公开(公告)号：EP2010483A2

公开(公告)日：2009-01-07

申请号：EP07754958.2

申请日：2007-04-05

申请人： Wisconsin Alumni Research Foundation

发明人： SICINSKI, Rafal R. ,  CLAGETT-DAME, Margaret ,  DELUCA, Hector F. ,  PLUM, Lora A. ,  GLEBOCKA, Agnieszka

IPC分类号： C07C401/00 ,  A61K31/59 ,  A61P35/00 ,  A61P3/02

CPC分类号： C07C401/00 ,  C07C45/29 ,  C07C2602/24 ,  C07C49/443

摘要： Disclosed are 1α-hydroxy-2-(3'-hydroxypropylidene)-19-nor- vitamin D compounds, pharmaceutical compositions, and methods of making and treatment thereof. The compounds are generally directed to biologically active 2-alkylidene-19-nor-vitamin D compounds and analogs thereof characterized by the presence of a 3'-hydroxypropylidene moiety at C-2 and the presence of an abbreviated alkyl side-chain free of any hydroxyl moiety.

摘要翻译： 本发明公开了1α羟基-2-（3'-羟基亚）-19-去甲维生素D化合物，药物组合物，以及制备和它们的治疗方法。 这些化合物基因反弹涉及不含任何生物活性2-亚烷基-19-降 - 维生素D化合物及其类似物在C-2通过一个3“羟基亚部分的存在及其特点和缩写的烷基侧链的存在 羟基基团。

公开(公告)号：EP1828115A2

公开(公告)日：2007-09-05

申请号：EP05851832.5

申请日：2005-11-18

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： DELUCA, Hector F. ,  PLUM, Lori A. ,  CLAGETT-DAME, Margaret

IPC分类号： C07C401/00

CPC分类号： C07C401/00 ,  Y02P20/55

摘要： Compounds of formula (I) are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

摘要翻译： 提供式（I）化合物，其中X 1和X 2独立地选自H或羟基保护基。 此类化合物可用于制备药物组合物并可用于治疗各种生物学病症。

公开(公告)号：EP1981843A2

公开(公告)日：2008-10-22

申请号：EP07763317.0

申请日：2007-01-31

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： DELUCA, Hector F. ,  CHIELLINI, Grazia ,  GRZYWACZ, Pawel ,  PLUM, Lori A. ,  CLAGETT-DAME, Margaret

IPC分类号： C07C401/00 ,  A61K31/59 ,  A61P13/12 ,  A61P17/06 ,  A61P19/00 ,  A61P35/00

CPC分类号： C07C401/00 ,  C07F7/1856 ,  Y02P20/55

摘要： Compounds of formula IA or IB are provided where X1, X2 and X3 are independently selected from H or hydroxy protecting groups and R1 is selected from straight or branched chain alkyl groups having from 1 to 8 carbon atoms; straight or branched chain alkenyl groups having from 2 to 8 carbon atoms; straight or branched chain hydroxy-substituted alkyl groups having from 1 to 8 carbon atoms; straight and branched chain hydroxy-substituted alkenyl groups having from 2 to 8 carbon atoms. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

公开(公告)号：EP1848442A1

公开(公告)日：2007-10-31

申请号：EP06734708.8

申请日：2006-02-10

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： DELUCA, Hector F. ,  PLUM, Lori A. ,  CLAGETT-DAME, Margaret

IPC分类号： A61K31/569 ,  C07C401/00

CPC分类号： C07C401/00 ,  Y02P20/55

摘要： Compounds of formula I are provided where X1, X2, and X3 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

公开(公告)号：EP1482951B1

公开(公告)日：2006-10-04

申请号：EP02795796.8

申请日：2002-12-10

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： DELUCA, Hector F. ,  PLUM, Lori, A. ,  CLAGETT-DAME, Margaret

IPC分类号： A61K31/59 ,  C07C401/00 ,  A61P17/00 ,  A61P17/06 ,  A61P35/00

CPC分类号： C07C401/00 ,  A61K31/59 ,  C07C2601/14 ,  C07C2602/24

摘要： This invention discloses 1 alpha -a-hydroxy-2-methylene-19-nor-pregnacalciferol and pharamaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkels, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any calcemic activity and therefore may be used to treat immune disorders in humans as well as renal osteodystrophy.

摘要翻译： 本发明公开了1α-羟基-2-亚甲基-19-去甲孕酮和其制药用途。 该化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤， 皮肤干燥，皮脂分泌不足。 该化合物也具有很少（如果有的话）钙活性，因此可用于治疗人类的免疫疾病以及肾性骨营养不良。

公开(公告)号：EP2509943A1

公开(公告)日：2012-10-17

申请号：EP10834012.6

申请日：2010-11-29

申请人： Wisconsin Alumni Research Foundation

发明人： DELUCA, Hector F. ,  GRZYWACZ, Pawel ,  PLUM, Lori A. ,  CLAGETT-DAME, Margaret

IPC分类号： C07C401/00 ,  A61K31/59 ,  A61K31/593 ,  A61P11/06 ,  A61P17/00 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00

CPC分类号： C07C401/00 ,  A61K31/593 ,  C07C2601/14 ,  C07C2602/24 ,  Y02P20/55

摘要： Compounds of formula I are provided where X
1 and X
2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

摘要翻译： 提供式I化合物，其中X 1和X 2独立地选自H或羟基保护基。 这些化合物可用于制备药物组合物，并且可用于治疗各种生物学条件。

公开(公告)号：EP1848442B1

公开(公告)日：2012-04-25

申请号：EP06734708.8

申请日：2006-02-10

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： DELUCA, Hector F. ,  PLUM, Lori A. ,  CLAGETT-DAME, Margaret

IPC分类号： A61K31/569 ,  C07C401/00 ,  A61P19/10 ,  A61P35/00

CPC分类号： C07C401/00 ,  Y02P20/55

摘要： Compounds of formula I are provided where X1, X2, and X3 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

公开(公告)号：EP1827452B1

公开(公告)日：2011-03-02

申请号：EP05849207.5

申请日：2005-11-18

申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION

发明人： DELUCA, Hector F. ,  PLUM, Lori A. ,  CLAGETT-DAME, Margaret

IPC分类号： A61K31/59 ,  C07C401/00

CPC分类号： C07C401/00 ,  Y02P20/55

摘要： Compounds of formula (I) are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.

摘要翻译： 提供式（I）化合物，其中X 1和X 2独立地选自H或羟基保护基。 此类化合物可用于制备药物组合物并可用于治疗各种生物学病症。

公开(公告)号：EP1981843B1

公开(公告)日：2009-12-09

申请号：EP07763317.0

申请日：2007-01-31

申请人： Wisconsin Alumni Research Foundation

发明人： DELUCA, Hector F. ,  CHIELLINI, Grazia ,  GRZYWACZ, Pawel ,  PLUM, Lori A. ,  CLAGETT-DAME, Margaret

IPC分类号： C07C401/00 ,  A61K31/59 ,  A61P13/12 ,  A61P17/06 ,  A61P19/00 ,  A61P35/00

CPC分类号： C07C401/00 ,  C07F7/1856 ,  Y02P20/55

公开(公告)号：EP2069297A1

公开(公告)日：2009-06-17

申请号：EP07843120.2

申请日：2007-09-25

申请人： Wisconsin Alumni Research Foundation

发明人： DELUCA, Hector F. ,  CLAGETT-DAME, Margaret ,  PLUM, Lori A. ,  CHIELLINI, Grazia ,  GRZYWACZ, Pawel

IPC分类号： C07C401/00 ,  A61K31/59 ,  A61P35/00 ,  A61P3/04 ,  A61P17/06

CPC分类号： C07C401/00 ,  Y02P20/55

摘要： This invention discloses 2-methylene-(20R,25S)-19,27-dinor-(22E)-vitamin D analogs, and specifically 2-methylene-(20R,25S)-19,27-dinor-(22E)-lα,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.