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61. 发明授权

US5990145A Vitronectin receptor antagonists, their preparation and their use 失效
标题翻译： Vitronectin受体拮抗剂，其制备及其应用
公开(公告)号：US5990145A
公开(公告)日：1999-11-23
申请号：US995522
申请日：1997-12-22
申请人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Karlheinz Scheunemann , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
发明人： Volkmar Wehner , Hans Ulrich Stilz , Anuschirwan Peyman , Karlheinz Scheunemann , Jean-Marie Ruxer , Denis Carniato , Jean-Michel Lefrancois , Thomas Richard Gadek , Robert McDowell
IPC分类号： C07D295/18 , A61K31/33 , A61K31/415 , A61K31/4184 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/536 , A61K31/5375 , A61K31/55 , A61K31/66 , A61P9/00 , A61P19/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D235/30 , C07D239/84 , C07D243/06 , C07D243/24 , C07D253/06 , C07D253/08 , C07D263/52 , C07D265/12 , C07D265/18 , C07D267/08 , C07D277/60 , C07D279/00 , C07D471/04 , C07D521/00 , C07F9/6561 , C07D405/12
CPC分类号： C07D243/24
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I，A-B-D-E-F-G（I）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。

62. 发明授权

US5438118A HIV protease inhibitors 失效
标题翻译： HIV蛋白酶抑制剂
公开(公告)号：US5438118A
公开(公告)日：1995-08-01
申请号：US66136
申请日：1993-07-26
申请人： James F. Callahan , William F. Huffman , Michael L. Moore , Kenneth A. Newlander
发明人： James F. Callahan , William F. Huffman , Michael L. Moore , Kenneth A. Newlander
IPC分类号： A61K31/55 , A61K38/00 , A61K38/55 , A61P9/12 , A61P31/12 , A61P43/00 , C07C69/757 , C07D223/04 , C07D223/06 , C07D223/08 , C07D223/10 , C07D233/54 , C07D243/06 , C07D243/08 , C07K1/113 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/097 , C07K7/02 , C07K14/81 , C12N9/99 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07D233/64 , C07C69/757 , C07D223/04 , C07D223/06 , C07D243/08 , C07K5/06052 , C07K5/06139 , C07K5/0821 , C07K7/02 , A61K38/00
摘要： Peptide mimics, having a constrained peptide backbone conformation, are HIV protease inhibitors. A compound of this invention is, for example, 3-Benzyl-5(alaninyl-1-aminoethyl)-2,3,6,7-tetrahydro-N-azepinyl-2-propionyl-valinyl-valinyl methyl ester.
摘要翻译： PCT No.PCT / US91 / 08850 Sec。 371日期：1993年7月26日 102（e）日期1993年7月26日PCT 1991年11月25日PCT公布。出版物WO92 / 09297 日期：1992年6月11日。具有约束肽骨架构象的肽模拟物是HIV蛋白酶抑制剂。本发明的化合物是例如3-苄基-5（丙烯酰基-1-氨基乙基）-2,3,6,7-四氢-N-氮杂基-2-丙酰基 - 缬氨酰基 - 缬氨酰基甲基酯。

63. 发明授权

US3966711A 4-Alkyl-1,4-diaza-5-oxo-cycloheptanes and their 1-oxyls 失效
标题翻译： 4-烷基-1,4-二氮杂-5-氧代 - 环庚烷及其1-氧基
公开(公告)号：US3966711A
公开(公告)日：1976-06-29
申请号：US476366
申请日：1974-06-05
申请人： Michael Rasberger
发明人： Michael Rasberger
IPC分类号： C07D243/08 , C08K5/00 , C08K5/3442 , C08L23/00 , C08L101/00 , C07D243/06
CPC分类号： C08K5/3442
摘要： 2,2,7,7-Tetraalkyl- and 2,7-dispiroalkylene-5-oxo-1,4-diazacycloheptanes substituted in 4-position by mono- or tetravalent radicals are powerful light-stabilizers for organic polymers. They possess higher compatibility than their 4-unsubstituted homologues, from which they may synthesized by reactions known for N-alkylation. Preferred substituents in 4-position are alkyl, alkylene, alkenyl, aralkyl and esteralkyl groups. The 1-nitroxyls derived from the imidazolidines by oxydation with hydrogen peroxide or percarboxylic acids too are good light stabilizers.
摘要翻译：通过单 - 或四价基团在4-位取代的2,2,7,7-四烷基 - 和2,7-二亚烷基-5-氧代-1,4-二氮杂环庚烷是有机聚合物的强光稳定剂。它们具有比它们的4-取代的同系物更高的相容性，可以从它们可以通过已知用于N-烷基化的反应合成。 4-位优选的取代基是烷基，亚烷基，烯基，芳烷基和酯烷基。通过用过氧化氢或过羧酸氧化由咪唑烷衍生的1-硝酰基也是良好的光稳定剂。

64. 发明公开

EP4192504A2 THERAPEUTIC CURE-PRO COMPOUNDS FOR TARGETED DEGRADATION OF BET DOMAIN PROTEINS, AND METHODS OF MAKING AND USING THEM 审中-实审
公开(公告)号：EP4192504A2
公开(公告)日：2023-06-14
申请号：EP21852893.3
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

65. 发明授权

EP1461038B9 ARYLSULFONAMIDE DERIVATIVES FOR USE AS CCR3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND IMMUNOLOGICAL DISORDERS 有权
标题翻译： ACRYLSULFONAMIDDERIVATE用作CCR3拮抗剂炎症和免疫疾病的治疗
公开(公告)号：EP1461038B9
公开(公告)日：2009-09-23
申请号：EP02772265.1
申请日：2002-09-04
申请人： Actimis Pharmaceuticals, Inc.,
发明人： LI, Yingfu , WATANABE, Akihiko , LOWINGER, Timothy, B. , BACON, Kevin , KAWAMURA, Norihiro , SHINTANI, Takuya , KIKUCHI, Tetsuo , MORIWAKI, Toshiya , URBAHNS, Klaus , FUKUSHIMA, Keiko , NUNAMI, Noriko , YOSHINO, Takashi , MURATA, Toshiki , YAMAUCHI, Megumi , YOSHINO, Hiroko
IPC分类号： A61K31/445 , A61K31/496 , A61P11/06 , A61P37/00 , A61P29/00 , C07D295/22 , C07D471/04 , C07D211/58 , C07D243/06 , C07D211/28 , C07C311/18 , C07D211/96 , C07D307/14 , C07D207/14 , C07D213/71
CPC分类号： C07D213/70 , C07C311/29 , C07C323/67 , C07D207/14 , C07D207/48 , C07D209/08 , C07D211/28 , C07D211/58 , C07D211/96 , C07D213/65 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D241/04 , C07D241/06 , C07D243/08 , C07D257/04 , C07D295/088 , C07D295/13 , C07D295/194 , C07D295/26 , C07D307/14 , C07D333/38 , C07D471/04 , C07D487/04 , C07D487/08
摘要： The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.

66. 发明公开

EP0110521A2 Phenylindene derivatives, acid addition salts thereof, and methods of preparation 失效
标题翻译： Phenylinden-Derivate，ihre Salze，und Verfahren zu ihrer Herstellung。
公开(公告)号：EP0110521A2
公开(公告)日：1984-06-13
申请号：EP83305987.6
申请日：1983-10-03
申请人： KEFALAS A/S
发明人： Perregaard, Jens Kristian
IPC分类号： C07D211/22 , C07D211/70 , C07D211/18 , C07D401/06 , C07D243/06 , C07D417/06 , C07D211/12 , C07D211/14 , C07D211/20 , C07D211/34 , A61K31/445
CPC分类号： C07D213/30 , C07D211/12 , C07D211/14 , C07D211/18 , C07D211/20 , C07D211/22 , C07D211/24 , C07D211/34 , C07D211/70 , C07D401/06 , C07D413/06 , C07D417/06
摘要： Novel phenylindene derivatives of the present invention are represented by the following formula:
wherein the dotted lines indicate optional bonds;

R 1 is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxymethyl, lower alkoxymethyl, cyano, trifluoromethyl, lower alkylthio or lower alkylsulfonyl;
R 2 is halogen, lower alkyl or trlfluoromethyl; and
R 3 is hydrogen, alkyl or alkenyl (straight or branched chain with C 1 -C 6 inclusive) optionally substituted with one or two hydroxy groups, any hydroxy group present being optionally esterified with an aliphatic carboxylic acid having from two to twenty-four carbon atoms inclusive, or R 3 is
wherein Z ist NR 4 , 0 or S, where R 4 is H or lower alkyl, and W is 0 or S, as well as pharmaceutically acceptable acid addition salts of the compounds of Formula I.

The phenylindene derivatives of Formula I have Interesting pharmacodynamic properties indicating strong antipsychotic activity.
Methods for the preparation of said derivatives are also described, as well as novel intermediates, wich are useful in the methods.
摘要翻译：本发明的新型苯基茚衍生物由下式表示：... ...其中虚线表示任选的键; R 1是氢，卤素，低级烷基，低级烷氧基，羟甲基，低级烷氧基甲基，氰基，三氟甲基，低级烷硫基或低级烷基磺酰基; R 2是卤素，低级烷基或三氟甲基; 和R 3是任选被一个或两个羟基取代的氢，烷基或烯基（具有C 1 -C 6的直链或支链），任何存在的羟基任选地被具有二至二十二个碳原子的脂族羧酸酯化， 4个碳原子，或者R 3为... CHEM，其中Z为NR 4，O或S，其中R 4为H或低级烷基，W为O或S，以及药学上式I化合物的可接受的酸加成盐。式I的苯基茚衍生物具有表现出强抗精神病活性的有趣的药效学性质。还描述了制备所述衍生物的方法，以及在该方法中有用的新型中间体。

67. 发明申请

WO2020192637A1 固体形式的BRD4抑制剂化合物及其制备方法与应用审中-公开
公开(公告)号：WO2020192637A1
公开(公告)日：2020-10-01
申请号：PCT/CN2020/080741
申请日：2020-03-23
申请人：石药集团中奇制药技术(石家庄)有限公司
发明人：沈春莉 , 刘勇 , 卞桓钰 , 吴成德 , 吴家虎
IPC分类号： C07D495/14 , A61K45/00 , C07D243/06 , A61P35/00 , A61K31/55 , A61P43/00
摘要：一种作为BRD4抑制剂的式（1）所示化合物的固体形式、晶型及其制备方法，以及其在制备治疗BRD4相关疾病药物中的应用。(I)

68. 发明申请

WO0071518A3 HETEROCYCLIC ANALGESIC COMPOUNDS AND THEIR USE 审中-公开
标题翻译：杂环化学化合物及其用途
公开(公告)号：WO0071518A3
公开(公告)日：2001-10-18
申请号：PCT/US0014579
申请日：2000-05-25
申请人： SEPRACOR INC
发明人： CUNY GREGORY D , SHAO LIMING , HAUSKE JAMES R , HEFFERNAN MICHELE L R , AQUILA BRIAN M , WU XINHE , WANG FENGJIAN , BANNISTER THOMAS D
IPC分类号： A61K31/397 , A61K31/435 , A61K31/438 , A61K31/445 , A61K31/4525 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/495 , A61K31/5375 , A61K31/55 , A61K31/551 , A61K31/553 , A61P25/04 , A61P25/30 , A61P27/16 , A61P43/00 , C07D205/04 , C07D211/26 , C07D211/42 , C07D211/56 , C07D211/60 , C07D221/04 , C07D223/04 , C07D223/10 , C07D241/04 , C07D243/08 , C07D265/30 , C07D267/10 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D491/10 , C07D491/113 , A61K31/40 , A61K31/535 , C07D207/09 , C07D207/16 , C07D223/12 , C07D243/06
CPC分类号： C07D221/04 , C07D205/04 , C07D211/26 , C07D211/42 , C07D211/56 , C07D223/04 , C07D241/04 , C07D243/08 , C07D265/30 , C07D267/10 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D491/10
摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other the G-protein coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
摘要翻译：本发明的一个方面涉及新的杂环化合物。本发明的第二方面涉及新型杂环化合物作为各种细胞受体（包括阿片受体，其他G蛋白偶联受体）和离子通道的配体的用途。本发明的另一方面涉及新型杂环化合物作为止痛剂的用途。

69. 发明申请

US20080132490A1 Substituted diazepan orexin receptor antagonists 有权
标题翻译：取代的二氮杂菜素食欲肽受体拮抗剂
公开(公告)号：US20080132490A1
公开(公告)日：2008-06-05
申请号：US11998812
申请日：2007-11-30
申请人： Jeffrey M. Bergman , Michael J. Breslin , Paul J. Coleman , Christopher D. Cox , Swati P. Mercer , Anthony J. Roecker
发明人： Jeffrey M. Bergman , Michael J. Breslin , Paul J. Coleman , Christopher D. Cox , Swati P. Mercer , Anthony J. Roecker
IPC分类号： A61K31/551 , A61P43/00 , C07D243/06
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/052 , C07D495/04
摘要： The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲素受体的拮抗剂的取代的二氮杂环庚烷化合物，其可用于治疗或预防涉及食欲肽受体的神经和精神病症和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。

70. 发明申请

US20080004258A1 BUTYL AND BUTYNYL BENZYL AMINE COMPOUNDS 有权
标题翻译：丁基和丁基苄基化合物
公开(公告)号：US20080004258A1
公开(公告)日：2008-01-03
申请号：US11766151
申请日：2007-06-21
申请人： John M. Keith , Michael A. Letavic , Emily M. Stocking
发明人： John M. Keith , Michael A. Letavic , Emily M. Stocking
IPC分类号： A61K31/551 , A61K31/135 , A61K31/445 , A61K31/495 , A61P21/00 , A61P29/00 , C07C211/00 , C07D243/06 , C07D295/00 , C07D221/00 , A61P3/00 , A61P25/00 , A61P15/00 , A61K31/5375 , A61K31/54
CPC分类号： C07C323/21 , C07C217/58 , C07C323/20 , C07C2601/02 , C07D211/38 , C07D213/64 , C07D213/65 , C07D213/70 , C07D241/08 , C07D243/08 , C07D295/08 , C07D295/096 , C07D295/135
摘要： Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.
摘要翻译：某些取代的丁基和丁炔基苄胺化合物是可用于治疗组胺H 3受体和/或5-羟色胺介导的疾病的组胺H 3 N 3受体和/或5-羟色胺转运蛋白调节剂。

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