公开(公告)号：US10258626B2

公开(公告)日：2019-04-16

申请号：US15428493

申请日：2017-02-09

Applicant: LES LABORATOIRES SERVIER ,  VERNALIS (R&D) LTD

Inventor： Thierry Le Diguarher ,  Patrick Casara ,  Jérôme-Benoît Starck ,  Jean-Michel Henlin ,  James Edward Paul Davidson ,  James Brooke Murray ,  Christopher John Graham ,  I-Jen Chen ,  Olivier Geneste ,  John Hickman ,  Stéphane Depil ,  Arnaud Le Tiran ,  Mikl{dot over (o)}s Nyerges ,  Guillaume De Nanteuil

IPC: A61K31/55 ,  A61K31/475 ,  A61K31/496 ,  A61K31/541 ,  A61K31/553 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/5383 ,  C07D491/052 ,  C07D401/02 ,  C07D401/12 ,  A61N5/10 ,  C07D471/00 ,  C07D471/04 ,  C07D487/04 ,  C07D207/30 ,  C07D211/06 ,  C07D211/80 ,  A61K45/06 ,  C07D498/04

Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

公开(公告)号：US10137107B2

公开(公告)日：2018-11-27

申请号：US15512493

申请日：2015-09-18

Applicant: New York Blood Center, Inc. ,  The United States of America, as Represented by the Secretary, Department of Health and Human Services

Inventor： Asim Kumar Debnath ,  Francesca Curreli ,  Peter D. Kwong ,  Young Do Kwon

IPC: C07D403/12 ,  A61K31/40 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D207/34 ,  C07C25/00 ,  C07C233/01 ,  C07D207/30 ,  C07D277/20 ,  A61P31/18

Abstract: Substituted phenylpyrrolecarboxamide compounds such as those represented by Formula A can be used in the treatment of HIV infection and related conditions.

公开(公告)号：US09266831B2

公开(公告)日：2016-02-23

申请号：US14303238

申请日：2014-06-12

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tomomi Ikemoto ,  Toshiaki Nagata ,  Naohiro Fukuda

IPC: C07D207/34 ,  C07D207/337 ,  C07D207/333 ,  C07D207/36 ,  C07D401/12 ,  C07C225/14 ,  C07D207/30 ,  C07D207/48

CPC classification number: C07D207/337 ,  C07D207/30 ,  C07D207/333 ,  C07D207/34 ,  C07D207/36 ,  C07D207/48 ,  C07D401/12

Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Abstract translation: 本发明提供了可用作药物的磺酰基吡咯化合物的制备方法，用于该方法的中间体的制备方法和新的中间体。 本发明涉及一种制备磺酰基吡咯化合物（Ⅷ）的方法，其包括还原化合物（III）并水解还原产物得到化合物（Ⅳ），使化合物（Ⅳ）进行磺酰化反应得到化合物（Ⅵ）， 并使化合物（VI）进行胺化反应。

公开(公告)号：US09006249B2

公开(公告)日：2015-04-14

申请号：US13490562

申请日：2012-06-07

Applicant: Gary Mark Coppola ,  Yuki Iwaki ,  Rajeshri Ganesh Karki ,  Toshio Kawanami ,  Gary Michael Ksander ,  Muneto Mogi ,  Robert Sun

Inventor： Gary Mark Coppola ,  Yuki Iwaki ,  Rajeshri Ganesh Karki ,  Toshio Kawanami ,  Gary Michael Ksander ,  Muneto Mogi ,  Robert Sun

IPC: A61K31/505 ,  A61K31/44 ,  A61K31/415 ,  A61K31/40 ,  A61K31/38 ,  A61K31/34 ,  A61K31/335 ,  A61K31/195 ,  C07D239/24 ,  C07D211/00 ,  C07D213/81 ,  C07D233/54 ,  C07D231/10 ,  C07D207/30 ,  C07D333/38 ,  C07D229/02 ,  C07C233/87 ,  C07C233/47 ,  C07C233/63 ,  C07C235/52 ,  C07C251/12 ,  C07C257/06 ,  C07C271/12 ,  C07C275/16 ,  C07C311/19 ,  C07C317/44 ,  C07D207/34 ,  C07D209/18 ,  C07D213/56 ,  C07D213/82 ,  C07D231/14 ,  C07D239/28 ,  C07D271/10 ,  C07D277/64 ,  C07D285/12 ,  C07D303/48 ,  C07D307/68 ,  C07D309/40 ,  C07D333/24 ,  C07D333/40 ,  C07D261/18

CPC classification number: A61K31/194 ,  A61K45/06 ,  C07C233/47 ,  C07C233/63 ,  C07C233/87 ,  C07C235/52 ,  C07C235/74 ,  C07C235/82 ,  C07C251/12 ,  C07C257/06 ,  C07C271/12 ,  C07C275/16 ,  C07C311/19 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07D207/34 ,  C07D209/18 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D239/28 ,  C07D261/18 ,  C07D271/10 ,  C07D277/64 ,  C07D285/12 ,  C07D303/48 ,  C07D307/68 ,  C07D309/40 ,  C07D333/24 ,  C07D333/40

Abstract: The present invention provides a compound of formula I′; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract translation: 本发明提供式I'化合物; 或其药学上可接受的盐，其中R1，R2，R3，X和n如本文所定义。 本发明还涉及制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。

公开(公告)号：US08841332B2

公开(公告)日：2014-09-23

申请号：US13876381

申请日：2009-07-30

Applicant: Samir Bennabi ,  Jurgen Benting ,  Stephane Brunet ,  Philippe Desbordes ,  Peter Dahmen ,  Stephanie Gary ,  Marie-Claire Grosjean-Cournoyer ,  Rachel Rama ,  Philippe Rinolfi ,  Valerie Toquin ,  Arnd Voerste ,  Ulrike Wachendorff-Neumann

Inventor： Samir Bennabi ,  Jurgen Benting ,  Stephane Brunet ,  Philippe Desbordes ,  Peter Dahmen ,  Stephanie Gary ,  Marie-Claire Grosjean-Cournoyer ,  Rachel Rama ,  Philippe Rinolfi ,  Valerie Toquin ,  Arnd Voerste ,  Ulrike Wachendorff-Neumann

IPC: A61K31/415 ,  A61K31/4164 ,  A61K31/41 ,  A61K31/425 ,  A61K31/42 ,  A61K31/40 ,  A61K31/34 ,  C07D285/06 ,  C07D417/02 ,  C07D277/20 ,  C07D413/02 ,  C07D231/02 ,  C07D207/30 ,  A01N43/08 ,  A01N43/78 ,  A01N43/36 ,  A01N43/82 ,  A01N43/56 ,  A01N43/80 ,  C07D231/20 ,  C07D277/56 ,  C07D261/18 ,  C07D207/34 ,  C07D307/68 ,  C07D231/14

CPC classification number: A01N43/56 ,  A01N43/08 ,  A01N43/36 ,  A01N43/78 ,  A01N43/80 ,  A01N43/82 ,  C07D207/34 ,  C07D231/14 ,  C07D231/20 ,  C07D261/18 ,  C07D277/56 ,  C07D285/06 ,  C07D307/68

Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogs, their process of 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. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.

Abstract translation: 本发明涉及式（I）的杀真菌剂N-（2-苯氧基乙基）甲酰胺衍生物，它们的氮杂，硫杂和硅烷类似物，其制备方法，它们作为杀真菌剂的用途，特别是以杀真菌组合物和方法的形式 使用这些化合物或其组合物控制植物的致病真菌。 式（1）其中A，T，W，X，n和Z 3至Z 7表示各种取代基。

公开(公告)号：US08609713B2

公开(公告)日：2013-12-17

申请号：US12775735

申请日：2010-05-07

Applicant: Ramin Faghih ,  Gregory A. Gfesser ,  Christopher L. Lynch ,  Murali Gopalakrishnan ,  Sujatha Gopalakrishnan ,  John Malysz ,  Earl J. Gubbins ,  Rachid El Kouhen ,  Jinhe Li

Inventor： Ramin Faghih ,  Gregory A. Gfesser ,  Christopher L. Lynch ,  Murali Gopalakrishnan ,  Sujatha Gopalakrishnan ,  John Malysz ,  Earl J. Gubbins ,  Rachid El Kouhen ,  Jinhe Li

IPC: A61K31/40 ,  C07D207/30

CPC classification number: C07D207/34 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10

Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.

Abstract translation: 本发明涉及一系列取代的吡咯衍生物，包含其的组合物，以及使用这些化合物和组合物治疗病症和病症的方法。

公开(公告)号：US08450500B2

公开(公告)日：2013-05-28

申请号：US12995714

申请日：2009-06-04

Applicant: Dinesh U. Chimmanamada ,  Weiwen Ying

Inventor： Dinesh U. Chimmanamada ,  Weiwen Ying

IPC: C07D207/30 ,  A61K31/40

CPC classification number: C07D207/34 ,  A61K31/40 ,  C07D207/335 ,  C07D405/06 ,  C07D405/14

Abstract: The present invention relates to substituted pyrrole compounds and compositions comprising substituted pyrrole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted pyrrole compound of the invention, or a pharmaceutical composition comprising such a compound.

公开(公告)号：US08217073B2

公开(公告)日：2012-07-10

申请号：US12775253

申请日：2010-05-06

Applicant: Warren S. Weiner ,  Rachel M. Slade ,  Yevgeniya I. Klimova ,  Ruth J. Walton ,  Mark B. Anderson

Inventor： Warren S. Weiner ,  Rachel M. Slade ,  Yevgeniya I. Klimova ,  Ruth J. Walton ,  Mark B. Anderson

IPC: A61K31/40 ,  C07D207/30

CPC classification number: C07D207/327 ,  C07D207/325 ,  C07D207/33 ,  C07D207/34

Abstract: Novel pyrrole derivatives are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the Aβ42 peptide.

Abstract translation: 公开了新颖的吡咯衍生物作为治疗和预防神经变性疾病的42降低剂，其特征在于包含Aβ42肽的淀粉样蛋白斑的形成或积累。

公开(公告)号：US08110598B2

公开(公告)日：2012-02-07

申请号：US12018555

申请日：2008-01-23

Applicant: Braj Bhushan Lohray ,  Vidya Bhushan Lohray ,  Vijay Kumar Gajubhai Barot

Inventor： Braj Bhushan Lohray ,  Vidya Bhushan Lohray ,  Vijay Kumar Gajubhai Barot

IPC: A61K31/40 ,  C07D295/02 ,  C07D207/30

CPC classification number: C07D207/325 ,  C07D207/33 ,  C07D207/333 ,  C07D207/335 ,  C07D207/36 ,  C07D207/48 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  G06F3/14 ,  G06F3/1438 ,  G09G5/363 ,  G09G2360/122

Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.

Abstract translation: 本发明涉及新的取代吡咯化合物，其衍生物，其类似物，其互变异构形式，其立体异构体，其多晶型物，其药学上可接受的盐，其药学上可接受的溶剂化物和含有它们的药学上可接受的组合物。 本发明特别涉及通式（I）的新型取代吡咯化合物，其类似物，其衍生物，其多晶型物，其互变异构形式，其药学上可接受的盐，其药学上可接受的溶剂合物及其含有它们的药物组合物。 本发明还涉及制备这种化合物的方法，含有这种化合物的组合物以及这种化合物和组合物在医药中的用途。

公开(公告)号：US20110313158A1

公开(公告)日：2011-12-22

申请号：US13203228

申请日：2010-02-26

Applicant: Pravin R. Likhar ,  R. Arundhati ,  M. Lakshmi Kantam

Inventor： Pravin R. Likhar ,  R. Arundhati ,  M. Lakshmi Kantam

IPC: C07D295/06 ,  C07D211/08 ,  C07D211/18 ,  C07C215/74 ,  C07D207/04 ,  C07C253/00 ,  C07C229/52 ,  C07C209/68 ,  B01J31/28 ,  C07D207/30

CPC classification number: B01J31/1616 ,  B01J21/04 ,  B01J23/72 ,  B01J31/2213 ,  B01J37/0203 ,  B01J37/0209 ,  B01J2231/4283 ,  B01J2531/0266 ,  B01J2531/16 ,  C07C209/10 ,  C07C213/02 ,  C07C221/00 ,  C07C227/08 ,  C07C253/30 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D207/323 ,  C07D207/325 ,  C07D207/327 ,  C07D295/033 ,  C07D295/073 ,  Y02P20/584 ,  C07C215/76 ,  C07C223/06 ,  C07C229/56 ,  C07C229/60 ,  C07C255/58 ,  C07C211/52

Abstract: The invention describes the development of highly efficient, recyclable two component system, CuAl-hydrotalcite/rac 1,1′-Binaphthalene-2,2′-diol catalytic system for the N-alkylation of electron deficient aryl chlorides in presence of potassium carbonate as a base at room temperature in 3-6 h, wherein the process is provided for the preparation of various secondary amines via C—N coupling reaction of aliphatic amines(aliphatic open chain, acyclic, benzyl amines and heterocyclic amines) with various aryl chlorides.

Abstract translation: 本发明描述了在碳酸钾存在下电子缺乏芳基氯化物的N-烷基化的高效，可回收的双组分体系CuAl-水滑石/外消旋1,1'-二萘-2,2'-二醇催化体系的开发 碱在3-6小时内室温，其中该方法用于通过脂族胺（脂族开链，无环，苄胺和杂环胺）与各种芳基氯的C-N偶联反应来制备各种仲胺。