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81. 发明申请

US20180230168A1 Ataxia Telengiectasia And Rad3-Related (ATR) Protein Kinase Inhibitors 审中-公开
公开(公告)号：US20180230168A1
公开(公告)日：2018-08-16
申请号：US15951302
申请日：2018-04-12
申请人： Atrin Pharmaceuticals LLC
发明人： Henry Joseph Breslin , Oren Gilad
IPC分类号： C07D519/00 , C07D515/18 , C07D498/18 , C07D498/08 , C07D515/08
CPC分类号： C07D519/00 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D498/08 , C07D498/18 , C07D515/08 , C07D515/18
摘要： Macrocyclic compounds having the structure of Formula (A), or pharmaceutically acceptable salts thereof, are provided: wherein R1, R2, R3, R4 and R5 are defined herein. Also provided are pharmaceutical compositions comprising the macrocyclic compound and methods for treating cancer in a patient comprising administering to the patient the macrocyclic compound.

82. 发明授权

US10017481B2 Conformationally constrained, fully synthetic macrocyclic compounds 有权
公开(公告)号：US10017481B2
公开(公告)日：2018-07-10
申请号：US14385689
申请日：2013-03-15
申请人： POLYPHOR AG
发明人： Daniel Obrecht , Philipp Ermert , Said Oumouch , Arnaud Piettre , Jean-François Gosalbes , Marc Thommen
IPC分类号： C07D273/02 , C07D498/04 , C07D498/18 , C07D498/08 , C07D515/18 , C07D291/08 , C07D515/06 , C07D515/22 , C07D515/08
CPC分类号： C07D273/02 , C07D291/08 , C07D498/04 , C07D498/08 , C07D498/18 , C07D515/06 , C07D515/08 , C07D515/18 , C07D515/22
摘要： The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

83. 发明授权

US08497270B2 Macrocyclic integrase inhibitors 有权
标题翻译：大环整合酶抑制剂
公开(公告)号：US08497270B2
公开(公告)日：2013-07-30
申请号：US13395891
申请日：2010-10-13
申请人： Johannes Wilhelmus J Thuring , Jean-Francois Bonfanti , Jerome Michel Claude Fortin
发明人： Johannes Wilhelmus J Thuring , Jean-Francois Bonfanti , Jerome Michel Claude Fortin
IPC分类号： C07D471/18 , C07D498/18 , C07D513/18 , C07D515/18 , C07D498/22 , A61K31/547 , A61P31/18
CPC分类号： C07D513/18 , C07D471/18 , C07D498/18 , C07D498/22 , C07D515/18
摘要： Compound having formula (I), wherein —W is NH—, —N(CH3)— or piperazine, —X is a bond, —C(═O)— or S(═O)2—, —Y is C3-7alkylene, and —Z is NH—C(═O)— or —O—, and pharmaceutically acceptable salts thereof, their pharmaceutical formulations and use as HIV inhibitors.
摘要翻译：具有式（I）的化合物，其中-W是NH-，-N（CH 3） - 或哌嗪，-X是键，-C（= O） - 或S（= O）2 - ， - 7亚烷基和-Z是NH-C（= O） - 或-O-，及其药学上可接受的盐，它们的药物制剂和用作HIV抑制剂。

84. 发明授权

US4076724A Polycyclic macrocyclic compounds 失效
标题翻译：多环大环化合物
公开(公告)号：US4076724A
公开(公告)日：1978-02-28
申请号：US295083
申请日：1972-10-04
申请人： Jean-Marie Lehn
发明人： Jean-Marie Lehn
IPC分类号： B01J45/00 , C07D487/18 , C07D498/18 , C07D513/18 , C07D515/18 , C07K1/12 , C08J5/22 , C22B3/36
CPC分类号： C07D498/18 , C07D513/18 , C07K1/126 , C08J5/2218 , C22B3/0036 , Y02P10/234
摘要： Novel polycyclic macrocyclic compounds having four tertiary nitrogen bridgehead atoms and six bridging chains, each of which have not more than twelve directly connecting atoms between each pair of bridgehead nitrogens, said bridging chains being hydrocarbon chains and hetero-substituted hydrocarbon chains having at least one hetero connecting atom selected from the group consisting of oxygen, sulfur, and nitrogen, at least two of said chains being hetero substituted. When admixed with a compatible cation-donor compound, the polycyclic macrocyclic compounds form stable cation-containing macrocyclic complexes which, in turn, can be conveniently dissociated by addition of acid or a quaternizing acid. The novel polycyclic macrocyclics are valuable for use in the same way and for the same purposes as chelating agents.The polycyclic macrocyclic compounds are prepared by condensation reactions utilizing high dilution techniques, e.g. by condensing a monocyclic macrocyclic having secondary nitrogen bridgeheads with a substituted hydrocarbon di-carbonyl halide followed by reduction of the resulting lactam or, alternatively, by condensing a monocyclic macrocyclic having secondary nitrogen bridgeheads with a substituted hydrocarbon dihalide (or di-sulfonate).
摘要翻译：具有四个三氮桥头原子和六个桥连链的新型多环大环化合物，其每一个在每对桥头氮之间不超过十二个直接连接的原子，所述桥连链是烃链和具有至少一个杂原子的杂取代烃链连接选自氧，硫和氮的原子，所述链中的至少两个是被取代的。当与相容的阳离子供体化合物混合时，多环大环化合物形成稳定的含阳离子的大环络合物，其又可以通过加入酸或季铵化酸来方便地解离。新型多环大环化合物以与螯合剂相同的方式和相同的目的使用是有价值的。

86. 发明公开

EP2871957A4 MACROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：大环化合物ALS HIV整合酶抑制剂
公开(公告)号：EP2871957A4
公开(公告)日：2016-01-27
申请号：EP13817154
申请日：2013-07-10
申请人： MERCK SHARP & DOHME
发明人： REGER THOMAS , WALJI ABBAS , SANDERS JOHN , WAI JOHN , WANG LIPING
IPC分类号： C07D487/18 , A61K31/427 , A61K31/513 , A61K31/55 , A61K31/553 , A61K45/06 , C07D498/18 , C07D515/18
CPC分类号： C07D498/18 , A61K31/427 , A61K31/55 , A61K31/553 , A61K45/06 , C07D487/18 , C07D515/18 , A61K31/513 , A61K2300/00

87. 发明授权

EP2488521B1 MACROCYCLIC INTEGRASE INHIBITORS 有权转让
标题翻译：大环整合
公开(公告)号：EP2488521B1
公开(公告)日：2013-12-18
申请号：EP10772998.0
申请日：2010-10-13
申请人： Elanco Animal Health Ireland Limited
发明人： THURING, Johannes Wilhelmus J. , BONFANTI, Jean-François , FORTIN, Jérôme Michel Claude
IPC分类号： C07D471/18 , C07D498/18 , C07D513/18 , C07D515/18 , A61K31/547 , A61P31/18 , C07D498/22
CPC分类号： C07D513/18 , C07D471/18 , C07D498/18 , C07D498/22 , C07D515/18
摘要： Compound having formula (I), wherein -W is NH-, -N(CH3)- or piperazine, -X is a bond, -C(=O)- or S(=O)2-, -Y is C3-7alkylene, and -Z is NH-C(=O)- or -O-, and pharmaceutically acceptable salts thereof, their pharmaceutical formulations and use as HIV inhibitors.

88. 发明授权

EP1557418B1 QUINOXALINE DERIVATIVES 有权
标题翻译： CHINOXALINDERIVATE
公开(公告)号：EP1557418B1
公开(公告)日：2012-04-04
申请号：EP03758937.1
申请日：2003-10-27
申请人： MSD K.K.
发明人： HIRAI, Hiroshi; c/o BANYU PHARMACEUTICAL CO., LTD , KAWANISHI, Nobuhiko; c/o BANYU PHARMACEUTICAL CO. , HIROSE, Masaaki; c/o BANYU PHARMACEUTICAL CO.,LTD , SUGIMOTO, Tetsuya; c/o BANYU PHARMACEUTICAL CO., , KAMIJYO, Kaori; c/o BANYU PHARMACEUTICAL CO., , SHIBATA, Jun; c/o BANYU PHARMACEUTICAL CO., LTD. , MASUTANI, Kouta; c/o BANYU PHARMACEUTICAL CO.,
IPC分类号： A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/55 , C07D487/18 , C07D498/18 , C07D498/22 , C07D515/18 , C07D515/22 , A61P35/00
CPC分类号： C07D487/18 , A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/55 , C07D498/18 , C07D498/22 , C07D515/18 , C07D515/22
摘要： Quinoxaline derivatives represented by the general formula (I) or pharmaceutically acceptable salts or esters thereof: (I) wherein X is NH, S, or the like; Y is O or the like; the group represented by the general formula (II): (II) is, e.g., (III) [wherein B1, B2, ..., Bn-1, and Bn (wherein n is 4, 5, or 6) are each independently CH, N, or the like; and B’1, B’2, ..., B’n-1, and B’n (wherein n is 4, 5, or 6) are each independently hydrogen or the like]; and R is hydrogen, lower alkyl, or the like.

89. 发明公开

US20230365587A1 MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 审中-公开
公开(公告)号：US20230365587A1
公开(公告)日：2023-11-16
申请号：US18248065
申请日：2021-10-06
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： Jason MCCARTNEY , Alexander Russell ABELA , Sunny ABRAHAM , Corey Don ANDERSON , Vijayalaksmi ARUMUGAM , Jaclyn CHAU , Jeremy CLEMENS , Thomas CLEVELAND , Timothy A. DWIGHT , Bryan A. FRIEMAN , Peter GROOTENHUIS , Sara Sabina HADIDA RUAH , Yoshihiro ISHIHARA , Paul KRENITSKY , Mark Thomas MILLER , Fabrice PIERRE , Alina SILINA , Jinglan ZHOU
IPC分类号： C07D513/04 , C07D515/18 , C07D515/04
CPC分类号： C07D513/04 , C07D515/18 , C07D515/04
摘要： This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having the core structure: pharmaceutical compositions containing at least one such modulator, methods of treatment of cystic fibrosis using such modulators and pharmaceutical compositions, combination therapies, and processes and intermediates for making such modulators.

90. 发明申请

US20220071971A1 MACROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF DISEASE 有权
公开(公告)号：US20220071971A1
公开(公告)日：2022-03-10
申请号：US17415335
申请日：2019-12-18
申请人： NOVARTIS AG
发明人： Mihai Azimioara , Badry Bursulaya , Songchun Jiang , Casey Jacob Nelson MATHISON , Victor Ivanovich NIKULIN , Truc Ngoc NGUYEN , Barun OKRAM , Sejal PATEL , Dean Paul PHILLIPS , Lewis WHITEHEAD , Baogen WU , Shanshan YAN , Xuefeng ZHU
IPC分类号： A61K31/439 , A61K45/06 , C07D515/18 , C07D513/22 , C07D513/18 , A61K31/5377
摘要： The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.

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