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1. 发明专利

AU2009322342A1 Morpholinone compounds as factor IXa inhibitors 未知
公开(公告)号：AU2009322342A1
公开(公告)日：2011-06-30
申请号：AU2009322342
申请日：2009-12-03
申请人： MERCK SHARP & DOHME , MOCHIDA PHARMACEUTICAL CO LTD
发明人： HIDEMITSU NISHIDA , FUMIHIKO SAITOH , TOMOKAZU HIRABAYASHI , SAMUEL CHACKALAMANNIL , TIN-YAU CHAN , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , DWYER MICHAEL P , GREENLEE WILLIAM J , YAN XIA
IPC分类号： C07D265/30 , A61K31/4725 , A61K31/5355 , A61K31/54 , A61K31/553 , A61P7/00 , C07D265/32 , C07D267/10 , C07D279/06 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/04
摘要： The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.

2. 发明专利

AU2008200842B2 Tricyclic thrombin receptor antagonists 未知
公开(公告)号：AU2008200842B2
公开(公告)日：2011-09-15
申请号：AU2008200842
申请日：2008-02-22
申请人： MERCK SHARP & DOHME
发明人： WENXUE WU , SAMUEL CHACKALAMANNIL , YAN XIA , MARIAPPAN CHELLIAH , CLASBY MARTIN C , VELTRI ENRICO P , YUGUANG WANG , GREENLEE WILLIAM J
IPC分类号： C07D405/06 , A61K31/443 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P13/12 , A61P29/00 , A61P35/00 , A61P43/00 , C07D405/14 , C07D417/14
摘要： Heterocyclic-substituted tricyclics of the formula (I) or a pharmaceutically acceptable salt thereof, wherein: 5 the dotted line represents an optional single bond; ----- represents an optional double bond; n is 0-2; Q is cycloalkyl, optionally substituted by R'3 and R14 ; each R" is independently selected from H, (C,-C6 )alkyl, (03 -C5 )cycloalkyl, 10 -(CH 2)neNHC(O)OR'*O, -(CH 2)neNHC(O)R'", -(CH 2),,6NHC(O)NR 4 R5, -(CH 2)neNHSO 2 R0 , -(CH 2)n6 NH S0 2N R4R, and -(CH 2)nsC(O)NR 28 R29 where ne is 0-4, haloalkyl, and halogen; each R14 is independently selected from H, (C,-C)alkyl, -OH, (C-C)alkoxy, R27-aryl(C1-C5)alkyl, heteroaryl, heteroarylalkyl, heterocycyl, is heterocycylalkyl, -(CH 2)n6NHC(O)OR'b, -(CH2)neNHC(O)R'Ib, -(CH 2)neNHC(O)NR 4R5, -(CH 2)meNHSO 2 R, -(CH 2)n6NHSO 2NR4R5 , and -(CH 2)neC(O)NRaR" where n, is 0-4, halogen and haloalkyl; or R's and R14 taken together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms; 20 wherein at least one of R'5 or R" is selected from the group consisting of -(CH 2)neNHC(O)OR"", -(CH 2)neNHC(O) R'O, -(CH 2)neNHC(O)NR 4R', -(CH2)sNHSO 2 R'6 , -(CH 2),nNHSO 2NRR 6, and -(CH 2)neC(O)NR 2 R29 where na is 04; Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and 25 B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. 30 Combination therapy with other cardiovascular agents is also claimed. y- R .3 10 (CH 2)n, R x R R Q (I) Het

3. 发明专利

AU2007207706A1 Cannibinoid receptor modulators 未知
公开(公告)号：AU2007207706A1
公开(公告)日：2007-07-26
申请号：AU2007207706
申请日：2007-01-16
申请人： MERCK SHARP & DOHME
发明人： CLASBY MARTIN C , WANG YUGUANG , CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , GREENLEE WILLIAM J , SCOTT JACK D , XIA YAN , EAGEN KEITH A
IPC分类号： C07D209/44 , C07C233/05 , C07C233/59 , C07D209/46 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.

4. 发明专利

AU2010286933A1 Morpholinone compounds as factor IXa inhibitors 未知
公开(公告)号：AU2010286933A1
公开(公告)日：2012-03-15
申请号：AU2010286933
申请日：2010-06-01
申请人： MERCK SHARP & DOHME , MOCHIDA PHARMACEUTICAL CO LTD
发明人： NISHIDA HIDEMITSU , SAITOH FUMIHIKO , HIRABAYASHI TOMOKAZU , CHACKALAMANNIL SAMUEL , CHAN TIN-YAU , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , DWYER MICHAEL P , GREENLEE WILLIAM J , XIA YAN , NEELAMKAVIL SANTHOSH , SHAH UNMESH G
IPC分类号： C07D265/32 , A61K31/5377 , A61P7/02 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The present invention provides compounds having the formula (I) or a pharmaceutically acceptable salt or a solvate thereof, pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

5. 发明专利

AU2003221932B2 Tricyclic thrombin receptor antagonists 未知
公开(公告)号：AU2003221932B2
公开(公告)日：2007-11-22
申请号：AU2003221932
申请日：2003-04-14
申请人： MERCK SHARP & DOHME
发明人： XIA YAN , CHACKALAMANNIL SAMUEL , GREENLEE WILLIAM J , CHELLIAH MARIAPPAN , CLASBY MARTIN C , VELTRI ENRICO P , WANG YUGUANG
IPC分类号： C07D405/06 , A61K31/443 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P13/12 , A61P29/00 , A61P35/00 , A61P43/00 , C07D405/14 , C07D417/14
摘要： The bisulfate salt of the compound: and its use for the treatment of thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, myocardial infarction, glomerulonephritis, thrombotic stroke, thromboembolic stroke, peripheral vascular diseases, inflammatory disorders, cerebral ischemia or cancer.

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