公开(公告)号：US09957251B2

公开(公告)日：2018-05-01

申请号：US15304623

申请日：2015-04-16

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Takaharu Hirayama ,  Jun Fujimoto ,  Douglas Robert Cary ,  Masanori Okaniwa ,  Yasuhiro Hirata

IPC: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D491/08 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4704 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/499 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/553 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107 ,  C07D498/08 ,  C07D213/64

CPC classification number: C07D401/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4704 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/499 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/553 ,  C07D213/64 ,  C07D401/14 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

Abstract: The present invention provides a heterocyclic compound having a CDK8 and/or CDK19 inhibitory effect. The present invention provides a compound represented by formula (I) (in the formula, the symbols are as defined in the description) or a salt thereof.

公开(公告)号：US09951065B2

公开(公告)日：2018-04-24

申请号：US15153527

申请日：2016-05-12

Applicant: Gilead Sciences, Inc.

Inventor： Mark J. Bartlett ,  Julian Andrew Codelli ,  Britton Kenneth Corkey ,  Jennifer Leigh Cosman ,  Kristyna Elbel ,  Jennifer Alissa Loyer-Drew ,  David Sperandio ,  Joshua Van Veldhuizen ,  Hai Yang ,  Suet Chung Yeung

IPC: C07D235/06 ,  C07D235/24 ,  C07D295/125 ,  C07D401/12 ,  C07D471/04 ,  A61K45/06 ,  C07D235/08 ,  A61K31/4184 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/437 ,  A61K31/506 ,  A61K31/497 ,  A61K31/55 ,  A61K31/541 ,  A61K31/439 ,  C07D405/12 ,  C07D405/14 ,  C07D471/08 ,  A61K31/553 ,  C07D235/30 ,  C07D235/14 ,  C07D401/04 ,  C07D235/12 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/538 ,  A61K31/5386 ,  A61K31/438 ,  C07D403/12 ,  A61K31/4439 ,  C07D413/12 ,  A61K31/496 ,  C07D487/04 ,  A61K31/4725 ,  C07D235/28 ,  C07D235/16 ,  C07D409/12

CPC classification number: C07D471/04 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D235/06 ,  C07D235/08 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D235/24 ,  C07D235/28 ,  C07D235/30 ,  C07D295/125 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D471/08 ,  C07D487/04

Abstract: The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.

公开(公告)号：US20170312217A9

公开(公告)日：2017-11-02

申请号：US14664522

申请日：2015-03-20

Applicant: Hsin-Yung Lin

Inventor： Hsin-Yung Lin

IPC: A61K9/00 ,  A61K31/46 ,  A61K31/277 ,  A61K31/198 ,  A61K31/137 ,  A61K47/02 ,  A61K31/635 ,  A61K31/616 ,  A61K31/554 ,  A61K31/55 ,  A61K31/519 ,  A61K31/498 ,  A61K31/445 ,  A61K31/4422 ,  A61K31/4406 ,  A61K31/439 ,  A61K31/4365 ,  A61K31/4152 ,  A61K31/405 ,  A61K31/34 ,  A61K31/27 ,  A61K31/21 ,  A61K31/197 ,  A61K31/192 ,  A61K31/165 ,  A61K31/13 ,  A61K31/48 ,  A61K31/5386

CPC classification number: A61K9/0004 ,  A61K9/007 ,  A61K9/0073 ,  A61K9/0078 ,  A61K31/13 ,  A61K31/137 ,  A61K31/165 ,  A61K31/192 ,  A61K31/195 ,  A61K31/197 ,  A61K31/198 ,  A61K31/21 ,  A61K31/27 ,  A61K31/277 ,  A61K31/34 ,  A61K31/405 ,  A61K31/4152 ,  A61K31/4365 ,  A61K31/439 ,  A61K31/4406 ,  A61K31/4422 ,  A61K31/445 ,  A61K31/46 ,  A61K31/48 ,  A61K31/498 ,  A61K31/519 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/554 ,  A61K31/616 ,  A61K31/635 ,  A61K47/02

Abstract: The present invention provides an inhalation-type pharmaceutical composition for gout and preparation method thereof, comprising a first gas and an atomized medicine. The first gas comprises hydrogen. The gas volume concentration of hydrogen in the inhalation-type pharmaceutical composition is between 2 to 96%. The atomized medicine is selected from a group comprising colchicine, allopurinol, probenecid, sulfinpyrazone, and any combination thereof. The inhalation-type pharmaceutical composition of the present invention can remove harmful radicals in the body of the patient through the use of hydrogen while also increases the absorption effect of the medicine for the patient by using an atomized medicine. At the same time, because the use of the small amount of the vaporized pharmaceutical liquid can indirectly reduce the side effects on the user.

公开(公告)号：US20170275283A1

公开(公告)日：2017-09-28

申请号：US15505277

申请日：2015-10-26

Applicant: Alexander PASTERNAK ,  Fa-Xiang DING ,  Shuzhi DONG ,  Jinlong JIANG ,  Haifeng TANG ,  Xin GU ,  Reynalda K. DEJESUS ,  Jessica FRIE ,  Qinghong FU ,  Takao SUZUKI ,  Zhifa PU ,  Merck Sharp & Dohme Corp.

Inventor： Alexander Pasternak ,  Fa-Xiang Ding ,  Shuzhi Dong ,  Jinlong Jiang ,  Haifeng Tang ,  Xin Gu ,  Reynalda K. DeJesus ,  Jessica Frie ,  Qinghong Fu ,  Takao Suzuki ,  Zhifa Pu

IPC: C07D471/10 ,  C07D498/10 ,  A61K31/5386 ,  A61K45/06 ,  A61K31/435 ,  A61K31/537 ,  C07D498/20 ,  A61K31/553 ,  A61K31/499 ,  A61K31/55

CPC classification number: C07D471/10 ,  A61K31/401 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/4422 ,  A61K31/499 ,  A61K31/537 ,  A61K31/5386 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D487/10 ,  C07D498/10 ,  C07D498/20 ,  A61K2300/00

Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

公开(公告)号：US20170253615A1

公开(公告)日：2017-09-07

申请号：US15511443

申请日：2015-09-14

Applicant: CHRONOS THERAPEUTICS LIMITED

Inventor： Susanna CREMONESI ,  Tim LUKER ,  Teresa SEMERARO ,  Fabrizio MICHELI

IPC: C07D498/10 ,  C07D471/10 ,  C07D491/20 ,  C07D513/10

CPC classification number: C07D498/10 ,  A61K31/438 ,  A61K31/499 ,  A61K31/5386 ,  A61K31/547 ,  A61K31/551 ,  C07D471/10 ,  C07D491/20 ,  C07D493/20 ,  C07D513/10

Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter); and methods of treating patients with such compounds; wherein R1, R2, R3, R4, R5, R6, R9, R10, Q, X, Y, Z, A, L, B, m, n and p are as defined herein.

公开(公告)号：US09750719B2

公开(公告)日：2017-09-05

申请号：US14802982

申请日：2015-07-17

Applicant: CONVERGENCE PHARMACEUTICALS LIMITED

Inventor： Paul Beswick ,  Robert James Gleave ,  Shuji Hachisu ,  Sadie Vile ,  Nicolas Bertheleme ,  Simon E. Ward

IPC: A61K31/41 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/5386 ,  C07D257/04 ,  C07D257/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  C07D471/10 ,  C07D487/14 ,  C07D487/08 ,  C07D491/08 ,  C07D513/04 ,  C07D471/04 ,  C07D487/04 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551

CPC classification number: A61K31/41 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  C07D257/04 ,  C07D257/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D513/04

Abstract: The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial. Formula (I) wherein A is: (II) or (III) wherein A is

公开(公告)号：US09725465B2

公开(公告)日：2017-08-08

申请号：US14473597

申请日：2014-08-29

Applicant: Ambit Biosciences Corporation

Inventor： Mark W. Holladay ,  Gang Liu ,  Martin W. Rowbottom

IPC: C07D498/08 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/655 ,  A61K45/06 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D403/12 ,  C07D413/14 ,  C07D498/14

CPC classification number: C07D498/08 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/655 ,  A61K45/06 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/14

Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.

公开(公告)号：US20170217897A1

公开(公告)日：2017-08-03

申请号：US15500870

申请日：2015-08-03

Applicant: Zhigan JIANG ,  Jianhua XIA ,  Haiying HE ,  NOVARTIS AG

Inventor： Javier de Vicente FIDALGO ,  Haiying HE ,  Cheng HU ,  Zhigan JIANG ,  Xiaolin LI ,  Peichao LU ,  Wosenu MERGO ,  Daniel MUTNICK ,  Folkert RECK ,  Alexey RIVKIN ,  Colin Keith SKEPPER ,  Xiaojing Michael WANG ,  Jianhua XIA ,  Yongjin XU

IPC: C07D215/38 ,  A61K31/4709 ,  A61K31/496 ,  C07D401/14 ,  C07D413/14 ,  C07D419/14 ,  C07D405/14 ,  C07D471/04 ,  C07D498/10 ,  A61K31/5377 ,  A61K31/5386 ,  C07D487/10 ,  C07D471/10 ,  A61K45/06 ,  C07D401/04

CPC classification number: C07D215/38 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D215/22 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D419/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/10 ,  C07D498/10 ,  Y02A50/406 ,  Y02A50/47 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/481

Abstract: This invention is in the field of medicinal chemistry and relates to compounds, and pharmaceutical compositions thereof, that inhibit bacterial gyrase. The compounds are useful as inhibitors of bacterial gyrase activity and bacterial infections, and have the structure of Formula (I) as further described herein. The invention further provides pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds and compositions to treat bacterial infections.

公开(公告)号：US20170189401A1

公开(公告)日：2017-07-06

申请号：US15466925

申请日：2017-03-23

Applicant: GlaxoSmithKline Intellectual Property (No.2) Limited

Inventor： Dominique AMANS ,  Stephen John ATKINSON ,  Lee Andrew HARRISON ,  David Jonathan HIRST ,  Robert Peter LAW ,  Matthew LINDON ,  Alexander PRESTON ,  Jonathan Thomas SEAL ,  Christopher Roland WELLAWAY

IPC: A61K31/506

CPC classification number: A61K31/506 ,  A61K31/4375 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/5386 ,  C07D215/227 ,  C07D215/44 ,  C07D215/46 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08 ,  C07D498/04 ,  C07D498/08

Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.

公开(公告)号：US09688695B2

公开(公告)日：2017-06-27

申请号：US14396771

申请日：2013-04-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  Universite De Montreal

Inventor： Jacques Banville ,  Roger Rémillard ,  Edward H. Ruediger ,  Daniel H. Deon ,  Marc Gagnon ,  Laurence Dubé ,  Julia Guy ,  Eldon Scott Priestley ,  Shoshana L. Posy ,  Brad D. Maxwell ,  Pancras C. Wong ,  R. Michael Lawrence ,  Michael M. Miller

IPC: C07D513/04 ,  C07D487/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/553

CPC classification number: C07D513/04 ,  A61K31/433 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  A61K51/0453 ,  C07B59/002 ,  C07B2200/05 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.