公开(公告)号：US07754717B2

公开(公告)日：2010-07-13

申请号：US11503551

申请日：2006-08-11

Applicant: Erin F. Dimauro ,  Jean E. Bemis ,  Stuart C. Chaffee ,  Ning Chen ,  Essa Hu ,  Roxanne Kunz ,  Matthew W. Martin ,  David C. McGowan ,  Shannon Rumfelt

Inventor： Erin F. Dimauro ,  Jean E. Bemis ,  Stuart C. Chaffee ,  Ning Chen ,  Essa Hu ,  Roxanne Kunz ,  Matthew W. Martin ,  David C. McGowan ,  Shannon Rumfelt

IPC: A01N43/60 ,  A01N43/54 ,  A01N43/42 ,  A61K31/495 ,  A61K31/50 ,  A61K31/501 ,  A61K31/4965 ,  A61K31/51 ,  A61K31/47 ,  C07D239/42 ,  C07D401/04 ,  C07D237/30 ,  C07D401/00

CPC classification number: C07D213/75 ,  C07D215/38 ,  C07D239/42 ,  C07D239/48 ,  C07D239/50 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, L, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of the present invention, methods of use such as treatment of Lck and/or c-Kit kinase mediated diseases by administering the compounds of the invention, or compositions including one or more compounds of the invention, and intermediates and processes useful for the preparation of compounds of the present invention.

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括自身免疫疾病和炎症的化合物。 在一个实施方案中，化合物具有通式I，其中A1，A2，A3，A4，L，R1，R2和R3如本文所定义。 本发明还包括药物组合物，其包含一种或多种本发明化合物，通过施用本发明化合物来治疗Lck和/或c-Kit激酶介导的疾病的使用方法，或包含一种或多种本发明化合物的组合物 发明，以及可用于制备本发明化合物的中间体和方法。

公开(公告)号：US07700607B2

公开(公告)日：2010-04-20

申请号：US11879830

申请日：2007-07-18

Applicant: Essa Hu ,  Jason Brooks Human ,  Roxanne Kunz ,  Andrew Tasker ,  Ryan White

Inventor： Essa Hu ,  Jason Brooks Human ,  Roxanne Kunz ,  Andrew Tasker ,  Ryan White

IPC: A61K31/517

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括能够调节c-kit受体的新一类化合物，因此可用于治疗c-kit介导的疾病，包括各种炎性，纤维化和/或肥大细胞介导的疾病如肥大细胞增多症。 化合物具有通式I，其中R1-6在本文中定义。 本发明还包括药物组合物，用于治疗c-kit介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

公开(公告)号：US20070287716A1

公开(公告)日：2007-12-13

申请号：US11665422

申请日：2005-10-24

Applicant: Essa Hu ,  Jean-Michel Vernier ,  Peter Chua ,  John Hutchinson ,  Nicholas Cosford

Inventor： Essa Hu ,  Jean-Michel Vernier ,  Peter Chua ,  John Hutchinson ,  Nicholas Cosford

IPC: A61K31/47 ,  A61P25/00 ,  C07D215/12 ,  C07D239/28

CPC classification number: C07D239/26 ,  C07D215/06

Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

Abstract translation: 本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

公开(公告)号：US20060194807A1

公开(公告)日：2006-08-31

申请号：US10551709

申请日：2004-03-30

Applicant: Nicholas Cosford ,  Brian Eastman ,  Dehua Huang ,  Nicholas Smith ,  Lida Tehrani ,  Essa Hu

Inventor： Nicholas Cosford ,  Brian Eastman ,  Dehua Huang ,  Nicholas Smith ,  Lida Tehrani ,  Essa Hu

IPC: A61K31/506 ,  A61K31/498 ,  A61K31/4709 ,  A61K31/4439 ,  C07D403/14

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D417/14 ,  C07D471/04

Abstract: Novel pyrazole compounds such as compounds of the formula (I): (where A, A1, A2, B, R11, W, X, Y and Z are as defined herein) in which the pyrazole is substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, obesity, drug addiction, drug abuse, drug withdrawal and other diseases.

Abstract translation: 新的吡唑化合物，例如式（I）的化合物：其中A，A 1，A 2，B，R 11，W ，X，Y和Z如本文所定义），其中吡唑直接被取代，或通过桥取代，其中i）杂芳基部分含有与杂芳基的连接点相邻的N，和ii）另一个杂芳基或芳基环 ，其中至少一个环被另一个环取代，是用于治疗精神病和情绪障碍的mGluR5调节剂，例如精神分裂症，焦虑症，抑郁症，恐慌症和双相情感障碍，以及在 治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，肥胖，药物成瘾，药物滥用，戒毒等疾病。

公开(公告)号：US08637500B2

公开(公告)日：2014-01-28

申请号：US12639931

申请日：2009-12-16

Applicant: Jennifer R. Allen ,  Ning Chen ,  James R. Falsey ,  Michael J. Frohn ,  Paul E. Harrington ,  Essa Hu Harrington ,  Matthew R. Kaller ,  Roxanne K. Kunz ,  Thomas T. Nguyen ,  Alexander J. Pickrell ,  Andreas Reichelt ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Kelvin Sham ,  Aaron C. Siegmund ,  Guomin Yao

Inventor： Jennifer R. Allen ,  Ning Chen ,  James R. Falsey ,  Michael J. Frohn ,  Paul E. Harrington ,  Essa Hu Harrington ,  Matthew R. Kaller ,  Roxanne K. Kunz ,  Thomas T. Nguyen ,  Alexander J. Pickrell ,  Andreas Reichelt ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Kelvin Sham ,  Aaron C. Siegmund ,  Guomin Yao

IPC: A61K31/551 ,  A61K31/553 ,  A61K31/5377 ,  A61K31/497 ,  C07D243/08 ,  C07D267/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14

CPC classification number: C07D401/04 ,  C07D213/74 ,  C07D213/84 ,  C07D401/12 ,  C07D401/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14

Abstract: Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 吡啶和嘧啶化合物或其药学上可接受的盐，其中m，n，R1，R2，R3，R4，R5，R6，R7，X1，X2，X3，X4，X5，X6，X7，X8和Y为 如说明书中所定义; 或其药学上可接受的盐，其中环A，m，n，y，R2，R3，R4，R5，R6，R7，R8，R9，X1，X2和环A如说明书中所定义; 和其药学上可接受的盐，其中m，n，y，R2，R3，R4，R5，R6，R7，R9，X1，X2和环A如说明书中所定义; 含有它们的组合物，以及制备这些化合物的方法。 本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相情感障碍，强迫症等。

公开(公告)号：US20110306588A1

公开(公告)日：2011-12-15

申请号：US13106718

申请日：2011-05-12

Applicant: Jennifer R. Allen ,  Daniel B. Horne ,  Essa Hu ,  Matthew R. Kaller ,  Holger Monenschein ,  Thomas T. Nguyen ,  Andreas Reichelt ,  Robert M. Rzasa

Inventor： Jennifer R. Allen ,  Daniel B. Horne ,  Essa Hu ,  Matthew R. Kaller ,  Holger Monenschein ,  Thomas T. Nguyen ,  Andreas Reichelt ,  Robert M. Rzasa

IPC: A61K31/497 ,  C07D413/14 ,  C07D491/107 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/553 ,  A61K31/551 ,  A61K31/498 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  A61P25/00 ,  A61P25/14 ,  A61P25/24 ,  A61P25/30 ,  C07D401/14

CPC classification number: C07D491/107 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10

Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 杂环氧基杂环基化合物和含有它们的组合物，以及这些化合物的制备方法。 本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，亨廷顿舞蹈病，双相情感障碍，强迫症等。

公开(公告)号：US20110306587A1

公开(公告)日：2011-12-15

申请号：US13105860

申请日：2011-05-11

Applicant: Jennifer R. ALLEN ,  Jian J. Chen ,  Michael J. Frohn ,  Essa Hu ,  Qingyian Liu ,  Alexander J. Pickrell ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Wenge Zhong

Inventor： Jennifer R. ALLEN ,  Jian J. Chen ,  Michael J. Frohn ,  Essa Hu ,  Qingyian Liu ,  Alexander J. Pickrell ,  Shannon Rumfelt ,  Robert M. Rzasa ,  Wenge Zhong

IPC: A61K31/4439 ,  A61K31/497 ,  C07D417/14 ,  A61K31/4545 ,  C07D413/14 ,  C07D409/14 ,  C07D491/107 ,  C07D487/10 ,  C07D405/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/00 ,  A61P25/28 ,  A61P25/30 ,  A61P25/24 ,  A61P3/04 ,  A61P25/14 ,  C07D401/14

CPC classification number: C07D401/14 ,  C07C53/18 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/056 ,  C07D491/08 ,  C07D491/107 ,  C07D513/04

Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 式（I）的不饱和氮杂环化合物：如说明书中所定义，含有它们的组合物，以及制备这些化合物的方法。 本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，亨廷顿舞蹈病，非胰岛素依赖性糖尿病，精神分裂症，双相障碍，强迫症等。

公开(公告)号：US08063055B2

公开(公告)日：2011-11-22

申请号：US12711167

申请日：2010-02-23

Applicant: Essa Hu ,  Jason Brooks Human ,  Roxanne Kunz ,  Andrew Tasker ,  Ryan White

Inventor： Essa Hu ,  Jason Brooks Human ,  Roxanne Kunz ,  Andrew Tasker ,  Ryan White

IPC: A61K31/517

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括能够调节c-kit受体的新一类化合物，因此可用于治疗c-kit介导的疾病，包括各种炎性，纤维化和/或肥大细胞介导的疾病如肥大细胞增多症。 化合物具有通式I，其中A0-3和R1-6在本文中定义。 本发明还包括药物组合物，用于治疗c-kit介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

公开(公告)号：US20100125062A1

公开(公告)日：2010-05-20

申请号：US12619573

申请日：2009-11-16

Applicant: Jennifer R. Allen ,  Kaustav Biswas ,  Frank Chavez, Jr. ,  Ning Chen ,  Frenel Fils Demorin ,  James R. Falsey ,  Mike Frohn ,  Paul Harrington ,  Dan Horne ,  Essa Hu ,  Matthew R. Kaller ,  Roxanne Kunz ,  Holger Monenschein ,  Tom Nguyen ,  Alex Pickrell ,  Andreas Reichelt ,  Shannon Rumfelt ,  Rob Rzasa ,  Kelvin Sham ,  Guomin Yao

Inventor： Jennifer R. Allen ,  Kaustav Biswas ,  Frank Chavez, Jr. ,  Ning Chen ,  Frenel Fils Demorin ,  James R. Falsey ,  Mike Frohn ,  Paul Harrington ,  Dan Horne ,  Essa Hu ,  Matthew R. Kaller ,  Roxanne Kunz ,  Holger Monenschein ,  Tom Nguyen ,  Alex Pickrell ,  Andreas Reichelt ,  Shannon Rumfelt ,  Rob Rzasa ,  Kelvin Sham ,  Guomin Yao

IPC: A61K31/4439 ,  C07D401/12 ,  C07D471/04 ,  C07D473/00 ,  C07D413/14 ,  C07D401/14 ,  A61K31/437 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/397 ,  A61P25/00

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/00

Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 吡啶和嘧啶化合物，以及含有它们的组合物，以及制备这些化合物的方法。 本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖型糖尿病，精神分裂症，双相情感障碍，强迫症等。

公开(公告)号：US20090062291A1

公开(公告)日：2009-03-05

申请号：US12196145

申请日：2008-08-21

Applicant: Essa Hu ,  Roxanne Kunz ,  Tom Nixey ,  Stephen Hitchcock

Inventor： Essa Hu ,  Roxanne Kunz ,  Tom Nixey ,  Stephen Hitchcock

IPC: A61K31/502 ,  C07D401/04

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04

Abstract: The present invention is directed to compounds, useful as PDE10 inhibitors, having the formula where R1, R2, R3, R4, X, Y and Z are as defined herein, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

Abstract translation: 本发明涉及可用作PDE10抑制剂的化合物，其具有下式其中R 1，R 2，R 3，R 4，X，Y和Z如本文所定义，含有这些化合物的药物组合物及其制备方法。 本发明还涉及治疗PDE10介导的疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，双相障碍，强迫症等。