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1. 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。

2. 发明授权

US08367648B2 Substituted 16,17-annellated steroid compounds for use in womens healthcare 有权
标题翻译：取代16,17-环状类固醇化合物，用于妇女保健
公开(公告)号：US08367648B2
公开(公告)日：2013-02-05
申请号：US12795970
申请日：2010-06-08
申请人： Fredericus Antonius Dijcks , Hubert Jan Jozef Loozen , Samira Addo , Antonius Gerardus Hendrikus Ederveen
发明人： Fredericus Antonius Dijcks , Hubert Jan Jozef Loozen , Samira Addo , Antonius Gerardus Hendrikus Ederveen
IPC分类号： A61K31/56 , C07J53/00
CPC分类号： C07J53/00 , C07J53/002
摘要： The present invention relates to substituted steroid compounds having the formula Wherein R1 is H or halogen; R2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R3 is H or halogen; R4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R5 is methyl or ethyl; R6 is H or methyl; R7 is H or methyl; R8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.
摘要翻译：本发明涉及具有下式的取代的类固醇化合物：其中R1是H或卤素; R2是H，（1C-4C）烷基，（1C-4C）酰基，葡糖醛酸或氨磺酰基; R3是H或卤素; R4是H，（1C-4C）烷基，（2C-4C）烯基或（2C-4C）炔基; R5是甲基或乙基; R6是H或甲基; R7是H或甲基; R8是H或酰基，用于治疗和预防子宫内膜异位，避孕，绝经期和绝经后妇女的激素治疗，治疗骨质疏松症和治疗子宫肌瘤和其他月经相关疾病，如功能障碍崩漏。

3. 发明申请

US20100331292A1 SUBSTITUTED 16,17-ANNELLATED STERIOD COMPOUNDS FOR USE IN WOMENS HEALTHCARE 有权
标题翻译：用于妇女健康服用的16,17-ANNELLATED STERIOD化合物
公开(公告)号：US20100331292A1
公开(公告)日：2010-12-30
申请号：US12795970
申请日：2010-06-08
申请人： Fredericus Antonius Dijcks , Hubert Jan Jozef Loozen , Samira Addo , Antonius Gerardus Hendrikus Ederveen
发明人： Fredericus Antonius Dijcks , Hubert Jan Jozef Loozen , Samira Addo , Antonius Gerardus Hendrikus Ederveen
IPC分类号： A61K31/567 , C07J53/00 , A61P15/18 , A61P15/00
CPC分类号： C07J53/00 , C07J53/002
摘要： The present invention relates to substituted steroid compounds having the formula Wherein R1 is H or halogen; R2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R3 is H or halogen; R4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R5 is methyl or ethyl; R6 is H or methyl; R7 is H or methyl; R8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.
摘要翻译：本发明涉及具有下式的取代的类固醇化合物：其中R1是H或卤素; R2是H，（1C-4C）烷基，（1C-4C）酰基，葡糖醛酸或氨磺酰基; R3是H或卤素; R4是H，（1C-4C）烷基，（2C-4C）烯基或（2C-4C）炔基; R5是甲基或乙基; R6是H或甲基; R7是H或甲基; R8是H或酰基，用于治疗和预防子宫内膜异位，避孕，绝经期和绝经后妇女的激素治疗，治疗骨质疏松症和治疗子宫肌瘤和其他月经相关疾病，如功能障碍崩漏。

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明授权

US07696190B2 16Alpha-methyl or ethyl substituted estrogens 失效
标题翻译： 16α-甲基或乙基取代的雌激素
公开(公告)号：US07696190B2
公开(公告)日：2010-04-13
申请号：US10343293
申请日：2001-07-23
申请人： Jordi Mestres , Hubert Jan Jozef Loozen , Gerrit Herman Veeneman
发明人： Jordi Mestres , Hubert Jan Jozef Loozen , Gerrit Herman Veeneman
IPC分类号： A61K31/56 , C07J1/00 , C07J7/00
CPC分类号： C07J1/0096 , C07J51/00 , C07J71/001
摘要： The invention makes a 16α-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a Δ5-10 double bond; R1 is (C1-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R2 is (C1-C4;)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor α selective treatment
摘要翻译：本发明制备了具有式1的16α-取代的甾族化合物，其中虚线环是完全饱和的，完全芳族的或具有＆Dgr; 5-10双键的饱和环; R1是（C1-C3）烷基或（C2-C3）烯基，这些基团可以被一个或多个卤素取代; R2是（C1-C4）烷基，（C2-C4）烯基或亚甲基，这些基团中的每一个可被一个或多个卤素取代; R3是甲基或乙基; 或其前药，该化合物可用于雌激素受体α选择性治疗

10. 发明授权

US06881728B1 14-β, 17-α-hydroxymethylandrostane derivatives as androgens 有权
标题翻译： 14-β，17-α-羟甲基雄甾烷衍生物作为雄激素
公开(公告)号：US06881728B1
公开(公告)日：2005-04-19
申请号：US09890845
申请日：2000-03-02
申请人： Hubert Jan Jozef Loozen , Dirk D. Leysen , Jaap van der Louw
发明人： Hubert Jan Jozef Loozen , Dirk D. Leysen , Jaap van der Louw
IPC分类号： A61K31/568 , A61K31/565 , A61K31/57 , A61P5/26 , A61P15/16 , C07J3/00 , C07J5/00 , C07J15/00 , C07J53/00 , A61K31/56 , C07J1/00
CPC分类号： C07J15/00
摘要： Androgenic steroids having a (14β,17α-)-17-(hydroxymetheyl) configuration, useful for the preparation of male contraceptives and pharmaceutical formulations for the treatment of androgen insufficiency.
摘要翻译：具有（14beta，17α - ） - 17-（羟甲基）构型的雄激素类固醇可用于制备男性避孕药和用于治疗雄激素不全的药物制剂。

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