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41. 发明专利

MY144040A TRICYCLIC THROMBIN RECEPTOR ANTAGONISTS 未知
公开(公告)号：MY144040A
公开(公告)日：2011-07-29
申请号：MYPI20031400
申请日：2003-04-14
申请人： SCHERING CORP
发明人： SAMUEL CHACKALAMANNIL , CLASBY MARTIN C , GREENLEE WILLIAM J , YUGUANG WANG , YAN XIA , VELTRI ENRICO P , MARIAPPAN CHELLIAH , WU WENXUE
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： OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, WHEREIN:THE DOTTED LINE REPRESENTS AN OPTIONAL SINGLE BOND;-------- REPRESENTS AN OPTIONAL DOUBLE BOND;N IS 0-2; Q IS CYCLOALKYL, OPTIONALLY SUBSTITUTED BY R13 AND R14; R13 AND R14 ARE IDEPENDENTLY SELECTED FROM (C1-C6)ALKYL, (C3-C8)CYCLOALKYL, -OH,(C1-C6)ALKOXY, R27-ARYL(C1-C6)ALKYL, HETEROARYL, HETEROARYLALKYL, HETEROCYCLYL, HETEROCYCLYLALKYL, HALOGEN AND HALOALKYL; OR R13 AND R14 TOGETHER FORM A SPIROCYCLIC OR A HETEROSPIROCYCLIC RING OF 3-6 ATOMS; HET IS A MONO- OR BI-CYCLIC OPTIONALLY SUBSTITUTED HETEROARYL GROUP; AND 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, HEAT FAILURE, AND CANCER BY ADMINISTERING SAID COMPOUNDS. COMBINATION THERAPY WITH OTHER CARDIOVASCULAR AGENTS IS ALSO CLAIMED.

42. 发明专利

MY143987A CONSTRAINED HIMBACINE ANALOGS AS THROMBIN RECEPTOR ANTAGONISTS 未知
公开(公告)号：MY143987A
公开(公告)日：2011-07-29
申请号：MYPI20052380
申请日：2005-05-25
申请人： SCHERING CORP
发明人： CHELLIAH MARIAPPAN V , TEDDY KOSOGLOU , MADHU CHINTALA , SAMUEL CHACKALAMANNIL , YAN XIA , CLASBY MARTIN C , GREENLEE WILLIAM J , YUGUANG WANG , VELTRI ENRICO P , WENXUE WU , GRAZIANO MICHAEL P
IPC分类号： C07D405/08 , A61K31/443 , A61K31/4433 , A61P9/00 , A61P11/00 , A61P25/28 , C07D405/06 , C07D493/04
摘要： A COMPOUND REPRESENTED BY THE STRUCTURAL FORMULA AND PHARMACEUTICALLY ACCEPTABLE SALTS AND SOLVENTS THEREOF IS DISCLOSED, WHEREIN: THE SINGLE-DASHED LINE---- BETWEEN THE RING CARBONS TO WHICH R¹⁰ AND R³⁴ ARE ATTACHED REPRESENTS EITHER A SINGLE BOND OR A DOUBLE BOND; THE DOUBLE-DASHED LINE ==== BETWEEN X AND THE CARBON TO WHICH Y IS ATTACHED REPRESENTS EITHER A SINGLE BOND OR AN ABSENT BOND; X IS -O- OR -NR⁶- WHEN THE DOUBLE-DASHED LINE REPRESENTS A SINGLE BOND; X IS H, -OH OR -NHR²⁰ WHEN THE DOUBLE-DASHED LINE REPRESENTS AN ABSENT BOND; AND OTHER PARAMETERS ARE AS DEFINED HEREIN. ALSO DISCLOSED ARE PHARMACEUTICAL COMPOSITIONS AND COMBINATIONS CONTAINING SAID COMPOUNDS AND THEIR USES AS THROMBIN RECEPTOR ANTAGONISTS AND BINDERS TO CANNABINOID RECEPTORS.

43. 发明专利

NO330500B1 未知
公开(公告)号：NO330500B1
公开(公告)日：2011-05-02
申请号：NO20044963
申请日：2004-11-15
申请人： SCHERING CORP
发明人： GREENLEE WILLIAM J , CHACKALAMANNIL SAMUEL , WANG YUGUANG , XIA YAN , CLASBY MARTIN C , CHELLIAH MARIAPPAN , VELTRI ENRICO P , WU WENXUE
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.

44. 发明专利

CL2009001214A1 Compuestos derivados de heterociclo, moduladores de serina proteasas composicion fa 未知
公开(公告)号：CL2009001214A1
公开(公告)日：2010-12-31
申请号：CL2009001214
申请日：2009-05-18
申请人： SCHERING CORP
发明人： CHACKALAMANNIL SAMUEL , XIA YAN , GREENLEE WILLIAM J , CLASBY MARTIN C , GAO XIAOBANG , CHELLIAH MARIAPPAN V , EAGEN
IPC分类号： A61K31/4155 , A61P7/02 , C07D209/00 , C07D213/06 , C07D231/18 , C07D235/00 , C07D235/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D487/04
摘要： Compuestos heterocíclicos moduladores de la serina proteasa, composición farmacéutica, útil para el tratamiento de un trastorno mediado por el factor ixa, donde dicho trastorno es un trastorno tromboembólico.

45. 发明专利

SG164279A1 TRICYCLIC THROMBIN RECEPTOR ANTAGONISTS 未知
公开(公告)号：SG164279A1
公开(公告)日：2010-09-29
申请号：SG2006072177
申请日：2003-04-14
申请人： SCHERING CORP
发明人： CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , XIA YAN , VELTRI ENRICO P , CHELLIAN MARIAPPAN , WU WENXUE
IPC分类号： A61K31/443 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P13/12 , A61P29/00 , A61P35/00 , A61P43/00 , C07D405/06 , C07D405/14 , C07D417/14
摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond; represents an optional double bond; n is 0-2; Q is R-substituted cycloalkyl, optionally additionally substituted by R13 and R14; R is ûNHCOOR16b, -NHCOR16b, -NHCONR4R5 or -NHSO2R16; Het is a mono- or bi-cyclic optionally substituted heteroaromatic group; and 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. Combination therapy with other cardiovascular agents is also claimed.

46. 发明专利

CA2745121A1 MORPHOLINONE COMPOUNDS AS FACTOR IXA INHIBITORS 未知
公开(公告)号：CA2745121A1
公开(公告)日：2010-06-10
申请号：CA2745121
申请日：2009-12-03
申请人： MOCHIDA PHARM CO LTD , SCHERING CORP
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
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.

47. 发明专利

AT457988T 未知
公开(公告)号：AT457988T
公开(公告)日：2010-03-15
申请号：AT07796492
申请日：2007-06-25
申请人： SCHERING CORP
发明人： CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , STAMFORD ANDREW
IPC分类号： C07D487/04 , A61K31/522 , A61P25/16
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein: X1 and X2 are 1-3 substituents independently selected from the group consisting of H, alkyl, halo, —CF3, —OCF3, alkoxy, —OH and —CN; n is 0, 1 or 2; and R and R1 are H or alkyl; also disclosed is the use of the compounds in the treatment of CNS diseases such as Parkinson's disease, alone or in combination with other agents for treating CNS diseases, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

48. 发明专利

PE20091972A1 COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DEL FACTOR IXA 未知
公开(公告)号：PE20091972A1
公开(公告)日：2010-01-15
申请号：PE2009000694
申请日：2009-05-18
申请人： SCHERING CORP
发明人： CLASBY MARTIN C , GREENLEE WILLIAM J , CHACKALAMANNIL SAMUEL , XIA YAN , GAO XIAOBANG , CHELLIAH MARIAPPAN V , EAGEN KEITH A , VACCARO HENRY A , CHAN TIN-YAU , MCKITTRICK BRIAN A , WANG LI YUAN , PU HAIYAN
IPC分类号： A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , C07D231/18
摘要： SE REFIERE A DERIVADOS HETEROCICLICOS DE FORMULA (I), DONDE A Y ES UN ANILLO HETEROARILO; X ES N, NR; Y ES N, NR, O, S; L ES -C(=O)N(R)-, -N(R)-C(=O)-, -S(=O)2NR, -N(R)S(=O)2; Q ES NR, S, O; R ES H, ALQUILO, HALOALQUILO, ENTRE OTROS; R1 ES CICLOALQUILO, CICLOALQUENILO, HETEROCICLILO, ENTRE OTROS; R2 Y R3 SON CADA UNO H, ALQUILO, CICLOALQUILO, ENTRE OTROS; n ES 0-2; Z ES H, HALO, ALQUILO, ENTRE OTROS. TAMBIEN SE REFIERE A UN METODO DE PREPARACION PARA COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENE. DICHOS COMPUESTOS SON INHIBIDORES SELECTIVOS DEL FACTOR IXa DE LA CASCADA DE LA COAGULACION, SIENDO DE UTILIDAD EN EL TRATAMIENTO DE TRASTORNOS TROMBOEMBOLICOS TAL COMO SINDROME CORONARIO AGUDO, FIBRILACION ATRIAL, ENTRE OTROS

49. 发明专利

ES2327145T3 ANATAGONISTAS DEL RECEPTOR DE ADENOSINA A2A DE PIRAZOLO(1,5-A)PIRIMIDINA SUSTITUIDOS. 未知
公开(公告)号：ES2327145T3
公开(公告)日：2009-10-26
申请号：ES05854388
申请日：2005-12-19
申请人： SCHERING CORP
发明人： CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , NEUSTADT BERNARD R , GAO XIAOBANG
IPC分类号： C07D487/04
摘要： Un compuesto representado por la fórmula estructural I ** ver fórmula** o una de sus sales farmacéuticamente aceptables, donde: A es alquileno, R 16 -arileno, R 16 -cicloalquileno o R 16 -heteroarildiilo; X es -C(O)- o -S(O)2-; R 1 es alquilo o cicloalquilo; R 2 es hidrógeno, halo o -CN; R 3 es hidrógeno o alquilo; R 4 es hidrógeno, alquilo, alcoxi, hidroxialquilo, -alquil-NR 14 R 15 , cicloalquilo, heterocicloalquilo, heterocicloalquilo sustituido con alquilo, R 8 -arilalquilo o R 8 -heteroarilalquilo; o R 3 y R 4 , junto con el nitrógeno al que están anclados, forman un anillo de 5-7 miembros, comprendiendo opcionalmente dicho anillo un miembro anular heteroatómico adicional seleccionado del grupo que consiste en -O-, -S- y -N(R 17 )-, estando opcionalmente sustituido dicho anillo con alquilo, hidroxialquilo, R 8 -arilalquilo, R 8 - heteroaril-alquilo, -N(R 9 )-C(O)alquilo, -CO2-alquilo, -C(O)NR 10 R 11 o heterocicloalquilo; o R 3 y R 4 , junto con el nitrógeno al que están anclados, forman el grupo ** ver fórmula** R 7 es alquilo, R 12 -fenilo, R 12 -heteroarilo, cicloalquilo, halo, morfolinilo,** ver fórmula** n es 1 o 2; R 8 es de 1 a 3 sustituyentes seleccionas independientemente del grupo que consiste en hidrógeno, alquilo, halo, alcoxi, -CO 2H, -CO 2-alquilo, -CF 3, -CN, -CO 2NR 14 R 15 , -SO 2-alquilo, -SO 2NR 14 R 15 y -NR 14 R 15 ; R 9 es hidrógeno o alquilo; R 10 y R 11 se seleccionan independientemente del grupo que consiste en alquilo y cicloalquilo; o R 10 y R 11 forman una cadena alquilénica C4-C5 y junto con el nitrógeno al que están anclados, forman un anillo de 5 o 6 miembros; R 12 es de 1 a 3 sustituyentes seleccionas independientemente del grupo que consiste en hidrógeno, alquilo, halo, alcoxi, -CO2H, -CO2-alquilo, -CF3, -CN, -CO2NR 14 R 15 , -SO2-alquilo, -SO2NR 14 R 15 y -NR 14 R 15 ; R 13 es H, OH, hidroxialquilo o alquilo; R 14 y R 15 se seleccionan independientemente del grupo que consiste en hidrógeno, alquilo y cicloalquilo; donde: R 16 es de 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en hidrógeno, alquilo, halo, OH y alcoxi; y R 17 es hidrógeno, alquilo, cicloalquilo o R 8 -arilalquilo; "alquilo" significa un grupo hidrocarbonado alifático que puede ser lineal o ramificado y que comprende de 1 a 6 átomos de carbono en la cadena; "alquileno" significa una cadena alquílica divalente; "alcoxi" significa un grupo alquil-O- en el que el grupo alquilo se describe como antes; "halo" significa fluoro, cloro, bromo o yodo; "arilo" significa un anillo carbocíclico aromático sencillo o un anillo carbocíclico fusionado bicíclico de 6 a 10 átomos de carbono; "heteroarilo" significa un grupo heteroaromático de anillo sencillo de 5 a 6 átomos que comprende de 2 a 5 átomos de carbono y de 1 a 3 heteroátomos seleccionados independientemente del grupo que consiste en N, O y S, o un grupo heteroaromático bicíclico de 5 a 10 átomos que comprende de 1 a 9 átomos de carbono y de 1 a 3 heteroátomos seleccionados independientemente del grupo que consiste en N, O y S, siempre que los anillos no incluyan átomos de oxígeno y/o azufre adyacentes; "heteroarildiilo" significa un anillo de heteroarilo unido a dos grupos diferentes; "arileno" significa un anillo de arilo divalente, esto es, un anillo de arilo unido a dos grupos diferentes; "cicloalquilo" significa un sistema anular mono- o multicíclico no aromático que comprende de 3 a 10 átomos de carbono; "cicloalquileno" significa un anillo de cicloalquilo divalente, esto es, un anillo de cicloalquilo unido a dos grupos diferentes; y "heterocicloalquilo" significa un anillo saturado de 3 a 6 miembros que comprende de 2 a 5 átomos de carbono y 1 o 2 heteroátomos seleccionados del grupo que consiste en N, S y O, siempre que dos heteroátomos no sean adyacentes entre sí.

50. 发明专利

DE602005014891D1 未知
公开(公告)号：DE602005014891D1
公开(公告)日：2009-07-23
申请号：DE602005014891
申请日：2005-12-19
申请人： SCHERING CORP
发明人： CLASBY MARTIN C , CHACKALAMANNIL SAMUEL , NEUSTADT BERNARD R , GAO XIAOBANG
IPC分类号： C07D487/04
摘要： Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.

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