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1. 发明申请

US20140155406A1 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES BTK INHIBITORS 审中-公开
标题翻译： 4-咪唑并吡嗪-1-基-L-苯甲酰胺和4-咪唑氧基-1-YL-苯甲酮BTK抑制剂
公开(公告)号：US20140155406A1
公开(公告)日：2014-06-05
申请号：US14233429
申请日：2012-07-11
申请人： Petrus Antonius De Adrianus Man , Jacobus C.H.M. Wijkmans , Jan-Gerard Sterrenburg , Han C.A. Raaijmakers , Tjeerd A. Barf , Rogier Christian Buijsman , Arthur A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Herman Thijs Stock
发明人： Petrus Antonius De Adrianus Man , Jacobus C.H.M. Wijkmans , Jan-Gerard Sterrenburg , Han C.A. Raaijmakers , Tjeerd A. Barf , Rogier Christian Buijsman , Arthur A. Oubrie , Johannes Bernardus Maria Rewinkel , Christiaan Gerardus Johannes Maria Jans , Herman Thijs Stock
IPC分类号： A61K31/506 , C07D487/04 , A61K31/4985
CPC分类号： A61K31/506 , A61K31/4985 , C07D487/04 , C07D519/00
摘要： The present invention relates to 6-5 membered fused pyridine ring compounds of formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
摘要翻译：本发明涉及式（I）的6-5元稠合吡啶环化合物或其药学上可接受的盐，或涉及包含这些化合物的药物组合物及其在治疗中的用途。特别地，本发明涉及6-5元稠合吡啶环化合物在治疗布鲁特酪氨酸激酶（Btk）介导的病症中的用途。

2. 发明授权

US08431564B2 Ring-annulated dihydropyrrolo[2,1-α]isoquinolines 有权
标题翻译：环状二氢吡咯并[2,1-α]异喹啉
公开(公告)号：US08431564B2
公开(公告)日：2013-04-30
申请号：US12844007
申请日：2010-07-27
申请人： Cornelis Marius Timmers , Hubert Jan Jozef Loozen , Herman Thijs Stock
发明人： Cornelis Marius Timmers , Hubert Jan Jozef Loozen , Herman Thijs Stock
IPC分类号： C07D471/00 , C07D491/00 , C07D498/00 , C07D513/00 , C07D515/00 , A61K31/00 , A61K31/553 , A61K31/554 , A61K31/55 , A61K31/54 , A61K31/535 , A61K31/44 , A61K31/50
CPC分类号： C07D471/04 , A61K31/397 , A61K31/4439 , A61K31/444 , A61K31/4745 , A61K31/496 , A61K31/55 , A61K45/06 , C07D487/04 , C07D487/14 , C07D498/14 , A61K2300/00
摘要： The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
摘要翻译：本发明涉及根据通式I的环状二氢吡咯并[2,1-a]异喹啉化合物或其药学上可接受的盐。该化合物可用于治疗不育症。

3. 发明授权

US07795280B2 Indoles useful in the treatment of androgen-receptor related diseases 失效
标题翻译：用于治疗雄激素受体相关疾病的吲哚
公开(公告)号：US07795280B2
公开(公告)日：2010-09-14
申请号：US10534945
申请日：2003-11-03
申请人： Pedro Harold Han Hermkens , Herman Thijs Stock , Jaap Van Der Louw , Neeltje Miranda Teerhuis , Johannes Petrus Maria Lommerse
发明人： Pedro Harold Han Hermkens , Herman Thijs Stock , Jaap Van Der Louw , Neeltje Miranda Teerhuis , Johannes Petrus Maria Lommerse
IPC分类号： A61K31/4439 , C07D401/06
CPC分类号： C07D401/06 , C07D209/30 , 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 or a salt or hydrate form thereof.
摘要翻译：本发明提供了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的结构或其盐或水合物形式的非甾体化合物。

4. 发明授权

US08063102B2 Tetrahydronaphthalen-2-ol derivatives 有权
标题翻译：四氢萘-2-醇衍生物
公开(公告)号：US08063102B2
公开(公告)日：2011-11-22
申请号：US12721842
申请日：2010-03-11
申请人： Herman Thijs Stock , Neeltje Miranda Teerhuis , Gerrit Herman Veeneman
发明人： Herman Thijs Stock , Neeltje Miranda Teerhuis , Gerrit Herman Veeneman
IPC分类号： A61K31/277 , A61K31/085 , A61K31/05 , C07C255/50 , C07C43/21 , C07C39/17
CPC分类号： C07C255/54 , A61K31/05 , A61K31/09 , A61K31/222 , A61K31/277 , C07C43/21 , C07C43/225 , C07C43/23 , C07C255/53 , 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。

5. 发明授权

US07812036B2 Androgens 失效
标题翻译：雄激素
公开(公告)号：US07812036B2
公开(公告)日：2010-10-12
申请号：US11587192
申请日：2005-04-21
申请人： Jaap Van Der Louw , Neeltje Miranda Teerhuis , Johannes Petrus Maria Lommerse , Herman Thijs Stock , Pedro Harold Han Hermkens
发明人： Jaap Van Der Louw , Neeltje Miranda Teerhuis , Johannes Petrus Maria Lommerse , Herman Thijs Stock , Pedro Harold Han Hermkens
IPC分类号： A61K31/4439 , C07D401/06
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 each of the substituents is given the definition as set forth in the specification and claims, or a salt or hydrate form thereof.
摘要翻译：本发明的化合物具有根据式I的结构：其中每个取代基被给出如说明书和权利要求中所述的定义，或其盐或水合物形式。

6. 发明申请

US20100240748A1 TETRAHYDRONAPHTHALEN-2-OL DERIVATIVES 有权
标题翻译：四氢萘-2-醛衍生物
公开(公告)号：US20100240748A1
公开(公告)日：2010-09-23
申请号：US12721842
申请日：2010-03-11
申请人： Herman Thijs Stock , Neeltje Miranda Teerhuis , Gerrit Herman Veeneman
发明人： Herman Thijs Stock , Neeltje Miranda Teerhuis , Gerrit Herman Veeneman
IPC分类号： A61K31/277 , C07C43/225 , A61K31/09 , A61P35/00 , A61P19/02 , A61P25/22 , A61P25/24 , A61P13/02 , A61P13/08 , C07C255/54 , C07C69/16 , A61K31/222 , C07C39/17 , A61K31/05
CPC分类号： C07C255/54 , A61K31/05 , A61K31/09 , A61K31/222 , A61K31/277 , C07C43/21 , C07C43/225 , C07C43/23 , C07C255/53 , 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。

7. 发明授权

US09540361B2 N-substituted azetidine derivatives 有权
标题翻译： N-取代的氮杂环丁烷衍生物
公开(公告)号：US09540361B2
公开(公告)日：2017-01-10
申请号：US13995237
申请日：2011-12-16
申请人： Fredericus Antonius Dijcks , Scott James Lusher , Herman Thijs Stock , Arthur Oubrie , Gerrit Herman Veeneman
发明人： Fredericus Antonius Dijcks , Scott James Lusher , Herman Thijs Stock , Arthur Oubrie , Gerrit Herman Veeneman
IPC分类号： C07D417/14 , C07D413/12 , C07D417/12 , C07D413/14 , C07D205/04 , C07D405/12 , C07D409/12 , C07D409/14
CPC分类号： C07D413/14 , C07D205/04 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to novel N-substituted azetidine derivatives to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancer, ovarian cancer, endometriosis, osteoporosis, prostate cancer, benign prostatic hypertrophy, and breast cancer, in particular ER-positive breast cancer, more in particular ER-positive, hormone treatment-resistant breast cancer. Said N-substituted azetidine derivatives have estrogen receptor alpha (ERa) antagonistic and—in certain embodiments—selective estrogen receptor downregulating (SERD) activity in ER-positive breast cancer cells.
摘要翻译：本发明涉及式（I）的新型N-取代氮杂环丁啶衍生物; 其中SERMF是选择性雌激素受体调节剂片段; X是无原子，O，S，CH 2，羰基，N-R 5; R1为H，（C1-8）烷基，（C3-8）环烷基，（C3-6）杂环烷基，（C2-6）烯基，（C2-6）炔基，（C1-4）烷基羰基，（C1-4 ）烷氧基（C 2-4）烷基，（C 3-6）环烷基（C 1-3）烷基，（C 3-6）杂环烷基（C 1-3）烷基，各自独立地被一个或多个卤素，腈，羟基或（C1-2）烷基; R5是H，（C1-3）烷基，任选被一个或多个氟取代; R 17，R 18和R 19彼此独立地为H，氟，腈或（C 1-3） - 烷基，任选被一个或多个氟取代; 或其前体药物，同位素标记的衍生物或其药学上可接受的盐>包含这些化合物的药物组合物及其在治疗中的用途，特别是其用于预防或治疗排卵功能障碍，子宫癌，子宫内膜癌，卵巢癌，子宫内膜异位症，骨质疏松症，前列腺癌，良性前列腺肥大和乳腺癌，特别是ER阳性乳腺癌，更特别是ER阳性，激素治疗抗性乳腺癌。所述N-取代的氮杂环丁烷衍生物在ER阳性乳腺癌细胞中具有雌激素受体α（ERα）拮抗和 - 在某些实施方案中选择性雌激素受体下调（SERD）活性。

8. 发明授权

US08124647B2 Non-steroidal androgens compounds 失效
标题翻译：非甾体雄激素化合物
公开(公告)号：US08124647B2
公开(公告)日：2012-02-28
申请号：US12875295
申请日：2010-09-03
申请人： Pedro Harold Han Hermkens , Herman Thijs Stock , Jaap Van Der Louw , Neeltje Miranda Teerhuis , Johannes Petrus Maria Lommerse
发明人： Pedro Harold Han Hermkens , Herman Thijs Stock , Jaap Van Der Louw , Neeltje Miranda Teerhuis , Johannes Petrus Maria Lommerse
IPC分类号： A61K31/404 , C07D209/30
CPC分类号： C07D401/06 , C07D209/30 , 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 or a salt or hydrate form thereof.
摘要翻译：本发明提供了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的结构或其盐或水合物形式的非甾体化合物。

9. 发明申请

US20110009428A1 NOVEL ANDROGENS 审中-公开
标题翻译：新世界
公开(公告)号：US20110009428A1
公开(公告)日：2011-01-13
申请号：US12887607
申请日：2010-09-22
申请人： Jaap Van Der Louw , Neeltje Miranda Teerhuis , Johannes Petrus Maria Lommerse , Herman Thijs Stock , Pedro Harold Han Hermkens
发明人： Jaap Van Der Louw , Neeltje Miranda Teerhuis , Johannes Petrus Maria Lommerse , Herman Thijs Stock , Pedro Harold Han Hermkens
IPC分类号： A61K31/506 , C07D209/30 , A61K31/4045 , C07D401/02 , A61K31/4439 , C07D403/02 , C07D413/02 , A61K31/422 , A61K31/42 , C07D417/02 , A61K31/427 , A61P19/10
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 SO2; R1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally substituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C-4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO2H, CO2(1C-4C)alkyl, C(O)NR5R6, S(O)(1C-4C)alkyl or S(O)2(1C-4C)alkyl; R2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R3 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; R4 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, CO2(1C-4C)alkyl, C(O)NH2, cyano, nitro, or CH═NOR7, and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; or R4 is 2-pyridyl optionally substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; R5 and R6 are independently hydrogen or (1C-4C)alkyl; R7 is hydrogen or C(O)(1C-4C)alkyl; R8, R9, R10 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; R1为（1C-6C）烷基，（3C-6C）烯基或（3C-6C）炔基，各自任选被（3C-6C）环烷基取代，OH，OC（O）（C 1-4）烷基，C（O）（C 1 -C 4）烷基，CO 2 H，CO 2（1C-4C）烷基，C（O）NR 5 R 6，S（O）（O）2（1C-4C）烷基; R2是氢，（1C-4C）烷基或C（O）（1C-4C）烷基; （1C-4C）烷基，（1C-4C）氟烷基，（1C-4C）烷氧基，（1C-4C）氟烷氧基，卤素，氰基或硝基取代的苯基; 或者R 3是任选被（1C-4C）烷基，（1C-4C）氟烷基，（1C-4C）烷氧基，卤素或氰基取代的5-或6-元芳族杂环结构; R4是在邻位被1-羟基（1C-4C）烷基，（1C-4C）烷氧基，C（O）（1C-4C）烷基，CO 2（1C）取代的苯基或芳香族6-元杂环 -4C）烷基，C（O）NH 2，氰基，硝基或CH = NOOR 7，并任选进一步被（1C-2C）烷基，（1C-2C）氟烷基或卤素取代; 或R 4是任选被（1C-2C）烷基，（1C-2C）氟烷基或卤素取代的2-吡啶基; R5和R6独立地是氢或（1C-4C）烷基; R7是氢或C（O）（1C-4C）烷基; R8，R9，R10独立地为氢，（1C-2C）烷基，氟或氯; 或其盐或水合物形式。

10. 发明申请

US20160130262A1 N-SUBSTITUTED AZETIDINE DERIVATIVES 有权
标题翻译： N-取代的AZETIDINE衍生物
公开(公告)号：US20160130262A1
公开(公告)日：2016-05-12
申请号：US13995237
申请日：2011-12-16
申请人： Fredericus Antonius Dijcks , Scott James Lusher , Herman Thijs Stock , Arthur Oubrie , Gerrit Herman Veeneman
发明人： Fredericus Antonius Dijcks , Scott James Lusher , Herman Thijs Stock , Arthur Oubrie , Gerrit Herman Veeneman
IPC分类号： C07D413/14 , C07D409/14 , C07D413/12 , C07D409/12
CPC分类号： C07D413/14 , C07D205/04 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The present invention relates to novel N-substituted azetidine derivatives to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancer, ovarian cancer, endometriosis, osteoporosis, prostate cancer, benign prostatic hypertrophy, and breast cancer, in particular ER-positive breast cancer, more in particular ER-positive, hormone treatment-resistant breast cancer. Said N-substituted azetidine derivatives have estrogen receptor alpha (ERα) antagonistic and—in certain embodiments—selective estrogen receptor downregulating (SERD) activity in ER-positive breast cancer cells.
摘要翻译：本发明涉及式（I）的新型N-取代氮杂环丁啶衍生物; 其中SERMF是选择性雌激素受体调节剂片段; X是无原子，O，S，CH 2，羰基，N-R 5; R1为H，（C1-8）烷基，（C3-8）环烷基，（C3-6）杂环烷基，（C2-6）烯基，（C2-6）炔基，（C1-4）烷基羰基，（C1-4 ）烷氧基（C 2-4）烷基，（C 3-6）环烷基（C 1-3）烷基，（C 3-6）杂环烷基（C 1-3）烷基，各自独立地被一个或多个卤素，腈，羟基或（C1-2）烷基; R5是H，（C1-3）烷基，任选被一个或多个氟取代; R 17，R 18和R 19彼此独立地为H，氟，腈或（C 1-3） - 烷基，任选被一个或多个氟取代; 或其前体药物，同位素标记的衍生物或其药学上可接受的盐>包含这些化合物的药物组合物及其在治疗中的用途，特别是其用于预防或治疗排卵功能障碍，子宫癌，子宫内膜癌，卵巢癌，子宫内膜异位症，骨质疏松症，前列腺癌，良性前列腺肥大和乳腺癌，特别是ER阳性乳腺癌，更特别是ER阳性，激素治疗抗性乳腺癌。所述N-取代的氮杂环丁烷衍生物在ER阳性乳腺癌细胞中具有雌激素受体α（ERα）拮抗和 - 在某些实施方案中选择性雌激素受体下调（SERD）活性。

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