公开(公告)号：US09493436B2

公开(公告)日：2016-11-15

申请号：US14114077

申请日：2012-04-25

Applicant: Zhong-Yin Zhang ,  Yantao He ,  Li-Fan Zeng

Inventor： Zhong-Yin Zhang ,  Yantao He ,  Li-Fan Zeng

IPC: C07D417/12 ,  C07D413/12 ,  C07D407/06 ,  C07D307/80 ,  C07D401/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/06 ,  C07D209/42 ,  C07D307/84

CPC classification number: C07D307/80 ,  C07D209/42 ,  C07D307/84 ,  C07D401/12 ,  C07D405/12 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06 ,  C07D413/12 ,  C07D417/12

Abstract: A variety of benzofurans and indole derivatives some with an alkynyl linker are disclosed herein. These compounds are not highly charged at physiological pH and have good bioavailability characteristics. These compounds exhibit selective or at least preferential affinity for the active sites of various sub-sets of protein tyrosine phosphatases. Some of these compounds are excellent inhibitors of Mycobacterium protein tyrosine phosphatase B (mPTPB) a protein tyrosine phosphatase expressed in Mycobacterium tuberculosis and characterized as a virulence factor in the causal agent of tuberculosis. Accordingly, many of these compounds and pharmaceutically acceptable salts thereof are useful for the treatment of diseases such as tuberculosis.

Abstract translation: 本文公开了一些具有炔基接头的各种苯并呋喃和吲哚衍生物。 这些化合物在生理pH下没有高度充电并且具有良好的生物利用度特性。 这些化合物对蛋白酪氨酸磷酸酶的各种亚组的活性位点表现出选择性或至少优先亲和力。 这些化合物中的一些是分枝杆菌蛋白酪氨酸磷酸酶B（mPTPB）在结核分枝杆菌中表达的蛋白酪氨酸磷酸酶的优异抑制剂，其特征在于结核病致病因子中的毒力因子。 因此，这些化合物和其药学上可接受的盐中的许多可用于治疗疾病如结核病。

公开(公告)号：US09487478B2

公开(公告)日：2016-11-08

申请号：US14872967

申请日：2015-10-01

Applicant: Cayman Chemical Company, Inc.

Inventor： Stephen Douglas Barrett ,  Fred Lawrence Ciske ,  Joseph Michael Colombo ,  Gregory William Endres ,  Bradlee David Germain ,  Andriy Kornilov ,  James Bernard Kramer ,  Adam Uzieblo ,  Kirk M. Maxey

IPC: A61K31/4015 ,  A61K31/4025 ,  C07D207/26 ,  C07D409/06 ,  C07D207/273

CPC classification number: C07D207/273 ,  A61K31/4015 ,  A61K31/4025 ,  A61L24/0015 ,  A61L24/0042 ,  A61L24/02 ,  A61L27/12 ,  A61L27/3608 ,  A61L27/365 ,  A61L27/54 ,  A61L27/58 ,  A61L2300/412 ,  A61L2300/604 ,  A61L2430/02 ,  C07D207/26 ,  C07D409/06

Abstract: Disclosed herein are compounds of formula (I) and therapeutic methods of treatment with compounds of formula (I), wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.

Abstract translation: 和式（I）化合物的治疗方法，其中L1，L2，L4，R1，R4，R5，R6和s如说明书中所定义。 式（I）化合物是可用于治疗青光眼，神经性疼痛和相关疾病的EP4激动剂。

公开(公告)号：US20160318916A1

公开(公告)日：2016-11-03

申请号：US15108089

申请日：2014-12-26

Applicant: SHIONOGI & CO., LTD.

Inventor： Satoru TANAKA ,  Tomoyuki OGAWA ,  Yuki OGATA ,  Masahide FUJITA

IPC: C07D417/06 ,  C07D213/85 ,  C07D213/69 ,  C07D239/54 ,  C07D239/47 ,  C07D239/36 ,  C07D401/06 ,  C07D413/06 ,  C07D409/10 ,  C07D405/06 ,  C07D409/06 ,  C07D401/04 ,  C07D405/14 ,  C07D403/04 ,  C07D409/04 ,  C07D237/14 ,  C07D213/68

CPC classification number: C07D417/06 ,  C07D213/68 ,  C07D213/69 ,  C07D213/85 ,  C07D237/14 ,  C07D239/36 ,  C07D239/46 ,  C07D239/47 ,  C07D239/54 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/10 ,  C07D413/06

Abstract: A compound represented by formula (I): wherein Z1 is C(R2) or N; Z3 is CH or N; Z2 is C(R3) or N; provided that Z1 is C(R2) and Z3 is CH when Z2 is N; Ring A is a substituted or unsubstituted aromatic carbocycle, or the like; R1 is substituted or unsubstituted alkyl, or the like; R2 is a hydrogen atom, halogen, or the like; R3 is a hydrogen atom, halogen, or the like; or a pharmaceutically acceptable salt thereof.

公开(公告)号：US09464075B2

公开(公告)日：2016-10-11

申请号：US13119060

申请日：2009-08-21

Applicant: William F. DeGrado ,  Jun Wang

Inventor： William F. DeGrado ,  Jun Wang

IPC: A61K31/44 ,  C07D409/06 ,  A61K31/438 ,  A61K31/4465 ,  C07D211/08 ,  C07D401/04 ,  C07D401/06 ,  C07D413/06

CPC classification number: C07D409/06 ,  A61K31/438 ,  A61K31/4465 ,  C07D211/08 ,  C07D401/04 ,  C07D401/06 ,  C07D413/06

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract translation: 提供能够通过与M2跨膜蛋白相互作用来调节甲型流感病毒的活性的化合物。 还提供了用于治疗受甲型流感感染的疾病状态或感染的方法，其包括施用包含已被鉴定为能够与M2蛋白相互作用的一种或多种化合物的组合物。

公开(公告)号：US09464055B2

公开(公告)日：2016-10-11

申请号：US14615575

申请日：2015-02-06

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： Bart DeCorte ,  Mark Macielag ,  Michael Greco ,  Yue-Mei Zhang ,  Christopher Teleha

IPC: C07D215/44 ,  C07D417/14 ,  C07D409/14 ,  C07D417/06 ,  C07D405/14 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D215/04 ,  C07D215/42 ,  C07D401/04

CPC classification number: C07D215/44 ,  C07D215/04 ,  C07D215/42 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14 ,  C09B11/02

Abstract: The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders.

公开(公告)号：US09453005B2

公开(公告)日：2016-09-27

申请号：US13119052

申请日：2009-08-21

Applicant: William F. DeGrado ,  Jun Wang

Inventor： William F. DeGrado ,  Jun Wang

IPC: A61K31/44 ,  C07D409/06 ,  A61K31/438 ,  A61K31/4465 ,  C07D211/08 ,  C07D401/04 ,  C07D401/06 ,  C07D413/06

CPC classification number: C07D409/06 ,  A61K31/438 ,  A61K31/4465 ,  C07D211/08 ,  C07D401/04 ,  C07D401/06 ,  C07D413/06

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract translation: 提供能够通过与M2跨膜蛋白相互作用来调节甲型流感病毒的活性的化合物。 还提供了用于治疗受甲型流感感染的疾病状态或感染的方法，其包括施用包含已被鉴定为能够与M2蛋白相互作用的一种或多种化合物的组合物。

公开(公告)号：US09447047B2

公开(公告)日：2016-09-20

申请号：US14421757

申请日：2013-03-14

Applicant: Sergei Nekhai ,  Alexander Bukreyev

Inventor： Sergei Nekhai ,  Alexander Bukreyev

IPC: A61K31/47 ,  C07D219/04 ,  A61K31/473 ,  C07D221/16 ,  C07D409/06 ,  C07D417/12

CPC classification number: C07D219/04 ,  A61K31/473 ,  C07D221/16 ,  C07D409/06 ,  C07D417/12

Abstract: Inhibitors of protein phosphatase-1 (PP-1) and their use in a method for the treatment or prevention of viral infections caused by HIV or ebola virus are disclosed. Inhibitors of protein phosphatase-1 in effective amounts have been shown to slow down viral replication upon contacting ebola virus or cells containing the ebola virus.

Abstract translation: 公开了蛋白质磷酸酶-1（PP-1）的抑制剂及其在治疗或预防HIV或埃博拉病毒引起的病毒感染的方法中的用途。 有迹象的蛋白磷酸酶-1的抑制剂已被证明可减缓接触埃博拉病毒或含有埃博拉病毒的细胞时的病毒复制。

公开(公告)号：US20160257699A1

公开(公告)日：2016-09-08

申请号：US15153699

申请日：2016-05-12

Applicant: Forma Therapeutics, Inc.

Inventor： Kenneth W. BAIR ,  Torsten HERBERTZ ,  Goss S. KAUFFMAN ,  Katherine J. KAYSER-BRICKER ,  George P. LUKE ,  Matthew W. MARTIN ,  David S. MILLAN ,  Shawn E.R. SCHILLER ,  Adam C. TALBOT ,  Mark J. TEBBE

IPC: C07D498/04 ,  A61K31/498 ,  A61K45/06 ,  C07D405/14 ,  C07D417/14 ,  C07D417/10 ,  C07D241/42 ,  C07D409/14 ,  C07D405/06 ,  C07D413/14 ,  A61K31/506 ,  C07D413/04 ,  C07D401/04 ,  A61K31/517 ,  C07D471/04 ,  A61K31/4985 ,  C07D401/14 ,  C07D403/10 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K31/55 ,  A61K31/553 ,  C07D403/04

CPC classification number: C07D498/04 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D241/42 ,  C07D241/50 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D495/04 ,  A61K2300/00

Abstract: The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R1, R2, R4 and R7 are defined herein.

公开(公告)号：US09434690B2

公开(公告)日：2016-09-06

申请号：US14780925

申请日：2014-03-27

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： Susanne Röhrig ,  Alexander Hillisch ,  Julia Straβburger ,  Stefan Heitmeier ,  Martina Victoria Schmidt ,  Karl-Heinz Schlemmer ,  Adrian Tersteegen ,  Anja Buchmüller ,  Christoph Gerdes ,  Martina Schäfer ,  Tom Kinzel ,  Henrik Teller ,  Hartmut Schirok ,  Jürgen Klar ,  Eloisa Jimenez Nunez

IPC: C07D213/64 ,  C07D401/12 ,  A61K31/4412 ,  C07D413/14 ,  C07D213/85 ,  C07D405/06 ,  C07D409/06 ,  C07D413/12 ,  C07D417/12 ,  C07D213/69 ,  C07D213/84

CPC classification number: C07D405/06 ,  C07B2200/05 ,  C07D213/64 ,  C07D213/69 ,  C07D213/84 ,  C07D213/85 ,  C07D401/12 ,  C07D409/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

Abstract translation: 本发明涉及取代的氧代吡啶衍生物及其制备方法，以及它们用于制备用于治疗和/或预防疾病，特别是心血管疾病，优选血栓形成或血栓栓塞性疾病，以及眼药水以及眼科疾病的药物的用途 。

公开(公告)号：US20160244433A1

公开(公告)日：2016-08-25

申请号：US15028004

申请日：2014-10-07

Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFT

Inventor： Philippe DESBORDES ,  Philippe RINOLFI ,  Tomoki TSUCHIYA

IPC: C07D403/06 ,  A01N61/00 ,  C07D405/14 ,  A01N43/56 ,  C07D401/06 ,  A01N43/36 ,  C07D405/06 ,  C07D417/06 ,  A01N43/78 ,  A01N43/647 ,  C07D409/06

CPC classification number: C07D403/06 ,  A01N43/36 ,  A01N43/56 ,  A01N43/647 ,  A01N43/78 ,  A01N61/00 ,  C07D207/06 ,  C07D211/12 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D417/06

Abstract: The present invention relates to fungicidal N-hetarylcarbonyl-2-(benzocycloalken-1-yl)piperidines or pyrrolidines of formula (I), and their thiocarbonyl derivatives, wherein A represents a carbo-linked, unsaturated or partially saturated, 5-membered heterocyclyl group that can be substituted by up to four groups R that can be the same or different; T represents 0 or S; n represents 1 or 2; m represents 1, 2 or 3; p represents 1, 2, 3 or 4, L1 and L2 independently represent CZ4Z5, NZ6, 0, S, S(O) or S(0)2; and R and Z1-Z6 are as defined in the claims; their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

Abstract translation: 本发明涉及式（I）的杀真菌N-叔丁基羰基-2-（苯并环烯烃-1-基）哌啶或吡咯烷及其硫代羰基衍生物，其中A表示碳连接的不饱和或部分饱和的5元杂环基 可以被最多四个可以相同或不同的R基团取代的基团; T表示0或S; n表示1或2; m表示1,2或3; p表示1,2,3或4，L1和L2独立地表示CZ4Z5，NZ6,0，S，S（O）或S（0）2; 并且R和Z1-Z6如权利要求中所定义; 它们的制备方法和用于其制备的中间体化合物，它们用作杀真菌剂，特别是以杀真菌剂的形式和用于使用这些化合物或其组合物控制植物病原性真菌的方法。