公开(公告)号：US5324736A

公开(公告)日：1994-06-28

申请号：US107426

申请日：1993-08-16

申请人： Robert A. Magarian ,  Joseph T. Pento ,  Kwasi S. Avor

发明人： Robert A. Magarian ,  Joseph T. Pento ,  Kwasi S. Avor

IPC分类号： A61K31/03 ,  C07C309/66 ,  C07D295/092 ,  A61K31/445 ,  A61K31/495 ,  C07D211/20

CPC分类号： C07D295/088 ,  A61K31/03 ,  C07C309/66 ,  C07C2101/02

摘要： Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes substituents comprising a hydroxy group, a hydrogen atom, an acetate group or a substituted or unsubstituted alkoxy group. The compounds are useful as antiestrogens and anti-tumor agents.

摘要翻译： 二苯基环丙基类似物，其中一个或多个苯环包括含羟基，氢原子，乙酸基或取代或未取代的烷氧基的取代基。 该化合物可用作抗雌激素和抗肿瘤剂。

公开(公告)号：US4623666A

公开(公告)日：1986-11-18

申请号：US668810

申请日：1984-11-06

申请人： Thomas P. Kennedy

发明人： Thomas P. Kennedy

IPC分类号： A61K31/03

CPC分类号： A61K31/03

摘要： Methods are disclosed for employing diphenylhalonium ion to elicit sodium nitroprusside-like effects in vivo, and to enhance cardiac contractility.

摘要翻译： 公开了使用二苯基离子在体内引起硝普钠样效应的方法，并且增强心脏收缩力。

公开(公告)号：US20190022029A1

公开(公告)日：2019-01-24

申请号：US16058437

申请日：2018-08-08

申请人： BioMendics, LLC

发明人： Chun-che Tsai ,  Karen M. McGuire ,  James M. Jamison ,  Jack L. Summers

IPC分类号： A61K31/05 ,  A61K8/67 ,  A61K9/00 ,  A61K8/60 ,  A61K8/33 ,  A61K8/34 ,  A61Q7/00 ,  A61Q19/08 ,  A61K47/40 ,  A61K47/36 ,  A61K9/06 ,  A61K45/06 ,  A61K31/7034 ,  A61K31/09 ,  A61K31/085 ,  A61K8/73 ,  A61K9/08 ,  A61K9/19 ,  A61K8/70 ,  A61K31/03 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655

CPC分类号： A61K31/05 ,  A61K8/33 ,  A61K8/347 ,  A61K8/602 ,  A61K8/676 ,  A61K8/70 ,  A61K8/733 ,  A61K8/738 ,  A61K9/0019 ,  A61K9/06 ,  A61K9/08 ,  A61K9/19 ,  A61K31/03 ,  A61K31/085 ,  A61K31/09 ,  A61K31/167 ,  A61K31/375 ,  A61K31/655 ,  A61K31/7034 ,  A61K45/06 ,  A61K47/36 ,  A61K47/40 ,  A61Q7/00 ,  A61Q19/08 ,  Y02A50/401 ,  A61K2300/00

摘要： Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I): wherein: L represents a linker selected from —C≡C—, (a tolan), —CH═CH— (a stilbene, preferably trans); or —CRa═CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q; R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3′, 4, 4′, and/or 5, 5′; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ≥1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein. The formulation may include a hydrogel formed by the compounds themselves or otherwise and may include salts and/or complexes.

公开(公告)号：US20180280354A1

公开(公告)日：2018-10-04

申请号：US15997028

申请日：2018-06-04

申请人： Orion Corporation

发明人： Olli TÖRMÄKANGAS ,  Terhi HEIKKINEN

IPC分类号： A61K31/4155 ,  A61K31/277 ,  A61K31/166 ,  A61K31/03

CPC分类号： A61K31/4155 ,  A61K31/03 ,  A61K31/166 ,  A61K31/277 ,  C07D231/14

摘要： The present disclosure relates to solid crystalline forms of N—((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)-propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide (I) and the diastereomers thereof, and to methods for preparing such crystalline forms. Compound (I) and the diastereomers thereof are potent androgen receptor (AR) modulators useful as a medicament.

公开(公告)号：US09943505B2

公开(公告)日：2018-04-17

申请号：US15697878

申请日：2017-09-07

申请人： Corcept Therapeutics, Inc.

发明人： Hazel Hunt ,  Thaddeus S. Block

IPC分类号： A61K31/416 ,  A61K31/03 ,  A61K31/473 ,  A61K31/44 ,  A61K31/4192 ,  A61K31/18

CPC分类号： A61K31/416 ,  A61K31/03 ,  A61K31/18 ,  A61K31/337 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/473 ,  A61K31/513 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

摘要： Methods and compositions for treating a subject hosting a non-ACTH-secreting pancreatic tumor are disclosed. The methods include administering to the subject a chemotherapeutic agent and a glucocorticoid receptor modulator (GRM), preferably a selective glucocorticoid receptor modulator (SGRM), to reduce the tumor load in the subject. The GRM may be a nonsteroidal GRM, and may be a nonsteroidal SGRM. The non-ACTH-secreting pancreatic tumor may be an exocrine pancreatic tumor.The nonsteroidal SGRM may be a nonsteroidal compound comprising: a fused azadecalin structure; a heteroaryl ketone fused azadecalin structure; or an octahydro fused azadecalin structure. Pharmaceutical compositions comprising a chemotherapeutic agent and a GRM are disclosed. The GRM in such pharmaceutical compositions may be a nonsteroidal GRM, and may be a SGRM, such as a nonsteroidal SGRM. The nonsteroidal SGRM may comprise: a fused azadecalin structure; a heteroaryl ketone fused azadecalin structure; or an octahydro fused azadecalin structure.

公开(公告)号：US20180071255A1

公开(公告)日：2018-03-15

申请号：US15697878

申请日：2017-09-07

申请人： Corcept Therapeutics, Inc.

发明人： Hazel Hunt ,  Thaddeus S. Block

IPC分类号： A61K31/416 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/18 ,  A61K31/473 ,  A61K31/03

CPC分类号： A61K31/416 ,  A61K31/03 ,  A61K31/18 ,  A61K31/337 ,  A61K31/4192 ,  A61K31/44 ,  A61K31/473 ,  A61K31/513 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

摘要： Methods and compositions for treating a subject hosting a non-ACTH-secreting pancreatic tumor are disclosed. The methods include administering to the subject a chemotherapeutic agent and a glucocorticoid receptor modulator (GRM), preferably a selective glucocorticoid receptor modulator (SGRM), to reduce the tumor load in the subject. The GRM may be a nonsteroidal GRM, and may be a nonsteroidal SGRM. The non-ACTH-secreting pancreatic tumor may be an exocrine pancreatic tumor.The nonsteroidal SGRM may be a nonsteroidal compound comprising: a fused azadecalin structure; a heteroaryl ketone fused azadecalin structure; or an octahydro fused azadecalin structure. Pharmaceutical compositions comprising a chemotherapeutic agent and a GRM are disclosed. The GRM in such pharmaceutical compositions may be a nonsteroidal GRM, and may be a SGRM, such as a nonsteroidal SGRM. The nonsteroidal SGRM may comprise: a fused azadecalin structure; a heteroaryl ketone fused azadecalin structure; or an octahydro fused azadecalin structure.

公开(公告)号：US09877937B2

公开(公告)日：2018-01-30

申请号：US15170682

申请日：2016-06-01

申请人： Millendo Therapeutics, Inc. ,  The Regents of the University of Michigan

发明人： Gary Hammer ,  Tom Kerppola ,  Raili Kerppola

IPC分类号： A61K31/17 ,  A61K31/03 ,  A61K31/155 ,  A61K31/436 ,  A61K45/06 ,  A61K31/568 ,  A61K31/567 ,  A61K31/573 ,  A61K31/58 ,  A61K9/00

CPC分类号： A61K31/17 ,  A61K9/0053 ,  A61K31/03 ,  A61K31/155 ,  A61K31/436 ,  A61K31/567 ,  A61K31/568 ,  A61K31/573 ,  A61K31/58 ,  A61K45/06 ,  A61K2300/00

摘要： Methods and compositions are provided for treatment of disorders associated with aberrant adrenal cortex cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC), Cushing's syndrome and/or pituitary ACTH excess (Cushing's Disease). Such methods involve administration of an effective amount N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethyl amino)phenyl)cyclopentyl)-methyl)urea hydrochloride to the patient.

公开(公告)号：US20180015176A1

公开(公告)日：2018-01-18

申请号：US15536112

申请日：2015-12-10

申请人： Bayer Pharma Aktiengesellschaft

发明人： Hans-Georg LERCHEN ,  Sven WITTROCK ,  Yolanda CANCHO GRANDE ,  Beatrix STELTE-LUDWIG ,  Anette SOMMER ,  Sandra BERNDT ,  Christoph MAHLERT ,  Anne-Sophie REBSTOCK ,  Carsten TERJUNG ,  Simone GREVEN

IPC分类号： A61K31/4025 ,  A61K31/131 ,  A61K31/03 ,  A61K38/00 ,  A61K31/4192 ,  A61K31/497 ,  A61K31/16

CPC分类号： A61K47/6803 ,  A61K31/03 ,  A61K31/131 ,  A61K31/16 ,  A61K31/4025 ,  A61K31/4192 ,  A61K31/497 ,  A61K38/00 ,  A61K47/6851

摘要： The present application relates to novel binder drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prophylaxis of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

公开(公告)号：US20170196207A1

公开(公告)日：2017-07-13

申请号：US15314647

申请日：2015-06-03

申请人： Arturo SOLIS HERRERA, M.D., Ph.D.

发明人： Arturo SOLIS HERRERA, M.D., Ph.D.

IPC分类号： A01K67/027 ,  A61K49/00

CPC分类号： A01K67/027 ,  A01K2227/10 ,  A01K2267/035 ,  A61K31/03 ,  A61K31/05 ,  A61K49/0008

摘要： Methods of producing non-human animal models of corneal angiogenesis and corneal ectatic diseases, such as corneal keratoconus, by applying an aromatic compound to the eye of a non-human animal are described. Also described are non-human animal models of corneal angiogenesis and corneal ectatic diseases, and methods of using the non-human animal models to screen compounds that modulate corneal angiogenesis and corneal ectatic diseases.

公开(公告)号：US20160279119A9

公开(公告)日：2016-09-29

申请号：US12880591

申请日：2010-09-13

申请人： Joseph R. HOLTMAN ,  Peter A. Crooks ,  Linda P. Dwoskin ,  J. Michael McIntosh ,  Elzbieta Pogonowska Wala

发明人： Joseph R. HOLTMAN ,  Peter A. Crooks ,  Linda P. Dwoskin ,  J. Michael McIntosh ,  Elzbieta Pogonowska Wala

IPC分类号： A61K31/4725 ,  A61P29/00 ,  A61K31/03 ,  A61K31/047 ,  A61K31/444 ,  A61K31/4709

CPC分类号： C07D401/14 ,  A61K31/03 ,  A61K31/047 ,  A61K31/4425 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12

摘要： Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.

摘要翻译： 提供使用双季铵化合物治疗炎性疼痛，神经性疼痛和伤害性疼痛的方法。