公开(公告)号：US20240279184A1

公开(公告)日：2024-08-22

申请号：US18565844

申请日：2022-06-03

申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  UNIVERSITÉ DE STRASBOURG ,  UNIVERSITE DE HAUTE ALSACE

发明人： Elisabeth DAVIOUD-CHARVET ,  Maxime DONZEL ,  Matthieu ROIGNANT ,  Mourad ELHABIRI

IPC分类号： C07D239/30 ,  C07C41/30 ,  C07C43/275 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/84 ,  C07D215/14 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D239/42 ,  C07D277/62 ,  C07D307/42 ,  C07D307/46 ,  C07D333/22 ,  C07D405/12

CPC分类号： C07D239/30 ,  C07C41/30 ,  C07C43/275 ,  C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D213/84 ,  C07D215/14 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D239/42 ,  C07D277/62 ,  C07D307/42 ,  C07D307/46 ,  C07D333/22 ,  C07D405/12

摘要： A compound having the formula (I):




wherein:



R1 is selected from the group consisting of: H, F, (C1-C6)alkoxy, and halo(C1-C6)alkyl; and
R2 is an optionally substituted heteroaryl group, as well as processes for the preparation of the compound, and intermediate compounds.

公开(公告)号：US20240270701A1

公开(公告)日：2024-08-15

申请号：US18694362

申请日：2022-09-22

申请人： Curasen Therapeutics, Inc.

发明人： Jiaxin Yu ,  Anthony P. Ford ,  Wei Chen

IPC分类号： C07D241/42 ,  A61K31/4045 ,  A61K31/416 ,  A61K31/417 ,  A61K31/426 ,  A61K31/437 ,  A61K31/44 ,  A61K31/47 ,  A61K31/498 ,  A61K31/517 ,  C07D209/34 ,  C07D213/38 ,  C07D213/61 ,  C07D213/73 ,  C07D215/14 ,  C07D215/233 ,  C07D231/56 ,  C07D235/08 ,  C07D235/26 ,  C07D237/20 ,  C07D239/42 ,  C07D239/74 ,  C07D277/40 ,  C07D277/68 ,  C07D471/04

CPC分类号： C07D241/42 ,  A61K31/4045 ,  A61K31/416 ,  A61K31/417 ,  A61K31/426 ,  A61K31/437 ,  A61K31/44 ,  A61K31/47 ,  A61K31/498 ,  A61K31/517 ,  C07D209/34 ,  C07D213/38 ,  C07D213/61 ,  C07D213/73 ,  C07D215/14 ,  C07D215/233 ,  C07D231/56 ,  C07D235/08 ,  C07D235/26 ,  C07D237/20 ,  C07D239/42 ,  C07D239/74 ,  C07D277/40 ,  C07D277/68 ,  C07D471/04

摘要： The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor. An advantage of the compounds provided herein is that a broad range of pharmacological activities is possible, consistent with modulation of beta-adrenergic receptors. In addition, the disclosure provides methods of using the compounds described herein for the treatment of diseases associated with an adrenergic receptor, including but not limited to neurodegenerative diseases and disorders.

公开(公告)号：US20240124410A1

公开(公告)日：2024-04-18

申请号：US18266525

申请日：2022-03-24

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education ,  THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Peter C. Lucas ,  Linda M. McAllister ,  Heejae Kang ,  Beibei Chen ,  Lisa Maurer ,  Dong Hu ,  Jing Cheng ,  Linda Klei ,  Zaneta Nikolovska-Coleska

IPC分类号： C07D317/58 ,  A61P35/00 ,  C07C317/26 ,  C07D209/14 ,  C07D209/38 ,  C07D215/14 ,  C07D235/14 ,  C07D241/42 ,  C07D249/18 ,  C07D263/56 ,  C07D277/64 ,  C07D333/58 ,  C07D471/04

CPC分类号： C07D317/58 ,  A61P35/00 ,  C07C317/26 ,  C07D209/14 ,  C07D209/38 ,  C07D215/14 ,  C07D235/14 ,  C07D241/42 ,  C07D249/18 ,  C07D263/56 ,  C07D277/64 ,  C07D333/58 ,  C07D471/04

摘要： Small molecule inhibitors that block the interaction between B-cell lymphoma 10 protein (BCL10) and mucosa- associated lymphoid tissue lymphoma translocation protein 1 (MALT1), thereby inhibiting both the protease and scaffolding activities of MALT1, and MALT1- dependent downstream signaling, including IL-6 and IL-10 secretion by B-cell lymphoma cells and IL-2 transcription and secretion by Jurkat T cells.

公开(公告)号：US20230322680A1

公开(公告)日：2023-10-12

申请号：US18336332

申请日：2023-06-16

申请人： NISSAN CHEMICAL CORPORATION

发明人： Paul Adriaan VAN DER SCHAAF ,  Fritz BLATTER ,  Martin SZELAGIEWICZ ,  Kai-Uwe SCHOENING

IPC分类号： C07D215/14

CPC分类号： C07D215/14 ,  C07B2200/13

摘要： The present invention is directed to new crystalline forms of Pitavastatin hemicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous forms.

公开(公告)号：US20230255963A1

公开(公告)日：2023-08-17

申请号：US18137210

申请日：2023-04-20

申请人： Global Blood Therapeutics, Inc. ,  The Regents of the University of California

发明人： Brian Metcalf ,  Chihyuan Chuang ,  Jeffrey Warrington ,  Matthew P. Jacobson

IPC分类号： A61K31/4985 ,  C07D213/80 ,  C07D231/56 ,  C07D401/04 ,  C07D257/04 ,  C07D211/62 ,  C07D213/30 ,  C07C69/76 ,  C07C65/30 ,  C07D215/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/192 ,  A61K31/235 ,  A61K31/41 ,  A61K31/416 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/47

CPC分类号： A61K31/4985 ,  C07D213/80 ,  C07D231/56 ,  C07D401/04 ,  C07D257/04 ,  C07D211/62 ,  C07D213/30 ,  C07C69/76 ,  C07C65/30 ,  C07D215/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/192 ,  A61K31/235 ,  A61K31/41 ,  A61K31/416 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/47

摘要： Provided are substituted benzaldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.

公开(公告)号：US11718631B2

公开(公告)日：2023-08-08

申请号：US16756358

申请日：2018-10-12

申请人： Novartis AG

发明人： Shankar Venkatraman ,  Shomir Ghosh ,  William R. Roush ,  Dong-Ming Shen ,  Jason Katz ,  Hans Martin Seidel

IPC分类号： C07D498/04 ,  C07C311/51 ,  C07D231/12 ,  C07D317/46 ,  C07D209/04 ,  C07D215/14 ,  C07D307/54 ,  C07D471/04 ,  C07D487/04 ,  C07D409/12 ,  C07D277/30

CPC分类号： C07D498/04 ,  C07C311/51 ,  C07D209/04 ,  C07D215/14 ,  C07D231/12 ,  C07D277/30 ,  C07D307/54 ,  C07D317/46 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04

摘要： In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: wherein the variables shown in Formula AA can be as defined anywhere herein. Compounds AA are modulators of NLRP1 and/or NLRP3

公开(公告)号：US11701373B2

公开(公告)日：2023-07-18

申请号：US17307138

申请日：2021-05-04

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Alaric J. Dyckman ,  T. G. Murali Dhar ,  Hai-Yun Xiao ,  John L. Gilmore ,  Michael G. Yang ,  Zili Xiao ,  David Marcoux

IPC分类号： A61K31/695 ,  C07F7/08 ,  A61K31/135 ,  C07D215/14 ,  C07D241/04 ,  C07C323/29 ,  C07C251/38 ,  C07C251/42 ,  C07C251/44 ,  C07D209/46 ,  C07D213/38 ,  C07C275/26 ,  C07C217/74 ,  C07C323/25 ,  C07C235/46 ,  C07F9/54 ,  C07F9/572 ,  C07F9/09 ,  C07C215/42 ,  C07C217/52 ,  C07C217/58 ,  C07C219/24 ,  C07C233/41 ,  C07C233/65 ,  C07C251/50 ,  C07C251/52 ,  C07C251/54 ,  C07C271/34 ,  C07C317/28 ,  C07C317/32 ,  C07C321/16 ,  C07C321/22 ,  C07C321/28 ,  C07D213/32 ,  C07D213/69 ,  C07D213/70 ,  C07D215/12 ,  C07D217/24 ,  C07D231/12 ,  C07D231/20 ,  C07D239/26 ,  C07D241/12 ,  C07D277/24 ,  C07D305/08 ,  C07D309/06 ,  C07D309/12 ,  C07D311/58 ,  C07D311/76 ,  C07D319/20 ,  C07D333/16 ,  C07F9/117 ,  C07F9/62 ,  C07F9/6503 ,  C07F9/6509 ,  C07F9/655 ,  C07F9/6553 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K31/166 ,  A61K31/17 ,  A61K31/222 ,  A61K31/24 ,  A61K31/27 ,  A61K31/337 ,  A61K31/351 ,  A61K31/352 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/661

CPC分类号： A61K31/695 ,  A61K31/135 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K31/166 ,  A61K31/17 ,  A61K31/222 ,  A61K31/24 ,  A61K31/27 ,  A61K31/337 ,  A61K31/351 ,  A61K31/352 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/661 ,  C07C215/42 ,  C07C217/52 ,  C07C217/58 ,  C07C217/74 ,  C07C219/24 ,  C07C233/41 ,  C07C233/65 ,  C07C235/46 ,  C07C251/38 ,  C07C251/42 ,  C07C251/44 ,  C07C251/50 ,  C07C251/52 ,  C07C251/54 ,  C07C271/34 ,  C07C275/26 ,  C07C317/28 ,  C07C317/32 ,  C07C321/16 ,  C07C321/22 ,  C07C321/28 ,  C07C323/25 ,  C07C323/29 ,  C07D209/46 ,  C07D213/32 ,  C07D213/38 ,  C07D213/69 ,  C07D213/70 ,  C07D215/12 ,  C07D215/14 ,  C07D217/24 ,  C07D231/12 ,  C07D231/20 ,  C07D239/26 ,  C07D241/04 ,  C07D241/12 ,  C07D277/24 ,  C07D305/08 ,  C07D309/06 ,  C07D309/12 ,  C07D311/58 ,  C07D311/76 ,  C07D319/20 ,  C07D333/16 ,  C07F7/08 ,  C07F7/081 ,  C07F9/091 ,  C07F9/117 ,  C07F9/5442 ,  C07F9/5728 ,  C07F9/62 ,  C07F9/65031 ,  C07F9/65522 ,  C07F9/650952 ,  C07F9/655345 ,  C07B2200/05 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2602/10 ,  C07C2603/74

摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):




and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

公开(公告)号：US20220401384A1

公开(公告)日：2022-12-22

申请号：US17826770

申请日：2022-05-27

申请人： McMaster University

发明人： Eric Brown ,  Omar M Elhalfawy ,  Nick Jentsch ,  Xiong Zhang ,  Jakob Magolan

IPC分类号： A61K31/055 ,  C07C39/19 ,  C07D213/30 ,  C07D261/08 ,  C07C205/18 ,  C07D333/38 ,  C07D307/48 ,  C07D239/42 ,  C07D239/26 ,  C07D215/14 ,  C07C49/78 ,  C07C43/275 ,  A61K38/12 ,  A61K31/05 ,  A61K31/4418 ,  A61K31/42 ,  A61K31/381 ,  A61K31/341 ,  A61K31/505 ,  A61K31/11 ,  A61K31/47 ,  A61K31/121 ,  A61P31/04

摘要： Provided herein are novel synthetic compounds having the structure of formula (1), wherein X is a substituted or unsubstituted aromatic or heteroaromatic mono- or polycyclic ring system; and Y is substituted or unsubstituted C5-C10 alkyl or alkenyl group, or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions. The compounds and pharmaceutical compositions are useful for inhibiting growth of a bacterium.

公开(公告)号：US11512069B2

公开(公告)日：2022-11-29

申请号：US16948432

申请日：2020-09-18

申请人： Merck Patent GmbH

发明人： Brian A. Sherer ,  Xiaoling Chen ,  Esther Cleary ,  Nadia Brugger

IPC分类号： A61K31/4523 ,  C07D401/14 ,  C07D215/18 ,  C07D413/04 ,  C07D401/12 ,  A61K31/4709 ,  A61P35/00 ,  C07D215/12 ,  C07D215/14 ,  C07D241/42 ,  C07D401/04 ,  C07D413/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04

摘要： A method of administering to a patient in need thereof or contacting with a biological sample, a compound related to Formula I-e or pharmaceutically acceptable compositions thereof, is useful to inhibit activity of TLR7/8 or a mutant thereof and/or to treat a TLR7/8-mediated disorder.

公开(公告)号：US11266640B2

公开(公告)日：2022-03-08

申请号：US16649455

申请日：2018-09-20

申请人： Hangzhou Innogate Pharma Co., Ltd.

发明人： Hancheng Zhang ,  Xiangyang Ye

IPC分类号： A61K31/4709 ,  A61K31/47 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5383 ,  A61K39/395 ,  C07D215/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D417/12 ,  C07D498/04

摘要： Compounds as IDO inhibitors and/or dual inhibitors of IDO-HDAC are described. Specifically, the compounds represented by the following formula (I) are described, wherein each group is defined as described in the specification. The compounds have IDO inhibitory activity or IDO-HDAC dual inhibitory activity and can be used for preventing or treating diseases associated with IDO and/or IDO-HDAC activity or expression levels. At the same time, the compounds of the present invention can be combined with an anti-tumor antibody such as PD-1 and PD-L1, and such a combination can greatly increase the anti-tumor response rate of the antibody and broaden the types of tumors to be treated.