公开(公告)号：US20170312252A1

公开(公告)日：2017-11-02

申请号：US15482584

申请日：2017-04-07

Applicant: GENENTECH, INC. ,  CONSTELLATION PHARMACEUTICALS, INC.

Inventor： Kwong Wah Lai ,  Jun Liang ,  Birong Zhang ,  Sharada Labadie ,  Daniel Ortwine ,  Peter Dragovich ,  James Kiefer ,  Victor S. Gehling ,  Jean-Christophe Harmange

IPC: A61K31/41 ,  A61K31/4025 ,  C07D207/04 ,  C07D237/04

CPC classification number: A61K31/41 ,  A61K31/4025 ,  C07D207/04 ,  C07D237/04 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

Abstract: The present invention relates to compounds useful as inhibitors of one or more histone demethylses, such as KDM5. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

公开(公告)号：US20160370700A1

公开(公告)日：2016-12-22

申请号：US15252553

申请日：2016-08-31

Applicant: JSR CORPORATION

Inventor： Hayato NAMAI ,  Norihiko IKEDA ,  Takanori KAWAKAMI

IPC: G03F7/004 ,  G03F7/038 ,  C07D207/416 ,  C07C381/12 ,  C07D295/185 ,  C07D493/10 ,  C07D307/94 ,  C07D311/20 ,  C07C309/17 ,  C07D317/24 ,  C07D307/93 ,  C07D327/04 ,  C07D307/33 ,  C07D307/60 ,  C07D211/46 ,  C07D237/04 ,  C07C309/18 ,  C07D319/06 ,  C07C309/27 ,  C07D321/12 ,  G03F7/039

CPC classification number: G03F7/0045 ,  C07C309/17 ,  C07C309/18 ,  C07C309/27 ,  C07C381/12 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D207/416 ,  C07D211/46 ,  C07D237/04 ,  C07D237/16 ,  C07D295/18 ,  C07D295/185 ,  C07D307/33 ,  C07D307/60 ,  C07D307/64 ,  C07D307/93 ,  C07D307/94 ,  C07D311/20 ,  C07D311/74 ,  C07D313/06 ,  C07D317/24 ,  C07D319/06 ,  C07D321/12 ,  C07D327/04 ,  C07D493/10 ,  G03F7/0046 ,  G03F7/027 ,  G03F7/038 ,  G03F7/0388 ,  G03F7/039 ,  G03F7/0392 ,  G03F7/0397 ,  G03F7/11 ,  G03F7/2041

Abstract: A photoresist composition containing (A) a polymer having a structural unit (I) that includes an acid-labile group, and (I) a compound represented by the following formula (1). In the following formula (1), R1, R2, R3 and R represent a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms. X represents a single bond, an oxygen atom or —NRa—. Ra represents a hydrogen atom, a hydroxy group or a monovalent organic group having 1 to 20 carbon atoms, and optionally taken together represents a ring structure by binding with R each other. A− represents —SO3− or —CO2−. M+ represents a monovalent onium cation.

公开(公告)号：US20160347761A1

公开(公告)日：2016-12-01

申请号：US15234675

申请日：2016-08-11

Applicant: The General Hospital Corporation d/b/a Massachusetts General Hospital ,  The Broad Institute, Inc. ,  Massachusetts Institute of Technology

Inventor： Edward Holson ,  Florence Fevrier Wagner ,  Michel Weiwer ,  Li-Huei Tsai ,  Stephen J. Haggarty ,  Yan-Ling Zhang

IPC: C07D491/107 ,  A61K31/381 ,  C07C233/43 ,  A61K31/167 ,  C07D409/12 ,  A61K31/397 ,  A61K31/4535 ,  C07D213/40 ,  A61K31/4418 ,  C07D241/12 ,  A61K31/4965 ,  C07D211/62 ,  A61K31/445 ,  C07D309/08 ,  A61K31/351 ,  C07D407/12 ,  A61K31/4433 ,  A61K31/403 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/496 ,  C07D295/185 ,  C07D491/08 ,  A61K31/439 ,  C07D403/12 ,  A61K31/501 ,  C07D487/10 ,  C07D237/04 ,  A61K31/50 ,  C07D231/04 ,  A61K31/415 ,  C07D205/04 ,  A61K31/4545 ,  C07C233/42 ,  C07D211/34 ,  A61K31/4178 ,  C07D209/52 ,  C07D311/04 ,  A61K31/352 ,  C07D209/44 ,  A61K31/4035 ,  C07D487/04 ,  A61K31/519 ,  C07D471/04 ,  A61K31/437 ,  C07D333/20

Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

Abstract translation: 或其药学上可接受的盐，水合物，溶剂合物或前药，其中U，J，V，X，R 2a，R 2b，R 2c，R 5和t如本文所述。 本发明一般涉及组蛋白脱乙酰酶的抑制剂及其制备和使用方法。 这些化合物可用于促进认知功能和增强学习和记忆形成。 此外，这些化合物可用于治疗，减轻和/或预防各种病症，包括例如神经障碍，记忆和认知功能障碍/损伤，灭绝学习障碍，真菌疾病和感染，炎性疾病，血液疾病和 人类和动物中的肿瘤性疾病。

公开(公告)号：US20130338162A1

公开(公告)日：2013-12-19

申请号：US13953558

申请日：2013-07-29

Applicant: Lijun Sun ,  Keizo Koya ,  Shoujun Chen ,  Zachary Demko ,  Zhi-Qiang Xia

Inventor： Lijun Sun ,  Keizo Koya ,  Shoujun Chen ,  Zachary Demko ,  Zhi-Qiang Xia

IPC: C07C327/56 ,  C07D277/50 ,  C07D213/81 ,  C07D231/08 ,  C07D237/04

CPC classification number: C07C327/56 ,  C07C243/24 ,  C07C255/56 ,  C07C255/58 ,  C07C337/02 ,  C07C337/06 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/34 ,  C07D213/81 ,  C07D213/86 ,  C07D231/08 ,  C07D237/04 ,  C07D277/50 ,  C07D303/48 ,  C07D307/66 ,  C07D307/68 ,  C07D309/38 ,  C07D333/36 ,  C07D333/38

Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

Abstract translation: 公开了使用本发明化合物治疗患有增殖性疾病如癌症的受试者的化合物和方法，以及用于治疗响应于Hsp70诱导和/或自然杀伤诱导的病症的方法。 此外，公开了包含本发明化合物和药学上可接受的载体的药物组合物。

公开(公告)号：US08357689B2

公开(公告)日：2013-01-22

申请号：US12669978

申请日：2008-07-25

Applicant: Holger Wagner ,  Elke Langkopf ,  Matthias Eckhardt ,  Ruediger Streicher ,  Corinna Schoelch ,  Annette Schuler-Metz ,  Alexander Pautsch

Inventor： Holger Wagner ,  Elke Langkopf ,  Matthias Eckhardt ,  Ruediger Streicher ,  Corinna Schoelch ,  Annette Schuler-Metz ,  Alexander Pautsch

IPC: A61K31/404 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  C07D237/04 ,  C07D403/04

CPC classification number: C07F9/5728 ,  C07F9/65038 ,  C07F9/65068 ,  C07F9/65324 ,  C07F9/6541 ,  C07F9/655354 ,  C07F9/65583 ,  C07F9/65586

Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

Abstract translation: 本发明涉及以下通式的取代芳基磺酰氨基甲基膦酸衍生物其中R，X，Y和Z如权利要求1所定义，其互变异构体，对映异构体，非对映体，其混合物及其盐具有有价值的药理学性质， 的糖原磷酸化酶a与糖原相关蛋白磷酸酶1（PP1）的GL亚基的相互作用，以及它们作为药物组合物的用途。

公开(公告)号：US20120190124A1

公开(公告)日：2012-07-26

申请号：US13389625

申请日：2010-08-09

Applicant: Mark Smith ,  Stephen Caddick ,  James Baker

Inventor： Mark Smith ,  Stephen Caddick ,  James Baker

IPC: C07K1/00 ,  C07D207/456 ,  C07K1/14 ,  C07D237/04 ,  G01N21/75 ,  C07K14/655 ,  C07D495/04

CPC classification number: C07K14/655 ,  A61K47/551 ,  A61K47/60 ,  A61K47/62 ,  A61K49/0017 ,  C07D207/416 ,  C07D207/456 ,  C07D209/52 ,  C07K14/435 ,  G01N33/58 ,  Y02P20/55

Abstract: The present invention relates to the use of a compound containing a moiety of formula (I) as a reagent for linking a compound of formula R1—H which comprises a first functional moiety of formula F1 to a second functional moiety of formula F2 wherein X, X′, Y, R1, F1 and F2 are as defined herein. The present invention also provides related processes and products. The present invention is useful for creating functional conjugate compounds, and specifically conjugates in which at least one of the constituent molecules carries a thiol group.

Abstract translation: 本发明涉及含有式（I）部分的化合物作为将包含式F1的第一功能部分的式R 1 -H的化合物与式F2的第二功能部分连接的试剂的用途，其中X， X'，Y，R1，F1和F2如本文所定义。 本发明还提供了相关的方法和产品。 本发明可用于产生功能性缀合化合物，特别是缀合物，其中至少一种构成分子携带巯基。

公开(公告)号：US20120165524A1

公开(公告)日：2012-06-28

申请号：US13384211

申请日：2010-07-12

Applicant: Dharmaraj Ramachandra Rao ,  Rajendra Narayanrao Kankan ,  Manjinder Singh Phull ,  Ashwini Amol Sawant

Inventor： Dharmaraj Ramachandra Rao ,  Rajendra Narayanrao Kankan ,  Manjinder Singh Phull ,  Ashwini Amol Sawant

IPC: C07D237/04

CPC classification number: C07D237/04

Abstract: In an embodiment, the present invention provides a process for preparing (−)-6-(4-aminophenyl)-5-methylpyridazin-3-(2H)-one, which process comprises: a) reacting racemic 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone of formula II with a chiral tartaric acid derivative to obtain a diastereomeric salt of (−)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone and the chiral tartaric acid derivative; and b) reacting the diastereomeric salt with a base to obtain (−)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone. The (−)-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone may be used to prepare levosimendan.

Abstract translation: 在一个实施方案中，本发明提供了制备（ - ） - 6-（4-氨基苯基）-5-甲基哒嗪-3-（2H） - 酮的方法，该方法包括：a）使外消旋的6-（4-氨基苯基） ）-4,5-二氢-5-甲基-3-（2H） - 哒嗪酮与手性酒石酸衍生物反应，得到（ - ） - 6-（4-氨基苯基） 二氢-5-甲基-3-（2H） - 哒嗪酮和手性酒石酸衍生物; 和b）使非对映体盐与碱反应，得到（ - ） - 6-（4-氨基苯基）-4,5-二氢-5-甲基-3-（2H） - 哒嗪酮。 （ - ） - 6-（4-氨基苯基）-4,5-二氢-5-甲基-3-（2H） - 哒嗪酮可用于制备左西孟旦。

公开(公告)号：US20110251208A1

公开(公告)日：2011-10-13

申请号：US13126541

申请日：2009-11-23

Applicant: Juergen Daemmgen ,  Olaf Joens

Inventor： Juergen Daemmgen ,  Olaf Joens

IPC: A61K31/501 ,  C07D401/04 ,  C07D237/04 ,  C07D233/70 ,  A61P9/00 ,  A61K31/444 ,  A61K31/50 ,  A61K31/4166 ,  A61K31/4439 ,  C07D403/10 ,  C07D401/06

CPC classification number: C07D237/04 ,  A61K31/00 ,  A61K31/10 ,  A61K31/277 ,  A61K31/33 ,  A61K31/4166 ,  A61K31/4178 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/501 ,  A61K31/635 ,  C07D403/04 ,  A61K2300/00

Abstract: The present invention relates to a phosphodiesterase type III (PDE III) inhibitor and/or Ca2+- sensitizing agent or a pharmaceutically acceptable derivative thereof for the treatment of a patient suffering from hypertrophic cardiomyopathy (HCM). According to another aspect the present invention relates to the use of a PDE III inhibitor and/or Ca2+-sensitizing agent for the preparation of a medicament for the treatment of a patient suffering from HCM.

Abstract translation: 本发明涉及用于治疗肥厚性心肌病（HCM）患者的磷酸二酯酶III型（PDE III）抑制剂和/或Ca 2+增敏剂或其药学上可接受的衍生物。 根据另一方面，本发明涉及PDE III抑制剂和/或Ca 2+敏化剂在制备用于治疗患有HCM的患者的药物中的用途。

公开(公告)号：US20100184602A1

公开(公告)日：2010-07-22

申请号：US12638180

申请日：2009-12-15

Applicant: Stefan Lehr ,  Thomas Schenke ,  Christopher Hugh Rosinger ,  Reiner Fischer ,  Isolde Häuser-Hahn ,  Dieter Feucht ,  Jan Dittgen ,  Pierre Cristau ,  Oliver Gaertzen ,  Stefan Herrmann ,  Olga Malsam ,  Eva-Maria Franken

Inventor： Stefan Lehr ,  Thomas Schenke ,  Christopher Hugh Rosinger ,  Reiner Fischer ,  Isolde Häuser-Hahn ,  Dieter Feucht ,  Jan Dittgen ,  Pierre Cristau ,  Oliver Gaertzen ,  Stefan Herrmann ,  Olga Malsam ,  Eva-Maria Franken

IPC: A01N43/58 ,  C07D237/04 ,  A01P21/00

CPC classification number: C07D237/16

Abstract: The invention describes phenyl-substituted pyridazinones of the formula (I) as herbicides and insecticides. In this formula (I), A, B, G, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen, nitro and cyano.

Abstract translation: 本发明描述了作为除草剂和杀虫剂的式（I）的苯基取代的哒嗪酮。 在该式（I）中，A，B，G，X，Y和Z是诸如氢，有机基团如烷基和其它基团如卤素，硝基和氰基的基团。

公开(公告)号：US07511038B2

公开(公告)日：2009-03-31

申请号：US10578594

申请日：2004-11-08

Applicant: Vittorio Dal Piaz ,  Nuria Aguilar Izquierdo ,  Maria Antonia Buil Albero ,  Yolanda Garrido Rubio ,  Maria Paola Giovannoni ,  Jordi Gracia Ferrer ,  Wenceslao Lumeras Amador ,  Claudia Vergelli

Inventor： Vittorio Dal Piaz ,  Nuria Aguilar Izquierdo ,  Maria Antonia Buil Albero ,  Yolanda Garrido Rubio ,  Maria Paola Giovannoni ,  Jordi Gracia Ferrer ,  Wenceslao Lumeras Amador ,  Claudia Vergelli

IPC: C07D237/04 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  A61K31/501

CPC classification number: C04B35/632 ,  C07D237/22 ,  C07D237/24 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04

Abstract: New pyridazin-e-(2H)-one derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of phosphodiesterase 4.

Abstract translation: 公开了具有通式（I）化学结构的新的哒嗪e-（2H） - 酮衍生物; 以及其制备方法，包含它们的药物组合物及其在治疗中作为磷酸二酯酶抑制剂4的用途。