公开(公告)号：US20090099210A1

公开(公告)日：2009-04-16

申请号：US12340855

申请日：2008-12-22

Applicant: Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Sandra Ann Filla ,  Timothy Pontz ,  Daniel John Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

Inventor： Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Sandra Ann Filla ,  Timothy Pontz ,  Daniel John Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

IPC: A61K31/519 ,  A61P35/00

CPC classification number: C07D498/04 ,  C07D513/04

Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

Abstract translation: 本发明涉及具有结构式（I）的新化合物及其药物组合物及其使用方法。 这些新化合物提供癌症的治疗或预防。

公开(公告)号：US20090054469A1

公开(公告)日：2009-02-26

申请号：US11574036

申请日：2005-08-28

Applicant: Brian Aquila ,  Paul Lyne ,  Timothy Pontz

Inventor： Brian Aquila ,  Paul Lyne ,  Timothy Pontz

IPC: A61K31/517 ,  C07D239/72 ,  A61P35/04

CPC classification number: C07D239/90

Abstract: The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

公开(公告)号：US20060211864A1

公开(公告)日：2006-09-21

申请号：US11364506

申请日：2006-02-28

Applicant: Brian Aquila ,  Thomas Bannister ,  Gregory Cuny ,  James Hauske ,  Michele Heffernan ,  Michael Hoemann ,  Donald Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger Xie

Inventor： Brian Aquila ,  Thomas Bannister ,  Gregory Cuny ,  James Hauske ,  Michele Heffernan ,  Michael Hoemann ,  Donald Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger Xie

IPC: C07D211/06 ,  C07D211/60 ,  C07D211/26 ,  C07D211/28

CPC classification number: C07D211/22 ,  C07D211/26

Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

公开(公告)号：US20090149484A1

公开(公告)日：2009-06-11

申请号：US12297336

申请日：2007-04-17

Applicant: Brian Aquila ,  Paul Lyne ,  Timothy Pontz

Inventor： Brian Aquila ,  Paul Lyne ,  Timothy Pontz

IPC: A61K31/517 ,  C07D239/72 ,  A61P35/00

CPC classification number: C07D239/90 ,  C07D239/88 ,  C07D401/12

Abstract: The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

Abstract translation: 本发明涉及具有B-Raf抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于人或动物体的治疗方法。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

公开(公告)号：US20080153854A1

公开(公告)日：2008-06-26

申请号：US12032438

申请日：2008-02-15

Applicant: Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Sandra Filla ,  Richard William Luke ,  Timothy Pontz ,  Daniel John Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

Inventor： Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Sandra Filla ,  Richard William Luke ,  Timothy Pontz ,  Daniel John Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

IPC: A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC classification number: C07D513/04

Abstract: This invention relates to novel compounds having the formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

Abstract translation: 本发明涉及具有式（I）的新化合物，其中R 1，R 2，R 3，R 4， R 5，R 5，R 6，R 7，R 8和R 9， SUP>如说明书及其药物组合物及其使用方法中所定义。 这些新化合物提供癌症的治疗或预防。

公开(公告)号：US20050080078A1

公开(公告)日：2005-04-14

申请号：US10771519

申请日：2004-02-04

Applicant: Brian Aquila ,  Thomas Bannister ,  Gregory Cuny ,  James Hauske ,  Joanne Holland ,  Paul Persons ,  Heike Radeke ,  Fengjiang Wang ,  Liming Shao

Inventor： Brian Aquila ,  Thomas Bannister ,  Gregory Cuny ,  James Hauske ,  Joanne Holland ,  Paul Persons ,  Heike Radeke ,  Fengjiang Wang ,  Liming Shao

IPC: A61K31/397 ,  A61K31/40 ,  A61K31/445 ,  A61K31/55 ,  C07B61/00 ,  C07C255/46 ,  C07D205/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D211/12 ,  C07D211/16 ,  C07D211/18 ,  C07D211/20 ,  C07D211/26 ,  C07D211/32 ,  C07D211/40 ,  C07D211/42 ,  C07D211/60 ,  C07D233/04 ,  C07D233/10 ,  C07D265/30 ,  C07D267/10 ,  C07D303/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  A61K31/54 ,  A61K31/495 ,  A61K31/496 ,  A61K31/537

CPC classification number: A61K31/397 ,  A61K31/40 ,  A61K31/445 ,  A61K31/55 ,  C07B2200/11 ,  C07C255/46 ,  C07C2601/04 ,  C07D205/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D211/12 ,  C07D211/16 ,  C07D211/18 ,  C07D211/20 ,  C07D211/26 ,  C07D211/32 ,  C07D211/40 ,  C07D211/42 ,  C07D211/60 ,  C07D233/04 ,  C07D233/10 ,  C07D265/30 ,  C07D267/10 ,  C07D303/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C40B40/04

Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.

Abstract translation: 本发明的一个方面涉及一种治疗哺乳动物药物成瘾或药物依赖的方法，其包括向有需要的哺乳动物施用治疗有效量的杂环化合物，例如3-取代哌啶的步骤。 在优选的实施方案中，本发明的方法治疗可卡因成瘾或甲基苯丙胺成瘾。

公开(公告)号：US20100317593A1

公开(公告)日：2010-12-16

申请号：US12796089

申请日：2010-06-08

Applicant: Brian Aquila ,  Edward Hennessy ,  Alexander Hird ,  Vibha Oza ,  Jamal Carlos Saeh ,  Li Sha

Inventor： Brian Aquila ,  Edward Hennessy ,  Alexander Hird ,  Vibha Oza ,  Jamal Carlos Saeh ,  Li Sha

IPC: A61K38/06 ,  C07K7/02 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D403/12

Abstract: Provided herein are 2,3-dihydro-1H-indene compounds, methods for making the compounds, pharmaceutical compositions containing the compounds. The described compounds inhibit IAP proteins and can be used to treat various cancers.

Abstract translation: 本文提供了2,3-二氢-1H-茚化合物，制备该化合物的方法，含有这些化合物的药物组合物。 所述的化合物抑制IAP蛋白并可用于治疗各种癌症。

公开(公告)号：US20080293744A1

公开(公告)日：2008-11-27

申请号：US11573683

申请日：2005-08-16

Applicant: Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Timothy Pontz ,  Daniel John Russell ,  Marie-Elena Theoclitou ,  XiaoLan Zheng

Inventor： Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Timothy Pontz ,  Daniel John Russell ,  Marie-Elena Theoclitou ,  XiaoLan Zheng

IPC: A61K31/519 ,  C07D513/04 ,  A61P35/00

CPC classification number: C07D498/04 ,  C07D513/04

Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

Abstract translation: 本发明涉及具有结构式（I）的新化合物及其药物组合物及其使用方法。 这些新化合物提供癌症的治疗或预防。

公开(公告)号：US20080146570A1

公开(公告)日：2008-06-19

申请号：US11814246

申请日：2006-01-24

Applicant: Brian Aquila ,  Paul Lyne ,  Timothy Pontz

Inventor： Brian Aquila ,  Paul Lyne ,  Timothy Pontz

IPC: A61K31/5377 ,  C07D295/00 ,  A61K31/506 ,  A61P35/00 ,  C07D239/00

CPC classification number: C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12

Abstract: The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof, of the formula (I): which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐：其具有B-Raf抑制活性，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。 本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

公开(公告)号：US20060041129A1

公开(公告)日：2006-02-23

申请号：US11207128

申请日：2005-08-18

Applicant: Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Timothy Pontz ,  Daniel John Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

Inventor： Brian Aquila ,  Michael Howard Block ,  Audrey Davies ,  Jayachandran Ezhuthachan ,  Timothy Pontz ,  Daniel John Russell ,  Maria-Elena Theoclitou ,  XiaoLan Zheng

IPC: A61K31/519 ,  C07D498/02 ,  C07D491/02

CPC classification number: C07D498/04 ,  C07D513/04

Abstract: This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.