公开(公告)号：US11760735B2

公开(公告)日：2023-09-19

申请号：US17711205

申请日：2022-04-01

Applicant: Novartis AG

Inventor： Gary Glick ,  Shomir Ghosh ,  William R. Roush

IPC: C07D263/46 ,  A61K31/41 ,  C07D333/34 ,  C07D405/12 ,  C07D417/12 ,  C07D295/096 ,  C07D213/34 ,  C07D307/64 ,  C07D311/54 ,  C07D213/71 ,  C07D277/36 ,  C07C317/22

CPC classification number: C07D263/46 ,  A61K31/41 ,  C07C317/22 ,  C07D213/34 ,  C07D213/71 ,  C07D277/36 ,  C07D295/096 ,  C07D307/64 ,  C07D311/54 ,  C07D333/34 ,  C07D405/12 ,  C07D417/12 ,  C07C2603/10

Abstract: In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured; Formula (I), Formula (II) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein.

公开(公告)号：US20230141913A2

公开(公告)日：2023-05-11

申请号：US17270652

申请日：2019-08-23

Applicant: XENIOPRO GmbH

Inventor： Viktoria REINMÜLLER ,  Roman MARTY ,  Olivier WAGNIÉRES ,  Jean-Baptiste GUALTIEROTTI ,  Verena KÜPPERS

IPC: A61K31/5375 ,  C07C43/275 ,  C07D213/647 ,  A61K31/09 ,  A61K31/44 ,  A61P35/02 ,  A61P35/00 ,  C07D295/096 ,  C07D453/02 ,  A61K31/351 ,  A61K31/451 ,  A61K31/495 ,  A61K31/439 ,  C07D305/06 ,  C07D331/04 ,  C07D205/04 ,  A61K31/337 ,  A61K31/38 ,  A61K31/397 ,  C07D407/12 ,  C07D411/12 ,  C07D405/12 ,  C07D409/12 ,  C07D401/12 ,  A61K31/5377 ,  A61K31/496 ,  C07D309/04 ,  A61K31/12 ,  A61K31/085 ,  C07C49/255 ,  C07C43/295 ,  C07C205/04 ,  C07C251/20 ,  C07C251/48 ,  A61K31/04 ,  A61K31/15 ,  A61K39/39

CPC classification number: A61K31/5375 ,  C07C43/275 ,  C07D213/647 ,  A61K31/09 ,  A61K31/44 ,  A61P35/02 ,  A61P35/00 ,  C07D295/096 ,  C07D453/02 ,  A61K31/351 ,  A61K31/451 ,  A61K31/495 ,  A61K31/439 ,  C07D305/06 ,  C07D331/04 ,  C07D205/04 ,  A61K31/337 ,  A61K31/38 ,  A61K31/397 ,  C07D407/12 ,  C07D411/12 ,  C07D405/12 ,  C07D409/12 ,  C07D401/12 ,  A61K31/5377 ,  A61K31/496 ,  C07D309/04 ,  A61K31/12 ,  A61K31/085 ,  C07C49/255 ,  C07C43/295 ,  C07C205/04 ,  C07C251/20 ,  C07C251/48 ,  A61K31/04 ,  A61K31/15 ,  A61K39/39

Abstract: The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

公开(公告)号：US20190002421A1

公开(公告)日：2019-01-03

申请号：US15854458

申请日：2017-12-26

Applicant: Apicore US LLC

Inventor： Ravishanker Kovi ,  Jayaraman Rao Kannapan ,  Ananda Babu Thirunavakarasu ,  Veerabhadra Rao Bobbili ,  Gaurav Yadav

IPC: C07D295/096

CPC classification number: C07D295/096 ,  A61K31/496 ,  C07B2200/13

Abstract: Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is disclosed. A novel crystalline form of vortioxetine hydrobromide propylene glycol solvate, designated form AC1, is disclosed along with a method for making same. Form AC1 may be characterized by an x-ray powder diffraction pattern with peaks at about 19.64, 22.85, 25.51, 29.57, 30.18±0.2 degrees 2-theta.

公开(公告)号：US20180346486A1

公开(公告)日：2018-12-06

申请号：US16002007

申请日：2018-06-07

Applicant: CADILA HEALTHCARE LIMITED

Inventor： Ranjit C. DESAI ,  Brijeshkumar SRIVASTAVA

IPC: C07D513/04 ,  C07F3/00 ,  A61K31/40 ,  C07D209/44 ,  C07D295/096 ,  C07D491/048 ,  C07D207/06 ,  C07D209/12 ,  C07D498/04 ,  C07D495/04 ,  C07D207/20 ,  C07D207/08 ,  C07D491/04 ,  C07D487/04 ,  C07D471/04 ,  C07D217/04 ,  C07D215/20 ,  C07D215/06 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/472 ,  A61K31/47 ,  A61K31/439 ,  A61K31/437 ,  A61K31/4365 ,  A61K31/4162 ,  A61K31/407 ,  A61K31/404 ,  C07D491/08 ,  A61K31/496 ,  A61K31/4453 ,  A61K31/4375 ,  A61K31/435 ,  C07D209/08

CPC classification number: C07D513/04 ,  A61K31/40 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/435 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/439 ,  A61K31/4453 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/519 ,  C07D207/06 ,  C07D207/08 ,  C07D207/20 ,  C07D209/08 ,  C07D209/12 ,  C07D209/44 ,  C07D215/06 ,  C07D215/20 ,  C07D217/04 ,  C07D295/096 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/08 ,  C07D495/04 ,  C07D498/04 ,  C07F3/00

Abstract: The present invention relates to a compound (3S)-3-(4-((3-(6-Oxa-3-azabicyclo [3.1.1]heptan-3-ylmethyl)benzyl)oxy)phenyl)hex-4-ynoic acid methods for use of this and other compounds.

公开(公告)号：US10071092B2

公开(公告)日：2018-09-11

申请号：US15304929

申请日：2015-04-21

Applicant: ALEMBIC PHARMACEUTICALS LIMITED

Inventor： Venkat Raman Jayaraman ,  Sanjiv Tomer ,  Piyush Rana ,  Kamlesh Kanzariya ,  Sunit Kumar ,  Nilav Patel ,  Manoj Borsaniya ,  Sudhir Shah ,  Anand Thirunavakarasu

IPC: A61K31/495 ,  C07D241/04

CPC classification number: A61K31/495 ,  C07D241/04 ,  C07D295/096

Abstract: The present invention provides polymorphic forms of Vortioxetine of and its pharmaceutically acceptable salts. Specifically the present invention relates to the novel crystalline forms of Vortioxetine or its pharmaceutically acceptable salts. Moreover, the present invention also provides an amorphous form of Vortioxetine hydrobromide and a stable amorphous co-precipitate of Vortioxetine hydrobromide with pharmaceutically acceptable excipients.

公开(公告)号：US20180230159A1

公开(公告)日：2018-08-16

申请号：US15891585

申请日：2018-02-08

Applicant: Celtaxsys, Inc.

Inventor： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC: C07D487/08 ,  C07D263/32 ,  C07C271/20 ,  C07D211/58 ,  C07C229/38 ,  C07C229/08 ,  C07D295/096 ,  C07C255/57 ,  C07D211/34 ,  C07D207/04 ,  C07D401/12 ,  C07D243/08 ,  C07D295/16 ,  C07D295/04 ,  C07D451/04 ,  C07D277/68 ,  C07D401/10 ,  C07C217/58 ,  C07D207/09 ,  C07D405/12 ,  C07D403/12 ,  C07D409/12 ,  C07D211/26 ,  C07D413/12 ,  C07D451/02 ,  C07D277/22 ,  C07C233/78 ,  C07D263/14 ,  C07D207/16

CPC classification number: C07D487/08 ,  C07B2200/07 ,  C07C217/58 ,  C07C229/08 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07C2601/14 ,  C07D207/04 ,  C07D207/09 ,  C07D207/16 ,  C07D211/26 ,  C07D211/34 ,  C07D211/58 ,  C07D243/08 ,  C07D263/14 ,  C07D263/32 ,  C07D277/22 ,  C07D277/68 ,  C07D295/04 ,  C07D295/096 ,  C07D295/16 ,  C07D401/10 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D451/02 ,  C07D451/04

Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

公开(公告)号：US09969723B2

公开(公告)日：2018-05-15

申请号：US14872745

申请日：2015-10-01

Applicant: HYUNDAI PHARM CO., LTD

Inventor： Jin Yang ,  Jin Woong Kim ,  Han Kyu Lee ,  Jae Hyun Kim ,  Chang Mo Son ,  kyu hwan Lee ,  Hyung-Ho Choi ,  daehoon Kim ,  Tae-Young Ha ,  Jaekeol Rhee

IPC: A61K31/497 ,  C07D413/04 ,  C07D213/85 ,  C07D215/06 ,  C07D217/04 ,  C07D221/20 ,  C07D317/72 ,  C07D239/42 ,  C07D271/07 ,  C07D277/82 ,  C07D209/44 ,  C07D211/14 ,  C07D295/073 ,  C07D295/096 ,  C07C51/367 ,  C07C51/373 ,  C07C59/72 ,  C07C59/90 ,  C07D207/06 ,  C07D211/70 ,  C07D213/74 ,  C07D215/04 ,  C07D217/24 ,  C07D239/28 ,  C07D295/155

CPC classification number: C07D413/04 ,  C07C51/367 ,  C07C51/373 ,  C07C59/72 ,  C07C59/90 ,  C07D207/06 ,  C07D209/44 ,  C07D211/14 ,  C07D211/70 ,  C07D213/74 ,  C07D213/85 ,  C07D215/04 ,  C07D215/06 ,  C07D217/04 ,  C07D217/24 ,  C07D221/20 ,  C07D239/28 ,  C07D239/42 ,  C07D271/07 ,  C07D277/82 ,  C07D295/073 ,  C07D295/096 ,  C07D295/155 ,  C07D317/72

Abstract: The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.

公开(公告)号：US09969684B2

公开(公告)日：2018-05-15

申请号：US15640342

申请日：2017-06-30

Applicant: Cardioxyl Pharmaceuticals, Inc. ,  The Johns Hopkins University

Inventor： John P. Toscano ,  Frederick Arthur Brookfield ,  Andrew D. Cohen ,  Stephen Martin Courtney ,  Lisa Marie Frost ,  Vincent Jacob Kalish

IPC: C07C311/48 ,  C07C317/00 ,  C07C323/00 ,  C07D213/00 ,  A61K31/00 ,  C07D213/74 ,  C07D261/10 ,  C07D263/58 ,  C07D285/125 ,  C07D295/096 ,  C07D307/82 ,  C07D333/62 ,  C07C317/14 ,  C07C323/67 ,  C07D309/12 ,  C07D317/14 ,  C07D231/18 ,  C07D333/34

CPC classification number: C07C311/48 ,  C07C317/14 ,  C07C323/67 ,  C07D213/74 ,  C07D231/18 ,  C07D261/10 ,  C07D263/58 ,  C07D285/125 ,  C07D295/096 ,  C07D307/82 ,  C07D309/12 ,  C07D317/14 ,  C07D333/34 ,  C07D333/62

Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.

公开(公告)号：US20180127389A1

公开(公告)日：2018-05-10

申请号：US15624417

申请日：2017-06-15

Applicant: H. Lundbeck A/S

Inventor： Thomas Ruhland ,  Garrick Paul Smith ,  Benny Bang-Andersen ,  Ask Puschl ,  Ejner Knud Moltzen ,  Kim Andersen

IPC: C07D295/145 ,  C07D295/033 ,  C07D211/20 ,  C07D243/08 ,  C07D211/70 ,  C07D295/096

CPC classification number: C07D295/145 ,  C07D211/20 ,  C07D211/70 ,  C07D243/08 ,  C07D295/033 ,  C07D295/096

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.

公开(公告)号：US09944666B2

公开(公告)日：2018-04-17

申请号：US15368454

申请日：2016-12-02

Applicant: BIOGEN MA INC.

Inventor： Kevin M. Guckian ,  Gnanasambandam Kumaravel ,  Bin Ma ,  Sha Mi ,  Hairuo Peng ,  Zhaohui Shao ,  Lihong Sun ,  Arthur G. Taveras ,  Zhili Xin ,  Lei Zhang

IPC: C07D401/04 ,  C07D215/38 ,  C07D217/12 ,  A61K31/47 ,  C07F7/08 ,  A61K45/06 ,  C07C229/50 ,  A61K31/196 ,  C07D215/12 ,  A61K31/4545 ,  A61K31/506 ,  C07D295/096 ,  A61K31/495 ,  C07D213/74 ,  A61K31/496 ,  A61K31/551 ,  C07D239/42 ,  C07D241/20 ,  A61K31/497 ,  C07D211/14 ,  A61K31/451 ,  C07D205/04 ,  A61K31/397 ,  C07D401/06 ,  A61K31/4709 ,  C07D491/107 ,  C07D209/52 ,  A61K31/403 ,  C07D451/02 ,  A61K31/439 ,  A61K31/695 ,  C07C233/60 ,  C07D451/14

CPC classification number: C07F7/081 ,  A61K31/195 ,  A61K31/196 ,  A61K31/397 ,  A61K31/403 ,  A61K31/41 ,  A61K31/439 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/695 ,  A61K45/06 ,  C07C211/38 ,  C07C217/58 ,  C07C229/46 ,  C07C229/50 ,  C07C233/60 ,  C07C233/61 ,  C07C235/66 ,  C07C2102/10 ,  C07C2102/42 ,  C07C2102/44 ,  C07C2102/50 ,  C07C2103/62 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/42 ,  C07C2602/44 ,  C07C2602/46 ,  C07C2602/50 ,  C07C2603/62 ,  C07C2603/74 ,  C07D205/04 ,  C07D209/52 ,  C07D211/14 ,  C07D213/74 ,  C07D215/12 ,  C07D215/20 ,  C07D215/38 ,  C07D217/22 ,  C07D239/42 ,  C07D241/20 ,  C07D295/096 ,  C07D401/04 ,  C07D401/06 ,  C07D451/02 ,  C07D451/14 ,  C07D471/08 ,  C07D491/107 ,  C07F7/0805 ,  A61K2300/00

Abstract: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).