 514/336000, 544/212000, 540/574000, 544/330000

Abstract:

N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF- expression utilizing compounds of the present invention are also disclosed.

US Patent:

20050176792, Aug 11, 2005

Filed:

Jan 7, 2005

Appl. No.:

11/035876

Inventors:

Kevin Moriarty - East Norriton PA, US
Lei Qiao - Dowington PA, US
Gregory Roth - Woodstock CT, US

Assignee:

Boehringer Ingelheim Pharmaceuticals, Inc. - Ridgefield CT

International Classification:

A61K031/42
A61K031/4184
C07D413/02
C07D045/02

US Classification:

514379000, 514394000, 548248000, 548304700

Abstract:

Disclosed are ketone substituted benzimidazole compounds of formula(I): wherein R, R, R, Rand Xare defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.

US Patent:

20070054909, Mar 8, 2007

Filed:

Nov 8, 2006

Appl. No.:

11/594432

Inventors:

John Baldwin - Gwynedd PA, US
Edward McDonald - Surrey, GB
Kevin Moriarty - Norristown PA, US
Christopher Sarko - New Milford CT, US
Nobuo Machinaga - Tokyo, JP
Atsushi Nakayama - Tokyo, JP
Jun Chiba - Tokyo, JP
Shin Iimura - Tokyo, JP
Yoshiyuki Yoneda - Tokyo, JP

Assignee:

Daiichi Pharmaceutical Co., Ltd. - Tokyo
Pharmacopeia Drug Discovery, Inc. - Cranbury NJ

International Classification:

A61K 31/5375
A61K 31/496
A61K 31/4439
A61K 31/426
A61K 31/401
A61K 31/405
C07D 403/02

US Classification:

514237800, 514381000, 514423000, 514415000, 514254010, 514326000, 514343000, 514365000, 544372000, 546207000, 546279100, 548482000, 548530000

Abstract:

Compounds that selectively inhibit the binding of ligands to α4β1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion.