公开(公告)号：EP2556055A2

公开(公告)日：2013-02-13

申请号：EP11766857.4

申请日：2011-04-11

申请人： The Research Foundation of the State University of New York ,  Syracuse University Technology Transfer And Industrial Development Office

发明人： KERR, William G. ,  CHISHOLM, John D.

IPC分类号： C07C401/00 ,  A61K31/565 ,  A61K31/575 ,  A61K31/56 ,  A61P35/00

CPC分类号： C07J41/0005 ,  A61K31/56 ,  A61K31/565 ,  A61K31/575 ,  C07J1/0007 ,  C07J1/0011 ,  C07J9/00 ,  C07J31/003 ,  C07J31/006 ,  C07J41/0011 ,  C07J41/0027 ,  C07J41/005 ,  C07J41/0055

摘要： The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of
ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.

公开(公告)号：EP1304333A3

公开(公告)日：2005-03-09

申请号：EP02025269.8

申请日：1997-07-11

申请人： Inflazyme Pharmaceuticals, Ltd. ,  THE UNIVERSITY OF BRITISH COLUMBIA ,  UNIVERSITY OF ALBERTA

发明人： Piers, Edward ,  Chau, Joseph, H.L ,  Rogers, Christine ,  Salari, Hassan ,  Burgoyne, David, L. ,  Shen, Yaping ,  Langlands, John, M.

IPC分类号： C07J1/00 ,  A61K31/56 ,  C07J21/00 ,  C07J51/00 ,  C07J71/00 ,  C07J17/00 ,  C07J13/00 ,  C07J9/00 ,  C07J7/00 ,  C07J3/00 ,  C07J31/00 ,  C07J41/00

CPC分类号： C07J71/001 ,  C07J1/0007 ,  C07J1/0011 ,  C07J1/0022 ,  C07J3/00 ,  C07J7/002 ,  C07J9/00 ,  C07J13/005 ,  C07J13/007 ,  C07J17/00 ,  C07J21/008 ,  C07J31/006 ,  C07J41/0016 ,  C07J51/00 ,  C07J71/0026

摘要： Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6α and 7β oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6α and 7β oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and δ-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.

公开(公告)号：EP0924219A2

公开(公告)日：1999-06-23

申请号：EP98203950.5

申请日：1995-09-29

申请人： PHERIN CORPORATION

发明人： Berliner, David L. ,  Adams, Nathan William ,  Jennings-white, Clive L.

IPC分类号： C07J1/00 ,  A61K31/565 ,  C07J3/00 ,  C07J31/00 ,  C07J53/00 ,  C07J13/00 ,  C07J41/00 ,  C07J71/00 ,  A61K31/56

CPC分类号： C07J1/0081 ,  C07J1/0007 ,  C07J1/0055 ,  C07J3/00 ,  C07J13/002 ,  C07J13/005 ,  C07J13/007 ,  C07J31/006 ,  C07J41/0005 ,  C07J71/001 ,  C07J75/005

摘要： The invention relates to estrene steroids, which bind to neuroepithelial cells in the human vomeronasal organ. The steroids are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Figure (1) illustrates the synthesis of 1,3,5(10), 16-estratetraen-3-ol.

摘要翻译： 本发明涉及雌激素类固醇，其结合人类犁鼻器官中的神经上皮细胞。 类固醇优选以含有一种或多种药学上可接受的载体的药物组合物的形式施用。 图（1）说明1,3,5（10），16-雌四烯-3-醇的合成。

公开(公告)号：EP0783513A1

公开(公告)日：1997-07-16

申请号：EP95935237.0

申请日：1995-09-29

申请人： PHERIN CORPORATION

发明人： BERLINER, David, L. ,  ADAMS, Nathan, W. ,  JENNINGS-WHITE, Clive, L.

IPC分类号： A61P25 ,  C07J1 ,  C07J3 ,  C07J13 ,  C07J31 ,  C07J41 ,  C07J53 ,  C07J71 ,  C07J75

CPC分类号： C07J1/0081 ,  C07J1/0007 ,  C07J1/0055 ,  C07J3/00 ,  C07J13/002 ,  C07J13/005 ,  C07J13/007 ,  C07J31/006 ,  C07J41/0005 ,  C07J71/001 ,  C07J75/005

摘要： The invention relates to estrene steroids, which bind to neuroepithelial cells in the human vomeronasal organ. The steroids are preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers. Figure (1) illustrates the synthesis of 1,3,5(10),16-estratetraen-3-ol.

摘要翻译： 本发明涉及与人犁鼻器官中的神经上皮细胞结合的雌激素类固醇。 类固醇优选以含有一种或多种药学上可接受的载体的药物组合物的形式施用。 图（1）说明了1,3,5（10），16-雌三烯-3-醇的合成。

公开(公告)号：EP2980096A4

公开(公告)日：2016-11-16

申请号：EP14774834

申请日：2014-03-28

申请人： GUANGZHOU CELLPROTEK PHARMACEUTICAL CO LTD

发明人： ZHANG JINGXIA ,  LIN SUIZHEN ,  XIE MINYU

IPC分类号： C07J1/00 ,  A61K31/568 ,  A61P25/00 ,  A61P35/00 ,  C07J31/00 ,  C07J71/00

CPC分类号： C07J1/0007 ,  A61K31/568 ,  A61K45/06 ,  C07J1/007 ,  C07J31/006 ,  C07J71/001

摘要： The present invention discloses compound 2²,3±,5±-trihydroxy-androst-6-one, having the structure of formula (I). The present invention also discloses a plurality of methods for preparing the compound and a use of the compound.

公开(公告)号：EP2556055A4

公开(公告)日：2014-02-19

申请号：EP11766857

申请日：2011-04-11

申请人： UNIV NEW YORK STATE RES FOUND ,  SYRACUSE UNIVERSITY TECHNOLOGY TRANSFER AND IND DEV OFFICE

发明人： KERR WILLIAM G ,  CHISHOLM JOHN D

IPC分类号： C07C401/00 ,  A61K31/56 ,  A61K31/565 ,  A61K31/575 ,  A61P35/00

CPC分类号： C07J41/0005 ,  A61K31/56 ,  A61K31/565 ,  A61K31/575 ,  C07J1/0007 ,  C07J1/0011 ,  C07J9/00 ,  C07J31/003 ,  C07J31/006 ,  C07J41/0011 ,  C07J41/0027 ,  C07J41/005 ,  C07J41/0055

摘要： The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.

公开(公告)号：EP2688901A1

公开(公告)日：2014-01-29

申请号：EP12765822.7

申请日：2012-03-26

申请人： Université Laval

发明人： POIRIER, Donald ,  MALTAIS, René ,  ROY, Jenny

IPC分类号： C07J1/00 ,  A61K31/565 ,  A61K31/566 ,  A61K31/58 ,  A61K31/675 ,  A61K31/69 ,  A61K51/04 ,  A61P35/00 ,  C12N9/04

CPC分类号： C07J41/0005 ,  A61K31/566 ,  A61K31/567 ,  A61K31/5685 ,  A61K31/58 ,  A61K31/675 ,  A61K31/69 ,  A61K45/06 ,  A61K51/04 ,  C07J1/0007 ,  C07J1/0062 ,  C07J21/00 ,  C07J21/008 ,  C07J31/006 ,  C07J41/0011 ,  C07J41/0038 ,  C07J41/0072 ,  C07J43/003 ,  C07J43/006 ,  C07J51/00 ,  C12Y101/01051

摘要： The present application discloses 17ß hydroxy steroid dehydrogenase (17ß HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17ß HSDl inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17ß HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17ß HSDl and 17ß HSD3 that have a spiro-morpholine substituent at C20.

摘要翻译： 本申请公开了17β羟基类固醇脱氢酶（17βHSD）型1,3,10抑制剂及其在治疗癌症和其他疾病中的用途（单独和组合）。 17βHSD1抑制剂包括在C 16处具有氮杂 - 氨基甲酰基苄基取代基的雌二醇衍生物。17βHSD3 / HSD10抑制剂包括在C3位用磺酰胺哌嗪取代的雄甾酮衍生物。 还公开了在C20处具有螺 - 吗啉取代基的17βHSD1和17βHSD3两者的抑制剂的化合物。

公开(公告)号：EP2591785A4

公开(公告)日：2013-12-11

申请号：EP11803155

申请日：2011-07-08

申请人： GUANGZHOU CELLPROTEK PHARMACEUTICAL LTD

发明人： YAN GUANGMEI ,  HU HAIYAN ,  LENG TIANDONG ,  SANG HANFEI ,  ZHANG JINGXIA ,  QIU PENGXIN ,  ZHOU SHUJIA ,  CHEN JIESI ,  YOU XIUHUA

IPC分类号： A61K31/568 ,  A61P9/10 ,  A61P25/00

CPC分类号： A61K31/568 ,  C07J1/0007

公开(公告)号：EP2591785A1

公开(公告)日：2013-05-15

申请号：EP11803155.8

申请日：2011-07-08

申请人： Guangzhou Cellprotek Pharmaceutical Ltd.

发明人： YAN, Guangmei ,  HU, Haiyan ,  LENG, Tiandong ,  SANG, Hanfei ,  ZHANG, Jingxia ,  QIU, Pengxin ,  ZHOU, Shujia ,  CHEN, Jiesi ,  YOU, Xiuhua

IPC分类号： A61K31/568 ,  A61P25/00 ,  A61P9/10

CPC分类号： A61K31/568 ,  C07J1/0007

摘要： Disclosed is the use of 5α-androstane(alkyl)-3β,5,6β-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord ischemia or hypoxia and has no obvious toxic reaction within effective dose thereof.

摘要翻译： 公开了在制备神经保护药物中使用5α-雄甾烷（烷基）-3β，5,6β-三醇。 该化合物对由脑缺血，脊髓缺血或缺氧引起的神经元损伤具有显着的保护作用，并且在其有效剂量内没有明显的毒性反应。

公开(公告)号：EP0837874B1

公开(公告)日：2004-12-15

申请号：EP96919372.1

申请日：1996-06-06

申请人： Euro-Celtique S.A.

发明人： UPASANI, Ravindra, B. ,  FICK, David, B. ,  HOGENKAMP, Derk, J. ,  LAN, Nancy, C.

IPC分类号： C07J1/00 ,  C07J43/00 ,  C07J41/00

CPC分类号： C07J31/006 ,  C07J1/0007 ,  C07J1/0029 ,  C07J1/0055 ,  C07J1/0077 ,  C07J17/00 ,  C07J21/00 ,  C07J41/0005 ,  C07J41/005 ,  C07J43/003

摘要： The invention relates to 3 alpha -hydroxy, 17-(un)substituted derivatives of the androstane series and 3 alpha -hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having general structural formula (I), wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes pregnanes (R4 = methyl), 19-norandrostanes, and norpregnanes (R4 = H).