公开(公告)号：US20230172903A1

公开(公告)日：2023-06-08

申请号：US17865195

申请日：2022-07-14

申请人： Genzyme Corporation

发明人： Hanlan LIU ,  Chris WILLIS ,  Renu BHARDWAJ ,  Jianmei KOCHLING ,  Judith PETERSCHMITT ,  Craig SIEGEL

IPC分类号： A61K31/4025 ,  C07D405/06 ,  A61K45/06 ,  C07D319/16

CPC分类号： A61K31/4025 ,  C07D405/06 ,  A61K45/06 ,  C07D319/16

摘要： The hemitartrate salt of a compound represented by the following structural formula:




(Formula I Hemitartrate), which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of the Formula (I) Hemitartrate are characterized by a variety of properties and physical measurements. As well, methods of producing crystalline Formula (I) Hemitartrate, and using it to inhibit glucosylceramide synthase or lowering glycosphingolipid concentrations in subjects to treat a number of diseases, are also discussed. Pharmaceutical compositions are also described.

公开(公告)号：US20220388975A1

公开(公告)日：2022-12-08

申请号：US17663153

申请日：2022-05-12

申请人： WEIFANG MEDICAL UNIVERSITY

发明人： Haiyong Jia ,  Chuanju Li ,  Lei Zhang ,  Linyue Liu ,  Mei Wang ,  Xin Li ,  Xianghui Han

IPC分类号： C07D319/16 ,  C07D405/12 ,  C07D413/12

摘要： A sulfonamide benzamide derivative has the structure shown in Formula II that can be prepared as an anti-HBV (hepatitis B virus) pharmaceutical composition; it is prepared by sulfonation reaction, acylation reaction and sulfonylation reaction; the sulfonamide benzamide derivative has been shown effective activity for anti-HBV by inhibiting HBV DNA replication in vitro.

公开(公告)号：US11384048B2

公开(公告)日：2022-07-12

申请号：US16958588

申请日：2018-12-24

申请人： GUANGZHOU MAXINOVEL PHARMACEUTICALS CO., LTD.

发明人： Yuguang Wang ,  Nong Zhang ,  Tianzhi Wu ,  Min He

IPC分类号： C07C229/22 ,  C07D213/38 ,  C07D231/56 ,  C07D235/02 ,  C07D241/12 ,  C07D261/20 ,  C07D263/56 ,  C07D319/16 ,  C07D407/10 ,  C07D471/04 ,  C07D487/04

摘要： Disclosed in the present invention are an aromatic vinyl or aromatic ethyl derivative, a preparation method therefor, an intermediate, a pharmaceutical composition, and an application. The aromatic vinyl or aromatic ethyl derivative in the present invention is as represented by general formula (I). The aromatic vinyl or aromatic ethyl derivative in the present invention has an obvious inhibitory effect on PD-1/PD-L1, is a very effective small-molecule PD-1/PD-L1 inhibitor, and can effectively alleviate or treat relevant diseases such as cancer.

公开(公告)号：US20200223834A1

公开(公告)日：2020-07-16

申请号：US16577592

申请日：2019-09-20

申请人： Samumed, LLC

发明人： Sunil Kumar KC ,  David Mark Wallace ,  John Hood ,  Charlene F. Barroga

IPC分类号： C07D411/06 ,  C07D213/50 ,  C07D317/46 ,  C07D319/16 ,  C07D327/06 ,  C07D339/08 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D263/56 ,  C07D311/58 ,  C07D317/54 ,  C07D319/18 ,  C07D231/56 ,  C07D333/54 ,  C07D235/06 ,  C07D407/06 ,  C07D413/06 ,  C07D307/80 ,  A61P25/00

摘要： The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

公开(公告)号：US20190055227A1

公开(公告)日：2019-02-21

申请号：US15918086

申请日：2018-03-12

申请人： Samumed, LLC

发明人： Sunil Kumar KC ,  David Mark Wallace ,  John Hood ,  Charlene F. Barroga

IPC分类号： C07D411/06 ,  C07D409/06 ,  C07D231/56 ,  C07D339/08 ,  C07D405/06 ,  C07D327/06 ,  C07D213/50 ,  C07D317/46 ,  C07D319/16 ,  C07D413/06 ,  C07D333/54 ,  C07D235/06 ,  C07D263/56 ,  C07D407/06 ,  C07D317/54 ,  C07D311/58 ,  C07D319/18 ,  C07D307/80 ,  C07D401/06

摘要： The present disclosure provides γ-diketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries or spine injuries, brain atrophy/neurological disorders related to the differentiation and development of the central nervous system, including Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; otic disorders like cochlear hair cell loss; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, such as hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

公开(公告)号：US20180289664A1

公开(公告)日：2018-10-11

申请号：US15570969

申请日：2016-05-02

申请人： GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION ,  Emory University

发明人： Binghe Wang ,  Erwin Van Meir ,  Jalisa Nicole Holmes ,  Stefan Kaluz ,  Xingyue Ji

IPC分类号： A61K31/341 ,  A61K45/06 ,  A61K31/351 ,  A61K31/444 ,  A61K31/443 ,  A61K31/09 ,  A61K31/445 ,  A61K31/397 ,  A61K31/40 ,  A61K31/085 ,  A61K31/421 ,  A61K31/5375 ,  A61K31/495 ,  A61K31/352 ,  A61K31/436 ,  A61K31/343 ,  A61K31/538 ,  A61K31/357 ,  A61K31/381 ,  A61P35/00 ,  C07C43/295 ,  C07D307/20 ,  C07D309/10 ,  C07D213/65 ,  C07D405/12 ,  C07D211/46 ,  C07D205/04 ,  C07D207/12 ,  C07D263/32 ,  C07D295/096 ,  C07D307/12 ,  C07D311/70 ,  C07D491/052 ,  C07D307/79 ,  C07D265/36 ,  C07D319/16 ,  C07D333/54

摘要： This disclosure relates to benzhydrol derivatives for managing conditions related to the Hypoxia Inducible Factor (HIF) pathway such as uses in treating cancer. In certain embodiment, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiment, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof.

公开(公告)号：US20180230092A1

公开(公告)日：2018-08-16

申请号：US15933098

申请日：2018-03-22

申请人： DREXEL UNIVERSITY ,  BARUCH S. BLUMBERG INSTITUTE ,  ARBUTUS BIOPHARMA, INC.

发明人： XIAODONG XU ,  JU-TAO GUO ,  TONG XIAO ,  YANMING DU ,  TIMOTHY BLOCK ,  SIMON DAVID PETER BAUGH ,  HONG YE

IPC分类号： C07C311/16 ,  C07D319/16 ,  C07D309/04 ,  C07D305/08 ,  C07D295/32 ,  C07D295/30 ,  C07D295/26 ,  C07D277/52 ,  C07D277/46 ,  C07D263/58 ,  C07D263/50 ,  C07D263/48 ,  C07D261/14 ,  C07D239/26 ,  C07D231/42 ,  C07D231/40 ,  C07D217/24 ,  C07D215/42 ,  C07D215/38 ,  C07D213/76 ,  C07D213/75 ,  C07D213/40 ,  C07D211/96 ,  C07D205/04 ,  C07D203/26 ,  C07C317/14 ,  C07C311/48 ,  C07C311/20 ,  C07C311/19 ,  C07C311/18 ,  C07C311/17 ,  C07C309/89 ,  C07C233/66 ,  C07D319/18

CPC分类号： C07C311/16 ,  C07B2200/07 ,  C07C233/66 ,  C07C309/89 ,  C07C311/17 ,  C07C311/18 ,  C07C311/19 ,  C07C311/20 ,  C07C311/48 ,  C07C317/14 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D203/26 ,  C07D205/04 ,  C07D211/96 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D215/38 ,  C07D215/42 ,  C07D217/24 ,  C07D231/40 ,  C07D231/42 ,  C07D239/26 ,  C07D261/14 ,  C07D263/48 ,  C07D263/50 ,  C07D263/58 ,  C07D277/46 ,  C07D277/52 ,  C07D295/26 ,  C07D295/30 ,  C07D295/32 ,  C07D305/08 ,  C07D309/04 ,  C07D319/16 ,  C07D319/18

摘要： The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly inhibitors for the treatment of viruses, especially but not exclusively, including pregenomic RNA encapsidation inhibitors of HBV for the treatment of Hepatitis B virus (HBV) infection and related conditions. including hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein A, R1, R2, R3, R4, R5, R6, R7, and R8 are defined herein.

公开(公告)号：US20160280643A1

公开(公告)日：2016-09-29

申请号：US15032613

申请日：2014-10-28

申请人： BIOMARIN PHARMACEUTICAL INC.

发明人： Bing Wang

IPC分类号： C07D207/16 ,  C07D405/14 ,  C07D401/12 ,  C07D417/14 ,  C07D409/04 ,  C07D409/12 ,  C07D401/04 ,  C07D471/04 ,  C07D409/14 ,  C07D405/12 ,  C07D319/16

CPC分类号： C07D207/16 ,  C07D319/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

摘要： Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and compounds I for use to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).

公开(公告)号：US09303010B2

公开(公告)日：2016-04-05

申请号：US14547858

申请日：2014-11-19

申请人： Samumed, LLC

发明人： Sunil Kumar KC ,  David Mark Wallace ,  John Hood ,  Charlene F. Barroga

IPC分类号： C07D409/06 ,  A61K31/357 ,  A61K31/381 ,  C07D319/16 ,  C07C49/784 ,  C07D213/50 ,  C07D319/18 ,  C07D405/06 ,  C07D405/10 ,  C07D407/10 ,  C07D409/10 ,  A61K9/00

CPC分类号： A61K31/4436 ,  A61K9/0014 ,  A61K31/12 ,  A61K31/357 ,  A61K31/381 ,  A61K31/4402 ,  A61K31/4433 ,  C07C49/784 ,  C07D213/50 ,  C07D319/16 ,  C07D319/18 ,  C07D405/06 ,  C07D405/10 ,  C07D407/10 ,  C07D409/06 ,  C07D409/10

摘要： The present application discloses a compound which is which activates Wnt/β-catenin signaling and thus treats or prevents diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

摘要翻译： 本申请公开了一种化合物，其活化Wnt / bgr-catenin信号传导，从而治疗或预防与信号转导相关的疾病，例如骨质疏松症和骨关节病; 成骨不全，骨缺损，骨折，牙周病，耳硬化症，伤口愈合，颅面缺损，溶瘤性骨病，与中枢神经系统分化和发育相关的创伤性脑损伤，包括帕金森病，中风，缺血性脑病，癫痫 ，阿尔茨海默病，抑郁症，双相性精神障碍，精神分裂症; 眼睛疾病如年龄相关性黄斑变性，糖尿病性黄斑水肿或视网膜色素变性以及与干细胞分化和生长相关的疾病，包括脱发，造血相关疾病和组织再生相关疾病。

公开(公告)号：US09169224B2

公开(公告)日：2015-10-27

申请号：US13965722

申请日：2013-08-13

申请人： Janssen Pharmaceutica NV

发明人： Richard Apodaca ,  J. Guy Breitenbucher ,  Kanaka Pattabiraman ,  Mark Seierstad ,  Wei Xiao

IPC分类号： A61K31/497 ,  C07D295/195 ,  C07D207/335 ,  C07D209/08 ,  C07D209/14 ,  C07D209/82 ,  C07D211/16 ,  C07D213/38 ,  C07D213/61 ,  C07D213/75 ,  C07D215/12 ,  C07D215/18 ,  C07D239/42 ,  C07D241/42 ,  C07D295/215 ,  C07D307/79 ,  C07D317/46 ,  C07D317/58 ,  C07D319/18 ,  C07D333/58 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D213/56 ,  C07D307/81 ,  C07D319/16 ,  C07D333/60

CPC分类号： C07D295/195 ,  C07D207/335 ,  C07D209/08 ,  C07D209/14 ,  C07D209/82 ,  C07D211/16 ,  C07D213/38 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D215/12 ,  C07D215/18 ,  C07D239/42 ,  C07D241/42 ,  C07D295/20 ,  C07D295/215 ,  C07D307/79 ,  C07D307/81 ,  C07D317/46 ,  C07D317/58 ,  C07D319/16 ,  C07D319/18 ,  C07D333/58 ,  C07D333/60 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

摘要： Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).