公开(公告)号：US20250009693A1

公开(公告)日：2025-01-09

申请号：US18441209

申请日：2024-02-14

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Thuy-Anh TRAN ,  Weichao CHEN ,  Bryan A. KRAMER ,  Abu J.M. SADEQUE ,  Anna SHIFRINA ,  Young-Jun SHIN ,  Pureza VALLAR ,  Ning ZOU

IPC: A61K31/195 ,  A61K31/27 ,  A61K31/325 ,  A61K31/381 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4965 ,  C07C271/12 ,  C07C271/28 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C309/15 ,  C07D213/75 ,  C07D241/20 ,  C07D277/48 ,  C07D333/36

Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease, a congenital heart disease, portal hypertension, HIV infection, ingestion of a drug or toxin, hereditary hemorrhagic telangiectasia, splenectomy, pulmonary veno-occlusive disease (PVOD) or pulmonary capillary hemangiomatosis (PCH); PAH with significant venous or capillary involvement; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis, and chronic obstructive pulmonary disorder (COPD).

公开(公告)号：US11459293B2

公开(公告)日：2022-10-04

申请号：US16758396

申请日：2018-10-26

Applicant: ImmuneBridge Inc.

Inventor： Jesse Cotari ,  Timothy Webb ,  Zhan Wang

IPC: C07C235/56 ,  C07C233/33 ,  C07C225/22 ,  C07C251/44 ,  C07C271/30 ,  C07C275/28 ,  C07D309/08 ,  A61K35/28 ,  A61K31/4709

Abstract: This invention is directed to, inter alia, compounds, methods, systems, and compositions for the maintenance, enhancement, and expansion of hematopoietic stem cells derived from one or more sources of CD34+ cells. Sources of CD34+ cells include bone marrow, cord blood, mobilized peripheral blood, and non-mobilized peripheral blood. Also provided herein are compounds of Formula I which are useful in maintaining, enhancing, and expanding of hematopoietic stem cells.

公开(公告)号：US20210393600A1

公开(公告)日：2021-12-23

申请号：US17047247

申请日：2019-04-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： Liangqin Guo ,  Hongjun Zhang ,  Ping Chen ,  Dane Clausen ,  Xavier Fradera ,  Yongxin Han ,  Shuwen He ,  Xianhai Huang ,  Alexander Pasternak ,  Qinglin Pu ,  Li Xiao ,  Feng Ye

IPC: A61K31/44 ,  A61K45/06 ,  C07C237/22 ,  C07C255/60 ,  C07D213/75 ,  C07C271/36 ,  C07C233/78 ,  C07C271/24 ,  C07C233/79 ,  C07D213/81 ,  C07D271/06 ,  C07D239/28 ,  C07D215/48 ,  C07C275/30 ,  C07C275/28 ,  C07D239/42 ,  C07D305/06 ,  C07D261/08 ,  C07D471/04 ,  C07D261/20 ,  C07D209/34 ,  C07D277/56 ,  C07D217/02 ,  C07D231/14 ,  C07D237/28 ,  C07D241/24 ,  C07D217/26 ,  A61K31/167 ,  A61K31/27 ,  A61K31/4245 ,  A61K31/47 ,  A61K31/17 ,  A61K31/505 ,  A61K31/337 ,  A61K31/437 ,  A61K31/42 ,  A61K31/426 ,  A61K31/472 ,  A61K31/415 ,  A61K31/4965

Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

公开(公告)号：US10858338B2

公开(公告)日：2020-12-08

申请号：US16084465

申请日：2017-03-14

Applicant: The Regents of the University of California

Inventor： Bruce Hammock ,  Sean Kodani

IPC: C07D401/06 ,  C07D271/10 ,  C07D211/16 ,  C07D211/46 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/04 ,  C07C275/28 ,  C07C275/34 ,  A61P35/00 ,  C07C275/36

Abstract: The present invention provides compounds that are dual inhibitors of soluble epoxide hydrolase and fatty acid amide hydrolase. The present invention also provides methods of using the compounds to inhibit soluble epoxide hydrolase and fatty acid amide hydrolase, and to treat cancer.

公开(公告)号：US10125116B2

公开(公告)日：2018-11-13

申请号：US14571673

申请日：2014-12-16

Applicant: Brandeis University ,  University of Georgia Research Foundation, Inc. ,  The Brigham and Women's Hospital, Inc.

Inventor： Lizbeth K. Hedstrom ,  Gregory D. Cuny ,  Deviprasad R. Gollapalli ,  Sivapriya Kirubakaran ,  Sushil K. Maurya ,  Boris Striepen ,  Suresh K. Gorla ,  Corey R. Johnson ,  Mandapati Kavitha ,  Jihan Khan

IPC: C07D401/12 ,  C07C233/15 ,  C07C235/24 ,  C07C235/38 ,  C07C237/20 ,  C07C255/60 ,  C07C275/28 ,  C07C275/30 ,  C07C275/42 ,  C07C309/15 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D215/38 ,  C07D235/26 ,  C07D237/32 ,  C07D263/56 ,  C07D263/57 ,  C07D295/192 ,  C07D401/04 ,  C07D401/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/08 ,  C07D491/052 ,  C07D249/06

Abstract: Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.

公开(公告)号：US20170305840A1

公开(公告)日：2017-10-26

申请号：US15374329

申请日：2016-12-09

Applicant: Paratek Pharmaceuticals, Inc.

Inventor： Mark L. Nelson ,  Kwasi Ohemeng ,  Paul Abato ,  Victor Amoo ,  Haregewein Assefa ,  Joel Berniac ,  Beena Bhatia ,  Todd Bowser ,  Jackson Chen ,  Mark Grier ,  Laura Honeyman ,  Mohamed Y. Ismail ,  Oak K. Kim ,  Jude Mathews ,  Rachid Mechiche

IPC: C07C237/48 ,  C07C275/28 ,  C07C271/54 ,  C07C271/22 ,  C07C275/30 ,  C07C237/26 ,  C07C2603/46 ,  A61K31/65 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/02

CPC classification number: C07C237/48 ,  A61K31/65 ,  C07C237/26 ,  C07C271/22 ,  C07C271/54 ,  C07C275/28 ,  C07C275/30 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2603/46 ,  Y02A50/411 ,  Y02A50/473

Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

公开(公告)号：US09718782B2

公开(公告)日：2017-08-01

申请号：US15023634

申请日：2014-09-17

Applicant: MERCK SHARP & DOHME CORP

Inventor： Andrew J. Cooke ,  Craig A. Stump ,  Xu-Fang Zhang ,  Chun Sing Li ,  Qinghua Mao

IPC: C07D213/75 ,  C07D405/04 ,  C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D513/04 ,  C07D471/04 ,  C07D231/40 ,  C07D239/42 ,  C07D261/14 ,  C07D277/44 ,  C07D311/88 ,  C07D233/88 ,  C07D405/12 ,  C07D249/08 ,  C07C275/28 ,  C07D257/04 ,  C07D263/32 ,  C07D271/10 ,  C07D277/48 ,  C07D285/12 ,  C07D295/135 ,  C07D498/04

CPC classification number: C07D213/75 ,  C07C275/28 ,  C07D231/40 ,  C07D233/88 ,  C07D239/42 ,  C07D249/08 ,  C07D257/04 ,  C07D261/14 ,  C07D263/32 ,  C07D271/10 ,  C07D277/44 ,  C07D277/48 ,  C07D285/12 ,  C07D295/135 ,  C07D311/88 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.

公开(公告)号：US09310364B1

公开(公告)日：2016-04-12

申请号：US14174564

申请日：2014-02-06

Applicant: STC. UNM ,  TORREY PINES INSTITUTE FOR MOLECULAR STUDIES

Inventor： Bruce S. Edwards ,  Larry A. Sklar ,  Clemencia Pinilla ,  Richard A. Houghten ,  Jon R. Appel ,  Marc A. Giulianotti ,  Jose Medina-Franco

IPC: A61K38/00 ,  A61K31/17 ,  C07D241/08 ,  C40B30/02 ,  G01N33/566 ,  C07D403/14 ,  A61K31/496 ,  A61K45/06 ,  C07C275/28 ,  C07K1/04

CPC classification number: G01N33/6845 ,  A61K31/17 ,  A61K31/496 ,  A61K38/00 ,  A61K45/06 ,  B01J2219/00585 ,  C07C275/28 ,  C07D241/08 ,  C07D403/14 ,  C07K1/047 ,  C40B30/02 ,  G01N33/74 ,  G01N2333/726 ,  A61K2300/00

Abstract: The present invention provides novel methods and assays for high-throughput screening of combinatorial libraries to identify FPR1 and/or FPR2 ligands (e.g., agonists and/or antagonists), preferably FPR1 agonists and/or FPR2 antagonists, by positional scanning deconvolution.The invention also provides novel FPR1 and FPR2 ligands (e.g, agonists and antagonists), related pharmaceutical compositions and methods of treating FPR1 and FPR2-related disorders.

Abstract translation: 本发明提供了用于通过位置扫描反卷积来组合文库以鉴定FPR1和/或FPR2配体（例如激动剂和/或拮抗剂），优选FPR1激动剂和/或FPR2拮抗剂的高通量筛选的新方法和测定法。 本发明还提供新的FPR1和FPR2配体（例如激动剂和拮抗剂），相关的药物组合物和治疗FPR1和FPR2相关疾病的方法。

公开(公告)号：US09115164B2

公开(公告)日：2015-08-25

申请号：US14003907

申请日：2012-03-09

Applicant: Masamichi Yamanaka ,  Daisuke Higashi

Inventor： Masamichi Yamanaka ,  Daisuke Higashi

IPC: C07C275/34 ,  C07C275/28 ,  C07C275/04 ,  C07H15/08 ,  C07H15/18 ,  C07H15/203 ,  A23L1/05

CPC classification number: C07H15/203 ,  C07C275/34 ,  C07H15/18 ,  C09K3/00 ,  G01N27/44747

Abstract: According to the present invention, a substituted aromatic compound represented by the following general formula (I) is provided. In general formula (I), A1, A2, and A3 each independently represent an aryl group substituted by a hydrophilic group.

Abstract translation: 根据本发明，提供由以下通式（I）表示的取代的芳族化合物。 在通式（I）中，A1，A2和A3各自独立地表示被亲水基取代的芳基。

公开(公告)号：US08952031B2

公开(公告)日：2015-02-10

申请号：US13412252

申请日：2012-03-05

Applicant: Sean G. Trapp ,  Michael R. Leadbetter ,  Daniel D. Long ,  Lan Jiang ,  Sabine Axt

Inventor： Sean G. Trapp ,  Michael R. Leadbetter ,  Daniel D. Long ,  Lan Jiang ,  Sabine Axt

IPC: A61K31/44 ,  A61K31/275 ,  A61K31/195 ,  A61K31/17 ,  A61K31/18 ,  C07C237/48 ,  C07C233/36 ,  C07C233/37 ,  C07C233/40 ,  C07C233/62 ,  C07C233/78 ,  C07C235/10 ,  C07C255/24 ,  C07C275/14 ,  C07C275/18 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C311/05 ,  C07C311/14 ,  C07C311/16 ,  C07C311/18 ,  C07C311/46 ,  C07C317/44 ,  C07C335/08 ,  C07C335/12 ,  C07C335/16 ,  C07D203/02 ,  C07D203/26

CPC classification number: C07C237/48 ,  C07C233/36 ,  C07C233/37 ,  C07C233/40 ,  C07C233/62 ,  C07C233/78 ,  C07C235/10 ,  C07C255/24 ,  C07C275/14 ,  C07C275/18 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/34 ,  C07C311/05 ,  C07C311/14 ,  C07C311/16 ,  C07C311/18 ,  C07C311/46 ,  C07C317/44 ,  C07C335/08 ,  C07C335/12 ,  C07C335/16 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D203/02 ,  C07D203/26

Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供式（I）的氨基 - 和酰氨基 - 氨基四氢化萘化合物：其中R1，R2，R3，R4，R5，R6，R7和n在本说明书中定义，或其药学上可接受的盐，其为拮抗剂 在μ阿片受体。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗与阿片样物质受体活性相关的病症的方法，以及可用于制备这些化合物的方法和中间体。