公开(公告)号：US20240360081A1

公开(公告)日：2024-10-31

申请号：US18571860

申请日：2022-06-24

申请人： Jazz Pharmaceuticals Ireland Limited

发明人： Davide MARINELLI ,  Prafulkumar Chovatia ,  Claudia BEATO ,  Gilles OUVRY

IPC分类号： C07D213/64 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4704 ,  A61K31/506 ,  A61K31/513 ,  C07D213/84 ,  C07D215/227 ,  C07D231/12 ,  C07D239/36 ,  C07D249/18 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D471/04

CPC分类号： C07D213/64 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4704 ,  A61K31/506 ,  A61K31/513 ,  C07D213/84 ,  C07D215/227 ,  C07D231/12 ,  C07D239/36 ,  C07D249/18 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D471/04

摘要： Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, A, L1, L2, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.

公开(公告)号：US20240336562A1

公开(公告)日：2024-10-10

申请号：US18264949

申请日：2022-02-10

申请人： Hangzhou Innogate Pharma Co., Ltd.

发明人： Hancheng ZHANG ,  Wei JIA ,  Congcong CAI

IPC分类号： C07C317/26 ,  A61K31/64 ,  C07D205/06 ,  C07D211/96 ,  C07D213/64 ,  C07D231/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

CPC分类号： C07C317/26 ,  A61K31/64 ,  C07D205/06 ,  C07D211/96 ,  C07D213/64 ,  C07D231/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12

摘要： The present invention provides a compound serving as an NLRP3 inhibitor. Specifically, the present invention provides a compound having a structure shown in the following formula (I), or an optical isomer, pharmaceutically acceptable salt, prodrug, deuterated derivative, hydrate, and solvate thereof. The compound can be used for treating or preventing diseases or disorders associated with the activity or expression level of NLRP3.

公开(公告)号：US20240316020A1

公开(公告)日：2024-09-26

申请号：US18665797

申请日：2024-05-16

申请人： ICAGEN, LLC ,  HOFFMANN-LA ROCHE INC.

发明人： Mark CHAPMAN ,  Nicholas Gareth Morse DAVIES ,  Aaron GERLACH ,  Sylvain LEBRETON ,  Ingrid MECHIN ,  David MOWREY ,  Karthigeyan NAGARAJAN ,  Anil NAIR ,  Roger David NORCROSS ,  Roger Lluis REDONDO PENA ,  Alena SAFAROVA ,  Martin SMRCINA

IPC分类号： A61K31/4439 ,  A61K9/20 ,  A61K31/443 ,  A61K31/4433 ,  C07D213/38 ,  C07D213/64 ,  C07D405/12 ,  C07D405/14

CPC分类号： A61K31/4439 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/443 ,  A61K31/4433 ,  C07D213/38 ,  C07D213/64 ,  C07D405/12 ,  C07D405/14

摘要： The invention provides new heterocyclic compounds having the general formula (I), or a solvate or a pharmaceutically acceptable salt thereof:




wherein R1, R2, R3, R4, R5, R6 and n are as defined herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：US20240285772A1

公开(公告)日：2024-08-29

申请号：US18106242

申请日：2023-02-06

申请人： University of Rhode Island Board of Trustees ,  Colgate University

发明人： Fang Wang ,  Jacob M. Goldberg ,  Bradley M. Lipka ,  Daniel S. Honeycutt

IPC分类号： A61K47/54 ,  C07D213/61 ,  C07D213/64 ,  C07D213/68 ,  C07D213/71 ,  C07D213/76 ,  C07D235/24 ,  C07D235/28 ,  C07D237/12 ,  C07D239/30 ,  C07D277/62

CPC分类号： A61K47/545 ,  C07D213/61 ,  C07D213/64 ,  C07D213/68 ,  C07D213/71 ,  C07D213/76 ,  C07D235/24 ,  C07D235/28 ,  C07D237/12 ,  C07D239/30 ,  C07D277/62

摘要： Disclosed are pnictogen-containing heterocyclic compounds of Formula (I)




Each of R1, the heterocyclic ring H, A+, LG, and X− is defined herein. Also provided are methods of modifying a substrate using such a compound, conjugated biomolecules thus modified, and pharmaceutical compositions containing one of the conjugated biomolecules.

公开(公告)号：US20240277723A1

公开(公告)日：2024-08-22

申请号：US18606903

申请日：2024-03-15

申请人： Epizyme, Inc.

发明人： Kevin W. KUNTZ ,  Richard CHESWORTH ,  Kenneth W. DUNCAN ,  Heike KEILHACK ,  Natalie WARHOLIC ,  Christine KLAUS ,  Sarah K. KNUTSON ,  Timothy J.N. WIGLE ,  Masashi SEKI ,  Suji SHIROTORI ,  Satoshi KAWANO

IPC分类号： A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

CPC分类号： A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

摘要： The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：US12030879B2

公开(公告)日：2024-07-09

申请号：US16977445

申请日：2019-03-01

申请人： Inflazome Limited

发明人： Matthew Cooper ,  David Miller ,  Jimmy Van Wiltenburg ,  Johannes Wilhem Georg Meissner ,  Jochem Theodoor Van Herpt ,  Zhou Min Lion ,  Jonathan Shannon ,  Stephen St-Gallay

IPC分类号： C07D471/04 ,  A61K9/00 ,  C07D213/64 ,  C07D213/643 ,  C07D213/71 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07F5/02

CPC分类号： C07D471/04 ,  A61K9/0014 ,  C07D213/64 ,  C07D213/643 ,  C07D213/71 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07F5/027

摘要： The present invention relates to compounds of formula (I) wherein Q is selected from O or S; R1 is a saturated or unsaturated, optionally substituted hydrocarbyl group optionally including one or more heteroatoms N, O or S; R2 is a cyclic group substituted at the a and a′ positions, wherein the substituent at the α-position is a monovalent heterocyclic group or a monovalent aromatic group, wherein the heterocyclic or aromatic group may optionally be substituted, and wherein the cyclic group may optionally be further substituted; R3 and R4 are each independently hydrogen, halogen, —OH, —NH2, —CN, —R5, —OR5, —NHR5 or —N(R5)2; or R3 and R4 together with the carbon atom to which they are attached may form a 3- to 7-membered saturated or unsaturated, optionally substituted cyclic group; and R5 is independently optionally substituted C1-C4 alkyl. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

公开(公告)号：US20240190822A1

公开(公告)日：2024-06-13

申请号：US18507616

申请日：2023-11-13

申请人： Ikena Oncology, Inc.

发明人： Alfredo C. CASTRO ,  Michael J. Burke ,  Thomas A. Wynn ,  Sabine K. Ruppel ,  Sergio L. Santillana Soto ,  Eric Haines ,  Lan Xu ,  Oksana Zavidij

IPC分类号： C07D213/64 ,  A61P35/00

CPC分类号： C07D213/64 ,  A61P35/00

摘要： The present disclosure provides MEK inhibitors, compositions thereof, and methods of using the same.

公开(公告)号：US20240173307A1

公开(公告)日：2024-05-30

申请号：US18330171

申请日：2023-06-06

申请人： Calico Life Sciences LLC ,  AbbVie Inc.

发明人： Kathleen Ann Martin ,  Carmela Sidrauski ,  Marina Pliushchev ,  Jennifer M. Frost ,  Yunsong Tong ,  Xiangdong Xu ,  Lei Shi ,  Qingwei Zhang ,  Zhaoming Xiong ,  Ramzi Farah Sweis ,  Michael J. Dart ,  Kathleen J. Murauski

IPC分类号： A61K31/44 ,  A61K31/165 ,  A61K31/18 ,  A61K31/341 ,  A61K31/35 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K45/06 ,  A61P25/28 ,  C07C237/24 ,  C07C311/46 ,  C07C323/40 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/75 ,  C07D213/85 ,  C07D231/12 ,  C07D233/64 ,  C07D235/14 ,  C07D237/14 ,  C07D239/34 ,  C07D239/47 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D405/12 ,  C07D471/04 ,  C07D471/08 ,  C07D493/08

CPC分类号： A61K31/44 ,  A61K31/165 ,  A61K31/18 ,  A61K31/341 ,  A61K31/35 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/443 ,  A61K31/444 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K45/06 ,  A61P25/28 ,  C07C237/24 ,  C07C311/46 ,  C07C323/40 ,  C07D213/40 ,  C07D213/64 ,  C07D213/71 ,  C07D213/75 ,  C07D213/85 ,  C07D231/12 ,  C07D233/64 ,  C07D235/14 ,  C07D237/14 ,  C07D239/34 ,  C07D239/47 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/28 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D405/12 ,  C07D471/04 ,  C07D471/08 ,  C07D493/08

摘要： Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

公开(公告)号：US20240165121A1

公开(公告)日：2024-05-23

申请号：US18188700

申请日：2023-03-23

申请人： Epizyme, Inc.

发明人： Kevin Wayne KUNTZ ,  John Emmerson Campbell ,  Masashi Seki ,  Syuji Shirotori ,  Wataru Itano ,  Wanjun Zheng

IPC分类号： A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  A61K31/5375 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14

CPC分类号： A61K31/5377 ,  A61K31/4412 ,  A61K31/4545 ,  A61K31/5375 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14

摘要： The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：US11884680B2

公开(公告)日：2024-01-30

申请号：US17139963

申请日：2020-12-31

申请人： CELGENE QUANTICEL RESEARCH, INC.

发明人： Amogh Boloor

IPC分类号： C07D498/04 ,  C07D217/24 ,  C07D413/04 ,  C07D401/04 ,  C07D471/04 ,  C07D405/04 ,  C07D487/04 ,  C07D211/94 ,  C07D401/14 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D237/14 ,  C07D239/54 ,  C07D239/56 ,  C07D241/20 ,  C07D403/04 ,  C07D405/12 ,  C07D409/04 ,  C07D413/06 ,  C07D417/14 ,  C07D491/048 ,  C07D495/04 ,  C07D213/69 ,  C07D213/70 ,  C07D401/12 ,  C07D405/06

CPC分类号： C07D498/04 ,  C07D211/94 ,  C07D213/64 ,  C07D213/69 ,  C07D213/70 ,  C07D213/73 ,  C07D213/74 ,  C07D217/24 ,  C07D237/14 ,  C07D239/54 ,  C07D239/56 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/06 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04

摘要： The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.