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1. 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.

3. 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。

4. 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。

5. 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。

6. 发明授权

US5663417A Carbocyclic sulfonamides 失效
标题翻译：碳环磺酰胺
公开(公告)号：US5663417A
公开(公告)日：1997-09-02
申请号：US187008
申请日：1994-01-27
申请人： Nobuyuki Hamanaka , Tsumoru Miyamoto
发明人： Nobuyuki Hamanaka , Tsumoru Miyamoto
IPC分类号： A61K31/557 , A61P43/00 , C07C303/38 , C07C303/40 , C07C311/07 , C07C311/10 , C07C311/11 , C07C311/12 , C07C311/13 , C07C311/14 , C07C311/19 , C07C311/20 , C07C311/27 , C07C311/29 , C07D493/08 , A61K31/215 , A61K31/18 , C07C69/608
CPC分类号： C07C311/19 , C07C311/07 , C07C311/10 , C07C311/11 , C07C311/13 , C07C311/14 , C07C311/20 , C07C311/27 , C07C311/29
摘要： (1) Prostaglandin (PG) E.sub.2 antagonist or agonist containing carbocyclic sulfonamides represented by the compound of the formula (I): ##STR1## cyclodextrin clathrates thereof, non-toxic salts thereof as active ingredient, (2) carbocyclic sulfonamides represented by the compound of the formula (II): ##STR2## cyclodextrin clathrates thereof, non-toxic salts thereof, (3) process for the preparation of the compound represented by the compound of the formula (II) described hereinbefore, (4) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (II) as active ingredient.The compounds represented by the compounds of the formula (I) and (II) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgetic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.2 antagonists, and an uterine contractile activity, a promoting effect of digestive peristalsis, a suppressive effect of gastric acid secretion, a hypotensive activity as PGE.sub.2 agonists, because they bind onto PGE.sub.2 receptor and have an activity of antagonist or agonist against the action thereof.
摘要翻译：（1）由式（I）化合物表示的前列腺素（PG）E2拮抗剂或含有碳环磺酰胺的激动剂：其作为活性成分的无毒盐，（2）代表的碳环磺酰胺通式（II）的化合物：其中，式（II）的环糊精包合物，其无毒盐，（3）由上述式（II）的化合物表示的化合物的制备方法，（ 4）含有由式（II）化合物表示的化合物作为活性成分的PGE 2拮抗剂或激动剂。由式（I）和（II）化合物表示的化合物可适用于具有子宫收缩抑制作用，止痛作用，消化性蠕动抑制作用，睡眠诱导作用PGE2拮抗剂的药物，因为它们结合PGE2受体并且具有针对其作用的拮抗剂或激动剂的活性，因此其作为PGE2激动剂具有低血压活性，作为消化道蠕动的促进作用，胃酸分泌的抑制作用。

7. 发明授权

US12024529B2 Compounds that inhibit MCL-1 protein 有权
公开(公告)号：US12024529B2
公开(公告)日：2024-07-02
申请号：US18313703
申请日：2023-05-08
申请人： AMGEN INC.
发明人： Robert Farrell
IPC分类号： C07D249/18 , C07C59/56 , C07C59/68 , C07C311/11 , C07D498/00 , C07D513/08 , C07D513/10
CPC分类号： C07D513/10 , C07C59/56 , C07C59/68 , C07C311/11 , C07D249/18 , C07D498/00 , C07D513/08
摘要： Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I,

and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

8. 发明公开

US20230210847A1 Substituted Alkynylene Compounds As Anticancer Agents 审中-公开
公开(公告)号：US20230210847A1
公开(公告)日：2023-07-06
申请号：US18120149
申请日：2023-03-10
申请人： AURIGENE ONCOLOGY LIMITED
发明人： Dinesh CHIKKANNA , Vinayak V. Khairnar , Muralidhara Ramachandra , Leena Khare Satyam
IPC分类号： A61K31/496 , A61P35/00 , A61K31/17 , A61K31/439 , A61K31/4468 , A61K31/454 , A61K31/495 , 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 , C07D471/08
CPC分类号： A61K31/496 , A61P35/00 , A61K31/17 , A61K31/439 , A61K31/4468 , A61K31/454 , A61K31/495 , 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 , 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.

9. 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。

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