公开(公告)号：US3121077A

公开(公告)日：1964-02-11

申请号：US19786262

申请日：1962-05-28

申请人： HOFFMANN LA ROCHE

发明人： OSCAR KELLER ,  NORBERT STEIGER ,  HENRYK STERNBACH LEO

IPC分类号： C07D243/20 ,  C07D243/24

CPC分类号： C07D243/24 ,  C07C205/45

公开(公告)号：US12129238B2

公开(公告)日：2024-10-29

申请号：US17415821

申请日：2019-01-30

申请人： Anatoliy Reder ,  Dmytro Pozigun

发明人： Anatoliy Reder ,  Dmytro Pozigun

IPC分类号： C07D243/24 ,  A61P25/02

CPC分类号： C07D243/24 ,  A61P25/02 ,  C07B2200/13

摘要： The invention relates to a crystalline form of the Compound (I), wherein the crystalline form displays its strongest reflection, stated as a 2Θ value, at 25±0.2°, in an X-ray powder diffraction pattern. The invention also relates to a method of making this crystalline form, as well as pharmaceutical compositions comprising thereof. Furthermore, the invention relates to methods of using this crystalline form as a medicament and in the treatment of pain.

公开(公告)号：US12077512B2

公开(公告)日：2024-09-03

申请号：US17442474

申请日：2020-03-25

申请人： President and Fellows of Harvard College

发明人： David D. Ginty ,  Lauren L. Orefice ,  Jinbo Lee

IPC分类号： C07D243/24

CPC分类号： C07D243/24

摘要： The present invention provides novel peripherally-restricted benzodiazepines with reduced blood brain barrier permeability and methods of use thereof for reducing tactile dysfunction, social impairment, and anxiety in a subject diagnosed with Autism Spectrum Disorder, Rett syndrome, Phelan McDermid syndrome, or Fragile X syndrome.

公开(公告)号：US10881666B2

公开(公告)日：2021-01-05

申请号：US16145768

申请日：2018-09-28

申请人： Enanta Pharmaceuticals, Inc.

发明人： Brian C. Shook ,  In Jong Kim ,  Thomas P. Blaisdell ,  Jianming Yu ,  Joseph Panarese ,  Kai Lin ,  Michael H. J. Rhodin ,  Nicole V. McAllister ,  Yat Sun Or

IPC分类号： A61K31/5513 ,  A61P31/14 ,  C07D491/04 ,  C07D213/12 ,  C07D213/14 ,  A61K31/7056 ,  A61K39/42 ,  A61K39/395 ,  C07D403/12 ,  C07K16/10 ,  C07D217/14 ,  C07D243/24 ,  A61K45/06 ,  C07D217/12 ,  A61K31/4439 ,  C07D498/08

摘要： The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a Respiratory Syncytial Virus (RSV) infection, wherein treatment comprises administering a compound effective to inhibit the function of the RSV and an additional compound or combinations of compounds having anti-RSV activity.

公开(公告)号：USRE47475E1

公开(公告)日：2019-07-02

申请号：US15267953

申请日：2016-09-16

申请人： WiSys Technology Foundation, Inc.

发明人： James M. Cook ,  Shengming Huang ,  Rahul Edwankar ,  Ojas A. Namjoshi ,  Zhi-Jian Wang ,  Qi Huang ,  Xiaohui He ,  Xiaoyan Li ,  Jianming Yu ,  Dongmei Han

IPC分类号： A61K31/5517 ,  C07D487/02 ,  C07D243/12 ,  C07D519/00 ,  C07D471/04 ,  C07D487/06 ,  C07D487/04 ,  C07D243/20 ,  C07D495/04 ,  C07D243/24 ,  C07D498/04

摘要： In preferred embodiments, the present invention provides methods of treatment and pharmaceutical compositions for the suppression, alleviation and prevention of the often chronic, severe and debilitating pain that can accompany inflammatory diseases and neuropathic insults, pain that is often unresponsive to conventional analgesic treatment. The preferred embodiments of the present invention further relate to methods of treatment and pharmaceutical compositions using benzodiazepine derivatives that provide suppression, alleviation and prevention of neuropathic pain, migraine-related pain and inflammatory pain with reduced sedative and ataxic side effects.

公开(公告)号：US10266534B2

公开(公告)日：2019-04-23

申请号：US15320866

申请日：2015-06-26

申请人： THE JOHNS HOPKINS UNIVERSITY ,  LIEBER INSTITUTE, INC.

发明人： Pankaj Pasricha ,  Yifang Huang ,  James Barrow

IPC分类号： A61K31/5517 ,  A61P25/00 ,  C07D487/04 ,  C07D243/12 ,  A61K45/06 ,  A61K31/5513 ,  C07D243/24

摘要： The present invention provides compounds and compositions which are positive allosteric modulators of GABA-A receptors that selectively target the peripheral nervous system and organs of the body, and which do not pass through the blood-brain barrier. The compounds and compositions of the present invention are useful for treatment of diseases or disorders which are mediated by GABA-A neuronal activity, such as, for example, visceral pain, gut motility, irritable bowel syndrome, functional abdominal pain, functional idiopathic diarrhea, inflammatory bowel diseases, drug induced pain, bile salt malabsorption, lactase or other carbohydrate intolerance.

公开(公告)号：US20170233386A1

公开(公告)日：2017-08-17

申请号：US15494798

申请日：2017-04-24

申请人： Commissariat a l'Energie Atomique et aux Energies Alternatives

发明人： Roman Lopez ,  Séverine Hebbe ,  Daniel Gillet ,  Julien Barbier

IPC分类号： C07D453/02 ,  C07C211/38 ,  C07C217/58 ,  C07C233/58 ,  C07C317/14 ,  C07D215/12 ,  C07D209/14 ,  C07D451/02 ,  C07C229/14 ,  C07C271/56 ,  C07C251/24 ,  C07D317/46 ,  C07D213/38 ,  C07D233/64 ,  C07C275/28 ,  C07C335/02 ,  C07D243/12 ,  C07D243/24 ,  C07D333/20 ,  C07D307/52

CPC分类号： C07D453/02 ,  A61K31/167 ,  A61K31/341 ,  A61K31/5513 ,  C07C211/27 ,  C07C211/38 ,  C07C215/10 ,  C07C215/42 ,  C07C215/44 ,  C07C217/16 ,  C07C217/58 ,  C07C229/14 ,  C07C229/22 ,  C07C229/38 ,  C07C229/48 ,  C07C233/06 ,  C07C233/58 ,  C07C233/65 ,  C07C237/40 ,  C07C251/24 ,  C07C271/56 ,  C07C275/28 ,  C07C317/14 ,  C07C335/02 ,  C07C2601/08 ,  C07C2602/46 ,  C07C2603/74 ,  C07D209/14 ,  C07D213/38 ,  C07D215/12 ,  C07D233/10 ,  C07D233/58 ,  C07D233/61 ,  C07D233/64 ,  C07D235/08 ,  C07D243/12 ,  C07D243/24 ,  C07D245/06 ,  C07D249/06 ,  C07D307/42 ,  C07D307/52 ,  C07D317/46 ,  C07D317/58 ,  C07D317/62 ,  C07D317/66 ,  C07D333/20 ,  C07D401/04 ,  C07D451/02 ,  C07D471/08 ,  C07D487/04 ,  Y02A50/471 ,  Y02A50/473

摘要： The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.

公开(公告)号：US09676760B2

公开(公告)日：2017-06-13

申请号：US15152231

申请日：2016-05-11

申请人： Gilead Sciences, Inc.

发明人： Britton Kenneth Corkey ,  Elfatih Elzein ,  Michael Graupe ,  Juan Guerrero ,  Robert H. Jiang ,  Rao V. Kalla ,  Dmitry Koltun ,  Xiaofen Li ,  Ruben Martinez ,  Eric Q. Parkhill ,  Thao Perry ,  Chandrasekar Venkataramani ,  Jeff Zablocki

IPC分类号： C07D413/06 ,  A61K31/553 ,  A61K31/5513 ,  C07D267/08 ,  C07D243/24 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/12 ,  C07D413/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D243/14 ,  C07B59/00 ,  C07D413/04 ,  C07D417/14

CPC分类号： C07D413/06 ,  A61K31/5513 ,  A61K31/553 ,  C07B59/002 ,  C07B2200/05 ,  C07D243/14 ,  C07D243/24 ,  C07D267/08 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

公开(公告)号：US09427442B2

公开(公告)日：2016-08-30

申请号：US14429958

申请日：2013-09-20

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Yufen Zhao ,  Ashvinikumar V. Gavai ,  Patrice Gill ,  Soong-Hoon Kim ,  Brian E. Fink ,  Libing Chen ,  Mark G. Saulnier ,  Wen-Ching Han

IPC分类号： C07D243/24 ,  A61K31/5513 ,  A61K45/06

CPC分类号： A61K31/5513 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/555 ,  A61K45/06 ,  C07D243/18 ,  C07D243/24 ,  C07D243/26 ,  A61K2300/00

摘要： Disclosed are compounds of Formula (I): (Formula (I)) wherein: R1 is —CH2CH2CF3; R2 is —CH2CH2CH2F, —CH2CF2CH3, —CH2CH2CF3, —CH2CH(CH3)CF3, —CH2CH2CF2CH3, (Formulae (II), (III), (IV), (V) or (VI): R3 is H or —CH3; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

摘要翻译： 公开了式（I）的化合物：（式（I））其中：R 1是-CH 2 CH 2 CF 3; R2是-CH2CH2CH2F，-CH2CF2CH3，-CH2CH2CF3，-CH2CH（CH3）CF3，-CH2CH2CF2CH3，（式（Ⅱ），（Ⅲ），（Ⅳ），（Ⅴ）或（Ⅵ）：R3是H或-CH3; 环A是苯基或吡啶基; Rx，Ry，Ra，Rb，y和z在本文中定义。还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物，这些化合物可用于 治疗，预防或减缓各种治疗领域（例如癌症）中的疾病或病症的发展。

公开(公告)号：US20150231152A1

公开(公告)日：2015-08-20

申请号：US14429958

申请日：2013-09-20

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Yufen Zhao ,  Ashvinikumar V. Gavai ,  Patrice Gill ,  Soong-Hoon Kim ,  Brian E. Fink ,  Libing Chen ,  Mark G. Saulnier ,  Wen-Ching Han

IPC分类号： A61K31/5513 ,  A61K45/06 ,  C07D243/24

CPC分类号： A61K31/5513 ,  A61K31/138 ,  A61K31/337 ,  A61K31/506 ,  A61K31/555 ,  A61K45/06 ,  C07D243/18 ,  C07D243/24 ,  C07D243/26 ,  A61K2300/00

摘要： Disclosed are compounds of Formula (I): (Formula (I)) wherein: R1 is —CH2CH2CF3; R2 is —CH2CH2CH2F, —CH2CF2CH3, —CH2CH2CF3, —CH2CH(CH3)CF3, —CH2CH2CF2CH3, (Formulae (II), (III), (IV), (V) or (VI): R3 is H or —CH3; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

摘要翻译： 公开了式（I）的化合物：（式（I））其中：R 1是-CH 2 CH 2 CF 3; R2是-CH2CH2CH2F，-CH2CF2CH3，-CH2CH2CF3，-CH2CH（CH3）CF3，-CH2CH2CF2CH3，（式（Ⅱ），（Ⅲ），（Ⅳ），（Ⅴ）或（Ⅵ）：R3是H或-CH3; 环A是苯基或吡啶基; Rx，Ry，Ra，Rb，y和z在本文中定义。还公开了使用这些化合物抑制Notch受体的方法，以及包含这些化合物的药物组合物，这些化合物可用于 治疗，预防或减缓各种治疗领域（例如癌症）中的疾病或病症的发展。