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81. 发明申请

US20100160291A1 TRICYCLIC SPIRO-OXINDOLE DERIVATIVES AND THEIR USES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：三螺旋氧化物衍生物及其作为治疗剂的用途
公开(公告)号：US20100160291A1
公开(公告)日：2010-06-24
申请号：US12445271
申请日：2007-10-12
申请人： Mikhail Chafeev , Sultan Chowdhury , Jianmin Fu , Ranjender Kamboj
发明人： Mikhail Chafeev , Sultan Chowdhury , Jianmin Fu , Ranjender Kamboj
IPC分类号： A61K31/554 , C07D267/08 , C07D487/22 , C07D487/20 , C07D243/06 , A61K31/553 , A61K31/551 , A61K31/55 , A61K31/407 , A61P25/00
CPC分类号： C07D513/22 , C07D491/20 , C07D498/22
摘要： This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
摘要翻译：本发明涉及式（I）的三环螺 - 羟吲哚衍生物，其中j，k，m，n，w，q，Y，Q，X，R 1，R 2和R 3如本文所定义，作为立体异构体，其互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。还公开了包含化合物的药物组合物以及制备和使用化合物的方法。

82. 发明申请

US20090176767A1 BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS 有权
标题翻译：联苯化合物有效作为MUSCARINIC受体拮抗剂
公开(公告)号：US20090176767A1
公开(公告)日：2009-07-09
申请号：US12402665
申请日：2009-03-12
申请人： Mathai Mammen , Yu-Hua Ji , YongQi Mu , Viengkham Malathong
发明人： Mathai Mammen , Yu-Hua Ji , YongQi Mu , Viengkham Malathong
IPC分类号： A61K31/55 , C07D211/40 , C07D243/06 , A61K31/445 , A61P11/06
CPC分类号： C07D211/46 , C07D211/60 , C07D211/62 , C07D401/12 , C07D405/12
摘要： This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
摘要翻译：本发明提供式I化合物：其中a，b，c，m，p，r，R1，R2，R3，R4，R5，R6，W和X1如说明书中所定义。式I化合物是毒蕈碱受体拮抗剂。本发明还提供含有这些化合物的药物组合物，用于制备这些化合物的方法和中间体以及使用这些化合物治疗肺部疾病的方法。

83. 发明申请

US20070191309A1 Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines 有权
标题翻译：吡咯并苯并二氮杂作为二聚细胞毒性吡咯并苯并二氮杂合成中的关键中间体
公开(公告)号：US20070191309A1
公开(公告)日：2007-08-16
申请号：US10598482
申请日：2005-03-01
申请人： Philip Howard , Gyoung-Dong Kang
发明人： Philip Howard , Gyoung-Dong Kang
IPC分类号： A61K31/695 , C07D243/06
CPC分类号： C07D487/04 , Y02P20/55
摘要： Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R2 and R3 are independently selected from —H, ═O, ═CH2, —CN, —R, OR, halo, ═CH—R, O—SO2—R, CO2R and COR; R10 is a carbamate-based nitrogen protecting group; and R11 is an oxygen protecting group.
摘要翻译：化合物和式（Ia）或（Ib）化合物的合成方法及其盐，溶剂合物和化学保护形式，其中虚线表示C1和C2或C2和C3之间任选存在双键; R 2和R 3独立地选自-H，-O，-CH 2，-CN，-R，OR，卤素， -CH-R，O-SO 2 -R，CO 2 R和COR; R 10是氨基甲酸酯基氮保护基; R 11是氧保护基。

84. 发明授权

US06867208B2 Vitronectin receptor antagonists, their preparation and their use 有权
标题翻译： Vitronectin受体拮抗剂，其制备及其应用
公开(公告)号：US06867208B2
公开(公告)日：2005-03-15
申请号：US10142975
申请日：2002-05-13
申请人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
发明人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Jochen Knolle , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
IPC分类号： C07D239/00 , A61K31/155 , A61K31/16 , A61K31/18 , A61K31/33 , A61K31/395 , A61K31/415 , A61K31/4184 , A61K31/47 , A61K31/472 , A61K31/55 , A61K38/04 , A61P9/00 , A61P19/08 , A61P19/10 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C279/20 , C07C279/24 , C07C311/64 , C07C313/30 , C07C327/00 , C07D217/24 , C07D233/04 , C07D235/16 , C07D243/06 , C07D253/06 , C07D253/08 , C07D263/52 , C07D267/08 , C07D277/60 , C07D471/02 , C07D471/04 , C07D487/04 , C07K5/04 , A61K31/437
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.
摘要翻译：本发明涉及式Iin的化合物，其中A，B，D，E，F和G具有专利权利要求中给出的含义，其制备和用作药物。本发明的化合物用作玻连蛋白受体拮抗剂和骨吸收抑制剂。

85. 发明申请

US20020010174A1 Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation 失效
标题翻译：可用作神经激肽1受体拮抗剂的二氮杂衍生物及其形成方法
公开(公告)号：US20020010174A1
公开(公告)日：2002-01-24
申请号：US09854885
申请日：2001-05-14
发明人： Guido Galley , Annick Goergler , Thierry Godel , Reinhard Heck
IPC分类号： C07D243/06
CPC分类号： C07D401/06 , C07D243/14 , C07D403/06 , C07D409/06 , C07D487/04
摘要： The invention relates to compounds of the formula 1 wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl; R3 is hydrogen, lower alkyl, null(CH2)nN(R)2, null(CH2)n-heteroaryl or is a null(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is nullO, nullN(CH2)nCH3 or nullN(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group nullCR5nullNnullNnull; R5 is hydrogen, null(CH2)nN(R)2, null(CH2)n-heteroaryl or is a null(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl; n is 0, 1, 2 or 3; and pharmaceutically acceptable acid addition salts and enantiomeric forms thereof. The compounds are useful in the treatment of diseases, related to the NK-1 receptor.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2彼此独立地为芳基或杂芳基，其中杂芳基含有一个或两个选自N，O或S的杂原子，其中芳基或杂芳基任选被取代 1至3个取代基，它们彼此独立地为卤素，CF 3，低级烷氧基或低级烷基; R 3是氢，低级烷基， - （CH 2）n N（R）2， - （CH 2）n - 杂芳基或是 - （CH 2）n - 非芳族杂环，其杂环任选被卤素，CF 3，低级烷氧基或低级烷基 R4为= O，= N（CH2）nCH3或= N（CH2）nN（R）2; R3和R4可以与它们所连接的N和C原子一起与基团-CR 5 = N-N =一起; R 5是氢， - （CH 2）n N（R）2， - （CH 2）n - 杂芳基或是 - （CH 2）n - 非芳族杂环，所述杂环任选被卤素，CF 3，低级烷氧基或低级烷基取代; R是氢或低级烷基; n为0,1,2或3; 及其药学上可接受的酸加成盐及其对映体形式。该化合物可用于治疗与NK-1受体有关的疾病。

86. 发明授权

US5470849A .gamma.-turn peptidomimetics as fibrinogen antagonists 失效
标题翻译： γ-转角肽模拟物作为纤维蛋白原拮抗剂
公开(公告)号：US5470849A
公开(公告)日：1995-11-28
申请号：US50178
申请日：1993-04-30
申请人： James F. Callahan , William F. Huffman
发明人： James F. Callahan , William F. Huffman
IPC分类号： A61K31/55 , A61K38/46 , A61P7/02 , A61P9/04 , C07D223/04 , C07D223/06 , C07D223/08 , C07D223/10 , C07D243/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/06 , C07D409/14 , C07D401/00 , C07D405/00 , C07D409/00
CPC分类号： C07D223/10 , C07D243/06
摘要： This invention relates to a method of inhibiting platelet aggregation, and compounds which are mimics of the peptide sequence Arg-Gly-Asp.
摘要翻译： PCT No.PCT / US91 / 08166 Sec。 371日期：1993年04月30日 102（e）日期1993年4月30日PCT 1991年10月31日提交PCT本发明涉及抑制血小板聚集的方法，以及模拟肽序列Arg-Gly-Asp的化合物。

87. 发明授权

US5463050A Method of preparing aryl(homo)piperazines 失效
标题翻译：制备芳基（同）哌嗪的方法
公开(公告)号：US5463050A
公开(公告)日：1995-10-31
申请号：US17497
申请日：1993-02-12
申请人： Wolter Ten Hoeve , Jantje R. G. Thiecke , Hans Wynberg , Chris G. Kruse
发明人： Wolter Ten Hoeve , Jantje R. G. Thiecke , Hans Wynberg , Chris G. Kruse
IPC分类号： C07D213/74 , C07D243/06 , C07D243/08 , C07D245/02 , C07D295/02 , C07D295/08 , C07D295/12 , C07D319/18 , C07D333/36
CPC分类号： C07D213/74 , C07D243/08 , C07D319/18 , C07D333/36
摘要： The present invention is concerned with a method for the preparation of a compound of the general formula 2 ##STR1## by reaction of a compound of the formula 3Ar--Y (3)with a compound of the general formula 4 ##STR2## wherein Ar means a (hetero)aryl group, preferably selected from phenyl, naphtyl, furyl, thienyl, pyridyl, bicylic heteroaryl and tricyclic heteroaryl, which (hetero)aryl group is optionally sustituted with one to five non-strongly-electron-withdrawing substituents;M is a metal from the groups I or II of the periodic table;R.sub.12 is an electronegative group; andis 0 or 1.The invention also relates to compounds prepared according to this method and to new substituted aryl(homo)piperazines.
摘要翻译：本发明涉及通过式3 Ar-Y（3）的化合物与通式4化合物（IMA）的反应制备通式2的化合物（2）的方法（4）其中Ar表示优选选自苯基，萘基，呋喃基，噻吩基，吡啶基，双环杂芳基和三环杂芳基的（杂）芳基，该（杂）芳基任选地被一至五个非 - 吸电子取代基; M是周期表第I或II族的金属; R12是电负性基团; 并且为0或1.本发明还涉及根据该方法制备的化合物和新的取代的芳基（同）哌嗪。

88. 发明公开

KR1020110115374A Ｔ-형 칼슘 채널에 대한 활성을 갖는 2-(4-치환-1,4-디아제판-1-일)아세트아마이드 화합물 有权
标题翻译：具有T型钙通道活性的2-（4-取代-1,4-二氮杂-1-基）乙酰胺化合物
公开(公告)号：KR1020110115374A
公开(公告)日：2011-10-21
申请号：KR1020100034846
申请日：2010-04-15
申请人： 한국과학기술연구원
发明人： 조용서 , 민선준 , 이재균 , 구수진 , 최연희 , 울라프,푼나레디 , 아미드,압둘와히드 , 배애님 , 추현아 , 임혜원 , 최기현 , 서선희 , 송치만
IPC分类号： C07D243/08 , C07D243/06 , A61P9/12
摘要： 본 발명은 T-형 칼슘 채널에 대한 활성을 갖는 2-(4-치환-1,4-디아제판-1-일)아세트아마이드 화합물, 상기 화합물의 제조방법, 그리고 상기 화합물을 유효성분으로 포함하는 약학조성물에 관한 것이다. 본 발명의 신규 2-(4-치환-1,4-디아제판-1-일)아세트아마이드 화합물 또는 약학적으로 허용 가능한 이의 염은 T-형 칼슘 채널에 대한 길항작용을 가지므로 간질, 고혈압 등의 뇌질환 치료제, 협심증 등의 심장질환 치료제, 만성 통증, 신경성 통증 등의 통증질환 치료제, 또는 항암제로 유용하다.

89. 发明申请

WO2022031774A2 THERAPEUTIC CURE-PRO COMPOUNDS FOR TARGETED DEGRADATION OF BET DOMAIN PROTEINS, AND METHODS OF MAKING AND USING THEM 审中-公开
公开(公告)号：WO2022031774A2
公开(公告)日：2022-02-10
申请号：PCT/US2021/044437
申请日：2021-08-04
申请人： CORNELL UNIVERSITY
发明人： BARANY, Francis , GIARDINA, Sarah, F. , WARREN, J., David
IPC分类号： A61K47/50 , A61K47/51 , A61K31/69 , A61K31/4035 , A61K31/445 , C07D243/06 , C07F5/02
摘要： The present application is directed to a therapeutically useful compound, comprised of two monomers that are linked to each other through two or more reversible covalent bonds. Each monomer is a polyfunctionalized molecule comprising a bioorthogonal linker element and ligand or pharmacophore, wherein the linker and ligand/pharmacophore are covalently coupled to each other either directly or through an optional connector moiety.

90. 发明申请

WO2021024191A2 COMBINATION TREATMENTS WITH BENZODIAZEPINONE COMPOUNDS AND PHOSPHOINOSITIDE 3-KINASE PATHWAY INHIBITORS FOR TREATING CANCER 审中-公开
公开(公告)号：WO2021024191A2
公开(公告)日：2021-02-11
申请号：PCT/IB2020/057385
申请日：2020-08-05
申请人： BRISTOL-MYERS SQUIBB COMPANY , AYALA PHARMACEUTICALS INC.
发明人： FISCHER, Bruce S. , GELBAUM, Dana
IPC分类号： C07D243/06 , C07D243/10 , C07D243/14 , A61P35/02 , C07D243/24 , A61K31/5513 , A61P35/00 , A61K45/06
摘要： The present invention provides methods for treating a proliferative disorder in a subject comprising administering to the subject a first composition comprising one or more gamma secretase inhibitors and a second composition comprising one or more phosphoinositide 3-kinase (PI3K) pathway antagonists/inhibitors. This invention also provides methods for treating T-cell acute lymphoblastic leukemia (T-ALL) in a subject in need thereof comprising identifying elevated expression of T-ALL-specific transcription factors and administering to the subject a gamma secretase inhibitor and, optionally, a (PI3K) pathway antagonist/inhibitor, a transcription factor inhibitor, or a combination thereof.

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