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1. 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。

2. 发明申请

US20110028450A1 Ring-annulated dihydropyrrolo[2,1-alpha]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：US20110028450A1
公开(公告)日：2011-02-03
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： A61K31/397 , C07D471/04 , A61K31/4745 , C07D487/04 , A61K31/55 , C07D498/14 , A61K31/444 , A61K31/4439 , C07D487/14 , A61K31/496 , A61P15/08
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

US08071589B2 Dihydrobenzoindazoles 有权
标题翻译：二氢苯并吲唑
公开(公告)号：US08071589B2
公开(公告)日：2011-12-06
申请号：US12845813
申请日：2010-07-29
申请人： Cornelis Marius Timmers , Hubert Jan Jozef Loozen
发明人： Cornelis Marius Timmers , Hubert Jan Jozef Loozen
IPC分类号： C07D243/00 , C07D487/00 , A61K31/55 , A61K31/415 , A61P5/06
CPC分类号： C07D231/54 , A61K31/416 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D401/04 , C07D403/06 , C07D403/12 , C07D409/04 , C07D409/14 , C07D413/02 , C07D413/12 , C07D417/04 , A61K2300/00
摘要： The invention relates to benzoindazole derivatives 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：本发明涉及通式I的苯并吲唑衍生物或其药学上可接受的盐。该化合物可用于治疗不育症。

4. 发明申请

US20110028451A1 Dihydrobenzoindazoles 有权
公开(公告)号：US20110028451A1
公开(公告)日：2011-02-03
申请号：US12845813
申请日：2010-07-29
申请人： Cornelis Marius Timmers , Hubert Jan Jozef Loozen
发明人： Cornelis Marius Timmers , Hubert Jan Jozef Loozen
IPC分类号： A61K31/5377 , C07D403/06 , C07D231/54 , C07D409/14 , C07D409/04 , C07D417/04 , C07D401/04 , C07D413/02 , C07D413/12 , C07D403/12 , A61K31/551 , A61K31/416 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/422 , A61K31/496 , A61P15/08
CPC分类号： C07D231/54 , A61K31/416 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D401/04 , C07D403/06 , C07D403/12 , C07D409/04 , C07D409/14 , C07D413/02 , C07D413/12 , C07D417/04 , A61K2300/00
摘要： The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.

5. 发明授权

US07868193B2 16,17-carbocyclic condensed steroid compounds having selective estrogenic activity 有权
标题翻译：具有选择性雌激素活性的16,17-碳环缩合类固醇化合物
公开(公告)号：US07868193B2
公开(公告)日：2011-01-11
申请号：US10297706
申请日：2001-05-01
申请人： Hubert Jan Jozef Loozen
发明人： Hubert Jan Jozef Loozen
IPC分类号： C07J1/00 , A61K31/56
CPC分类号： C07J53/002
摘要： The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; R6 is H, ═CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1-3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being α and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.
摘要翻译：本发明公开了具有式（1）的类固醇化合物，其中虚线键代表任选的双键; R6是H，= CH2或-CH3，或-CH2-CH3; R 7是H，C 1-4 - 烷基，C 2-5烯基或C 2-5炔基，其中烷基，烯基或炔基可以被独立地选自氟或氯原子的1至3个卤素原子取代; R 11为H，C 1-4 - 烷基，C 2-4 - 烯基，C 2-4 - 炔基或C 1-4亚烷基，其中烷基，烯基，炔基或亚烷基可以被1-3个独立地选自该组氟或氯原子; E与类固醇骨架的碳原子16和17一起为4至7元环，所述环为α并且相对于类固醇骨架为顺式构型，任选包含一个或两个内环键; 或其前药。这些化合物可用于治疗和选择性修饰雌激素受体活性的方法。

6. 发明授权

US07838516B2 15 β-substituted steroids having selective estrogenic activity 有权
标题翻译：具有选择性雌激素活性的15和bgr-取代的类固醇
公开(公告)号：US07838516B2
公开(公告)日：2010-11-23
申请号：US11662166
申请日：2005-09-05
申请人： Hubert Jan Jozef Loozen , Antonius Gerardus Hendrikus Ederveen , Fredericus Antonius Dijcks
发明人： Hubert Jan Jozef Loozen , Antonius Gerardus Hendrikus Ederveen , Fredericus Antonius Dijcks
IPC分类号： A61K31/565 , C07J1/00
CPC分类号： A61K31/56 , C07J1/00
摘要： The invention provides 15β-substituted steroidal compounds having selective estrogen receptor activity according to Formula I: wherein, R1 is H, C1-5 alkyl, C1-12 acyl, di-(C1-5 alkyl)aminocarbonyl, (C1-5alkyl)oxycarbonyl or sulfamoyl, R2 is H, C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl, each of which may be optionally substituted with a halogen, R3 is C1-2 alkyl, ethenyl or ethynyl, each of which may be optionally substituted with a halogen, and R4 is H or C1-12 acyl.
摘要翻译：本发明提供了具有根据式I的选择性雌激素受体活性的15-取代的甾族化合物：其中R1是H，C1-5烷基，C1-12酰基，二（C1-5烷基）氨基羰基，（C1-5烷基）氧羰基或氨磺酰基，R 2是H，C 1-3烷基，C 2-3烯基或C 2-3炔基，其各自可以任选被卤素取代，R 3是C 1-2烷基，乙烯基或乙炔基，其各自可以是任选被卤素取代，R 4是H或C 1-12酰基。

7. 发明授权

US07528123B1 Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11 失效
标题翻译：雌激素雌-1,3,5（10） - 三烯对α和β雌激素受体具有差异作用，具有位置11的5-9个碳原子的直链烃链
公开(公告)号：US07528123B1
公开(公告)日：2009-05-05
申请号：US09831954
申请日：1999-11-18
申请人： Hubert Jan Jozef Loozen , Wilhelmus Gerardus Eduardus Joseph Schoonen
发明人： Hubert Jan Jozef Loozen , Wilhelmus Gerardus Eduardus Joseph Schoonen
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J1/007 , C07J1/0059
摘要： Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11β-substitution. Said substitution is a hydrocarbon group which may be linear or branched, provided that it comprises, as the longest chain on carbon atom no. 11 of the steroid skeleton, one single linear chain having a length of from 5 to 9 carbon atoms, wherein said chain may be saturated or unsaturated. The resulting compounds have a desirable mixed agonist/antagonist profile for estrogen receptor α and estrogen receptor β.
摘要翻译：公开了一种基于雌二醇的新一类类固醇化合物，并具有11b取代基。所述取代是可以是直链或支链的烃基，条件是它包含作为碳原子上最长的链。 11的类固醇骨架，长度为5至9个碳原子的单个直链，其中所述链可以是饱和或不饱和的。所得化合物对于雌激素受体α和雌激素受体β具有期望的混合激动剂/拮抗剂特征。

8. 发明授权

US6037339A C-11 substituted steroids for treating menopausal complaints 失效
标题翻译： C-11替代类固醇用于治疗绝经期的投诉
公开(公告)号：US6037339A
公开(公告)日：2000-03-14
申请号：US8178
申请日：1998-01-16
申请人： Hubert Jan Jozef Loozen , Lodewijk Pieter Cornelis Schot , Jane Margretha Lena van der Werf-Pieters
发明人： Hubert Jan Jozef Loozen , Lodewijk Pieter Cornelis Schot , Jane Margretha Lena van der Werf-Pieters
IPC分类号： A61K31/565 , C07J1/00 , C07J11/00 , C07J21/00 , C07J33/00 , C07J41/00 , C07J51/00 , A61K31/56
CPC分类号： C07J33/007 , A61K31/565 , C07J1/0096 , C07J11/00 , C07J21/008 , C07J41/0044 , C07J41/0094 , C07J51/00
摘要： A C-11 substituted steroid and a method of use of a C-11 substituted steroid to treat osteoporosis.
摘要翻译： C-11替代的类固醇和使用C-11取代的类固醇治疗骨质疏松症的方法。

9. 发明申请

US20110224183A1 16, 17-CARBOCYCLIC CONDENSED STEROID COMPOUNDS HAVING SLECTIVE ESTROGENIC ACTIVITY 审中-公开
标题翻译：具有选择性雌激素活性的16,17-碳环稠合的甾族化合物
公开(公告)号：US20110224183A1
公开(公告)日：2011-09-15
申请号：US13112184
申请日：2011-05-20
申请人： Hubert Jan Jozef Loozen
发明人： Hubert Jan Jozef Loozen
IPC分类号： A61K31/567 , C07J53/00 , A61P15/18 , A61P19/10 , A61P5/30 , A61P35/00 , C12N5/00
CPC分类号： C07J53/002
摘要： The invention discloses a steroid compound having the formula (1): wherein dotted bonds represent optional double bonds; R6 is H, ═CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, Cl1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being α and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.
摘要翻译：本发明公开了具有式（1）的类固醇化合物：其中虚线键代表任选的双键; R6是H，= CH2或-CH3，或-CH2-CH3; R 7是H，C 1-4 - 烷基，C 2-5烯基或C 2-5炔基，其中烷基，烯基或炔基可以被独立地选自氟或氯原子的1至3个卤素原子取代; R 11是H，C 1-4 - 烷基，C 2-4 - 烯基，C 2-4 - 炔基或C 1-4 - 亚烷基，其中烷基，烯基，炔基或亚烷基可以被1至3个独立地选自该组氟或氯原子; E与类固醇骨架的碳原子16和17一起为4至7元环，所述环为α并且相对于类固醇骨架为顺式构型，任选包含一个或两个内环键; 或其前药。这些化合物可用于治疗和选择性修饰雌激素受体活性的方法。

10. 发明申请

US20100324021A1 (DIHYDRO)IMIDAZOISO[5,1-A]QUINOLINES 有权
标题翻译：（DIHYDRO）咪唑并[5,1-A]喹啉
公开(公告)号：US20100324021A1
公开(公告)日：2010-12-23
申请号：US12786996
申请日：2010-05-25
申请人： Hubert Jan Jozef Loozen , Cornelius Marius Timmers
发明人： Hubert Jan Jozef Loozen , Cornelius Marius Timmers
IPC分类号： A61K31/4745 , C07D471/04 , A61K31/5377 , A61K31/496 , A61K31/553 , A61K31/551 , A61P15/08
CPC分类号： C07D471/04
摘要： The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives 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的咪唑并[5,1-a]喹啉和5,6-二氢 - 咪唑并[5,1-a]喹啉衍生物或其药学上可接受的盐。该化合物可用于治疗不育症。

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