Pfizer Corporation

American Home Products Corporation

Wyeth

Other

American Cyanamid Company

Adam Matthew Gilbert

Matthew Frank Brown

Michael Aaron Brodney

Christopher Ryan Butler

Rayomand Jal Unwalla

Justin Ian Montgomery

Laura Ann McAllister

Roberto Pellicciari

Patrick Robert Verhoest

Mark Edward Flanagan

Ye Che

Elizabeth Mary Beck

Flavio Moroni

Zhen-jia Chen

Gary Paul Stack

Matthew Merrill Hayward

Atli Thorarensen

John Isidro Trujillo

Magda Asselin

Agustin Casimiro-Garcia

Jean-Baptiste Telliez

Richard Eric Mewshaw

Bruce Nelsen Rogers

Lei Zhang

Jotham Wadsworth Coe

Christopher John Helal

Erik Alphie LaChapelle

Megan Tran

Steven Victor O'Neil

Douglas Scott Johnson

Gerardo De Francisco

Jonathan David Langille

Damien Webb

Fuk-Wah Sum

Ping Zhou

Dahui Zhou

Deborah Ann Evrard

James Thomas Anderson

Kristin L Meagher

Eric Christian Hansen

Eugene Lvovich Piatnitski Chekler

Daniel Paul Uccello

Peter John Larkin

Matthew Gregory Bursavich

Eugene Lvovich Chekler

Aranapakam Mudumbai Venkatesan

Michael Sotirios Malamas

Joseph William Epstein

Phaik-Eng Sum

Russell Dushin

Christopher John O'Donnell

Edmund Lee Ellsworth

Lijing Chen

Lawrence Nathan Tumey

Sidney Xi Liang

Lee Dalton Jennings

George Theodore Grosu

Gary H Birnberg

Dennis William Powell

David Brian How

Joshua James Sabatini

Yixian Zhang

Jeffrey Michael Casavant

Scott Lee Kincaid

Anthony P Ricketts

Lee Richard Roberts

Gulnaz Khafizova

Jeremy Tyson Starr

Joseph Alan Abramite

Gary Frederick Filzen

Jeremy Clemens

Ludivine Moine

Jennifer Young

Feng Ling Qing

Sabrina Lombardi

Leif Mark Laakso

Yongbo Hu

Bruce Kipp Erickson

David P Thompson

Joseph A Abramite

Jeremy Starr

Daniel P Uccello

Christopher John O'donnell

The present invention provides a method for treating alopecia using certain pharmaceutically active pyrrolo[2,3-d]pyrimidinyl acrylamides having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description.

Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides

The present invention provides, in part, compounds of Formula I: or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: R, R, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.

5,7-dihydro-pyrrolo-pyridine derivatives

The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula: (wherein R, R, Het, D, E, X, Y, Z, m, n, p, q, r, s and t are as defined herein), methods for their preparation, their use in synthesizing antibody drug conjugates, and the resulting antibody drug conjugates made with components having heteroaryl sulfone-based conjugation handles.

Heteroaryl sulfone-based conjugation handles, methods for their preparation, and their use in synthesizing antibody drug conjugates

The present invention provides, in part, compounds of Formula I, or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound or the N-oxide, wherein: (R)a, (R)b, (R)c, L, A, and E are as described herein; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M4-mediated (or M4-associated) disorders including, e.g., Alzheimer's Disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder. 

Dihydro-pyrrolo-pyridine derivatives

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylam ides and analogues thereof, having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2-yl carbamate derivatives as MAGL inhibitors

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides, and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

Pyrrolo[2,3-D]pyrimidinyl, pyrrolo[2,3-B]pyrazinyl, pyrrolo[2,3-B]pyridinyl acrylamides and epoxides thereof

The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or &#x2014;CR&#x2014;, where Ris hydrogen, C-Clinear or branched chain alkyl, etc., Z is &#x2014;CR&#x2014;, or, &#x2014;N&#x2014;, where Ris hydrogen, C-Clinear or branched chain alkyl, etc.; Ris hydrogen, C-Clinear or branched chain alkyl, etc.; Rare independently hydrogen or C-Clinear or branched chain alkyl; Rand Rare independently hydrogen, C-Clinear or branched chain alkyl, etc.; Rand Rare independently hydrogen or C-Clinear or branched chain alkyl, etc.; Ris hydrogen, C-Clinear or branched chain alkyl, etc.; Rand Rare independently hydrogen or C-Clinear or branched chain alkyl, etc.; Q is &#x2014;CO&#x2014;, &#x2014;(CH)&#x2014;, &#x2014;(CHR)&#x2014;, or &#x2014;(CRR)&#x2014;, where Rand Rare independently C-Clinear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, for the treatment of certain diseases, particularly those affected or mediated by the androgen receptor; to combinations comprising such compounds with a second pharmaceutically active ingredient; to compositions containing such combinations; and to such combinations for the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.

Methods of use and combinations

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof, having the structure: or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof, as set forth in the Description. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or &#x2014;CR&#x2014;, where Ris hydrogen, C-Clinear or branched chain alkyl, etc., Z is &#x2014;CR&#x2014;, or, &#x2014;N&#x2014;, where Ris hydrogen, C-Clinear or branched chain alkyl, etc.; Ris hydrogen, C-Clinear or branched chain alkyl, etc.; Rare independently hydrogen or C-Clinear or branched chain alkyl; Rand Rare independently hydrogen, C-Clinear or branched chain alkyl, etc.; Rand Rare independently hydrogen or C-Clinear or branched chain alkyl, etc.; Ris hydrogen, C-Clinear or branched chain alkyl, etc.; Rand Rare independently hydrogen or C-Clinear or branched chain alkyl, etc.; Q is &#x2014;CO&#x2014;, &#x2014;(CH)&#x2014;, &#x2014;(CHR)&#x2014;, or &#x2014;(CRR)&#x2014;, where Rand Rare independently C-Clinear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.

Selective androgen receptor modulators

The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.

Thiazolyl- and oxazolyl-isoquinolinones and methods for using them

The present invention relates to substituted thienyl- and furanyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders.

Thienyl- and furanyl-isoquinolinones and methods for using them

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Guilford, CT, United States of America

Adam Matthew Gilbert