公开(公告)号：WO2009149259A3

公开(公告)日：2009-12-10

申请号：PCT/US2009/046259

申请日：2009-06-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  ALBANY MOLECULAR RESEARCH, INC. ,  LOBBEN, Paul ,  ZHAO, Rulin ,  WANG, Bei ,  CHEN, Bang-chi ,  LIU, Shuang ,  HU, Min ,  YANG, Yuh-Lin, Allen ,  ISHERWOOD, Matthew ,  AMIN, Rasidul ,  CUI, Wenge

Inventor： LOBBEN, Paul ,  ZHAO, Rulin ,  WANG, Bei ,  CHEN, Bang-chi ,  LIU, Shuang ,  HU, Min ,  YANG, Yuh-Lin, Allen ,  ISHERWOOD, Matthew ,  AMIN, Rasidul ,  CUI, Wenge

IPC: C07D401/04

Abstract: Disclosed are processes for preparing tetrahydroisoquinolines, intermediates useful in the preparation of tetrahydroisoquinolines, processes for preparing such intermediates, and a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. Also disclosed are pharmaceutical compositions comprising tetrahydroisoquinolines, methods of using tetrahydroisoquinolines in the treatment of depression and other conditions and methods for obtaining the crystalline form.

公开(公告)号：WO2006036949A3

公开(公告)日：2006-06-01

申请号：PCT/US2005034553

申请日：2005-09-27

Applicant: SQUIBB BRISTOL MYERS CO ,  ZHANG HUIPING ,  CHEN BANG-CHI ,  ZHAO RULIN

Inventor： ZHANG HUIPING ,  CHEN BANG-CHI ,  ZHAO RULIN

IPC: C07D211/40

CPC classification number: C07D213/64

Abstract: A novel process and intermediates thereof for making N-aryl pyridones of the type shown below from appropriate pyridinolates is described. These compounds are useful as intermediates for the synthesis of clinical candidates.

Abstract translation: 描述了由合适的吡啶盐酸盐制备下列类型的N-芳基吡啶酮的新方法及其中间体。 这些化合物可用作合成临床候选物的中间体。

公开(公告)号：WO2006036926B1

公开(公告)日：2007-03-15

申请号：PCT/US2005034511

申请日：2005-09-27

Applicant: SQUIBB BRISTOL MYERS CO ,  MUDRYK BOGUSLAW M ,  CUNIERE NICOLAS ,  HSIEH DAU-MING ,  ROSSANO LUCIUS ,  LIANG JING ,  CHEN BANG-CHI ,  ZHANG HUIPING ,  ZHAO RULIN ,  WANG BEI ,  DAVID ADRIAN

Inventor： MUDRYK BOGUSLAW M ,  CUNIERE NICOLAS ,  HSIEH DAU-MING ,  ROSSANO LUCIUS ,  LIANG JING ,  CHEN BANG-CHI ,  ZHANG HUIPING ,  ZHAO RULIN ,  WANG BEI ,  DAVID ADRIAN

IPC: C07D471/04 ,  A61K31/437 ,  A61P7/02

CPC classification number: C07D471/04

Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. Formula (I). These compounds can be useful as factor Xa inhibitors.

Abstract translation: 描述了从合适的苯基肼制备下文所示类型的4,5-二氢 - 吡唑并[3,4-c]吡啶-2-酮的新方法和中间体。 公式（I）。 这些化合物可用作Xa因子抑制剂。

公开(公告)号：WO2006036949A2

公开(公告)日：2006-04-06

申请号：PCT/US2005/034553

申请日：2005-09-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  ZHANG, Huiping ,  CHEN, Bang-Chi ,  ZHAO, Rulin

Inventor： ZHANG, Huiping ,  CHEN, Bang-Chi ,  ZHAO, Rulin

IPC: C07D213/70

CPC classification number: C07D213/64

Abstract: A novel process and intermediates thereof for making N-aryl pyridones of the type shown below from appropriate pyridinolates is described. These compounds are useful as intermediates for the synthesis of clinical candidates.

Abstract translation: 描述了用于从合适的吡啶醇合物制备下文所示类型的N-芳基吡啶酮的新方法和其中间体。 这些化合物可用作合成临床候选药物的中间体。

公开(公告)号：WO2005076990A2

公开(公告)日：2005-08-25

申请号：PCT/US2005/003807

申请日：2005-02-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  CHEN, Bang-Chi ,  ZHAO, Rulin ,  WANG, Bei

Inventor： CHEN, Bang-Chi ,  ZHAO, Rulin ,  WANG, Bei

IPC: C07D277/56 ,  C07D417/12

CPC classification number: C07D277/56 ,  C07D417/12

Abstract: The invention is directed to processes for preparing 2-aminothiazole-5-carboxamides of formula (I), wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined as set forth in the specification herein.

Abstract translation: 本发明涉及制备式（I）的2-氨基噻唑-5-甲酰胺的方法，其中R 1，R 2， R 3，R 4和R 5的定义如本文说明书中所述。

公开(公告)号：WO2004072030A2

公开(公告)日：2004-08-26

申请号：PCT/US2004/003223

申请日：2004-02-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  CHEN, Bang-Chi ,  ZHAO, Rulin ,  SUNDEEN, Joseph, Edward ,  LEFTHERIS, Katerina ,  HYNES, John ,  WROBLESKI, Stephen, T.

Inventor： CHEN, Bang-Chi ,  ZHAO, Rulin ,  SUNDEEN, Joseph, Edward ,  LEFTHERIS, Katerina ,  HYNES, John ,  WROBLESKI, Stephen, T.

IPC: C07D

CPC classification number: C07D487/04

Abstract: An improved process for the preparation of certain pyrrolotriazine compounds is disclosed. The compounds exhibit utility as kinase inhibitors.

Abstract translation: 公开了制备某些吡咯并三嗪化合物的改进方法。 这些化合物表现出作为激酶抑制剂的作用。

公开(公告)号：WO0158869B1

公开(公告)日：2002-02-21

申请号：PCT/US0104131

申请日：2001-02-08

Applicant: SQUIBB BRISTOL MYERS CO ,  LEFTHERIS KATERINA ,  ZHAO RULIN ,  CHEN BANG CHI ,  KIENER PETER ,  WU HONG ,  PANDIT CHENNAGIRI R ,  WROBLESKI STEPHEN ,  CHEN PING ,  HYNES JOHN JR ,  LONGPHRE MALINDA ,  NORRIS DEREK J ,  SPERGEL STEVEN ,  TOKARSKI JOHN

Inventor： LEFTHERIS KATERINA ,  ZHAO RULIN ,  CHEN BANG-CHI ,  KIENER PETER ,  WU HONG ,  PANDIT CHENNAGIRI R ,  WROBLESKI STEPHEN ,  CHEN PING ,  HYNES JOHN JR ,  LONGPHRE MALINDA ,  NORRIS DEREK J ,  SPERGEL STEVEN ,  TOKARSKI JOHN

IPC: A61K31/40 ,  A61K31/404 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4353 ,  A61K31/438 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/551 ,  A61K45/00 ,  A61P11/00 ,  A61P11/06 ,  C07D207/337 ,  C07D207/40 ,  C07D207/416 ,  C07D209/08 ,  C07D209/42 ,  C07D231/14 ,  C07D231/56 ,  C07D233/90 ,  C07D257/04 ,  C07D263/32 ,  C07D271/06 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D498/04 ,  C07D498/06 ,  C07D207/34 ,  C07D401/14 ,  C07D407/12

CPC classification number: C07D207/416 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  C07D209/42 ,  C07D231/14 ,  C07D231/56 ,  C07D233/90 ,  C07D257/04 ,  C07D263/32 ,  C07D271/06 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08

Abstract: Use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed. Compounds useful as cannabinoid receptor modulators for treating respiratory and non-respiratory leukocyte-activation associated diseases comprise compounds of formula (I), in which A and B are nitrogen or carbon, provided only one of A and B is nitrogen; and R1-R6 are as defined in the specification, wherein R2 with R5 may form a ring, and/or two R4 groups may form a six-membered aryl or heteroaryl ring, optionally having a substituent R6 forming a ring with R3.

Abstract translation: 公开了在化合物是大麻素受体调节剂的哺乳动物中用于治疗呼吸系统疾病的化合物的用途。 用作治疗呼吸道和非呼吸性白细胞活化相关疾病的大麻素受体调节剂的化合物包括式（I）化合物，其中A和B为氮或碳，只提供A和B之一为氮; 和R 1 -R 6如说明书中所定义，其中R 2与R 5可以形成环，和/或两个R 4基团可以形成六元芳基或杂芳基环，任选地具有与R 3形成环的取代基R 6。

公开(公告)号：WO2008014360A3

公开(公告)日：2008-01-31

申请号：PCT/US2007/074377

申请日：2007-07-26

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  CARTER, Percy, H. ,  DUNCIA, John, V. ,  MUDRYK, Boguslaw, M. ,  RANDAZZO, Michael, E. ,  XIAO, Zili ,  YANG, Michael, G. ,  ZHAO, Rulin

Inventor： CARTER, Percy, H. ,  DUNCIA, John, V. ,  MUDRYK, Boguslaw, M. ,  RANDAZZO, Michael, E. ,  XIAO, Zili ,  YANG, Michael, G. ,  ZHAO, Rulin

IPC: C07D403/12 ,  C07D207/273 ,  A61K31/4025 ,  C07D317/72

Abstract: The present invention provides a novel antagonist or partial agonists/antagonist of MCP-I receptor activity: N-((lR,2S,5R)-5-( tert -butylamino)-2- ((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l- yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((lR,2S,5R)-5-( tert -butylamino)-2-((S)-2-oxo-3-(6- (trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide: wherein R 1 , R 8 , R 9 , R 10 , and "HET" are as described herein. Compounds that are useful intermediates of the process are also provided herein.

公开(公告)号：WO2006135425A3

公开(公告)日：2007-02-22

申请号：PCT/US2005034551

申请日：2005-09-27

Applicant: SQUIBB BRISTOL MYERS CO ,  ZHAO RULIN ,  CHEN BANG-CHI ,  WANG BEI ,  ZHANG HUIPING

Inventor： ZHAO RULIN ,  CHEN BANG-CHI ,  WANG BEI ,  ZHANG HUIPING

IPC: C07D471/16

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4­ c]pyrid-2-ones of the type shown below, as well as the corresponding pyrazoles, from appropriate phenyl hydrazines is described. O (R2b) 0-2 R1 I I 1 1-a X 2 N N-, R a' ­ IV These compounds can be useful as factor Xa inhibitors.

Abstract translation: 描述了用于制备下列所示类型的4,5-二氢 - 吡唑并[3,4-C]吡啶-2-酮的新方法及其中间体，以及相应的吡唑。 O（R2b）0-2 R1 II 1 1-a X 2 N N - ， - - - SIPO - >这些化合物可用作 因子Xa抑制剂。

公开(公告)号：WO2006135425A2

公开(公告)日：2006-12-21

申请号：PCT/US2005/034551

申请日：2005-09-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  ZHAO, Rulin ,  CHEN, Bang-Chi ,  WANG, Bei ,  ZHANG, Huiping

Inventor： ZHAO, Rulin ,  CHEN, Bang-Chi ,  WANG, Bei ,  ZHANG, Huiping

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4­ c]pyrid-2-ones of the type shown below, as well as the corresponding pyrazoles, from appropriate phenyl hydrazines is described. O (R2b) 0-2 R1 I I 1 1-a X 2 N N-, R a' ­ IV These compounds can be useful as factor Xa inhibitors.

Abstract translation: 描述了用于制备下列所示类型的4,5-二氢 - 吡唑并[3,4-C]吡啶-2-酮的新方法及其中间体，以及相应的吡唑。 O（R2b）0-2 R1 II 1 1-a X 2 N N - ， - - - SIPO - >这些化合物可用作 因子Xa抑制剂。