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81. 发明专利

MXPA01011956A OXAZAHETEROCICLOS COMO INHIBIDORES DE PROTEASAS. 未知
公开(公告)号：MXPA01011956A
公开(公告)日：2002-06-21
申请号：MXPA01011956
申请日：2000-05-26
申请人： DIMENSIONAL PHARM INC
发明人： SOLL RICHARD M
IPC分类号： A61K38/00 , A61P1/18 , A61P7/02 , A61P9/10 , A61P11/00 , A61P29/00 , A61P43/00 , C07D413/12 , C07D413/14 , C07K5/06
摘要： La presente invencion describe compuestos de la formula (VII), en donde Het, R1, R7 y A se establecen en la especificacion, asi como hidratos, solvatos o sales farmaceuticamente aceptables de los mismos, que inhiben las enzimas proteoliticas tal como trombina. Tambien se describen metodos para preparar tales compuestos. Los compuestos de la invencion son potentes inhibidores de proteasas, especialmente serina proteasas similares a tripsina, tal como quimiotripsina, tripsina, trombina, plasmina y factor Xa. Ciertos de los compuestos exhiben actividad antitrombotica por via de inhibicion directa, selectiva de trombina. La invencion incluye una composicion para inhibir la perdida de plaquetas en la sangre, inhibir la formacion de agregados de plaquetas en la sangre, inhibir la formacion de fibrina, inhibir la formacion de trombo e inhibir la formacion de embolo en un mamifero, que comprende un compuesto de la invencion en un vehiculo farmaceuticamente aceptable. Otros usos de los compuestos de la invencion son como anticoagulantes ya sea acoplados en o enlazados fisiologicamente a materiales usados en la manufactura de dispositivos usados en la coleccion de sangre, circulacion de sangre y almacenamiento de sangre, tal como cateteres, maquinas de dialisis de sangre, jeringas y tubos de coleccion de sangre, lineas de sangre y cateteres. Adicionalmente, los compuestos pueden marcarse detectablemente y emplearse para la formacion de imagenes in vivo de trombos.

82. 发明专利

AT214693T 未知
公开(公告)号：AT214693T
公开(公告)日：2002-04-15
申请号：AT97948537
申请日：1997-11-26
申请人： DIMENSIONAL PHARM INC
发明人： TOMCZUK BRUCE E , SOLL RICHARD M , LU TIANBAO , FEDDE CYNTHIA L , ILLIG CARL R , MARKOTAN THOMAS P , STAGNARO THOMAS P
IPC分类号： C07D295/22 , A01N1/02 , A61K20060101 , A61K31/155 , A61K31/165 , A61K31/18 , A61K31/225 , A61K31/255 , A61K31/305 , A61K31/335 , A61K31/341 , A61K31/36 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/44 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/535 , A61K33/42 , A61L33/00 , A61P7/00 , A61P7/02 , A61P9/10 , A61P29/00 , C07C20060101 , C07C69/76 , C07C279/00 , C07C279/10 , C07C281/16 , C07C291/04 , C07C303/30 , C07C303/40 , C07C305/00 , C07C309/00 , C07C309/63 , C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/08 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C317/26 , C07C323/17 , C07D20060101 , C07D207/14 , C07D207/16 , C07D207/48 , C07D209/04 , C07D211/22 , C07D211/58 , C07D211/64 , C07D211/96 , C07D213/24 , C07D213/42 , C07D213/74 , C07D215/12 , C07D215/36 , C07D217/12 , C07D217/22 , C07D229/00 , C07D231/04 , C07D237/02 , C07D239/42 , C07D239/72 , C07D243/04 , C07D245/02 , C07D261/02 , C07D263/54 , C07D265/02 , C07D267/04 , C07D269/00 , C07D285/14 , C07D295/12 , C07D307/02 , C07D307/52 , C07D307/66 , C07D311/66 , C07D311/74 , C07D317/08 , C07D317/14 , C07D317/34 , C07D317/40 , C07D317/64 , C07D333/06 , C07D333/34 , C07D333/54 , C07D333/62 , C07D403/04 , C07D413/04 , C07F9/22
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula:wherein X is O or NR and R -R , R -R , R , R , R , R , R , Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.

83. 发明专利

AU7892701A Cyclic oxyguanidine pyrazinones as protease inhibitors 未知
公开(公告)号：AU7892701A
公开(公告)日：2002-01-30
申请号：AU7892701
申请日：2001-07-17
申请人： DIMENSIONAL PHARM INC
发明人： WANG AIHUA , TOMCZUK BRUCE E , LU TIANBAO , SOLL RICHARD M , SPURLINO JOHN C , BONE ROGER FRANCIS
IPC分类号： A61K31/5355 , A61K31/5395 , A61K51/00 , A61L33/00 , A61P7/02 , A61P43/00 , C07D413/12 , C07D413/14 , C07D241/00
摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R 3 , R 4 , R 5 , W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

84. 发明专利

CA2415932A1 CYCLIC OXYGUANIDINE PYRAZINONES AS PROTEASE INHIBICYCLIC OXYGUANIDINE PYRAZINONES AS PROTEASE INHIBITORS TORS 未知
公开(公告)号：CA2415932A1
公开(公告)日：2002-01-24
申请号：CA2415932
申请日：2001-07-17
申请人： DIMENSIONAL PHARM INC
发明人： BONE R GER FRANCIS , SPURLINO JOHN C , SOLL RICHARD M , TOMCZUK BRUCE E , LU TIANBAO , WANG AIHUA
IPC分类号： A61K31/5355 , A61K31/5395 , A61K51/00 , A61L33/00 , A61P7/02 , A61P43/00 , C07D413/12 , C07D413/14 , A61K31/497
摘要： Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula (I): wherein R3, R4, R5, W, and A are as set forth in the specidification, as well as hydrates, solvates or pharmaceutically acceptabl e salts thereof. The compounds of the invention are potent inhibitors of protease, especially trypsin-like serine proteases, such as chymotripsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of trombin. Compositions for inhibiting loss of blood platelas, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thromb us formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines an d stents. Additionally, the compounds can be detectably labeled and employed labeled and employed fot in vivo imaging of thrombi.

85. 发明专利

NO309810B1 未知
公开(公告)号：NO309810B1
公开(公告)日：2001-04-02
申请号：NO975740
申请日：1997-12-05
申请人： DIMENSIONAL PHARM INC
发明人： ILLIG CARL R , SOLL RICHARD M , SALVINO JOSEPH M , TOMCZUK BRUCE E , LU TIANBAO , SUBASINGHE NALIN L
IPC分类号： A61K31/18 , A61K31/195 , A61K31/245 , A61K31/27 , A61K31/435 , A61K31/44 , A61P25/00 , A61P29/00 , A61P35/00 , C07C311/21 , C07C311/44 , C07D213/40 , C07D453/02 , C07C307/02 , C07C317/14 , C07C381/04 , A61K31/165 , A61K31/24
摘要： The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: I or pharmaceutically acceptable salts thereof; wherein R1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 is one of hydrogen, alkyl, cycloalkyl or aryl; R3 is one of hydrogen, hydroxy or alkoxy; R4 is one of -NH2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of -CH2- or -C(O)-; and n is from zero to eleven; provided that when R4 is -NH2, then R3 is hydrogen and n is other than zero; and also provided that when R3 is hydroxy or alkoxy, then R4 is other than -NH2, and n is other than zero.

86. 发明专利

BR9909338A 未知
公开(公告)号：BR9909338A
公开(公告)日：2000-12-12
申请号：BR9909338
申请日：1999-04-05
申请人： DIMENSIONAL PHARM INC
发明人： SOLL RICHARD M , LU TIANBAO , TOMCZUK BRUCE E , MARKOTAN THOMAS P , SIEDEM COLLEEN
IPC分类号： C07D295/18 , A61K31/166 , A61K31/395 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/55 , A61L33/00 , A61P1/18 , A61P7/02 , A61P9/08 , A61P9/10 , A61P29/00 , A61P43/00 , C07C279/00 , C07D211/16 , C07D211/62 , C07D213/40 , C07D213/74 , C07D217/06 , C07D223/04 , C07D295/192
摘要： The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I:wherein X is O or NH, L is -O- or -SO2-, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage.

87. 发明专利

NO20004871A 未知
公开(公告)号：NO20004871A
公开(公告)日：2000-11-30
申请号：NO20004871
申请日：2000-09-28
申请人： DIMENSIONAL PHARM INC
发明人： SOLL RICHARD M , LU TIANBAO , TOMCZUK BRUCE E , MARKOTAN THOMAS P , SIEDEM COLLEEN
IPC分类号： C07D295/18 , A61K31/166 , A61K31/395 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/445 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/55 , A61L33/00 , A61P1/18 , A61P7/02 , A61P9/08 , A61P9/10 , A61P29/00 , A61P43/00 , C07C279/00 , C07D211/16 , C07D211/62 , C07D213/40 , C07D213/74 , C07D217/06 , C07D223/04 , C07D295/192
CPC分类号： C07D213/40 , C07C279/00 , C07D211/16 , C07D211/62 , C07D213/74 , C07D217/06 , C07D295/192

88. 发明专利

NZ319474A Guanidino protease inhibitors 未知
公开(公告)号：NZ319474A
公开(公告)日：2000-01-28
申请号：NZ31947496
申请日：1996-09-27
申请人： DIMENSIONAL PHARM INC
发明人： LU TIANBAO , ILLIG CARL R , TOMCZUK BRUCE E , SOLL RICHARD M , SUBASINGHE NALIN L , BONE ROGER F
IPC分类号： A61K31/00 , A61K31/155 , A61K31/24 , A61K31/445 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P29/00 , A61P43/00 , C07C279/04 , C07C279/08 , C07C279/12 , C07C309/73 , C07C311/21 , C07D211/22 , C07D211/26 , C07D211/34 , C07D295/215 , A61K31/18
摘要： he compounds of the present invention represent a novel class of potent inhibitors of metallo, acid, thiol and serine proteases. Examples of the serine proteases inhibited by compounds within the scope of the invention include leukocyte neutrophil elastase, a proteolytic enzyme implicated in the pathogenesis of emphysema, chymotrypsin and trypsin, digestive enzymes, pancreatic elastase, and cathepsin G, a chymotrypsin-like protease also associated with leukocytes; thrombin and factor Xa, proteolytic enzymes in the blood coagulation pathway. Inhibition of thermolysin, a metalloprotease and pepsin, an acid protease, are also contemplated uses of compounds of the present invention. An end use application of the compounds that inhibit chymotrypsin and trypsin is in the treatment of pancreatitis. R1 is C6-12 alkyl, cycloalkyl, alkenyl, alkynyl, aryl, aralkyl or heteroaryl, any of which may be optionally substituted; Z is -NR10SO2-, -SO2-NR10-,-NR10C(RyRz)-,-C(RyRz) -NR10-,-SO2-,-SO2O-, OC(RyRz)-,C(RyRz)O-, NR10CO-or -CONR10-, Y is -O-,-NR5-, -S-,-CR5R9- or a covalent bond; W is N or CR10 R2,R3,R4,Ra,Rb and Rc and other variables are common substituents as defined in the specification

89. 发明专利

CA2329929A1 AMINO ACID AMIDINOHYDRAZONES, ALKOXYGUANIDINES AND AMINOGUANIDINES AS PROTEASE INHIBITORS 未知
公开(公告)号：CA2329929A1
公开(公告)日：1999-11-04
申请号：CA2329929
申请日：1999-04-22
申请人： DIMENSIONAL PHARM INC
发明人： LU TIANBAO , SOLL RICHARD M , TOMCZUK BRUCE , MARKOTAN THOMAS P
IPC分类号： C07D223/16 , A61K31/40 , A61K38/00 , A61K51/00 , A61L33/00 , A61P7/02 , C07C279/24 , C07D207/16 , C07K5/02 , C07K5/06 , C07K5/065 , C07F9/06
摘要： The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula (I) wherein X is O or NR19 and A1, A2, R7-R10, R18, Ra, Rb, Rc, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula (I). Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage.

90. 发明专利

BR9609216A 未知
公开(公告)号：BR9609216A
公开(公告)日：1999-07-27
申请号：BR9609216
申请日：1996-06-07
申请人： DIMENSIONAL PHARM INC
发明人： ILLIG CARL R , SOLL RICHARD M , SALVINO JOSEPH M , TOMCZUK BRUCE E , LU TIANBAO , SUBASINGHE NALIN L
IPC分类号： A61K31/18 , A61K31/195 , A61K31/245 , A61K31/27 , A61K31/435 , A61K31/44 , A61P25/00 , A61P29/00 , A61P35/00 , C07C311/21 , C07C311/44 , C07D213/40 , C07D453/02 , A61K31/165 , A61K31/24 , C07C229/00 , C07C307/02 , C07C317/14 , C07C381/04 , C07D211/82
摘要： The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: I or pharmaceutically acceptable salts thereof; wherein R1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R2 is one of hydrogen, alkyl, cycloalkyl or aryl; R3 is one of hydrogen, hydroxy or alkoxy; R4 is one of -NH2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of -CH2- or -C(O)-; and n is from zero to eleven; provided that when R4 is -NH2, then R3 is hydrogen and n is other than zero; and also provided that when R3 is hydroxy or alkoxy, then R4 is other than -NH2, and n is other than zero.

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