公开(公告)号：US20240360154A1

公开(公告)日：2024-10-31

申请号：US18245167

申请日：2021-09-21

申请人： GENFLEET THERAPEUTICS (SHANGHAI) INC. ,  ZHEJIANG GENFLEET THERAPEUTICS CO., LTD.

发明人： Fusheng ZHOU ,  Tao JIANG ,  Yingtao LIU ,  Chonglan LIN ,  Leitao ZHANG ,  Zhubo LIU ,  Kai MA ,  Wan HE ,  Xiaoming XU ,  Lijian FENG ,  Xiaoling LAN ,  Qian DING ,  Qiang LV ,  Jiong LAN

IPC分类号： C07D498/22 ,  A61K31/4985 ,  A61K31/5386 ,  A61P35/00 ,  C07D471/14 ,  C07D471/22 ,  C07D491/22

CPC分类号： C07D498/22 ,  A61K31/4985 ,  A61K31/5386 ,  A61P35/00 ,  C07D471/14 ,  C07D471/22 ,  C07D491/22

摘要： Disclosed are an aroyl substituted tricyclic compound, a preparation method therefor and use thereof. Specifically, the aroyl substituted tricyclic compound of the present invention has a structure of formula (C), and has, as a BTK inhibitor, the advantages of high activity, good selectivity and low toxic and side effects.

公开(公告)号：US20240360126A1

公开(公告)日：2024-10-31

申请号：US18606123

申请日：2024-03-15

申请人： Hoffmann-La Roche Inc.

发明人： Dongdong Chen ,  Fabian Dey ,  Xin Hong ,  Xiaoqing Wang ,  Zhisen Zhang ,  Wei Zhu ,  Ge Zou

IPC分类号： C07D471/04 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00

CPC分类号： C07D471/04 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5386 ,  A61K31/553 ,  C07D519/00

摘要： The present invention relates to compounds of formula (I),






wherein R1 to R3, A, M, W and Q are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.

公开(公告)号：US20240327375A1

公开(公告)日：2024-10-03

申请号：US18560011

申请日：2022-05-13

申请人： Addex Pharma S.A.

发明人： Jean-Laurent Paparin ,  Jean-Philippe Rocher ,  Patrick Mäder ,  Tanja Stach ,  Guillaume Duvey ,  Lam Tang

IPC分类号： C07D401/04 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D237/32 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D491/107 ,  C07D498/08

CPC分类号： C07D401/04 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D237/32 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D491/107 ,  C07D498/08

摘要： The present invention relates to novel compounds of Formula (I), wherein A, m, Q, R1, R2, R3, R4 and R5 are defined as in Formula (I); which are negative allosteric modulators of the metabotropic glutamate receptor subtype 7 (mGlu7) and which are useful for the treatment or prevention of neurological, ear and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGlu7 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and such compositions, and to the use of such compounds for the prevention or treatment of neurological, ear and psychiatric disorders and diseases in which mGlu7 is involved.

公开(公告)号：US20240308976A1

公开(公告)日：2024-09-19

申请号：US18640889

申请日：2024-04-19

申请人： Monte Rosa Therapeutics, Inc.

发明人： Bernhard Fasching ,  Thomas Ryckmans ,  Oliv Eidam ,  Alexander Flohr ,  Laura Ann McAllister ,  Andreas Ritzén

IPC分类号： C07D401/10 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D491/107 ,  C07D498/08

CPC分类号： C07D401/10 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D491/107 ,  C07D498/08

摘要： Described herein, in part, are compounds that bind to and modulate the surface of cereblon and mediate the degradation of GSPT1, and are therefore useful in the treatment of various disorders, such as cancer.

公开(公告)号：US20240294519A1

公开(公告)日：2024-09-05

申请号：US18292856

申请日：2022-07-27

申请人： EPIRIUM BIO INC.

发明人： Sundeep DUGAR ,  Bruce FAHR ,  Roopa RAI ,  Michael J. GREEN

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/553 ,  C07D519/00

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/553 ,  C07D519/00

摘要： Disclosed herein are 15-hydroxyprostaglandin dehydrogenase inhibitor compounds, including variations of pyrrolopy-rimidines. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.

公开(公告)号：US20240239790A1

公开(公告)日：2024-07-18

申请号：US18279379

申请日：2022-03-10

申请人： adMare Therapeutics Society ,  LifeArc ,  Provincial Health Services Authority

发明人： Stephen Paul Arns ,  Tom Han Hsiao Hsieh ,  Fahimeh S. Shidmoossavee ,  Jason Samuel Tan ,  Leanna Yee ,  Jay John Paquette ,  James Brian Jaquith ,  Simon Andrew Osborne ,  Ela Smiljanic-Hurley ,  Callum Hamby ,  Elliott Smyth ,  Martin Ambler ,  Andrew I. Minchinton ,  Alastair H. Kyle ,  Jennifer H.E. Baker

IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  A61K48/00 ,  A61P35/00 ,  C07D519/00 ,  C12N9/22 ,  C12N15/11 ,  C12N15/63

CPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  A61K48/005 ,  A61P35/00 ,  C07D519/00 ,  C12N9/22 ,  C12N15/111 ,  C12N15/63 ,  C12N2310/20

摘要： The present disclosure provides compounds and methods for inhibiting DNA-dependent protein kinase (DNA-PK). Aspects of the present disclosure also include methods of using the compounds to treat diseases, including, but not limited to, cancer. In certain embodiments, the compounds inhibit DNA-PK and thus sensitize cancers to therapies such as chemotherapy and radiotherapy. Certain compounds of the present disclosure are in the form of prodrugs that release the DNA-PK inhibitor in hypoxic tissue such as is known to occur in cancers. Aspects of the present disclosure also include methods of using the compounds for repairing a DNA break in a target genomic region or for modifying expression of one or more genes or proteins. Compounds provided are of formula: (II)

公开(公告)号：US11957689B2

公开(公告)日：2024-04-16

申请号：US17960625

申请日：2022-10-05

申请人： Teon Therapeutics, Inc.

发明人： Elfatih Elzein ,  Jiwen Liu

IPC分类号： A61K31/5377 ,  A61K9/00 ,  A61K9/08 ,  A61K9/20 ,  A61K9/48 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5386 ,  A61K39/395 ,  A61P35/00 ,  C07D471/04 ,  C07D519/00

CPC分类号： A61K31/5377 ,  A61K9/0019 ,  A61K9/08 ,  A61K9/2054 ,  A61K9/4825 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5386 ,  A61K39/3955 ,  A61P35/00 ,  C07D471/04 ,  C07D519/00

摘要： Disclosed herein are compounds, compositions, and methods for modulating the Cannabinoid receptor 2 (CB2) with the compounds and compositions disclosed herein. Also described are methods of treating diseases or conditions that are mediated by the action of Cannabinoid receptor 2 (CB2) or that we benefit from modulating the Cannabinoid receptor 2 (CB2).

公开(公告)号：US20240091216A1

公开(公告)日：2024-03-21

申请号：US18503992

申请日：2023-11-07

申请人： AeroRx Therapeutics LLC

发明人： John CHAN ,  Keith Try UNG ,  Mei-Chang KUO ,  John Nigel Pritchard

IPC分类号： A61K31/4704 ,  A61K9/00 ,  A61K9/08 ,  A61K9/12 ,  A61K31/40 ,  A61K31/5386 ,  A61K31/58 ,  A61K47/10 ,  A61K47/26 ,  A61K47/69 ,  A61P11/00

CPC分类号： A61K31/4704 ,  A61K9/0078 ,  A61K9/08 ,  A61K9/12 ,  A61K31/40 ,  A61K31/5386 ,  A61K31/58 ,  A61K47/10 ,  A61K47/26 ,  A61K47/6951 ,  A61P11/00

摘要： Aqueous formulations of indacaterol are disclosed. The formulations may find use in the treatment of respiratory disorders, inflammatory disorders, or obstructive airway diseases. Methods of using the formulations and kits comprising the formulations are also encompassed by the disclosure.

公开(公告)号：US11903949B2

公开(公告)日：2024-02-20

申请号：US16539894

申请日：2019-08-13

申请人： OSSIFI THERAPEUTICS LLC

发明人： Debra Ellies ,  F. Scott Kimball ,  Robert N. Young

IPC分类号： C07D471/04 ,  C07D498/08 ,  C07D491/048 ,  A61K31/5377 ,  A61K39/395 ,  A61K31/444 ,  A61K31/496 ,  A61K35/32 ,  A61K31/5386 ,  A61P19/10 ,  A61K31/55

CPC分类号： A61K31/5377 ,  A61K31/444 ,  A61K31/496 ,  A61K31/5386 ,  A61K31/55 ,  A61K35/32 ,  A61K39/3955 ,  A61P19/10 ,  C07D471/04 ,  C07D491/048 ,  C07D498/08

摘要： In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease, diabetes, bone loss, and cancer, using a compound of Formula I.

公开(公告)号：US11844793B2

公开(公告)日：2023-12-19

申请号：US17449412

申请日：2021-09-29

申请人： AeroRx Therapeutics LLC

发明人： John Chan ,  Keith Try Ung ,  Mei-Chang Kuo ,  John Nigel Pritchard

IPC分类号： A61K31/4704 ,  A61K31/5386 ,  A61K31/40 ,  A61K9/00 ,  A61K47/69 ,  A61K47/26 ,  A61K31/58 ,  A61K9/08 ,  A61K9/12 ,  A61K47/10 ,  A61P11/00

CPC分类号： A61K31/4704 ,  A61K9/0078 ,  A61K9/08 ,  A61K9/12 ,  A61K31/40 ,  A61K31/5386 ,  A61K31/58 ,  A61K47/10 ,  A61K47/26 ,  A61K47/6951 ,  A61P11/00

摘要： Aqueous formulations of indacaterol are disclosed. The formulations may find use in the treatment of respiratory disorders, inflammatory disorders, or obstructive airway diseases. Methods of using the formulations and kits comprising the formulations are also encompassed by the disclosure.