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1. 发明授权

US07645799B2 Substituted biaryl compounds as factor XIa inhibitors 有权
标题翻译：取代的联芳基化合物作为因子XIa抑制剂
公开(公告)号：US07645799B2
公开(公告)日：2010-01-12
申请号：US12266659
申请日：2008-11-07
申请人： James R. Corte , Mimi L. Quan , Joanne M. Smallheer , Donald J. P. Pinto
发明人： James R. Corte , Mimi L. Quan , Joanne M. Smallheer , Donald J. P. Pinto
IPC分类号： A61K31/165 , A61K31/4409 , A61K31/27 , A61K31/40 , A61K31/195 , A61K31/18 , A61K31/41 , A61K31/5375 , A61K31/44 , A61K31/381 , A61K31/426 , A61K31/415 , C07C237/24 , C07C311/11 , C07C271/28 , C07D213/04 , C07D207/30 , C07D257/04 , C07D295/033 , C07D211/98 , C07D333/38 , C07D277/40 , C07D233/88
CPC分类号： C07C255/44 , C07C237/24 , C07C271/28 , C07C2601/14 , C07D207/335 , C07D213/40 , C07D213/73 , C07D213/75 , C07D215/04 , C07D215/227 , C07D231/56 , C07D233/88 , C07D257/04 , C07D277/40 , C07D295/135 , C07D333/40 , C07D409/04 , C07D413/12
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译：本发明提供式（I）化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂化物形式，其中变量A，L，Z，R 3和环B如本文所定义。式（I）的化合物可用作凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。特别地，它涉及作为选择性因子XIa抑制剂的化合物。本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。

3. 发明授权

US5744481A .beta.-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors 失效
标题翻译：可用作逆转录病毒蛋白酶抑制剂的β-氨基酸羟乙基氨基磺酰胺
公开(公告)号：US5744481A
公开(公告)日：1998-04-28
申请号：US845392
申请日：1997-04-25
申请人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
发明人： Michael L. Vazquez , Richard A. Mueller , John J. Talley , Daniel Getman , Gary A. DeCrescenzo , John N. Freskos
IPC分类号： C07D295/12 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4433 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K38/00 , A61P31/12 , C07C311/05 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C313/06 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/57 , C07C323/67 , C07C327/38 , C07D209/08 , C07D211/78 , C07D213/30 , C07D213/53 , C07D213/56 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/54 , C07D239/02 , C07D239/26 , C07D277/24 , C07D277/30 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/06 , C07K5/078 , A61K31/18 , A61K31/47
CPC分类号： C07C311/05 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/20 , C07C311/24 , C07C311/29 , C07C311/32 , C07C311/41 , C07C311/46 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/28 , C07C317/44 , C07C323/49 , C07C323/67 , C07D209/08 , C07D213/30 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/82 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139 , A61K38/00 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2101/18 , C07C2102/10
摘要： .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译： α-和β-氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。

4. 发明授权

US5728875A Microbicides 失效
标题翻译：杀菌剂
公开(公告)号：US5728875A
公开(公告)日：1998-03-17
申请号：US703300
申请日：1996-08-26
申请人： Martin Zeller
发明人： Martin Zeller
IPC分类号： C07D275/02 , A01N41/06 , C07C303/36 , C07C307/06 , C07C311/06 , C07C311/07 , C07C311/11 , C07C311/14 , C07C311/20 , C07C313/06 , C07C313/20 , C07C317/04 , C07C323/60 , C07C323/65 , C07D295/26 , C07C233/76 , A61K31/18 , C07C303/40 , C07C303/35
CPC分类号： C07D295/26 , C07C307/06 , C07C311/06 , C07C311/07 , C07C311/11 , C07C311/14 , C07C313/06 , C07C313/20 , C07C317/04 , C07C323/60 , C07C2101/08 , C07C2101/14
摘要： .alpha.-Amino acid amides of the formula I ##STR1## in which n is the number zero or one; R.sub.1 is C.sub.1 -C.sub.12 alkyl, which is unsubstituted or can be substituted by C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.3 -C.sub.8 cycloalkyl, cyano, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.3 -C.sub.6 alkenyloxycarbonyl or C.sub.3 -C.sub.6 alkynyloxycarbonyl; C.sub.3 -C.sub.8 cycloalkyl; C.sub.2 -C.sub.12 alkenyl; C.sub.2 -C.sub.12 alkynyl; C.sub.1 -C.sub.12 halogenoalkyl or a group NR.sub.13 R.sub.14 ; in which R.sub.13 and R.sub.14 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl or together are tetra- or pentamethylene; R.sub.2 and R.sub.3 independently of one another are hydrogen; C.sub.1 -C.sub.8 alkyl; C.sub.1 -C.sub.8 alkyl which is substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, mercapto or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.8 alkenyl; C.sub.3 -C.sub.8 alkynyl; C.sub.3 -C.sub.8 cycloalkyl or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl, or in which the two groups R.sub.2 and R.sub.3, together with the carbon atom to which they are bonded, form a three- to eight-membered carbocyclic ring; R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.5 is hydrogen; C.sub.1 -C.sub.6 alkyl or phenyl, which is unsubstituted or can be substituted by halogen, nitro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 halogenoalkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; and R.sub.6 is a group G ##STR2## in which R.sub.7 and R.sub.8 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl; p is the number zero or one; and R.sub.9, R.sub.10 and R.sub.11 independently of one another are hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halogenoalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.6 alkenyloxy, C.sub.3 -C.sub.6 alkynyloxy, C.sub.3 -C.sub.6 alkylthio, halogen or nitro are valuable microbicides. They can be employed in crop protection in the form of suitable compositions, for example for controlling fungal diseases.
摘要翻译： α型氨基酰胺，其中n是数字0或1; R 1是未被取代或可以被C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基磺酰基，C 3 -C 8环烷基，氰基，C 1 -C 6烷氧基羰基，C 3 -C 6烯氧基羰基或C 3 -C 6炔氧基羰基取代的C 1 -C 12烷基; C 3 -C 8环烷基; C 2 -C 12烯基; C 2 -C 12炔基; C 1 -C 12卤代烷基或NR 13 R 14基团; 其中R 13和R 14彼此独立地是氢或C 1 -C 6烷基或一起是四或五亚甲基; R2和R3彼此独立地是氢; C1-C8烷基; 被羟基，C 1 -C 4烷氧基，巯基或C 1 -C 4烷硫基取代的C 1 -C 8烷基; C3-C8链烯基; C3-C8炔基; C 3 -C 8环烷基或C 3 -C 8环烷基-C 1 -C 4烷基，或其中两个基团R 2和R 3与它们所键合的碳原子一起形成三至八元碳环; R4是氢或C1-C6烷基; R5是氢; 硝基，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基或C 1 -C 4烷硫基取代的C 1 -C 6烷基或苯基; 并且R 6是基团G G，其中R 7和R 8彼此独立地是氢或C 1 -C 6烷基; p是数字0或1; 并且R 9，R 10和R 11彼此独立地是氢，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 3 -C 6烯基，C 3 -C 6炔基，C 1 -C 6烷氧基，C 3 -C 6烯氧基，C 3 -C 6炔氧基，C 3 -C 6烷硫基，卤素或硝基是有价值的杀菌剂它们可以以合适的组合物的形式用于作物保护，例如用于防治真菌疾病。

5. 发明授权

US5693665A Alkylated (hetero) cyclic compounds 失效
标题翻译：烷基化（杂）环化合物
公开(公告)号：US5693665A
公开(公告)日：1997-12-02
申请号：US584465
申请日：1996-01-10
申请人： Daniel Lesieur , Eric Fourmaintraux , Patrick Depreux , Philippe Delagrange , Pierre Renard , Beatrice Guardiola-Lemaitre
发明人： Daniel Lesieur , Eric Fourmaintraux , Patrick Depreux , Philippe Delagrange , Pierre Renard , Beatrice Guardiola-Lemaitre
IPC分类号： A61K31/165 , A61K31/17 , A61K31/18 , A61K31/34 , A61K31/343 , A61K31/40 , A61K31/403 , A61K31/404 , A61P3/00 , A61P3/04 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07C231/02 , C07C233/02 , C07C233/05 , C07C233/08 , C07C233/09 , C07C233/58 , C07C273/02 , C07C275/24 , C07C275/26 , C07C303/38 , C07C311/03 , C07C311/10 , C07C311/11 , C07C327/38 , C07C335/12 , C07C335/14 , C07D209/14 , C07D307/81 , C07D333/58 , A61K31/38 , C07D335/06
CPC分类号： C07C233/08 , C07C233/05 , C07C233/58 , C07D307/81 , C07D333/58 , C07C2101/02 , C07C2101/04 , C07C2102/10
摘要： The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.
摘要翻译：本发明涉及选自这些式（I）的化合物：其中：R 1，R 2，R 3和A如说明书中所定义，和含有可用于治疗褪黑激素的药物紊乱。

6. 发明授权

US11633394B2 Substituted alkynylene compounds as anticancer agents 有权
公开(公告)号：US11633394B2
公开(公告)日：2023-04-25
申请号：US16962941
申请日：2019-01-17
申请人： Aurigene Oncology Limited
发明人： Dinesh Chikkanna , Vinayak V. Khairnar , Muralidhara Ramachandra , Leena Khare Satyam
IPC分类号： A61K45/06 , C07C237/24 , C07C275/26 , C07C311/11 , C07D205/04 , C07D207/16 , C07D211/58 , C07D211/72 , C07D231/56 , C07D261/04 , C07D295/215 , C07D333/28 , C07D401/04 , A61K31/496 , A61P35/00 , A61K31/17 , A61K31/439 , A61K31/4468 , A61K31/454 , A61K31/495 , C07D471/08
摘要： The present invention relates to substituted alkynylene compounds represented by the compounds of formula (I), pharmaceutically acceptable salts and stereoisomers thereof. The present invention further provides the therapeutic uses of the compounds of formula (I) as anti-cancer agents.

8. 发明申请

US20050058935A1 Sulfonamide compound, polymer compound, resist material and pattern formation method 有权
标题翻译：磺酰胺化合物，高分子化合物，抗蚀剂材料和图案形成方法
公开(公告)号：US20050058935A1
公开(公告)日：2005-03-17
申请号：US10932316
申请日：2004-09-02
申请人： Shinji Kishimura , Masayuki Endo , Masaru Sasago , Mitsuru Ueda , Hirokazu Imori , Toshiaki Fukuhara
发明人： Shinji Kishimura , Masayuki Endo , Masaru Sasago , Mitsuru Ueda , Hirokazu Imori , Toshiaki Fukuhara
IPC分类号： C07C311/11 , C07C311/10 , C07C311/12 , C07C311/13 , G03F7/004 , G03F7/039 , G03C1/76
CPC分类号： C08F220/18 , C08F212/02 , C08F228/02 , G03F7/0046 , G03F7/0392 , G03F7/0397 , Y10S430/106 , Y10S430/107 , Y10S430/108 , Y10S430/111
摘要： A base polymer of a resist material includes a unit represented by a general formula of the following Chemical Formula 3: wherein R1, R2 and R3 are the same or different and are a hydrogen atom, a fluorine atom, a straight-chain alkyl group, a branched or cyclic alkyl group or a fluoridated alkyl group with a carbon number not less than 1 and not more than 20; R4 is a straight-chain alkylene group or a branched or cyclic alkylene group with a carbon number not less than 0 and not more than 20; and R5 and R6 are the same or different and are a hydrogen atom, a straight-chain alkyl group, a branched or cyclic alkyl group, a fluoridated alkyl group with a carbon number not less than 1 and not more than 20, or a protecting group released by an acid.
摘要翻译：抗蚀剂材料的基础聚合物包括由以下化学式3的通式表示的单元：其中R 1，R 2和R 3相同或不同，为氢原子，氟原子，直链烷基，支链或环状烷基或碳数不小于1且不大于20的氟化烷基; R 4是直链亚烷基或碳数不小于0且不大于20的支链或环状亚烷基; R 5和R 6相同或不同，为氢原子，直链烷基，支链或环状烷基，碳数不小于1且不大于1的氟化烷基或者由酸释放的保护基。

9. 发明授权

US6124363A Dofetilide polymorphs 有权
标题翻译：多非替尼多晶型物
公开(公告)号：US6124363A
公开(公告)日：2000-09-26
申请号：US423986
申请日：1999-11-16
申请人： Ian Colin Appleby , Trevor Jack Newbury , Gary Nichols
发明人： Ian Colin Appleby , Trevor Jack Newbury , Gary Nichols
IPC分类号： A61P9/04 , A61K31/18 , A61P9/06 , C07C311/05 , C07C311/08 , C07C303/44 , C07C311/11
CPC分类号： C07C311/08 , Y10S514/821
摘要： The invention relates to the substantially pure dofetilide polymorphs P162, P162a and P143, and to processes for the preparation of, compositions containing and to the uses of, such polymorphs.
摘要翻译： PCT No.PCT / EP98 / 06641 Sec。 371日期：1999年11月16日 102（e）1999年11月16日PCT PCT 1998年10月9日PCT公布。公开号WO99 / 21829 日期1999年5月6日本发明涉及基本上纯的多非替尼多晶型物P162，P162a和P143，以及制备含这些多晶型物的用途的组合物的方法。

10. 发明授权

US5922763A Biphenyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them 失效
标题翻译：联苯衍生物，含有这些化合物的药物组合物及其制备方法
公开(公告)号：US5922763A
公开(公告)日：1999-07-13
申请号：US978739
申请日：1997-11-26
申请人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Gunter Linz , Thomas Muller , Wolfgang Eisert , Johannes Weisenberger
发明人： Frank Himmelsbach , Helmut Pieper , Volkhard Austel , Gunter Linz , Thomas Muller , Wolfgang Eisert , Johannes Weisenberger
IPC分类号： C07C211/44 , A61K38/00 , C07C211/48 , C07C211/50 , C07C211/53 , C07C233/65 , C07C237/36 , C07C237/38 , C07C243/22 , C07C255/54 , C07C255/56 , C07C255/57 , C07C255/58 , C07C255/59 , C07C255/60 , C07C257/18 , C07C271/64 , C07C275/28 , C07C275/32 , C07C275/38 , C07C275/42 , C07C279/18 , C07C307/10 , C07C309/11 , C07C311/04 , C07C311/06 , C07C311/08 , C07C311/11 , C07C311/16 , C07C311/19 , C07C311/21 , C07C311/29 , C07C317/14 , C07C317/44 , C07C317/46 , C07C321/24 , C07C323/60 , C07C323/62 , C07D207/08 , C07D207/26 , C07D211/34 , C07D211/60 , C07D211/62 , C07D211/70 , C07D257/04 , C07D295/192 , C07F9/40 , C07K5/06 , A61K31/24 , A61K31/19 , C07C229/34 , C07C251/16
CPC分类号： C07D295/192 , C07C237/36 , C07C237/38 , C07C243/22 , C07C255/56 , C07C255/57 , C07C255/59 , C07C255/60 , C07C257/18 , C07C271/64 , C07C275/42 , C07C307/10 , C07C309/11 , C07C311/04 , C07C311/06 , C07C311/08 , C07C311/19 , C07C311/21 , C07C311/29 , C07C317/44 , C07C317/46 , C07C323/60 , C07C323/62 , C07D211/34 , C07D211/60 , C07D211/62 , C07D211/70 , C07K5/06026 , A61K38/00 , C07C2101/14
摘要： The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
摘要翻译：本发明涉及通式的联苯衍生物，其中A至E和X如权利要求1所定义，其立体异构体包括它们的混合物及其盐，特别是其与无机或有机酸或碱的生理上可接受的盐，其具有有价值的性质，优选聚集抑制作用，含有这些化合物的药物组合物及其制备方法。

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