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1. 发明申请

WO2009124965A1 PYRROLO[2,3-d]PYRIMIDIN-2-YL-AMINE DERIVATIVES AS PKC-THETA INHIBITORS 审中-公开
标题翻译：吡咯并[<我
公开(公告)号：WO2009124965A1
公开(公告)日：2009-10-15
申请号：PCT/EP2009/054209
申请日：2009-04-08
申请人： N.V. ORGANON , PHARMACOPEIA, LLC , ROUGHTON, Andrew Laird , HO, Koc-Kan , OHLMEYER, Michael , DILLER, David , NEAGU, Irina , KINGSBURY, Celia , CHAN, Jui-Hsiang , LOMMERSE, Johannes, Petrus, Maria , TEERHUIS, Neeltje, Miranda , WIJKMANS, Jacobus Cornelis Henricus Maria , PLATE, Ralf
发明人： ROUGHTON, Andrew Laird , HO, Koc-Kan , OHLMEYER, Michael , DILLER, David , NEAGU, Irina , KINGSBURY, Celia , CHAN, Jui-Hsiang , LOMMERSE, Johannes, Petrus, Maria , TEERHUIS, Neeltje, Miranda , WIJKMANS, Jacobus Cornelis Henricus Maria , PLATE, Ralf
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKCθ mediated disorders.
摘要翻译：本发明涉及式（I）的吡咯并[2,3-d]嘧啶-2-基 - 胺衍生物，其中变量如说明书中所定义，或其药学上可接受的盐或溶剂合物。本发明还涉及包含一种或多种所述吡咯并[2,3-d]嘧啶-2-基胺衍生物的药物组合物及其在治疗中的用途，例如用于治疗PKC？介导的疾病。

2. 发明申请

WO2008051826A2 PURINES AS PKC-THETA INHIBITORS 审中-公开
标题翻译：作为PKC-THETA抑制剂
公开(公告)号：WO2008051826A2
公开(公告)日：2008-05-02
申请号：PCT/US2007/081899
申请日：2007-10-19
申请人： N.V. ORGANON , PHARMACOPEIA INC. , NEAGU, Irina , ROUGHTON, Andrew , HO, Koc-kan , DILLER, David , CHAN, Jui, Hsiang , KINGSBURY, Celia , OHLMEYER, Michael , WIJKMANS, Jacobus Cornelis, Henricus Maria , TEERHUIS, Neeltje, Miranda , LOMMERSE, Johannes Petrus, Maria
发明人： NEAGU, Irina , ROUGHTON, Andrew , HO, Koc-kan , DILLER, David , CHAN, Jui, Hsiang , KINGSBURY, Celia , OHLMEYER, Michael , WIJKMANS, Jacobus Cornelis, Henricus Maria , TEERHUIS, Neeltje, Miranda , LOMMERSE, Johannes Petrus, Maria
IPC分类号： C07D473/32 , A61K31/52 , A61P35/00
CPC分类号： C07D473/32
摘要： A chemical genus of purines, which are useful as PKC θ inhibitors, is disclosed. The genus is represented by the formula (I); A representative example is: (II)
摘要翻译：嘌呤的化学属，可用作PKC？抑制剂。该属由式（I）表示; 一个代表性的例子是：（二）

3. 发明申请

WO2005102998A1 NOVEL ANDROGENS 审中-公开
标题翻译：新世界
公开(公告)号：WO2005102998A1
公开(公告)日：2005-11-03
申请号：PCT/EP2005/051766
申请日：2005-04-21
申请人： AKZO NOBEL N.V. , VAN DER LOUW, Jaap , TEERHUIS, Neeltje, Miranda , LOMMERSE, Johannes, Petrus, Maria , STOCK, Herman, Thijs , HERMKENS, Pedro, Harold, Han
发明人： VAN DER LOUW, Jaap , TEERHUIS, Neeltje, Miranda , LOMMERSE, Johannes, Petrus, Maria , STOCK, Herman, Thijs , HERMKENS, Pedro, Harold, Han
IPC分类号： C07D209/40
CPC分类号： C07D209/40 , C07D209/30 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/06 , C07D413/04 , C07D413/06 , C07D417/06
摘要： The compounds of the subject invention have a structure according to formula I: wherein X is S or SO 2 ; R 1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally subst ituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C- 4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO 2 H, CO 2 (1C- 4C)alkyl, C(O)NR 5 R 6 , S(O)(1C-4C)alkyl or S(O) 2 (1C-4C)alkyl; R 2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R 3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R 3 is a 5- or 6-membered aromatic heterocyclic ring structure optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, halogen or cyano; R 4 is a phenyl group or an aromatic 6-membered heterocycle, substituted at the ortho position with 1-hydroxy(1C-4C)alkyl, (1C-4C)alkoxy, C(O)(1C- 4C)alkyl, CO 2 (1C-4C)alkyl, C(O)NH 2 , cyano, nitro, or CH=NOR 7 , and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; R 5 is 2-pyridyl optionally substituted with (1C-2C)alkyl, (1C- 2C)fluoroalkyl or halogen; or R 5 and R 6 are independently hydrogen or (1C-4C)alkyl; R 7 is hydrogen or C(O)(1C-4C)alkyl; R 8 , R 9 , R 10 are independently hydrogen, (1C-2C)alkyl, fluoro or chloro; or a salt or hydrate form thereof.
摘要翻译：本发明的化合物具有式I的结构：其中X是S或SO 2; 每个任选被（3C-6C）环烷基，OH，OC（O）（1C-4C）取代的（1C-6C）烷基，（3C-6C）烯基或（3C-6C）烷基，（1C-4C）烷氧基，卤素，氰基，甲酰基，C（O）（1C-4C）烷基，CO 2 H，CO 2（1C-4C）烷基，C（O）NR 5 R 6，（O）（1C-4C）烷基或S（O）2（1C-4C）烷基; R 2是氢，（1C-4C）烷基或C（O）（1C-4C）烷基; （1C-4C）烷基，（1C-4C）氟代烷基，（1C-4C）烷氧基，（1C-4C）氟烷氧基，卤素，氰基或硝基取代的苯基; 或（R 3）是任选被（1C-4C）烷基，（1C-4C）氟代烷基，（1C-4C）烷氧基，卤素或氰基取代的5或6元芳族杂环结构; R 4是在邻位被1-羟基（1C-4C）烷基，（1C-4C）烷氧基，C（O）（1C-4C）烷基取代的苯基或芳族六元杂环， CO 2（1C-4C）烷基，C（O）NH 2，氰基，硝基或CH = NOR 7，并任选进一步被（1C-2C）烷基，（1C-2C）氟烷基或卤素取代; R 5是任选被（1C-2C）烷基，（1C-2C）氟烷基或卤素取代的2-吡啶基; 或R 5和R 6独立地为氢或（1C-4C）烷基; R 7是氢或C（O）（1C-4C）烷基; R 8，R 9，R 10独立地是氢，（1C-2C）烷基，氟或氯; 或其盐或水合物形式。

4. 发明申请

WO2004041782A1 INDOLES USEFUL IN THE TREATMENT OF ANDROGEN-RECEPTOR RELATED DISEASES 审中-公开
标题翻译：吲哚美辛治疗有关的原癌基因相关疾病
公开(公告)号：WO2004041782A1
公开(公告)日：2004-05-21
申请号：PCT/EP2003/050783
申请日：2003-11-03
申请人： AKZO NOBEL N.V. , HERMKENS, Pedro, Harold, Han , STOCK, Herman, Thijs , TEERHUIS, Neeltje, Miranda , LOMMERSE, Johannes, Petrus, Maria , VAN DER LOUW, Jaap
发明人： HERMKENS, Pedro, Harold, Han , STOCK, Herman, Thijs , TEERHUIS, Neeltje, Miranda , LOMMERSE, Johannes, Petrus, Maria , VAN DER LOUW, Jaap
IPC分类号： C07D209/30
CPC分类号： C07D209/30 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/06 , C07D417/06
摘要： This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula (1) wherein X is S,SO or S0 2 ; R 1 is a 5- or 6-membered monocyclic, hetero- or homocyclic, saturated or unsaturated ring structure optionally substituted with one or more substituents selected from the group consisting of halogen, CN, (1C-4C)fluoroalkyl, nitro, (1C-4C)alkyl, (1C-4C)alkoxy or (1C-4C)fluoroalkoxy; R 2 is 2-nitrophenyl, 2-cyanophenyl, 2-hydroxymethyl-phenyl, pyridin-2-yl, pyridin-2-yl-N-oxide, 2-benzamide, 2-benzoic acid methyl ester or 2-methoxyphenyl; R 3 is H, halogen or (1C-4C)alkyl; R 4 is H, OH, (1C-4C)alkoxy, or halogen; R 4 is H, OH, (1C-4C)alkoxy, NH 2 , CN, halogen, (1C-4C)fluoroalkyl, N0 2 , hydroxy(1C-4C)alkyl, C0 2 H, C0 2 (1C-6C)alkyl, or R 5 is NHR 6 , wherein R 6 is (1C-6C)acyl optionally substituted with one or more halogens, S(O) 2 (1C-4C)alkyl, or S(O) 2 aryl optionally substituted with (1C-4C)alkyl or one or more halogens, or R 5 is C(O)N(R 8 ,R 9 ), wherein R 8 and R 9 each independently are H, (3C-6C)cycloalkyl, or CH 2 R 10 , wherein R 10 is H, (1C-5C)alkyl, (1C-5C)alkenyl, hydroxy(1C-3C)alkyl, (1C-4C)alkylester of carboxy(1C-4C)alkyl, (1C-3C)alkoxy(1C-3C)alkyl, (mono- or di(1C-4C)alkyl)aminomethyl, (mono- or di(1C-4C)alkyl)aminocarbonyl, or a 3-, 4-, 5- or 6-membered monocyclic, homo- or heterocyclic, aromatic or non-aromatic ring, or R 8 and R 9 form together with the N a heterocyclic 5- or 6-membered saturated or unsaturated ring optionally substituted with (1C-4C)alkyl; or a salt or hydrate form thereof.
摘要翻译：本发明提供具有对雄激素受体的亲和力的非甾体化合物和用于雄激素受体相关治疗的具有根据式（1）的结构的非甾体化合物，其中X是S，SO或SO 2; R 1是任选被一个或多个选自卤素，CN，（1C-4C）氟代烷基，硝基，C 1 -C 4烷氧基，（1C-4C）烷基，（1C-4C）烷氧基或（1C-4C）氟烷氧基; R 2是2-硝基苯基，2-氰基苯基，2-羟甲基 - 苯基，吡啶-2-基，吡啶-2-基-N-氧化物，2-苯甲酰胺，2-苯甲酸甲酯或2-甲氧基苯基; R 3是H，卤素或（1C-4C）烷基; R 4是H，OH，（1C-4C）烷氧基或卤素; R 4是H，OH，（1C-4C）烷氧基，NH 2，CN，卤素，（1C-4C）氟代烷基，NO 2，羟基（C 1 -C 4）烷基，CO 2 H，CO（C 1 -C 6） R 5是NHR 6，其中R 6是任选被一个或多个卤素，S（O）2（1C-4C）烷基或任选取代的S（O）2芳基）的（1C-6C）酰基（1C-4C）烷基或一个或多个卤素，或R 5是C（O）N（R 8，R 9），其中R 8和R 9各自独立地是H ，（C 1 -C 5）环烷基或CH 2 R 10，其中R 10是H，（1C-5C）烷基，（1C-5C）烯基，羟基（1C-3C）烷基，（1C-4C）烷基酯（1C-3C）烷基，（一或二（1C-4C）烷基）氨基甲基，（一或二（1C-4C）烷基）氨基羰基，或3-，4-，5-或6-元单环，均聚或杂环的芳族或非芳族环，或R 8和R 9与N a一起形成杂环的5-或6-元杂环，任选被（1C-4C）烷基取代的饱和或不饱和的环; 或其盐或水合物形式。

5. 发明申请

WO2010103095A1 TETRAHYDRONAPHTHALEN-2-OL DERIVATIVES 审中-公开
标题翻译：四氢萘-2-醛衍生物
公开(公告)号：WO2010103095A1
公开(公告)日：2010-09-16
申请号：PCT/EP2010/053167
申请日：2010-03-12
申请人： N.V. ORGANON , STOCK, Herman, Thijs , TEERHUIS, Neeltje, Miranda , VEENEMAN, Gerrit, Herman
发明人： STOCK, Herman, Thijs , TEERHUIS, Neeltje, Miranda , VEENEMAN, Gerrit, Herman
IPC分类号： C07C39/42 , C07C39/17 , C07C255/54 , C07C43/225 , C07C43/21 , C07C43/23 , C07C69/157 , C07C255/55 , A61K31/055 , A61K31/277 , A61K31/09 , A61K31/222 , A61P31/08 , A61P35/00 , A61P25/00
CPC分类号： C07C43/225 , C07C39/17 , C07C39/42 , C07C43/21 , C07C43/23 , C07C69/017 , C07C255/53 , C07C255/54 , C07C2602/10
摘要： The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms,benign prostate hyperplasia,prostate cancer,hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer.
摘要翻译：本发明涉及新的四氢萘-2-醇衍生物，包含这些化合物的药物组合物及其在治疗中的用途，特别是其用于制备用于预防或治疗下尿路症状的药物，良性前列腺增生，前列腺癌，热潮红，焦虑，抑郁，乳腺癌，甲状腺髓样癌，卵巢癌，炎性肠病，关节炎，子宫内膜异位症和结肠癌。

6. 发明公开

EP2294071A1 PYRROLO[2,3-d]PYRIMIDIN-2-YL-AMINE DERIVATIVES AS PKC-THETA INHIBITORS 审中-公开
标题翻译：吡咯并[2,3-D-]嘧啶-2-YL-氨基衍生物PKC-THETA-HEMMER
公开(公告)号：EP2294071A1
公开(公告)日：2011-03-16
申请号：EP09729779.0
申请日：2009-04-08
申请人： N.V. Organon , Pharmacopeia, LLC
发明人： ROUGHTON, Andrew Laird , HO, Koc-Kan , OHLMEYER, Michael , DILLER, David , NEAGU, Irina , KINGSBURY, Celia , CHAN, Jui-Hsiang , LOMMERSE, Johannes, Petrus, Maria , TEERHUIS, Neeltje, Miranda , WIJKMANS, Jacobus Cornelis Henricus Maria , PLATE, Ralf
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The present invention relates to a pyrrolo[2,3-d]pyrimidin-2-yl-amine derivative according to formula (I) wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said pyrrolo[2,3-d]pyrimidine-2-ylamine derivatives and to their use in therapy, for instance in the treatment of PKCθ mediated disorders.

7. 发明授权

EP1282615B1 CHROMAN DERIVATIVES AS ESTROGENIC COMPOUNDS 有权
标题翻译：色当雌激素CONNECTIONS
公开(公告)号：EP1282615B1
公开(公告)日：2011-10-19
申请号：EP01929361.2
申请日：2001-02-26
申请人： N.V. Organon
发明人： VEENEMAN, Gerrit, Herman , TEERHUIS, Neeltje, Miranda
IPC分类号： C07D311/60 , A61K31/35 , A61P5/30
CPC分类号： C07D311/60
摘要： The invention provides chroman compounds having Formula (1), wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is Hal, CF¿3?, OH or (1C-2C)alkyloxy; R?2, R3, and R5¿ are independently H, Hal, CF¿3?, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.

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