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1. 发明申请

WO02079146A3 COMPOUNDS USEFUL AS MODULATORS OF MELANOCORTIN RECEPTORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME 审中-公开
标题翻译：有用的化合物作为MELANOCORTIN受体的调节剂和包含其的药物组合物
公开(公告)号：WO02079146A3
公开(公告)日：2003-02-06
申请号：PCT/US0206581
申请日：2002-03-02
申请人： SQUIBB BRISTOL MYERS CO , YU GUIXUE , MACOR JOHN , HERPIN TIMOTHY , LAWRENCE R MICHAEL , MORTON GEORGE C , RUEL REJEAN , POINDEXTER GRAHAM S , RUEDIGER EDWARD H , THIBAULT CARL
发明人： YU GUIXUE , MACOR JOHN , HERPIN TIMOTHY , LAWRENCE R MICHAEL , MORTON GEORGE C , RUEL REJEAN , POINDEXTER GRAHAM S , RUEDIGER EDWARD H , THIBAULT CARL
IPC分类号： C07D233/64 , A61K31/4178 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4747 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/527 , A61K31/537 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K38/00 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/02 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/14 , A61P5/16 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P11/08 , A61P13/12 , A61P15/00 , A61P15/08 , A61P15/10 , A61P17/00 , A61P17/04 , A61P17/06 , A61P17/14 , A61P17/16 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/06 , A61P31/18 , A61P31/20 , A61P33/06 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D211/32 , C07D211/34 , C07D211/58 , C07D211/60 , C07D211/62 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D495/04 , C07D498/10 , C07K5/06 , C07K5/078 , A61K31/44 , A61K31/445 , A61K31/505 , C07D403/14
CPC分类号： C07D401/12 , A61K38/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10 , C07D487/04 , C07D491/10 , C07D495/04 , C07K5/06139 , C07K5/06191
摘要： Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is formula (II), X is N or CH, W is -NR16R17, -NR16C(=O)R22, -NR16CO2R22, -OR23, or a heteroaryl or heterocyclo group as defined in the specification, and R1 through R12, R16, R17, R22, R23, x, y, and z are as defined in the specification, are useful as modulators of melanocortin receptors, particularly MC-1R and MC-4R.
摘要翻译：式（I）化合物及其药学上可接受的盐，水合物和前药，其中E为式（II），X为N或CH，W为-NR16R17，-NR16C（= O）R22，-NR16CO2R22， -OR23或说明书中定义的杂芳基或杂环基，R1至R12，R16，R17，R22，R23，x，y和z如说明书中所定义，可用作黑皮质素受体的调节剂，特别是 MC-1R和MC-4R。

2. 发明申请

WO2005113511A9 UREA ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS 审中-公开
标题翻译： P2Y1受体的尿素拮抗剂用于治疗血栓病症
公开(公告)号：WO2005113511A9
公开(公告)日：2006-02-02
申请号：PCT/US2005016422
申请日：2005-05-11
申请人： SQUIBB BRISTOL MYERS CO , CHAO HANNGUANG J , TUERDI HUJI , HERPIN TIMOTHY , ROBERGE JACQUES YVES , LIU YALEI , LAWRENCE R MICHAEL , REHFUSS ROBERT P , CLARK CHARLES G , QIAO JENNIFER X , GUNGOR TIMUR , LAM PATRICK Y S , WANG TAMMY C , RUEL REJEAN , L HEUREUX ALEXANDRE L , THIBEAULT CARL , BOUTHILLIER GILLES , SCHNUR DORA M
发明人： CHAO HANNGUANG J , TUERDI HUJI , HERPIN TIMOTHY , ROBERGE JACQUES YVES , LIU YALEI , LAWRENCE R MICHAEL , REHFUSS ROBERT P , CLARK CHARLES G , QIAO JENNIFER X , GUNGOR TIMUR , LAM PATRICK Y S , WANG TAMMY C , RUEL REJEAN , L HEUREUX ALEXANDRE L , THIBEAULT CARL , BOUTHILLIER GILLES , SCHNUR DORA M
IPC分类号： A61K31/4439 , A61K31/444 , A61K31/501 , C07C275/30 , C07C275/32 , C07D213/40 , C07D213/75 , C07D213/89 , C07D231/40 , C07D231/50 , C07D237/22 , C07D333/36 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07F7/18 , A61P7/02
CPC分类号： C07D409/14 , C07C275/30 , C07C275/32 , C07D213/40 , C07D213/75 , C07D213/89 , C07D231/40 , C07D231/50 , C07D237/22 , C07D333/36 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07F7/1856
摘要： The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y 1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y 1 receptor activity.
摘要翻译：本发明提供了新的吡啶基或苯基脲及其类似物，它们是人P2Y 1受体的选择性抑制剂。本发明还提供了相同的各种药物组合物以及治疗对P2Y受体活性的调节作用的疾病的方法。

3. 发明申请

WO0212196A3 LACTAM COMPOUNDS AND THEIR USE AS INHIBITORS OF SERINE PROTEASES AND METHOD 审中-公开
标题翻译： LACTAM化合物及其作为丝氨酸蛋白酶和方法的抑制剂使用
公开(公告)号：WO0212196A3
公开(公告)日：2003-01-16
申请号：PCT/US0122829
申请日：2001-07-20
申请人： SQUIBB BRISTOL MYERS CO , BISACCHI GREGORY S , SEILER STEVEN M , LAWRENCE R MICHAEL , SUTTON JAMES C JR , SLUSARCHYK WILLIAM A , ZHAO GUOHUA
发明人： BISACCHI GREGORY S , SEILER STEVEN M , LAWRENCE R MICHAEL , SUTTON JAMES C JR , SLUSARCHYK WILLIAM A , ZHAO GUOHUA
IPC分类号： C07D223/12 , A61K31/55 , A61K38/00 , A61K45/00 , A61K45/06 , A61P1/00 , A61P1/04 , A61P1/16 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D223/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07K5/06 , C07K5/078 , A61K38/55
CPC分类号： C07D223/10 , A61K31/55 , A61K38/00 , A61K45/06 , C07K5/06139 , C07K5/06191 , A61K2300/00
摘要： Lactam inhibitors are provided which have the structure (I), x is (a) or (b) wherein Y is O or S and R is (i), (ii) or R at least one of R and R is hydrogen, and R , R , R , R , R , R , and R , are as defined herein. These compounds are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating asthma and related diseases are also provided.
摘要翻译：提供了具有结构（I），x是（a）或（b）的内酰胺抑制剂，其中Y是O或S，R 4是（i），（ii）或R 8中的至少一个R R 1和R 2都是氢，R 1，R 2，R 3，R 5，R 6，R 7和R 8分别为本文定义。这些化合物是类胰蛋白酶抑制剂，因此可用于治疗哮喘。还提供了治疗哮喘和相关疾病的方法。

4. 发明申请

WO2007062314A3 HETEROCYCLIC CETP INHIBITORS 审中-公开
标题翻译：杂环类CETP抑制剂
公开(公告)号：WO2007062314A3
公开(公告)日：2007-11-22
申请号：PCT/US2006060978
申请日：2006-11-16
申请人： SQUIBB BRISTOL MYERS CO , SALVATI MARK E , FINLAY HEATHER , HARIKRISHNAN LALGUDI S , JIANG JI , JOHNSON JAMES A , KAMAU MUTHONI G , LAWRENCE R MICHAEL , MILLER MICHAEL M , QIAO JENNIFER X , WANG TAMMY C , WANG YUFENG , YANG WU
发明人： SALVATI MARK E , FINLAY HEATHER , HARIKRISHNAN LALGUDI S , JIANG JI , JOHNSON JAMES A , KAMAU MUTHONI G , LAWRENCE R MICHAEL , MILLER MICHAEL M , QIAO JENNIFER X , WANG TAMMY C , WANG YUFENG , YANG WU
IPC分类号： C07D213/40 , A61K31/435 , A61P3/00 , A61P9/00 , C07D213/61 , C07D277/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
CPC分类号： C07D417/06 , C07D213/40 , C07D213/61 , C07D277/28 , C07D401/04 , C07D401/12 , C07D405/06 , C07D405/12 , C07D417/12
摘要： Compounds of formula Ia and Ib wherein A, B, C and R 1 are described herein.
摘要翻译：其中A，B，C和R 1'的式Ia和Ib化合物在本文中描述。

5. 发明申请

WO2004106295A3 SUBSTITUTED PIPERODINES AND PYRROLIDINES AS CALCIUM SENSING RECEPTOR MODULATORS AND METHOD 审中-公开
标题翻译：作为钙感测受体调节剂和方法的取代的哌嗪和吡咯烷
公开(公告)号：WO2004106295A3
公开(公告)日：2005-12-29
申请号：PCT/US2004016712
申请日：2004-05-27
申请人： SQUIBB BRISTOL MYERS CO , DICKSON JOHN K , LAWRENCE R MICHAEL , ROBERGE JACQUES Y , ROTELLA DAVID P , YANG WU
发明人： DICKSON JOHN K , LAWRENCE R MICHAEL , ROBERGE JACQUES Y , ROTELLA DAVID P , YANG WU
IPC分类号： A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/454 , A61K31/55 , C07D20060101 , C07D207/04 , C07D409/06
CPC分类号： C07D207/06 , C07D207/08 , C07D207/10 , C07D211/18 , C07D211/22 , C07D333/28
摘要： Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula (I) wherein m is 0, 1, 2, 3 or 4; each X is independently selected from the group consisting of hydrogen, halo, cyano, nitro, OCF3, hydroxy, amino, carboxyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, haloalkyl, alkoxy, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkylalkyl, R O, R R N, R OCO, R CO, R R NCO, R R NCONR , R OCONR , R CONR , R S, R SO, R SO2, R R NSO2, R R NSO2NR , and R SO2NR ; R is alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; R and R are the same or different and are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; n is 1, 2, or 3; W is O or H,R ; R is hydrogen or hydroxyl; Ar is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group; Q is hydrogen, F, or hydroxyl. In addition, a method for using these compounds to treat diseases associated with abnormal or mineral homeostasis is also provided.
摘要翻译：提供化合物，其是钙感应受体的拮抗剂，并具有通式（I），其中m为0,1,2,3或4; 每个X独立地选自氢，卤素，氰基，硝基，OCF 3，羟基，氨基，羧基，烷基，烯基，炔基，环烷基，环杂烷基，卤代烷基，烷氧基，烷氧基羰基烷基，羟基羰基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基烷基，R 1 O，R 1 R 2 N，R 1 OCO，R 1 CO，R 1 R 2 NCO，R 1 R 2， NCONR 2a，R 1 OCONR 2a，R 1 CONR 2a，R 1 S，R 1 SO，R 1 SO 2，R 1 R 2 NSO 2 R 1 R 2 NSO 2 NR 2a和R 1 SO 2 NR 2a; R 1是烷基，烯基，炔基，环烷基，环杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基; R 2和R 2a相同或不同并且独立地选自氢，烷基，烯基，炔基，环烷基，环杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基; n为1,2或3; W是O或H，R 3; R 3是氢或羟基; Ar是取代或未取代的芳基或取代或未取代的杂芳基; Q是氢，F或羟基。此外，还提供了使用这些化合物治疗与异常或矿物质内稳态相关疾病的方法。

6. 发明申请

WO02060894A3 SULFONAMIDE LACTAM INHIBITORS OF FACTOR XA 审中-公开
标题翻译：因子XA的磺酰胺衍生物抑制剂
公开(公告)号：WO02060894A3
公开(公告)日：2002-12-19
申请号：PCT/US0202542
申请日：2002-01-28
申请人： SQUIBB BRISTOL MYERS CO , O'CONNOR STEPHEN P , LAWRENCE R MICHAEL , SHI YAN , STEIN PHILIP P
发明人： O'CONNOR STEPHEN P , LAWRENCE R MICHAEL , SHI YAN , STEIN PHILIP P
IPC分类号： C07D487/08 , A61K31/37 , A61K31/42 , A61K31/4365 , A61K31/439 , A61K31/444 , A61K31/445 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/545 , A61K31/55 , A61K31/616 , A61K38/43 , A61K38/46 , A61K45/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P35/04 , A61P37/08 , A61P43/00 , C07D211/56 , C07D211/76 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/18 , C07D491/08 , C07D495/04 , C07D513/04
CPC分类号： C07D211/56 , C07D401/06 , C07D401/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/08 , C07D491/08
摘要： Sulfonamide lactams of the formula (I) wherein X, R , R , R , R , R , R , R , R , R , R and R are as described herein, are provided which inhibitors of Factor Xa and are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.
摘要翻译：式（I）的磺酰胺内酰胺，其中X，R 1，R 2，R 3，R 4，R 4a，R 5，R 5a，R 6， R 6a，R 7和R 8如本文所述，提供了因子Xa的哪种抑制剂并且可用作治疗与血栓形成相关的心血管疾病的抗凝剂。

7. 发明专利

IL268421D0 Modified relaxin polypeptides comprising a pharmacokinetic enhancer and uses thereof 未知
公开(公告)号：IL268421D0
公开(公告)日：2019-09-26
申请号：IL26842119
申请日：2019-08-01
申请人： SQUIBB BRISTOL MYERS CO , LAWRENCE R MICHAEL , HAN XIAOJUN , DUBOWCHIK GENE M , GUDMUNDSSON OLAFUR S , LIPOVSEK DASA , MADSEN CORT S , MAPELLI CLAUDIO , MORIN PAUL E , MYERS MICHAEL C
发明人： LAWRENCE R MICHAEL , HAN XIAOJUN , DUBOWCHIK GENE M , GUDMUNDSSON OLAFUR S , LIPOVSEK DASA , MADSEN CORT S , MAPELLI CLAUDIO , MORIN PAUL E , MYERS MICHAEL C
IPC分类号： C07K20060101
摘要： The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

8. 发明专利

IL259660D0 Apelin receptor agonists and methods of use 未知
公开(公告)号：IL259660D0
公开(公告)日：2018-07-31
申请号：IL25966018
申请日：2018-05-28
申请人： SQUIBB BRISTOL MYERS CO , MYERS MICHAEL C , CHAO HANNGUANG J , FINLAY HEATHER , MENG WEI , LAWRENCE R MICHAEL
发明人： MYERS MICHAEL C , CHAO HANNGUANG J , FINLAY HEATHER , MENG WEI , LAWRENCE R MICHAEL
IPC分类号： C07D20060101
摘要： The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

9. 发明专利

IL255951D0 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders 未知
公开(公告)号：IL255951D0
公开(公告)日：2018-01-31
申请号：IL25595117
申请日：2017-11-27
申请人： SQUIBB BRISTOL MYERS CO , JOHNSON JAMES A , KIM SOONG HOON , LAWRENCE R MICHAEL , MYERS MICHAEL C , CHAO HANNGUANG J , PHILLIPS MONIQUE , JIANG JI
发明人： JOHNSON JAMES A , KIM SOONG HOON , LAWRENCE R MICHAEL , MYERS MICHAEL C , CHAO HANNGUANG J , PHILLIPS MONIQUE , JIANG JI
IPC分类号： C07D20060101
摘要： The present invention provides compounds of Formula (I):wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

10. 发明专利

IL255951A 4-hydroxy-3-(heteroaryl)pyridine-2-one apj agonists for use in the treatment of cardiovascular disorders 未知
公开(公告)号：IL255951A
公开(公告)日：2021-06-30
申请号：IL25595117
申请日：2017-11-27
申请人： SQUIBB BRISTOL MYERS CO , JOHNSON JAMES A , KIM SOONG HOON , LAWRENCE R MICHAEL , MYERS MICHAEL C , CHAO HANNGUANG J , PHILLIPS MONIQUE , JIANG JI
发明人： JOHNSON JAMES A , KIM SOONG-HOON , LAWRENCE R MICHAEL , MYERS MICHAEL C , CHAO HANNGUANG J , PHILLIPS MONIQUE , JIANG JI
摘要： The present invention provides compounds of Formula (I):wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

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