公开(公告)号：US20180170859A1

公开(公告)日：2018-06-21

申请号：US15736981

申请日：2016-06-16

Applicant: BIOCON LIMITED

Inventor： Venkata Raghavendracharyulu Palle ,  Ramakrishna Parameshwar Bhat ,  Mariappan Kaliappan ,  Jithendra R. Babu ,  Rajmahendra Shanmughasamy

IPC: C07C255/23 ,  C07C253/14 ,  C07D261/08

CPC classification number: C07C255/23 ,  C07C253/00 ,  C07C253/14 ,  C07D261/08 ,  G01N23/20075 ,  G01N25/4866 ,  G01R33/46

Abstract: The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.

公开(公告)号：US10000456B2

公开(公告)日：2018-06-19

申请号：US14283322

申请日：2014-05-21

Applicant: AMIRA PHARMACEUTICALS, INC.

Inventor： Ryan Clark ,  Brian Andrew Stearns ,  Lucy Zhao ,  Thomas Jon Seiders ,  Deborah Volkots ,  Jeannie M. Arruda

IPC: C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D231/38 ,  C07D261/08 ,  C07D261/14 ,  C07D417/12 ,  C07D413/14

CPC classification number: C07D231/38 ,  C07D261/08 ,  C07D261/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

公开(公告)号：US09957242B2

公开(公告)日：2018-05-01

申请号：US15272313

申请日：2016-09-21

Applicant: Abide Therapeutics, Inc. ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Justin S. Cisar ,  Cheryl A. Grice ,  Todd K. Jones ,  Micah J. Niphakis ,  Jae Won Chang ,  Kenneth M Lum ,  Benjamin F. Cravatt

IPC: C07D213/55 ,  C07D231/12 ,  C07D261/08 ,  A61K31/496 ,  C07D295/205 ,  C07D405/14 ,  C07D215/42 ,  C07D213/40 ,  C07C271/12 ,  C07D317/46 ,  C07D317/58 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D263/32 ,  C07D205/04 ,  C07D491/107 ,  C07D207/14 ,  C07D271/06 ,  C07D295/26 ,  C07D307/79 ,  C07D401/04 ,  C07D407/06 ,  C07D413/06 ,  C07C271/10 ,  C07D207/09 ,  C07D213/38 ,  C07D215/46 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

CPC classification number: C07D295/205 ,  C07C271/10 ,  C07C271/12 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D213/38 ,  C07D213/40 ,  C07D213/55 ,  C07D215/42 ,  C07D215/46 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D295/26 ,  C07D307/79 ,  C07D317/46 ,  C07D317/58 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D405/14 ,  C07D407/06 ,  C07D413/06 ,  C07D413/10 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107

Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.

公开(公告)号：US09938278B2

公开(公告)日：2018-04-10

申请号：US14971825

申请日：2015-12-16

Applicant: Gilead Sciences, Inc.

Inventor： Christian Gege ,  Claus Kremoser ,  Olaf Kinzel ,  Peter A. Blomgren ,  Kevin S. Currie ,  Jeffrey E. Kropf ,  Aaron C. Schmitt ,  William J. Watkins ,  Jianjun Xu

IPC: A61K31/506 ,  C07D471/08 ,  C07D401/14 ,  C07D413/14 ,  C07D261/08 ,  C07D413/12 ,  C07D417/14

CPC classification number: C07D471/08 ,  C07D261/08 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

公开(公告)号：US09926278B2

公开(公告)日：2018-03-27

申请号：US15305407

申请日：2015-04-14

Applicant: E. I. DU PONT DE NEMOURS AND COMPANY

Inventor： Kanu Maganbhai Patel

IPC: C07C311/49 ,  C07D211/02 ,  C07D231/12 ,  C07D213/71 ,  C07D231/16 ,  C07D333/06 ,  C07D333/28 ,  C07D333/34 ,  C07D239/26 ,  C07D239/38 ,  C07D261/08 ,  C07D261/10 ,  C07D277/28 ,  C07D277/32 ,  C07D277/36 ,  C07D213/61 ,  C07D307/52 ,  C07D307/64 ,  C07C303/36

CPC classification number: C07D231/12 ,  C07C303/36 ,  C07C311/49 ,  C07D213/61 ,  C07D213/71 ,  C07D231/16 ,  C07D239/26 ,  C07D239/38 ,  C07D261/08 ,  C07D261/10 ,  C07D277/28 ,  C07D277/32 ,  C07D277/36 ,  C07D307/52 ,  C07D307/64 ,  C07D333/06 ,  C07D333/28 ,  C07D333/34

Abstract: Disclosed are compounds of Formula I, including all stereoisomers, (N-oxides), and salts thereof, wherein A and R are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula I, comprising reacting a compound of Formula II with an aroyl enolate salt of Formula III in the presence of an acid in an aqueous solvent mixture, wherein A, R and M are as defined in the disclosure.Also disclosed is a method for preparing a compound of Formula IV, comprising reacting a compound of Formula I with an aldehyde of Formula V in the presence of a secondary amine salt, wherein A, B and R are as defined in the disclosure

公开(公告)号：US20180079723A1

公开(公告)日：2018-03-22

申请号：US15563128

申请日：2016-03-30

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Ryo Mizojiri ,  Moriteru ASANO ,  Daisuke TOMITA ,  Hiroshi BANNO ,  Michiko TAWADA ,  Noriyuki NII ,  Krista E. GIPSON ,  Hironobu MAEZAKI ,  Shuntaro TSUCHIYA ,  Mayumi IMAI ,  Yuichiro AMANO

IPC: C07D213/65 ,  C07C233/25 ,  C07D401/12 ,  C07C255/54 ,  C07D213/69 ,  C07C233/18 ,  C07D263/42 ,  C07D263/32 ,  C07D413/04 ,  C07D239/34 ,  C07D241/18 ,  C07D277/34 ,  C07D231/12 ,  C07D207/12 ,  C07D261/08 ,  C07D417/04 ,  C07D237/14 ,  C07D211/46 ,  C07D213/74 ,  C07D213/81

CPC classification number: C07D213/65 ,  A61K31/165 ,  A61K31/167 ,  A61K31/277 ,  A61K31/381 ,  A61K31/402 ,  A61K31/415 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  C07C233/18 ,  C07C233/25 ,  C07C233/47 ,  C07C255/54 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/08 ,  C07D207/12 ,  C07D211/44 ,  C07D211/46 ,  C07D213/643 ,  C07D213/69 ,  C07D213/74 ,  C07D213/75 ,  C07D213/81 ,  C07D231/12 ,  C07D237/14 ,  C07D239/34 ,  C07D241/18 ,  C07D261/08 ,  C07D263/32 ,  C07D263/42 ,  C07D277/34 ,  C07D333/20 ,  C07D401/04 ,  C07D401/12 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C12N9/99 ,  C12N15/09

Abstract: The present invention relates to a compound which may be useful as an agent for the prophylaxis or treatment of cancer, hepatitis, hepatic fibrosis, fatty liver and the like.

公开(公告)号：US09895330B2

公开(公告)日：2018-02-20

申请号：US14903091

申请日：2014-07-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jay A Markwalder ,  James Aaron Balog ,  Audris Huang ,  Steven P Seitz

IPC: C07C233/55 ,  C07D257/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D409/12 ,  C07D413/12 ,  C07D487/08 ,  C07D405/12 ,  A61K31/196 ,  A61K31/41 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/422 ,  A61K31/4155 ,  A61K31/5377 ,  C07D417/12 ,  C07D261/08 ,  C07C255/57 ,  A61K45/06 ,  A61K31/427 ,  A61N5/10

CPC classification number: A61K31/196 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10 ,  C07C233/55 ,  C07C255/57 ,  C07C2601/14 ,  C07D257/04 ,  C07D261/08 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/08 ,  Y02A50/411 ,  Y02A50/414

Abstract: There are disclosed compounds of Formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-di-oxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compounds of the invention.

公开(公告)号：US20180016243A1

公开(公告)日：2018-01-18

申请号：US15550155

申请日：2016-02-12

Applicant: AZIENDA OSPEDALIERA UNIVERSITARIA SENESE

Inventor： Andreas MEYERHANS ,  Miguel-Angel MARTINEZ DE LA SIERRA ,  Annalaura BRAI ,  Roberta FAZI ,  Cristina TINTORI ,  Maurizio BOTTA ,  Jose-Este ARAQUE ,  Javier MARTINEZ

IPC: C07D249/06 ,  A61K31/4192 ,  C07D405/12 ,  C07D401/12 ,  C07D401/04 ,  C07D285/12 ,  C07D271/10 ,  C07D271/06 ,  C07D261/08 ,  A61K45/06 ,  A61K31/7056 ,  A61K31/675 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/433 ,  A61K31/4245 ,  A61K31/42 ,  C07F9/6518 ,  C07H15/18

CPC classification number: C07D249/06 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/675 ,  A61K31/7056 ,  A61K45/06 ,  C07D249/04 ,  C07D257/04 ,  C07D261/08 ,  C07D271/06 ,  C07D271/10 ,  C07D285/12 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07F9/6518 ,  C07H15/18

Abstract: The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.

公开(公告)号：US20170373256A1

公开(公告)日：2017-12-28

申请号：US15625290

申请日：2017-06-16

Applicant: Samsung Display Co., Ltd.

Inventor： Soobyung KO ,  Haejin KIM ,  Mieun JUN ,  Youngkook KIM ,  Seokhwan HWANG

IPC: H01L51/00 ,  C07D405/10 ,  C07D413/10 ,  C09K11/06 ,  C07D231/12 ,  C07D261/08 ,  C09K11/02 ,  H01L51/52 ,  H01L51/50

CPC classification number: H01L51/0067 ,  C07D231/12 ,  C07D261/08 ,  C07D405/10 ,  C07D413/10 ,  C09B1/00 ,  C09B23/148 ,  C09B57/00 ,  C09B57/001 ,  C09B57/008 ,  C09B57/02 ,  C09B57/10 ,  C09K11/025 ,  C09K11/06 ,  C09K2211/1018 ,  C09K2211/1466 ,  C09K2211/1475 ,  H01L51/0052 ,  H01L51/0054 ,  H01L51/0056 ,  H01L51/0058 ,  H01L51/0072 ,  H01L51/0073 ,  H01L51/5012 ,  H01L51/5016 ,  H01L51/5056 ,  H01L51/506 ,  H01L51/5072 ,  H01L51/5088 ,  H01L51/5092 ,  H01L51/5096 ,  H01L51/5206 ,  H01L51/5221

Abstract: A heterocyclic compound and an organic light-emitting device including the same are provided. The heterocyclic compound is represented by Formula 1: Details of R1, R2, R3, X1, L1, and a1 and b1 are provided in the disclosure.

公开(公告)号：US20170334893A1

公开(公告)日：2017-11-23

申请号：US15597417

申请日：2017-05-17

Applicant: Enanta Pharmaceuticals, Inc.

Inventor： Yat Sun Or ,  Jun Ma ,  Bin Wang ,  Yong He ,  Xuechao Xing ,  Ruichao Shen ,  Brett Granger ,  Jing He ,  Jiang Long ,  Guoqiang Wang

IPC: C07D413/12 ,  C07D261/08

CPC classification number: C07D413/12 ,  A61K31/42 ,  C07D261/08

Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated as FXR modulators. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR, and methods for their preparation and use.