公开(公告)号：US20240254132A1

公开(公告)日：2024-08-01

申请号：US18579846

申请日：2022-07-15

Applicant: Denali Therapeutics Inc.

Inventor： Alex L. Bagdasarian ,  Robert A. Craig, II ,  Javier de Vicente Fidalgo ,  Anthony A. Estrada ,  Benjamin J. Huffman ,  Katrina W. Lexa ,  Maksim Osipov ,  Arun Thottumkara

IPC: C07D487/04 ,  A61K31/4747 ,  A61K31/506 ,  A61K31/519 ,  C07D401/12 ,  C07D491/107

CPC classification number: C07D487/04 ,  A61K31/4747 ,  A61K31/506 ,  A61K31/519 ,  C07D401/12 ,  C07D491/107

Abstract: The present disclosure relates generally to small molecule modulators of NLR Family Pyrin Domain Containing 3 (NL-RP3), or a pharmaceutically acceptable salt, isotopically enriched analog, stereoisomer, mixture of stereoisomers, or prodrug thereof, methods of making and intermediates thereof, and methods of using thereof.

公开(公告)号：US20220401422A1

公开(公告)日：2022-12-22

申请号：US17241981

申请日：2021-04-27

Applicant: Novartis AG

Inventor： Robin Alec FAIRHURST ,  Christine FRITSCH ,  Marc GERSPACHER ,  Jürgen Hans-Hermann HINRICHS ,  Jean-Baptiste Georges Armand LANGLOIS ,  Catherine LEBLANC ,  Tengfei LI ,  Edwige Liliane Jeanne LORTHIOIS ,  Christophe MURA ,  Cristina Montserrat NIETO-OBERHUBER ,  Milen TODOROV ,  Andrea VAUPEL ,  Nicolas WARIN ,  Rainer WILCKEN

IPC: A61K31/437 ,  A61P35/00 ,  C07D471/10 ,  C07D471/20 ,  A61K31/4747 ,  C07D491/20 ,  C07D491/22 ,  A61K31/4375 ,  C07D495/20 ,  C07D495/22 ,  A61K31/436 ,  A61K31/675 ,  A61K31/155 ,  A61K31/5377 ,  A61K31/519 ,  A61K31/635 ,  A61K31/53

Abstract: The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease.

公开(公告)号：US10562857B2

公开(公告)日：2020-02-18

申请号：US15772365

申请日：2016-11-14

Applicant: AFASCI, Inc.

Inventor： Xinmin Xie ,  Frank Kayser

IPC: C07D221/20 ,  A61K31/4747 ,  C07D401/12 ,  C07D409/12 ,  C07D413/14 ,  C07D211/26 ,  C07D413/12 ,  C07D211/58 ,  C07D405/06

Abstract: The present invention is directed towards new chemical entities which primarily inhibit the human T-type calcium channels and differentially modulate other key ion channels to control cell excitability, and abnormal neuronal activity particularly involved in the development and maintenance of persistent or chronic pain, and/or neurological disorders. These novel compounds are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which these ion channels are involved. The invention is also directed towards pharmaceutical formulations comprising these compounds and the uses of these compounds.

公开(公告)号：US09809575B2

公开(公告)日：2017-11-07

申请号：US14357293

申请日：2012-11-12

Applicant: re:Viral Ltd

Inventor： Stuart Cockerill ,  Christopher Pilkington ,  James Lumley ,  Richard Angell ,  Neil Mathews

IPC: C07D403/06 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/4747 ,  A61K31/5386 ,  C07D401/06 ,  C07D413/06 ,  C07D471/10 ,  A61K31/5513 ,  A61K45/06 ,  C07D498/10

CPC classification number: C07D403/06 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/4747 ,  A61K31/5386 ,  A61K31/5513 ,  A61K45/06 ,  C07D401/06 ,  C07D413/06 ,  C07D471/10 ,  C07D498/10

Abstract: Benzimidazoles of formula (I): wherein: A is 5- to 12-membered aryl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, —(CH2)p—, —X—, —CH2—X—, or —X—CH2—; X is —O—, —S—, —N(R2)—, >C═O, >S(═O), >S(═O)2, —O—C(═O)—, —C(═O)—O—, N(R2)—C(═O)—, or —C(═O)—N(R2)—; each L is independently a single bond, C1-3alkylene, C2-3alkenylene or C2-3alkynylene; R1 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, each of which is unsubstituted or substituted; each Z is independently —N(R2)2, —OR2, —SR2, —S(═O)R2, —S(═O)2R2; each R2 is independently hydrogen, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

公开(公告)号：US09708321B2

公开(公告)日：2017-07-18

申请号：US14765615

申请日：2014-01-23

Applicant: Merck Patent GmbH

Inventor： Nadia Brugger ,  Brian L. Hodous ,  Amanda E. Sutton ,  Justin Potnick ,  Theresa L. Johnson ,  Thomas E. Richardson ,  Thomas Francis Nelson Haxell ,  James M. Dorsey ,  Robert James Foglesong

IPC: C07D471/10 ,  C07D239/91 ,  C07D487/10 ,  A61K31/4747 ,  A61K31/527 ,  A61K31/537 ,  C07D498/10

CPC classification number: C07D471/10 ,  A61K31/4747 ,  A61K31/527 ,  A61K31/537 ,  C07D239/91 ,  C07D487/10 ,  C07D498/10

Abstract: The present invention relates to novel spiro-quinazolinone derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.

公开(公告)号：US09457020B2

公开(公告)日：2016-10-04

申请号：US14855564

申请日：2015-09-16

Applicant: Helsinn Healthcare SA ,  Roche Palo Alto LLC

Inventor： Giorgio Calderari ,  Daniele Bonadeo ,  Roberta Cannella ,  Andrew Miksztal ,  Thomas Malefyt ,  Kathleen M Lee

IPC: A01N43/52 ,  A61K31/473 ,  A61K9/00 ,  A61K31/4178 ,  A61K31/4747 ,  A61K47/12 ,  A61K47/16 ,  A61K47/26 ,  A61J3/00 ,  B65B3/04 ,  B65B55/02 ,  A61K47/02 ,  A61K47/18

CPC classification number: A61K9/08 ,  A61J3/00 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/4178 ,  A61K31/473 ,  A61K31/4747 ,  A61K47/02 ,  A61K47/12 ,  A61K47/16 ,  A61K47/183 ,  A61K47/26 ,  B65B3/04 ,  B65B55/02

Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.

公开(公告)号：US09308266B2

公开(公告)日：2016-04-12

申请号：US14070981

申请日：2013-11-04

Applicant: Helsinn Healthcare S.A. ,  Roche Palo Alto LLC

Inventor： Giorgio Calderari ,  Daniele Bonadeo ,  Roberta Cannella ,  Alberto Macciocchi ,  Andrew Miksztal ,  Thomas Malefyt ,  Kathleen M Lee ,  Carmine Panuccio

IPC: A61K31/473 ,  A01N43/52 ,  A61K47/18 ,  A61K9/00 ,  A61K31/4178 ,  A61K31/4747 ,  A61K47/12 ,  A61K47/16 ,  A61K47/26 ,  A61J3/00 ,  B65B3/04 ,  B65B55/02 ,  A61K47/02

CPC classification number: A61K9/08 ,  A61J3/00 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/4178 ,  A61K31/473 ,  A61K31/4747 ,  A61K47/02 ,  A61K47/12 ,  A61K47/16 ,  A61K47/183 ,  A61K47/26 ,  B65B3/04 ,  B65B55/02

Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.

公开(公告)号：US08962612B2

公开(公告)日：2015-02-24

申请号：US13956924

申请日：2013-08-01

Applicant: Astellas Pharma Inc

Inventor： Wataru Hamaguchi ,  Isao Kinoyama ,  Yohei Koganemaru ,  Takehiro Miyazaki ,  Osamu Kaneko ,  Ryuichi Sekioka ,  Takuya Washio

IPC: A61K31/55 ,  C07D209/44 ,  A61K31/4035 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/4747 ,  C07D217/06 ,  C07D217/22 ,  C07D217/24 ,  C07D221/20 ,  C07D223/16 ,  C07D401/04

CPC classification number: C07D209/44 ,  A61K31/4035 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/4747 ,  A61K31/55 ,  C07D217/06 ,  C07D217/22 ,  C07D217/24 ,  C07D221/20 ,  C07D223/16 ,  C07D401/04

Abstract: To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HT5A receptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HT5A receptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed.

Abstract translation: 为了提供一种用于预防或治疗基于5-羟色胺5-HT5A受体调节作用的痴呆和精神分裂症的优异剂，发现以酰基胍基与四氢异喹啉环等的N原子结合的结构为特征的四氢异喹啉衍生物 并且结合不饱和环的环状基团具有有效的5-HT5A受体调节作用和基于调节作用的优异的药理作用，并且还发现四氢异喹啉衍生物可用作治疗或预防痴呆，精神分裂症和 从而完成了本发明。

公开(公告)号：US08945632B2

公开(公告)日：2015-02-03

申请号：US13810668

申请日：2011-07-19

Applicant: Avi Golan ,  Jacob Gopas ,  Janet Ozer ,  Nadav Eisner ,  Adelbert Bacher ,  Wolfgang Eisenreich ,  Elena Ostrozhenkova ,  Hila Winer

Inventor： Avi Golan ,  Jacob Gopas ,  Janet Ozer ,  Nadav Eisner ,  Adelbert Bacher ,  Wolfgang Eisenreich ,  Elena Ostrozhenkova ,  Hila Winer

IPC: A61K31/24 ,  A61K31/44 ,  A61K31/70 ,  A61K31/438 ,  A61K31/4747 ,  A61K36/62 ,  A61K31/7048 ,  A61K33/24

CPC classification number: A61K31/438 ,  A61K31/4747 ,  A61K31/7048 ,  A61K33/24 ,  A61K36/62 ,  A61K2300/00

Abstract: The current invention provides therapeutic methods which include inhibition of nuclear factor κb pathway in a cell based on the discovery of an active fraction of a plant extract termed NUP or a composition which includes NUP. NUP is used in treating and managing different diseases such as cancer, inflammation, and virus infections.

Abstract translation: 本发明提供了治疗方法，其包括基于发现称为NUP的植物提取物的活性部分或包含NUP的组合物在细胞中抑制核因子和细胞通路。 NUP用于治疗和治疗不同疾病，如癌症，炎症和病毒感染。

公开(公告)号：US20140308282A1

公开(公告)日：2014-10-16

申请号：US14357293

申请日：2012-11-12

Applicant: re:Viral Ltd

Inventor： Stuart Cockerill ,  Christopher Pilkington ,  James Lumley ,  Richard Angell ,  Neil Mathews

IPC: C07D403/06 ,  A61K31/437 ,  A61K45/06 ,  A61K31/5513 ,  C07D498/10 ,  A61K31/5386 ,  C07D401/06 ,  A61K31/4747 ,  C07D471/10 ,  A61K31/4184

CPC classification number: C07D403/06 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/4747 ,  A61K31/5386 ,  A61K31/5513 ,  A61K45/06 ,  C07D401/06 ,  C07D413/06 ,  C07D471/10 ,  C07D498/10

Abstract: Benzimidazoles of formula (I): wherein: A is 5- to 12-membered aryl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, —(CH2)p—, —X—, —CH2—X—, or —X—CH2—; X is —O—, —S—, —N(R2)—, >C═O, >S(═O), >S(═O)2, —O—C(═O)—, —C(═O)—O—, N(R2)—C(═O)—, or —C(═O)—N(R2)—; each L is independently a single bond, C1-3alkylene, C2-3alkenylene or C2-3alkynylene; R1 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, each of which is unsubstituted or substituted; each Z is independently —N(R2)2, —OR2, —SR2, —S(═O)R2, —S(═O)2R2; each R2 is independently hydrogen, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

Abstract translation: 式（I）的苯并咪唑：其中：A为5至12元芳基或5至12元杂芳基，其各自为未取代或取代的; Y是单键， - （CH 2）p - ， - X - ， - CH 2 -X-或-X-CH 2 - ; X是-O - ， - S - ， - N（R 2） - ，> C = O，S（= O），S（= O）2，-O-C（= O） - ， - =（O）-O - ， - N（R 2）-C（= O） - 或-C（= O）-N（R 2） - ; 每个L独立地是单键，C1-3亚烷基，C2-3亚烯基或C2-3亚炔基; R1是C1-6烷基，C2-6烯基或C2-6炔基，其各自为未取代或取代的; 每个Z独立地是-N（R 2）2，-OR 2，-SR 2，-S（= O）R 2，-S（= O）2 R 2; 每个R 2独立地是氢，C 1-6烷基，C 2-6烯基或C 2-6炔基，其中所述烷基，烯基和炔基是未取代的或取代的; m为0,1,2或3; n为1,2或3; 和p为1,2或3; 其药学上可接受的盐是RSV的抑制剂，因此可用于治疗或预防RSV感染。