公开(公告)号：US20240228468A1

公开(公告)日：2024-07-11

申请号：US18553412

申请日：2022-04-05

Applicant: Vanderbilt University

Inventor： Aaron M. Bender ,  Matthew Spock ,  Trever R. Carter ,  Melissa A. Korkmaz-Vaisys ,  Logan A. Baker ,  P. Jeffrey Conn ,  Craig W. Lindsley

IPC: C07D403/12 ,  A61K31/351 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/5377 ,  C07D237/12 ,  C07D237/24 ,  C07D309/06 ,  C07D309/08 ,  C07D401/14 ,  C07D405/14 ,  C07D495/04

CPC classification number: C07D403/12 ,  A61K31/351 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/5377 ,  C07D237/12 ,  C07D237/24 ,  C07D309/06 ,  C07D309/08 ,  C07D401/14 ,  C07D405/14 ,  C07D495/04

Abstract: The present invention relates to (6-((octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)benzamide (R2b is —C(O)N(RA1)(RA2) and N-(6-((octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl) phenyl) carboxamide (R2b is —N(RB)C(O)RC) derivatives of formula (I) wherein (II) R2b is —C(O)N(RA1)(RA2) or —N(RB)C(O)RC as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4) for the treatment of neurodegenerative disorders, movement disorders or brain disorders, such as e.g. Parkinson's disease, drug-induced Parkinsonism, dystonia, Tourette's syndrome, dyskinesias, schizophrenia, cognitive deficits associated with schizophrenia, excessive daytime sleepiness, attention deficit hyperactivity disorder (ADHD), Huntington's disease, chorea, cerebral palsy, and progressive supranuclear palsy. An exemplary compound is e.g. N-(4-(6-(((3aR,5s,6aS)-2-(2-fluorobenzyl)octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl) phenyl)acetamide (A1) (III).

公开(公告)号：US20240124385A1

公开(公告)日：2024-04-18

申请号：US18516407

申请日：2023-11-21

Applicant: CORSAIR PHARMA, INC.

Inventor： Xiaoming ZHANG ,  Meenakshi S. VENKATRAMAN ,  Cyrus K. BECKER

IPC: C07C69/734 ,  A61K9/70 ,  C07C53/136 ,  C07C59/11 ,  C07C59/13 ,  C07C69/28 ,  C07C69/675 ,  C07C69/68 ,  C07C69/708 ,  C07C69/712 ,  C07C69/74 ,  C07C69/75 ,  C07C69/96 ,  C07D305/08 ,  C07D307/24 ,  C07D307/30 ,  C07D309/08

CPC classification number: C07C69/734 ,  A61K9/7023 ,  C07C53/136 ,  C07C59/11 ,  C07C59/13 ,  C07C69/28 ,  C07C69/675 ,  C07C69/68 ,  C07C69/708 ,  C07C69/712 ,  C07C69/74 ,  C07C69/75 ,  C07C69/96 ,  C07D305/08 ,  C07D307/24 ,  C07D307/30 ,  C07D309/08 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/14

Abstract: The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.

公开(公告)号：US20230399297A1

公开(公告)日：2023-12-14

申请号：US18031893

申请日：2021-10-14

Applicant: Jacobio Pharmaceuticals Co., Ltd.

Inventor： Runze LI ,  Cunbo MA ,  Zhenchang LIAN ,  Jing XIONG ,  Yanping WANG ,  Wei LONG

IPC: C07D209/20 ,  C07C245/18 ,  C07D305/08 ,  C07D307/16 ,  C07D211/66 ,  C07D309/06 ,  C07D307/93 ,  C07D309/08 ,  C07D207/09 ,  C07D493/04 ,  C07D277/30 ,  C07D207/337 ,  C07D263/32 ,  C07D233/64 ,  C07D333/24 ,  C07D213/74 ,  C07D239/20 ,  C07D213/30 ,  C07D313/04 ,  C07D265/30 ,  C07D331/04 ,  A61P35/00

CPC classification number: C07D209/20 ,  C07C245/18 ,  C07D305/08 ,  C07D307/16 ,  C07D211/66 ,  C07D309/06 ,  C07D307/93 ,  C07D309/08 ,  C07D207/09 ,  C07D493/04 ,  C07D277/30 ,  C07D207/337 ,  C07D263/32 ,  C07D233/64 ,  C07D333/24 ,  C07D213/74 ,  C07D239/20 ,  C07D213/30 ,  C07D313/04 ,  C07D265/30 ,  C07D331/04 ,  A61P35/00 ,  C07C2601/18 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/04 ,  C07C2601/02 ,  C07C2601/08

Abstract: The invention relates to novel glutamine analogs, a composition containing the glutamine analogs and the use thereof.

公开(公告)号：US20230338373A1

公开(公告)日：2023-10-26

申请号：US18166789

申请日：2023-02-09

Applicant: InventisBio LLC

Inventor： Xing DAI ,  Yaolin WANG

IPC: A61K31/505 ,  A61K31/196 ,  A61K31/351 ,  A61K31/382 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4184 ,  C07C275/42 ,  C07D233/88 ,  C07D239/42 ,  C07D257/04 ,  C07D261/14 ,  C07D309/08 ,  C07D309/14 ,  C07D335/02 ,  C07D413/12

CPC classification number: A61K31/505 ,  A61K31/196 ,  A61K31/351 ,  A61K31/382 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4184 ,  C07C275/42 ,  C07D233/88 ,  C07D239/42 ,  C07D257/04 ,  C07D261/14 ,  C07D309/08 ,  C07D309/14 ,  C07D335/02 ,  C07D413/12

Abstract: The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating a disease associated with IDO, for example, cancer or an infectious disease (e.g., viral or bacterial infectious diseases). Also, provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.

公开(公告)号：US20180251426A1

公开(公告)日：2018-09-06

申请号：US15783993

申请日：2017-10-13

Applicant: AbbVie, Inc.

Inventor： Milan Bruncko ,  Yujia Dai ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Robert A. Mantei ,  Chang H. Park ,  Cheol-Min Park ,  Andrew M. Petros ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  William J. McClellan

IPC: C07D209/08 ,  A61K31/635 ,  C07D211/58 ,  C07D401/12 ,  C07D309/08 ,  C07D471/04 ,  C07D413/12 ,  C07D405/14 ,  C07D405/12 ,  C07D403/12 ,  C07D401/14 ,  C07D309/04 ,  C07D295/30 ,  C07D277/24 ,  C07D235/06 ,  C07D231/56 ,  C07D213/84 ,  C07D213/74 ,  C07D417/12

CPC classification number: C07D209/08 ,  A61K31/635 ,  C07D211/58 ,  C07D213/74 ,  C07D213/84 ,  C07D231/56 ,  C07D235/06 ,  C07D277/24 ,  C07D295/30 ,  C07D309/04 ,  C07D309/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20180244606A1

公开(公告)日：2018-08-30

申请号：US15758709

申请日：2016-09-16

Applicant: Metacrine, Inc.

Inventor： Nicholas D. SMITH ,  Steven P. GOVEK ,  Johnny Y. NAGASAWA

IPC: C07C233/54 ,  A61K45/06 ,  A61K31/216 ,  C07C271/28 ,  A61K31/27 ,  C07C255/57 ,  A61K31/277 ,  C07D309/08 ,  A61K31/351 ,  A61K31/337 ,  C07D305/08 ,  C07D335/02 ,  A61K31/382 ,  C07D205/04 ,  A61K31/397 ,  C07D265/30 ,  A61K31/5375 ,  C07C323/50 ,  C07C317/44 ,  C07D211/94 ,  A61K31/45 ,  C07C235/04 ,  C07C235/40 ,  C07D211/06 ,  A61K31/4453 ,  C07C235/82 ,  C07D231/12 ,  A61K31/415 ,  C07D213/40 ,  A61K31/4406 ,  C07D261/08 ,  A61K31/42 ,  C07D295/135 ,  A61K31/402 ,  C07D231/56 ,  A61K31/416 ,  A61K31/404 ,  C07D209/04 ,  C07D317/58 ,  A61K31/36 ,  C07D295/26 ,  C07D295/195 ,  C07D277/28 ,  A61K31/426 ,  A61K31/4184 ,  C07D235/08 ,  C07D249/18 ,  A61K31/4192 ,  C07D239/42 ,  A61K31/505 ,  C07D241/20 ,  A61K31/4965 ,  C07D237/20 ,  A61K31/50 ,  A61P1/16

CPC classification number: C07C233/54 ,  A61K31/16 ,  A61K31/216 ,  A61K31/27 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/36 ,  A61K31/382 ,  A61K31/397 ,  A61K31/402 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/426 ,  A61K31/4406 ,  A61K31/4453 ,  A61K31/45 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5375 ,  A61K45/06 ,  A61P1/16 ,  C07C233/63 ,  C07C233/65 ,  C07C233/81 ,  C07C233/87 ,  C07C235/04 ,  C07C235/16 ,  C07C235/40 ,  C07C235/56 ,  C07C235/64 ,  C07C235/82 ,  C07C237/24 ,  C07C255/57 ,  C07C255/60 ,  C07C271/24 ,  C07C271/28 ,  C07C311/07 ,  C07C311/08 ,  C07C317/32 ,  C07C317/44 ,  C07C323/50 ,  C07C323/61 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/16 ,  C07C2602/42 ,  C07C2603/74 ,  C07D205/04 ,  C07D209/04 ,  C07D211/06 ,  C07D211/62 ,  C07D211/76 ,  C07D211/94 ,  C07D211/96 ,  C07D213/40 ,  C07D231/12 ,  C07D231/56 ,  C07D235/04 ,  C07D235/08 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D249/18 ,  C07D261/08 ,  C07D265/30 ,  C07D277/28 ,  C07D295/088 ,  C07D295/135 ,  C07D295/195 ,  C07D295/26 ,  C07D305/08 ,  C07D309/08 ,  C07D317/58 ,  C07D319/12 ,  C07D335/02 ,  A61K2300/00

Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

公开(公告)号：US20180230084A1

公开(公告)日：2018-08-16

申请号：US15892302

申请日：2018-02-08

Applicant: Southern Research Institute

Inventor： Ashish Kumar Pathak ,  Syed Kaleem Ahmed ,  Corinne E. Augelli-Szafran ,  Joseph A. Maddry

IPC: C07C233/75 ,  C07D231/14 ,  C07D233/90 ,  C07D277/56 ,  C07D261/18 ,  C07D307/68 ,  C07D333/38 ,  C07D241/24 ,  C07D271/12 ,  C07D239/28 ,  C07C255/41 ,  C07D213/56 ,  C07D213/81 ,  C07D307/85 ,  C07D309/08 ,  C07D213/30 ,  C07D209/46 ,  C07D223/16 ,  A61P31/12

CPC classification number: C07C233/75 ,  A61P31/12 ,  C07C233/29 ,  C07C233/60 ,  C07C233/65 ,  C07C235/48 ,  C07C255/33 ,  C07C255/41 ,  C07C255/58 ,  C07C311/21 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2602/12 ,  C07C2603/74 ,  C07D209/46 ,  C07D213/30 ,  C07D213/56 ,  C07D213/81 ,  C07D223/16 ,  C07D231/14 ,  C07D233/90 ,  C07D239/28 ,  C07D241/24 ,  C07D261/18 ,  C07D271/12 ,  C07D277/56 ,  C07D307/68 ,  C07D307/85 ,  C07D309/08 ,  C07D333/38

Abstract: The present disclosure is concerned with benzo annulene compounds that are capable of inhibiting a viral infection and methods of treating viral infections such as, for example, chikungunya, Venezuelan equine encephalitis, dengue, influenza, and zika, using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：US20180194718A1

公开(公告)日：2018-07-12

申请号：US15806722

申请日：2017-11-08

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Erik Fenster ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07C243/38 ,  C07D493/10 ,  C07D491/107 ,  A61K31/192 ,  C07D405/06 ,  C07D401/04 ,  C07D309/08 ,  C07D307/68 ,  C07D295/32 ,  C07D265/30 ,  C07D261/04 ,  C07D261/02 ,  C07D239/36 ,  C07D233/06 ,  C07D213/87 ,  C07D213/86 ,  C07D213/75 ,  C07D213/65 ,  C07D213/61 ,  C07D213/56 ,  C07D211/62 ,  C07D211/60 ,  C07D211/48 ,  C07D211/46 ,  C07D211/42 ,  C07D211/38 ,  C07D211/22 ,  C07D207/16 ,  C07D207/14 ,  C07D207/12 ,  C07D207/09 ,  C07D207/08 ,  C07D205/04 ,  C07C259/04 ,  C07C243/32 ,  C07C243/24 ,  C07C235/80 ,  C07C235/78 ,  C07C235/74 ,  C07C235/34 ,  C07C235/20 ,  C07C235/12 ,  C07C233/56 ,  A61K45/06 ,  A61K31/5375 ,  A61K31/495 ,  A61K31/4409 ,  A61K31/4406 ,  A61K31/44 ,  A61K31/42 ,  A61K31/4015 ,  A61K31/40 ,  A61K31/397 ,  A61K31/341 ,  A61K31/197

CPC classification number: C07C243/38 ,  A61K31/192 ,  A61K31/197 ,  A61K31/341 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/495 ,  A61K31/5375 ,  A61K45/06 ,  C07C233/56 ,  C07C235/12 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C235/80 ,  C07C243/24 ,  C07C243/32 ,  C07C259/04 ,  C07C2601/08 ,  C07C2601/16 ,  C07D205/04 ,  C07D207/08 ,  C07D207/09 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/22 ,  C07D211/38 ,  C07D211/42 ,  C07D211/46 ,  C07D211/48 ,  C07D211/60 ,  C07D211/62 ,  C07D213/56 ,  C07D213/61 ,  C07D213/65 ,  C07D213/75 ,  C07D213/86 ,  C07D213/87 ,  C07D233/06 ,  C07D239/36 ,  C07D261/02 ,  C07D261/04 ,  C07D265/30 ,  C07D295/32 ,  C07D307/68 ,  C07D309/08 ,  C07D401/04 ,  C07D405/06 ,  C07D491/107 ,  C07D493/10

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US09879000B2

公开(公告)日：2018-01-30

申请号：US14685732

申请日：2015-04-14

Applicant: GRÜNENTHAL GMBH

Inventor： Stefan Schunk ,  Melanie Reich ,  Florian Jakob ,  Nils Damann ,  Michael Haurand ,  Achim Kless ,  Marc Rogers ,  Kathy MacKenzie

IPC: C07D405/04 ,  C07D309/02 ,  C07D413/04 ,  C07D309/08 ,  C07D405/12

CPC classification number: C07D413/04 ,  C07D309/08 ,  C07D405/04 ,  C07D405/12

Abstract: The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

公开(公告)号：US09708253B2

公开(公告)日：2017-07-18

申请号：US15109733

申请日：2015-01-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jingwu Duan ,  T. G. Murali Dhar ,  Bin Jiang ,  Ananta Karmakar ,  Arun Kumar Gupta ,  Zhonghui Lu ,  Carolyn A. Weigelt

IPC: C07C317/20 ,  C07C317/24 ,  C07C317/30 ,  C07D205/04 ,  C07D207/27 ,  C07D211/46 ,  C07D211/78 ,  C07D213/30 ,  C07D231/12 ,  C07D213/81 ,  C07D213/82 ,  C07D309/08 ,  C07D231/14 ,  C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D237/08 ,  C07D237/20 ,  C07D237/24 ,  C07D405/04 ,  C07D239/28 ,  C07C317/46 ,  C07D241/24 ,  C07D249/04 ,  C07D471/04 ,  C07D207/277 ,  C07D277/60 ,  C07D295/096 ,  C07D211/48 ,  C07D211/62 ,  C07D295/185 ,  C07D213/56 ,  C07D213/71 ,  C07D213/75 ,  C07D309/04 ,  C07D335/02 ,  C07D401/06 ,  C07D401/12 ,  C07D295/205 ,  C07D213/40 ,  C07D231/54 ,  C07D237/22 ,  C07D249/06 ,  C07D277/82 ,  C07D295/16 ,  C07D295/195

CPC classification number: C07C317/20 ,  C07C317/24 ,  C07C317/30 ,  C07C317/46 ,  C07C2601/02 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/27 ,  C07D207/277 ,  C07D211/46 ,  C07D211/48 ,  C07D211/62 ,  C07D211/78 ,  C07D213/30 ,  C07D213/40 ,  C07D213/56 ,  C07D213/71 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D231/12 ,  C07D231/14 ,  C07D231/54 ,  C07D231/56 ,  C07D237/08 ,  C07D237/20 ,  C07D237/22 ,  C07D237/24 ,  C07D239/28 ,  C07D241/24 ,  C07D249/04 ,  C07D249/06 ,  C07D277/60 ,  C07D277/82 ,  C07D295/096 ,  C07D295/16 ,  C07D295/185 ,  C07D295/195 ,  C07D295/205 ,  C07D309/04 ,  C07D309/08 ,  C07D335/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D471/04

Abstract: Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.