公开(公告)号：US20240316059A1

公开(公告)日：2024-09-26

申请号：US18570814

申请日：2022-06-20

申请人： Oncopeptides AB

发明人： Antonio BERMEJO GOMEZ ,  Praveen KUMAR CHINTHAKINDI ,  Charles DEMMER ,  Katarina FARNEGARDH ,  Mathias FARNEGARDH ,  Fredrik LEHMANN ,  Ellen SANTANGELO

IPC分类号： A61K31/5377 ,  A61K31/4184 ,  A61K31/437 ,  A61K45/06 ,  A61P35/00 ,  C07D235/16 ,  C07D471/04

CPC分类号： A61K31/5377 ,  A61K31/4184 ,  A61K31/437 ,  A61K45/06 ,  A61P35/00 ,  C07D235/16 ,  C07D471/04

摘要： The invention provides compounds of formula (I), that are peptidase enhanced cytotoxics. The invention further provides pharmaceutical compositions comprising the compounds, and the use of the compounds or pharmaceutical compositions as a medicament, particularly for use in the treatment or prophylaxis of cancers such as multiple myeloma, osteosarcoma, breast cancer, lung cancer, ovarian cancer, leukaemia and lymphoma.

公开(公告)号：US11851428B2

公开(公告)日：2023-12-26

申请号：US17328814

申请日：2021-05-24

申请人： ONO PHARMACEUTICAL CO., LTD. ,  VANDERBILT UNIVERSITY

发明人： Craig W. Lindsley ,  Joshua M. Wieting ,  Kevin M. Mcgowan ,  Jerod S. Denton ,  Kentaro Yashiro ,  Haruto Kurata ,  Yoko Sekioka ,  Takahiro Mori ,  Yuzo Iwaki

IPC分类号： C07D213/36 ,  C07D231/12 ,  C07D249/08 ,  C07D401/04 ,  A61K31/454 ,  C07D471/04 ,  C07C255/57 ,  C07C317/28 ,  C07D209/30 ,  C07D213/89 ,  C07D231/56 ,  C07D235/16 ,  C07D237/24 ,  C07D239/47 ,  C07D249/18 ,  C07D257/04 ,  C07D265/36 ,  C07D271/10 ,  C07D285/14 ,  C07D295/04 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07C255/57 ,  C07C317/28 ,  C07D209/30 ,  C07D213/89 ,  C07D231/56 ,  C07D235/16 ,  C07D237/24 ,  C07D239/47 ,  C07D249/08 ,  C07D249/18 ,  C07D257/04 ,  C07D265/36 ,  C07D271/10 ,  C07D285/14 ,  C07D295/04 ,  C07D401/04 ,  C07D513/04

摘要： Disclosed is a compound of formula (I):






wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.

公开(公告)号：US20180118711A1

公开(公告)日：2018-05-03

申请号：US15694342

申请日：2017-09-01

申请人： Omeros Corporation

发明人： Neil S. Cutshall ,  Jennifer Lynn Gage ,  Thomas Neil Wheeler

IPC分类号： C07D401/04 ,  C07C251/80 ,  C07D295/135 ,  C07C243/32 ,  C07D333/60 ,  C07D319/18 ,  C07D317/62 ,  C07D295/155 ,  C07D275/02 ,  C07D265/36 ,  C07D257/06 ,  C07D249/08 ,  C07D249/04 ,  C07D235/16 ,  C07D231/12 ,  C07D215/14 ,  C07D213/74 ,  C07D213/56 ,  C07C255/66 ,  C07C251/88 ,  C07C251/86 ,  A61K31/54 ,  A61K31/5375 ,  A61K31/47 ,  A61K31/425 ,  A61K31/4196 ,  A61K31/4184 ,  A61K31/415 ,  A61K31/41 ,  A61K31/40 ,  A61K31/36 ,  A61K31/357 ,  A61K31/15

CPC分类号： C07D401/04 ,  A61K31/15 ,  A61K31/357 ,  A61K31/36 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/425 ,  A61K31/47 ,  A61K31/5375 ,  A61K31/54 ,  C07C243/32 ,  C07C251/80 ,  C07C251/86 ,  C07C251/88 ,  C07C255/66 ,  C07C2601/08 ,  C07D213/56 ,  C07D213/74 ,  C07D215/14 ,  C07D231/12 ,  C07D235/16 ,  C07D249/04 ,  C07D249/08 ,  C07D257/06 ,  C07D265/36 ,  C07D275/02 ,  C07D295/135 ,  C07D295/155 ,  C07D317/62 ,  C07D319/18 ,  C07D333/60

摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

公开(公告)号：US09790188B2

公开(公告)日：2017-10-17

申请号：US14776184

申请日：2014-03-17

申请人： Whitehead Institute for Biomedical Research ,  Massachusetts Institute of Technology

发明人： Susan L. Lindquist ,  Stephen L. Buchwald ,  Daniel Tardiff ,  Nathan Jui

IPC分类号： C07D235/04 ,  A61K31/4184 ,  C07D235/16 ,  A61K45/06 ,  A61K31/4439 ,  C07D235/08 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/12

CPC分类号： C07D235/16 ,  A61K31/4184 ,  A61K31/4439 ,  A61K45/06 ,  C07D235/08 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/12 ,  A61K2300/00

摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and pharmaceutical compositions thereof. The present invention also provides methods and kits using the inventive compounds and pharmaceutical compositions for treating and/or preventing diseases associated with protein aggregation, such as amyloidoses (e.g., Parkinson's disease and Alzheimer's disease), treating and/or preventing neurodegenerative diseases, treating and/or preventing diseases associated with Tar DNA binding protein 43 kDa, reducing or preventing protein aggregation, and/or modulating E3 ubiquitin ligase in a subject in need thereof.

公开(公告)号：US20170029367A1

公开(公告)日：2017-02-02

申请号：US15294420

申请日：2016-10-14

申请人： Cephalon, Inc. ,  University of Hawaii ,  University of Utah Research Foundation

发明人： Bruce D. Dorsey ,  Scott K. Kuwada ,  Jay P. Theroff ,  Craig A. Zificsak

IPC分类号： C07C317/32 ,  C07C317/44 ,  C07D295/185 ,  C07D213/40 ,  C07D333/20 ,  C07D217/06 ,  C07D231/12 ,  C07D271/10 ,  C07D235/06 ,  C07D263/57 ,  C07D263/32 ,  C07C317/14 ,  C07D309/08 ,  C07D213/71 ,  C07D309/14 ,  C07D223/12

CPC分类号： C07C317/32 ,  C07C317/14 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07D213/40 ,  C07D213/57 ,  C07D213/70 ,  C07D213/71 ,  C07D215/36 ,  C07D217/06 ,  C07D223/10 ,  C07D223/12 ,  C07D231/12 ,  C07D235/06 ,  C07D235/16 ,  C07D263/32 ,  C07D263/56 ,  C07D263/57 ,  C07D271/07 ,  C07D271/10 ,  C07D295/18 ,  C07D295/185 ,  C07D295/192 ,  C07D309/08 ,  C07D309/14 ,  C07D333/20 ,  C07D333/24

摘要： Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.

摘要翻译： 其中D，n，Ra，Rb和Rc如本文所定义，以及使用式II化合物治疗或降低患者腹膜癌病变风险的药物组合物和方法。

公开(公告)号：US20160333009A1

公开(公告)日：2016-11-17

申请号：US15153527

申请日：2016-05-12

申请人： Gilead Sciences, Inc.

发明人： Mark J. Bartlett ,  Julian Andrew Codelli ,  Britton Kenneth Corkey ,  Jennifer Leigh Cosman ,  Kristyna Elbel ,  Jennifer Alissa Loyer-Drew ,  David Sperandio ,  Joshua Van Veldhuizen ,  Hai Yang ,  Suet Chung Yeung

IPC分类号： C07D471/04 ,  C07D235/08 ,  A61K31/4184 ,  A61K31/5377 ,  C07D401/12 ,  A61K31/454 ,  A61K31/437 ,  A61K31/506 ,  A61K31/497 ,  A61K31/55 ,  A61K31/541 ,  A61K31/439 ,  C07D405/12 ,  C07D405/14 ,  C07D471/08 ,  A61K31/553 ,  C07D235/30 ,  C07D235/14 ,  C07D401/04 ,  C07D235/12 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/538 ,  A61K31/5386 ,  A61K31/438 ,  C07D403/12 ,  A61K31/4439 ,  C07D235/24 ,  C07D413/12 ,  A61K31/496 ,  C07D487/04 ,  A61K31/4725 ,  C07D235/28 ,  A61K45/06

CPC分类号： C07D471/04 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/553 ,  A61K45/06 ,  C07D235/06 ,  C07D235/08 ,  C07D235/12 ,  C07D235/14 ,  C07D235/16 ,  C07D235/24 ,  C07D235/28 ,  C07D235/30 ,  C07D295/125 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D471/08 ,  C07D487/04

摘要： The present disclosure provides indoleamine 2,3-dioxygenase 1 (IDOL) inhibitors of Formula I: or pharmaceutically acceptable salts thereof, in which X, L, n, m, R1, R2a, R2b, Rn, Rm, and Rt are as defined herein, as well as pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using the same to treat conditions mediated by IDO1.

摘要翻译： 或其药学上可接受的盐，其中X，L，n，m，R1，R2a，R2b，Rn，Rm和Rt如本文所定义，以及包含式I化合物或其药学上可接受的盐的药物组合物 以及使用其来治疗由IDO1介导的病症的方法。

公开(公告)号：US09475805B2

公开(公告)日：2016-10-25

申请号：US14721680

申请日：2015-05-26

申请人： Kyowa Hakko Kirin Co., Ltd.

发明人： Arata Yanagisawa ,  Keiji Uehara ,  Masahiro Matsubara ,  Kimihisa Ueno ,  Michihiko Suzuki ,  Takeshi Kuboyama ,  Keisuke Yamamoto ,  Tomohiro Tamura

IPC分类号： C07D471/04 ,  C07D403/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D235/16 ,  A61K31/335 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/4353 ,  A61K31/4409 ,  C07C255/34 ,  C07C255/44 ,  C07D235/08 ,  C07D257/04 ,  C07D413/04 ,  C07D413/10

CPC分类号： C07D471/04 ,  A61K31/335 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/4353 ,  A61K31/4409 ,  C07C255/34 ,  C07C255/44 ,  C07D235/08 ,  C07D235/16 ,  C07D257/04 ,  C07D403/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14

摘要： The invention provides a method of activating PPAR γ and a method of treating or preventing a disease associated with PPAR γ by administering a tricyclic compound having a PPAR γ agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:

公开(公告)号：US09381196B2

公开(公告)日：2016-07-05

申请号：US14663180

申请日：2015-03-19

申请人： THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE

发明人： Tong Wang ,  Stephen Gately

IPC分类号： A01N37/28 ,  A61K31/19 ,  A61K31/506 ,  C07D235/16 ,  C07D403/04 ,  A61K31/4184 ,  A61K31/437 ,  A61K45/06

CPC分类号： A61K31/506 ,  A61K31/4184 ,  A61K31/437 ,  A61K45/06 ,  C07D235/16 ,  C07D403/04

摘要： The invention encompasses a compound derived from hydroxamic acid that may be used to slow the expansion of cancer cells and thus is effective in the treatment of cancer. Generally, the disclosed compound includes a benzimidazole group coupled to a hydroxyamide of five or more unsubstituted carbon atoms and any pharmaceutically acceptable salts, solvates and chemically protected forms thereof. Also disclosed are pharmacological compositions including the compound and methods of using the compound to slow the expansion of cancer cells as well as methods of using the compound to treat cancer.

公开(公告)号：US09376395B2

公开(公告)日：2016-06-28

申请号：US14345562

申请日：2012-09-14

申请人： Yu Chen ,  Lan Yang ,  Feiyu Feng ,  Qiufu Ge ,  Dianwu Guo ,  Yi Chen

发明人： Yu Chen ,  Lan Yang ,  Feiyu Feng ,  Qiufu Ge ,  Dianwu Guo ,  Yi Chen

IPC分类号： C07D235/16 ,  A61K47/40 ,  A61K31/16 ,  A61K31/4184 ,  A61K9/00 ,  A61K9/19 ,  A61K47/48

CPC分类号： C07D235/16 ,  A61K9/0019 ,  A61K9/19 ,  A61K31/16 ,  A61K31/4184 ,  A61K47/40 ,  A61K47/6951 ,  Y02A50/414

摘要： The present invention is directed to pharmaceutical compositions comprising: (a) a cyclopolysaccharide and (b) a compound of Formula (I) or its pharmaceutical acceptable salt: wherein X1, X2, Q, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compositions.

摘要翻译： 本发明涉及药物组合物，其包含：（a）环多糖和（b）式（I）化合物或其药学上可接受的盐：其中X 1，X 2，Q，Z和m如本文所定义。 还公开了用这些组合物治疗肿瘤疾病或免疫疾病的方法。

公开(公告)号：US20160159748A1

公开(公告)日：2016-06-09

申请号：US15045523

申请日：2016-02-17

申请人： Cephalon, Inc.

发明人： Martin Ian Cooper ,  Laurent D. Courvoisier ,  Mark Eddleston ,  Robert E. McKean

IPC分类号： C07D235/16 ,  A61K47/26 ,  A61K9/00 ,  A61K31/4184

CPC分类号： A61K31/4184 ,  A61K9/0019 ,  A61K9/14 ,  A61K9/19 ,  A61K47/26 ,  C07D235/16

摘要： Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.