公开(公告)号：EP0637296A1

公开(公告)日：1995-02-08

申请号：EP93910811.0

申请日：1993-04-21

申请人： LIGAND PHARMACEUTICALS, INC. ,  THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

发明人： PATHIRANA, I., Charles ,  BERGER, Tina, S. ,  STEIN, Robert, S. ,  FENICAL, William ,  JONES, Todd, K. ,  HAMANN, Lawrence, G. ,  FARMER, Luc

IPC分类号： C07C25 ,  C07C43 ,  C07C45 ,  C07C47 ,  C07C49 ,  C07C69 ,  C07C205 ,  C07K14

CPC分类号： C07K14/721 ,  C07C25/24 ,  C07C43/23 ,  C07C45/00 ,  C07C45/673 ,  C07C45/68 ,  C07C45/71 ,  C07C47/575 ,  C07C49/603 ,  C07C49/753 ,  C07C69/017 ,  C07C205/06 ,  C07C205/45 ,  C07C2601/06 ,  C07C2601/14 ,  C07C2601/16

摘要： Non-steroidal compounds which are high affinity, high specificity ligands for progesterone receptors are disclosed. The compounds include synthetic derivatives of cyclocymopol and its diastereomers, spectroscopically and chromatographically pure (3R)-cyclocymopol monomethyl ether, which functions as a progesterone receptor antagonist, and spectroscopically and chromatographically pure (3S)-cyclocymopol monomethyl ether, which functions as a progesterone receptor agonist. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by progesterone receptors and for treating patients requiring progesterone receptor agonist or antagonist therapy.

摘要翻译： 哪些是高亲和力，高特异性的配体为孕激素受体的非甾体化合物是游离缺失盘。 化合物包括cyclocymopol的合成衍生物和其非对映体，和光谱色谱纯（3R）-cyclocymopol单甲基醚，作为孕酮受体拮抗剂的功能，和光谱和色谱纯（3S）-cyclocymopol单甲基醚，作为孕激素受体发挥功能 激动剂。 所以圆盘游离缺失是采用用于调制由孕激素受体介导的过程的游离缺失盘化合物和用于治疗患者需要孕酮受体激动剂或拮抗剂治疗的方法。

公开(公告)号：EP0800519A1

公开(公告)日：1997-10-15

申请号：EP95944089.0

申请日：1995-12-13

申请人： LIGAND PHARMACEUTICALS, INC.

发明人： JONES, Todd, K. ,  GOLDMAN, Mark, E. ,  POOLEY, Charlotte, L., F. ,  WINN, David, T. ,  EDWARDS, James, E. ,  WEST, Sarah, J. ,  TEGLEY, Christopher, M. ,  ZHI, Lin ,  HAMANN, Lawrence, G. ,  FARMER, Luc, J. ,  DAVIS, Robert, J.

IPC分类号： A61K31 ,  A61P5 ,  C07D215 ,  C07D221 ,  C07D311 ,  C07D401 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D471 ,  C07D491 ,  C07D493 ,  C07D495

CPC分类号： C07D401/04 ,  C07D215/06 ,  C07D221/18 ,  C07D311/80 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04

摘要： Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

公开(公告)号：EP1175397B1

公开(公告)日：2004-08-18

申请号：EP00930201.9

申请日：2000-05-01

申请人： Wyeth ,  LIGAND PHARMACEUTICALS, INC.

发明人： ULLRICH, John, W. ,  FENSOME, Andrew ,  ZHI, Lin ,  JONES, Todd, K. ,  WROBEL, Jay, E. ,  TEGLEY, Christopher, M. ,  EDWARDS, James, P.

IPC分类号： C07D209/08 ,  A61K31/404 ,  A61P5/36

CPC分类号： C07D209/08

摘要： A compound of formula (I) and pharmaceutical compositions thereof useful as progesterone receptor antagonist wherein: R1 and R2 are H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, optionally substituted alkyl, O(alkyl), aryl, heteroaryl; or R1 and R2 are joined to form a ring, a double bond to CMe2; C(cycloalkyl), O, C(cycloether); R3 = H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl; RA = H, optionally substituted alkyl, alkoxy, aminoalkyl; R¿4? = H, halo, CN, NH2, optionally substituted alkyl, alkoxy, or aminoalkyl; R5 = optionally substituted phenyl, a 5- or 6-membered heterocycle; a 4- or 7-substituted indole or a substituted benzothiophene.

公开(公告)号：EP1175397A1

公开(公告)日：2002-01-30

申请号：EP00930201.9

申请日：2000-05-01

申请人： AMERICAN HOME PRODUCTS CORPORATION ,  LIGAND PHARMACEUTICALS, INC.

发明人： ULLRICH, John, W. ,  FENSOME, Andrew ,  ZHI, Lin ,  JONES, Todd, K. ,  WROBEL, Jay, E. ,  TEGLEY, Christopher, M. ,  EDWARDS, James, P.

IPC分类号： C07D209/08 ,  A61K31/404 ,  A61P5/36

CPC分类号： C07D209/08

摘要： A compound of formula (I) and pharmaceutical compositions thereof useful as progesterone receptor antagonist wherein: R1 and R2 are H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, optionally substituted alkyl, O(alkyl), aryl, heteroaryl; or R1 and R2 are joined to form a ring, a double bond to CMe2; C(cycloalkyl), O, C(cycloether); R3 = H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl; RA = H, optionally substituted alkyl, alkoxy, aminoalkyl; R¿4? = H, halo, CN, NH2, optionally substituted alkyl, alkoxy, or aminoalkyl; R5 = optionally substituted phenyl, a 5- or 6-membered heterocycle; a 4- or 7-substituted indole or a substituted benzothiophene.

摘要翻译： 其中：R1和R2为H，OH，OAc，烷基芳基，烷基杂芳基，1-丙炔基，任选取代的烷基，O（烷基），芳基，杂芳基; 或R1和R2连接形成环，与CMe2形成双键; C（环烷基），O，C（环醚）; R3 = H，OH，NH2，CORA或任选取代的链烯基或炔基; RA = H，任选取代的烷基，烷氧基，氨基烷基; R¿4？ = H，卤素，CN，NH 2，任选取代的烷基，烷氧基或氨基烷基; R5 =任选取代的苯基，5或6元杂环; 4-或7-取代的吲哚或取代的苯并噻吩。