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1. 发明授权

US09422324B2 6-substituted demethyl-estradiol derivatives as selective ER-β agonists 有权
标题翻译： 6-取代的脱甲基 - 雌二醇衍生物作为选择性ER-β激动剂
公开(公告)号：US09422324B2
公开(公告)日：2016-08-23
申请号：US14320110
申请日：2014-06-30
申请人： Endece, LLC
发明人： James G. Yarger , Steven H. Nye
IPC分类号： A61K31/56 , C07J1/00 , C07J31/00 , C07J41/00 , C07J17/00 , C07J51/00
CPC分类号： C07J1/007 , A61K31/56 , C07J1/0059 , C07J1/0074 , C07J17/00 , C07J31/006 , C07J41/0016 , C07J41/0044 , C07J51/00
摘要： Disclosed herein are 6-substituted 13-demethyl-estradiol derivatives as selective ERβ agonists. Also disclosed is a method for treating pain by administering these 6-substituted 13-demethyl-estradiol derivatives.
摘要翻译：本文公开了作为选择性ERβ激动剂的6-取代的13-去甲基 - 雌二醇衍生物。还公开了通过施用这些6-取代的13-去甲基 - 雌二醇衍生物来治疗疼痛的方法。

2. 发明申请

US20160068563A1 19-NOR NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF 审中-公开
标题翻译： 19-NOR神经营养甾体及其使用方法
公开(公告)号：US20160068563A1
公开(公告)日：2016-03-10
申请号：US14785162
申请日：2014-04-17
申请人： Boyd L. HARRISON , Albert Jean ROBICHAUD , Francesco g. SALITURO , Richard Thomas BERESIS
发明人： Gabriel Martinez Botella , Boyd L. Harrison , Albert Jean Robichaud , Francesco G. Salituro , Richard Thomas Beresis
IPC分类号： C07J43/00
CPC分类号： C07J43/003 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J21/00 , C07J31/006 , C07J71/001
摘要： Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.
摘要翻译：本文提供了根据式（I）的3,3-二取代的19-去甲甾族化合物及其药物组合物。考虑这样的化合物可用于预防和治疗各种CNS相关病症，例如睡眠障碍，情绪障碍，精神分裂症谱系障碍，记忆障碍和/或认知障碍，运动障碍，人格障碍，自闭症频谱疾病，疼痛，创伤性脑损伤，血管疾病，药物滥用障碍和/或戒断综合征，耳鸣，癫痫持续状态。

3. 发明授权

US06780854B2 Orally active androgens 失效
标题翻译：口服活性雄激素
公开(公告)号：US06780854B2
公开(公告)日：2004-08-24
申请号：US10280038
申请日：2002-10-24
申请人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
发明人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
IPC分类号： A61K3156
CPC分类号： C07J1/0074 , C07J1/007
摘要： Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C,1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
摘要翻译：新型口服活性雄激素为7α-取代的Delta 14-去甲内酯衍生物。化合物满足通式：其中R 1是O，（H，H），（H，OR），NOR，其中R是氢，（C 1-6）烷基或（C 1-6）酰基; 由（C2-4）烷基，（C2-4）烯基或（C2-4）炔基组成的基团，各自任选被卤素取代; 或者R 2是环丙基或环丙烯基，其各自任选地被（C 1-2）烷基或卤素取代; R 3是氢，（C 1-2）烷基或乙烯基; R 4是（C 1-2）烷基; R 5是氢或（ C1-15）酰基;虚线表示任选的键。

4. 发明授权

US06756366B1 Orally active androgens 失效
标题翻译：口服活性雄激素
公开(公告)号：US06756366B1
公开(公告)日：2004-06-29
申请号：US09937274
申请日：2001-09-24
申请人： Jaap van der Louw , Dirk Leysen , Roberta Burma Bursi
发明人： Jaap van der Louw , Dirk Leysen , Roberta Burma Bursi
IPC分类号： A61K3156
CPC分类号： C07J1/007 , C07J1/0074
摘要： Orally Active androgens are derivative of 7&agr;-methyl-19-nortestosterone. The compounds satisfy formula (I) wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl; R2 is selected from the group consisting of (C2-3)alkyl, isopropyl, (C2-3)1-alkenyl, isopropenyl, 1,2-proandienyl, or (C2-3)1-alynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2)alkyl, or halogen; R3 is hydrogen, (C1-2)alkyl, or ethenyl; R4 is (C1-2)alkyl; R5 is hydrogen, or (C1-15)acyl; and the dotted lines indicate optional bonds.
摘要翻译：口服活性雄激素是7α-甲基-19-去睾酮的衍生物。化合物满足式（I）其中R 1为O，（H，H），（H，OR），NOR，其中R为氢，（C 1-6）烷基或（C 1-6）酰基; R2选自（C2-3）烷基，异丙基，（C2-3）-1-链烯基，异丙烯基，1,2-环戊二烯基或（C2-3）-1-亚苄基，各自任选被卤素取代; 或R 2为环丙基或环丙烯基，各自任选被（C 1-2）烷基或卤素取代; R3是氢，（C1-2）烷基或乙烯基; R4是（C1-2）烷基; R5是氢，或（C1-15）酰基; 虚线表示可选的债券。

5. 发明申请

US20040029847A1 8Beta-substituted-11-beta-pentyl-and 11-beta-hexyl-estra-1,3,5(10)-triene derivatives 审中-公开
标题翻译： 8Beta取代的-11β-戊基和11-β-己基 - 雌-1,3,5（10） - 三烯衍生物
公开(公告)号：US20040029847A1
公开(公告)日：2004-02-12
申请号：US10257287
申请日：2003-07-08
发明人： Olaf Peters , Nico Braeuer , Alexander Hillisch , Christa Hegele-Hartung
IPC分类号： A61K031/58 , A61K031/56 , C07J043/00
CPC分类号： C07J1/007 , C07J1/0059 , C07J1/0062 , C07J1/0074 , C07J41/0072
摘要： This invention describes the new 8null-substituted estratrienes of general formula (I), in which R2, R3, R6, R6null, R7, R7null, R14, R15, R15null, R16, R16null, R17, and R17null have the meanings that are indicated in the description, R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl or prop-1-inyl radical, and R11 means an n-pentyl or n-hexyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably exert a preferential contraceptive action on the ovary without stimulating the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for contraception in men as well as the treatment of benign or malignant proliferative diseases of the ovary, such as, e.g., ovarian cancer, or granulosa cell tumors. 1
摘要翻译：本发明描述了通式（I）的新的8-取代的雌三烯，其中R 2，R 3，R 6，R 6'，R 7，R 7'， R 14，R 15，R 15，R 16，R 16'，R 17和R 17'具有在说明书中指出的含义，是指具有至多5个碳原子的直链或支链，任选部分或完全卤代的烷基或烯基，乙炔基或丙-1-茚基，R 11表示正戊基或n - 己基作为具有体外对来自大鼠前列腺的雌激素受体制剂的亲和力高于来自大鼠子宫内体内雌激素受体制剂的活性成分的药物活性成分优选地对卵巢施加优先避孕作用而不刺激子宫，其产生，其治疗用途和含有新化合物的药物分配形式。本发明还描述了这些化合物在男性中用于避孕的用途以及治疗卵巢的良性或恶性增殖性疾病，例如卵巢癌或颗粒细胞瘤。

6. 发明申请

US20030087886A1 Orally active androgens 失效
标题翻译：口服活性雄激素
公开(公告)号：US20030087886A1
公开(公告)日：2003-05-08
申请号：US10280038
申请日：2002-10-24
发明人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
IPC分类号： A61K031/56 , C07J041/00 , C07J001/00
CPC分类号： C07J1/0074 , C07J1/007
摘要： Novel, orally active androgens are 7null-substituted null14-nandrolone derivatives. The compounds satisfy the general formula: 1 wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C,1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
摘要翻译：新型口服活性雄激素为7α-取代的DELTA14-诺酮类衍生物。化合物满足通式：其中R 1为O，（H，H），（H，OR），NOR，R为氢，（C 1-6）烷基或（C 1-6）酰基; R2选自（C2-4）烷基，（C2-4）烯基或（C2-4）炔基，各自任选被卤素取代; 或R 2为环丙基或环丙烯基，各自任选被（C 1-2）烷基或卤素取代; R3是氢，（C1-2）烷基或乙烯基; R4是（C1-2）烷基; R5是氢，或（C1-15）酰基; 虚线表示可选的债券。

7. 发明授权

US06541465B2 Orally active androgens 失效
标题翻译：口服活性雄激素
公开(公告)号：US06541465B2
公开(公告)日：2003-04-01
申请号：US09918626
申请日：2001-07-31
申请人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
发明人： Hubert Jan Jozef Loozen , Dirk Leysen , Jaap van der Louw
IPC分类号： A61K3156
CPC分类号： C07J1/0074 , C07J1/007
摘要： Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
摘要翻译：新型口服活性雄激素为7α-取代的DELTA14-诺酮类衍生物。化合物满足通式：其中R 1为O，（H，H），（H，OR），NOR，R为氢，（C 1-6）烷基或（C 1-6）酰基; R 2选自由（C2-4）烷基，（C2-4）烯基或（C2-4）炔基组成的基团，各自任选被卤素取代; 或者R 2是环丙基或环丙烯基，其各自任选地被（C 1-2）烷基或卤素取代; R 3是氢，（C 1-2）烷基或乙烯基; R 4是（C 1-2）烷基; R 5是氢或（ C1-15）酰基;虚线表示任选的键。

8. 发明授权

US06437158B1 Testosterone derivative 失效
标题翻译：睾酮衍生物
公开(公告)号：US06437158B1
公开(公告)日：2002-08-20
申请号：US09719927
申请日：2000-12-18
申请人： Dirk Leysen D. , Hendrikus Adrianus Antonius Van Der Voort H.A.A
发明人： Dirk Leysen D. , Hendrikus Adrianus Antonius Van Der Voort H.A.A
IPC分类号： C07J100
CPC分类号： C07J1/0074
摘要： The invention is drawn to (7a, 17b)-7-methyl-17-(1-oxoundecyl)oxy-estr-4-en-3-one, (MENT undecanoate), their pharmaceutical formulation and method of use is described. Unexpected results of the said compound compared with testosterone undecanoate is disclosed.
摘要翻译：本发明涉及（7a，17b）-7-甲基-17-（1-氧代十二烷基）氧基-4-烯-3-酮（十一酸十一烷酸酯），描述了它们的药物制剂和使用方法。公开了所述化合物与十一酸睾酮相比的意想不到的结果。

9. 发明授权

US6060503A Benzopyran-containing compounds and method for their use 失效
标题翻译：含苯并吡喃的化合物及其使用方法
公开(公告)号：US6060503A
公开(公告)日：2000-05-09
申请号：US388207
申请日：1995-02-21
申请人： Fernand Labrie , Yves Merand , Sylvain Gauthier
发明人： Fernand Labrie , Yves Merand , Sylvain Gauthier
IPC分类号： C07D405/12 , A61K31/10 , A61K31/135 , A61K31/138 , A61K31/165 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/38 , A61K31/382 , A61K31/40 , A61K31/4025 , A61K31/445 , A61K31/4453 , A61K31/453 , A61K31/4535 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4725 , A61P35/00 , C07C215/64 , C07C217/18 , C07C235/34 , C07C317/18 , C07D215/14 , C07D217/16 , C07D295/092 , C07D295/096 , C07D295/185 , C07D311/60 , C07D335/06 , C07J1/00 , C07J17/00 , C07J21/00 , C07J41/00 , C07J51/00 , C07J53/00 , C07J71/00 , A61K31/44
CPC分类号： A61K31/10 , A61K31/135 , A61K31/138 , A61K31/165 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61K31/40 , A61K31/4025 , A61K31/445 , A61K31/4453 , A61K31/453 , A61K31/4535 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4725 , C07C215/64 , C07C217/18 , C07C235/34 , C07C317/18 , C07D215/14 , C07D217/16 , C07D295/088 , C07D295/096 , C07D295/185 , C07D311/60 , C07D335/06 , C07J1/0055 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J1/0085 , C07J17/00 , C07J21/006 , C07J21/008 , C07J41/0072 , C07J41/0094 , C07J51/00 , C07J53/008 , C07J71/001 , C07J71/0021 , C07C2102/10
摘要： Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailability, and preferred stereoisomers are shown to be more effective than racemic mixtures.
摘要翻译：公开了某些苯并吡喃抗雌激素用于治疗雌激素敏感性疾病如乳腺癌。前药形式提供易于制备，良好的保质期和生物利用度，优选的立体异构体显示出比外消旋混合物更有效。

10. 发明授权

US5840735A Sex steroid activity inhibitors 失效
标题翻译：性类固醇活性抑制剂
公开(公告)号：US5840735A
公开(公告)日：1998-11-24
申请号：US285354
申请日：1994-08-03
申请人： Fernand Labrie , Yves Merand
发明人： Fernand Labrie , Yves Merand
IPC分类号： C07D295/08 , A61K31/10 , A61K31/135 , A61K31/138 , A61K31/165 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61K31/40 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/435 , A61K31/445 , A61K31/4453 , A61K31/452 , A61K31/4523 , A61K31/453 , A61K31/4535 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4725 , A61K31/535 , A61K31/5375 , A61K31/565 , A61K31/57 , A61P5/28 , A61P5/32 , A61P15/16 , A61P17/08 , A61P17/14 , A61P35/00 , C07C215/64 , C07C217/18 , C07C235/34 , C07C235/40 , C07C317/10 , C07C317/18 , C07D209/08 , C07D209/12 , C07D215/06 , C07D215/14 , C07D215/20 , C07D217/04 , C07D217/16 , C07D235/18 , C07D295/084 , C07D295/092 , C07D295/096 , C07D295/185 , C07D311/02 , C07D311/04 , C07D311/60 , C07D335/06 , C07D335/08 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/12 , C07J1/00 , C07J17/00 , C07J21/00 , C07J41/00 , C07J51/00 , C07J53/00 , C07J71/00 , A61K31/44 , A61K31/545 , C07D401/00
CPC分类号： C07D295/185 , A61K31/10 , A61K31/135 , A61K31/138 , A61K31/165 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61K31/40 , A61K31/4025 , A61K31/445 , A61K31/4453 , A61K31/453 , A61K31/4535 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4725 , C07C215/64 , C07C217/18 , C07C235/34 , C07C317/18 , C07D215/14 , C07D217/16 , C07D235/18 , C07D295/088 , C07D295/096 , C07D311/60 , C07D335/06 , C07J1/0011 , C07J1/0022 , C07J1/0025 , C07J1/0055 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J1/0081 , C07J1/0085 , C07J1/0096 , C07J17/00 , C07J21/006 , C07J21/008 , C07J41/0072 , C07J41/0094 , C07J51/00 , C07J53/008 , C07J71/001 , C07J71/0021 , C07C2102/10
摘要： Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
摘要翻译：性类固醇活性的抑制剂，例如具有一般结构的那些，可以用作药物组合物的一部分，以提供抗雌激素作用和/或抑制雌激素合成。这样的药物组合物可用于治疗通过激活性类固醇受体来辅助其进展的乳腺癌或其它疾病。

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