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11. 发明申请

US20090275582A1 Bi-Aryl Meta-Pyrimidine Inhibitors of Kinases 有权
标题翻译：双芳基甲基嘧啶抑制剂的激酶
公开(公告)号：US20090275582A1
公开(公告)日：2009-11-05
申请号：US12253374
申请日：2008-10-17
申请人： Glenn Noronha , John D. Hood , Richard M. Soll
发明人： Glenn Noronha , John D. Hood , Richard M. Soll
IPC分类号： A61K31/506 , A61P35/00 , A61K31/5377 , A61K31/505
CPC分类号： C07D239/48 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non-receptor kinases.
摘要翻译：本发明提供具有一般结构（A）的联芳基间 - 嘧啶化合物。本发明的嘧啶化合物能够抑制激酶，例如Jak激酶家族的成员和各种其它特异性受体和非受体激酶。

12. 发明授权

US06638931B1 Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：氨基胍和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：US06638931B1
公开(公告)日：2003-10-28
申请号：US09722363
申请日：2000-11-28
申请人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan , Thomas P. Stagnaro
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan , Thomas P. Stagnaro
IPC分类号： A61K31255
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, 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 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.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12，说明书中列出的R a，R b，R c，Y，Z，n和m以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐是描述。还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。

13. 发明授权

US06518310B2 Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：氨基胍和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：US06518310B2
公开(公告)日：2003-02-11
申请号：US09809293
申请日：2001-03-16
申请人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L Fedde , Carl R Illig , Thomas P. Markotan , Thomas P Stagnaro
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L Fedde , Carl R Illig , Thomas P. Markotan , Thomas P Stagnaro
IPC分类号： A61K31255
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, 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 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.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X为O或NR 9，R 1 -R 4，R 6 -R 9，R 11，R 12，R a，R b，R c，Y，Z，n和m在说明书中阐述，以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐。还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。

14. 发明授权

US06344486B1 Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：苯甲酰胺和磺酰胺取代的氨基胍和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：US06344486B1
公开(公告)日：2002-02-05
申请号：US09283241
申请日：1999-04-01
申请人： Richard M. Soll , Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan , Colleen Siedem
发明人： Richard M. Soll , Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan , Colleen Siedem
IPC分类号： A61K31165
CPC分类号： C07D213/40 , C07C279/00 , C07D211/16 , C07D211/62 , C07D213/74 , C07D217/06 , 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.
摘要翻译：本发明涉及氨基胍和烷氧基胍化合物，包括式I化合物：其中X为O或NH，L为-O-或-SO 2 - ，R 1 -R 4，R 9 -R 19，R a，R b，R c，Y ，Z，n和m在说明书中列出，以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐。还描述了制备式I化合物的方法。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物。本发明化合物的其它用途是作为抗凝剂，其嵌入或用于制造用于采血，血液循环和血液储存中的装置的材料中物理连接。

15. 发明授权

US5891909A Amidinohydrazones as protease inhibitors 失效
标题翻译：酰胺腙类作为蛋白酶抑制剂
公开(公告)号：US5891909A
公开(公告)日：1999-04-06
申请号：US828160
申请日：1997-03-27
申请人： Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Bruce E. Tomczuk , Carl Illig
发明人： Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Bruce E. Tomczuk , Carl Illig
IPC分类号： A61K31/00 , A61K31/165 , A61K31/18 , A61K31/275 , A61K31/277 , A61K31/41 , A61K31/415 , A61K31/433 , A61K31/44 , A61K31/4406 , A61K31/47 , A61K31/472 , A61P1/00 , A61P1/18 , A61P7/00 , A61P7/02 , A61P43/00 , C07C45/29 , C07C45/71 , C07C47/277 , C07C281/18 , C07C309/67 , C07C309/73 , C07C309/74 , C07C309/75 , C07C309/77 , C07C311/21 , C07C323/66 , C07D213/70 , C07D213/71 , C07D215/36 , C07D217/02 , C07D231/14 , C07D231/18 , C07D233/52 , C07D285/14 , C07D317/40 , C07D333/34 , A61K31/155 , A61K31/255
CPC分类号： C07D285/14 , C07C281/18 , C07C309/73 , C07C309/74 , C07C309/75 , C07C309/77 , C07C311/21 , C07C323/66 , C07C45/29 , C07C45/71 , C07C47/277 , C07D213/71 , C07D215/36 , C07D217/02 , C07D231/18 , C07D233/52 , C07D317/40 , C07D333/34 , C07C2101/02
摘要： Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, 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.
摘要翻译：脒基和苯甲脒基化合物，包括下式的化合物：其中R 1 -R 4，R 6 -R 9，Y，Z，n和m在说明书中列出，以及其水合物，溶剂合物或其药学上可接受的盐，描述抑制蛋白水解酶如凝血酶的方法。还描述了制备式I化合物的方法。

16. 发明授权

US5741819A Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors 失效
标题翻译：芳基磺酰氨基苯衍生物及其作为因子Xa抑制剂的用途
公开(公告)号：US5741819A
公开(公告)日：1998-04-21
申请号：US488196
申请日：1995-06-07
申请人： Carl R. Illig , Richard M. Soll , Joseph M. Salvino , Bruce E. Tomczuk , Tianbao Lu , Nalin L. Subasinghe
发明人： Carl R. Illig , Richard M. Soll , Joseph M. Salvino , Bruce E. Tomczuk , Tianbao Lu , Nalin L. Subasinghe
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 , A61K31/24
CPC分类号： C07D213/40 , C07C311/21 , C07C311/44 , C07D453/02
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: ##STR1## or pharmaceutically acceptable salts thereof; wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R.sup.2 is one of hydrogen, alkyl, cycloalkyl or aryl; R.sup.3 is one of hydrogen, hydroxy or alkoxy; R.sup.4 is one of --NH.sub.2, 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 --CH.sub.2 -- or --C(O)--; and n is from zero to eleven; provided that when R.sup.4 is --NH.sub.2, then R.sup.3 is hydrogen and n is other than zero; and also provided that when R.sup.3 is hydroxy or alkoxy, then R.sup.4 is other than --NH.sub.2, and n is other than zero.
摘要翻译：本发明涉及可用于治疗动脉和静脉血栓闭塞障碍，炎症，癌症和神经变性疾病的非肽因子Xa抑制剂。因子Xa抑制剂提供以下结构的化合物：其中I或其药学上可接受的盐; 其中R 1是烷基，取代的烷基，环烷基，芳基，取代的芳基，杂芳基或取代的杂芳基; R2是氢，烷基，环烷基或芳基之一; R3是氢，羟基或烷氧基之一; R4是-NH2，苯基或吡啶基之一，其中所述苯基和所述吡啶基任选被一个或两个卤素，羟基，羟基烷基，烷氧基，氨基，单烷基氨基，二烷基氨基，氨基烷基，单烷基氨基烷基和/或二烷基氨基烷基取代。 X是-CH 2 - 或-C（O） - ; n为零至十一; 条件是当R4为-NH2时，则R3为氢，n为0以上。并且还提供当R3是羟基或烷氧基时，则R4不是-NH2，n不为0。

17. 发明授权

US5482942A (3,4-dioxocyclobuten-1-yl)chromene, indene, and dihydronaphthalenone derivatives as smooth muscle relaxants 失效
标题翻译：（3,4-二氧杂环丁烯-1-基）色烯，茚和二氢萘酮衍生物作为平滑肌松弛剂
公开(公告)号：US5482942A
公开(公告)日：1996-01-09
申请号：US267691
申请日：1994-06-28
申请人： Richard M. Soll , Paul J. Dollings
发明人： Richard M. Soll , Paul J. Dollings
IPC分类号： A61K31/35 , A61K31/352 , A61P9/00 , A61P9/02 , A61P11/00 , A61P13/02 , A61P15/00 , C07C225/20 , C07D311/58 , A61K31/495 , A61K31/415 , C07C229/40 , C07D211/82 , C07D241/02 , C07D311/74 , C07D407/02
CPC分类号： C07D311/58
摘要： This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.1-6 perfluoroacylamino, mono or di-C.sub.1-12 alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.6-10 arylsulfonyl, carboxyl, C.sub.1-12 mono or di-alkylaminocarbonyl, or hydrogen;a and b together form an --O-- linkage, C.dbd.O, or a direct bond:R.sub.3 and R.sub.4, independent from each other, are H or C.sub.1-6 alkyl, optionally substituted by fluorine;R.sub.5 is amino or C.sub.1-12 mono alkylamine;R.sub.6 is H, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.6-10 aryl, or mono or bicyclic heteroaryl containing 1-3 heteroatoms selected from N, O, or S.
摘要翻译：本发明涉及具有平滑肌松弛活性的新型4-（3,4-二氧杂环丁烯-1-基）色烯和二氢萘酮及其3-（3,4-二氧杂环丁烯-1-基）茚及其盐，用于治疗高血压以及治疗周围血管疾病，充血性心力衰竭，涉及尿路过度平滑肌收缩的疾病，例如失禁或胃肠道，例如肠易激综合征，哮喘和脱发，以及药物组合物含有发明化合物。本发明公开了由式（I）表示的化合物：其中：R 1和R 2彼此独立地选自如下：C 1-6全氟烷氧基，C 1-6全氟烷基，C 1-6烷基，C 1 1-6烷氧基，羟基，C 1-6烷氧基羰基，硝基，氰基，卤素，C 1-6烷基磺酰氨基，C 1-6全氟烷基磺酰氨基，氨基，C 1-6酰氨基，C 1-6全氟酰基氨基，单或二-C 1-12烷基氨基， 6烷基磺酰基，C 6-10芳基磺酰基，羧基，C 1-12单或二烷基氨基羰基或氢; a和b一起形成O-键，C = O或直接键：R 3和R 4彼此独立地是H或任选被氟取代的C 1-6烷基; R5是氨基或C1-12单烷基胺; R 6是H，C 1-6全氟烷基，C 1-6烷基，C 6-10芳基或含有1-3个选自N，O或S的杂原子的单或双环杂芳基。

18. 发明授权

US06409988B1 Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands 有权
标题翻译：放射性标记的1-芳基吡唑，其合成及其作为害虫GABA受体配体的用途
公开(公告)号：US06409988B1
公开(公告)日：2002-06-25
申请号：US09606051
申请日：2000-06-29
申请人： Daljit S. Dhanoa , Sanath Meegalla , Dario Doller , Richard M. Soll
发明人： Daljit S. Dhanoa , Sanath Meegalla , Dario Doller , Richard M. Soll
IPC分类号： A61K5100
CPC分类号： C07D231/44 , A61K51/0423 , A61K51/0453
摘要： The present invention is directed to radiolabeled compounds of Formula I: or salts thereof, where R1 represents R8, R8O, R8SO2, R8SO or R8S in which R8 is tritiated or deuterated methyl; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen or amino; and R3-R7 are defined in the specification. The invention is also directed to methods of using such compounds for demonstrating specific insect GABA receptors, qualitatively screening for compounds acting on an insect GABA receptor or quantitatively assaying concentrations of a compound acting on an insect GABA receptor.
摘要翻译：本发明涉及放射性标记的式I化合物或其盐，其中R 1表示R8，R8O，R8SO2，R8SO或R8S，其中R8为氚化或氘代甲基; X为卤素，氰基，C1-6烷氧基羰基，C2-6 炔基，任选取代的C 6-14芳基或经由碳 - 碳键与噻唑连接的任选取代的5至7元杂芳环; R 2是氢或氨基; 本发明还涉及使用这些化合物来证明特异性昆虫GABA受体的方法，定性筛选作用于昆虫GABA受体的化合物或定量测定作用于昆虫GABA受体的化合物的浓度。

19. 发明授权

US06274628B1 Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors 有权
公开(公告)号：US06274628B1
公开(公告)日：2001-08-14
申请号：US09283241
申请日：1999-04-01
申请人： Richard M. Soll , Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan , Colleen Siedem
发明人： Richard M. Soll , Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan , Colleen Siedem
IPC分类号： A61K31165
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.

20. 发明授权

US06225302B1 Amidino protease inhibitors 有权
标题翻译：脒基蛋白酶抑制剂
公开(公告)号：US06225302B1
公开(公告)日：2001-05-01
申请号：US09631107
申请日：2000-08-01
申请人： Tianbao Lu , Bruce E. Tomczuk , Carl R. Illig , Richard M. Soll
发明人： Tianbao Lu , Bruce E. Tomczuk , Carl R. Illig , Richard M. Soll
IPC分类号： A61K31445
CPC分类号： C07D295/195 , C07C309/73 , C07C311/21 , C07D211/22 , C07D211/26
摘要： Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.
摘要翻译：脒基和苯甲脒基化合物，包括下式的化合物：其中R1-R4，R6-R9，Y，Z，n和m在本说明书中列出，以及其水合物，溶剂合物或其药学上可接受的盐，其抑制数目的蛋白水解酶。还描述了制备式I化合物的方法。

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