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61. 发明申请

US20130309215A1 PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：药物组合物
公开(公告)号：US20130309215A1
公开(公告)日：2013-11-21
申请号：US13571799
申请日：2012-08-10
申请人： Bernd G. SEIGFRIED
发明人： Bernd G. SEIGFRIED
IPC分类号： A61K47/44 , A61P37/08 , A61P17/00 , A61P25/00 , A61P31/00 , A61K31/49 , A61P31/10 , A61K31/454 , A61K31/405 , A61K31/557 , A61P29/00 , A61P5/26 , A61P5/28 , A61K31/56 , A61P25/08 , A61P7/02 , A61K38/43 , A61K31/7105 , A61K31/711 , A61K31/713 , A61P17/04 , A61P3/10 , A61P31/12 , A61P37/06 , A61P17/12 , A61P17/02 , A61K36/00 , A61P25/18 , A61P25/20 , A61P21/02 , A61P1/08 , A61P33/00 , A61P1/16 , A61P9/00 , A61P11/10 , A61P31/04 , A61P11/14 , A61P11/06 , A61P7/10 , A61P37/02 , A61K31/196 , A61K31/192 , A61P25/16 , A61P3/02 , A61P23/02
CPC分类号： A61K31/196 , A61K9/0014 , A61K31/192 , A61K36/28 , A61K36/48 , A61K36/899 , A61K38/00 , A61K47/10 , A61K47/24 , A61K47/44 , A61K2300/00
摘要： A pharmaceutical composition for application in human and animals, with at least one systemically and/or locally acting, topically applicable active ingredient and with at least one phospholipid, improving the transport of the active ingredient trough the cell membrane and containing a concentration of at least 60% by weight phosphatidylcholine, referring to the phospholipid, is described. The composition shows such a liquid consistency, that it is able to be sprayed as droplets or as a foam, whereas in the composition such a phospholipid is included, that additionally contains oil in a concentration of maximum 7.5% by weight besides the at least 60% by weight phosphatidylcholine.
摘要翻译：一种用于人和动物的药物组合物，其具有至少一种全身和/或局部作用的局部应用的活性成分和至少一种磷脂，其改善了活性成分在细胞膜的运输并且至少含有至少涉及磷脂的60重量％磷脂酰胆碱被描述。该组合物显示出这样的液体稠度，其能够以小滴或泡沫形式喷雾，而在组合物中包含这样的磷脂，除了至少60重量份之外，还含有浓度最大为7.5重量％的油重量百分比的磷脂酰胆碱。

62. 发明申请

US20120309800A1 METALLOENZYME INHIBITOR COMPOUNDS 有权
公开(公告)号：US20120309800A1
公开(公告)日：2012-12-06
申请号：US13519801
申请日：2010-12-29
申请人： William J. Hoekstra , Robert J. Schotzinger , Stephen W. Rafferty
发明人： William J. Hoekstra , Robert J. Schotzinger , Stephen W. Rafferty
IPC分类号： A61K31/41 , A61P35/00 , A61P9/00 , A61P29/00 , A61P25/00 , A61P13/00 , A61P1/00 , A61P5/00 , A61P5/28 , A61P17/00 , A61P17/14 , A61P5/32 , A61P15/00 , A61P17/10 , A61P17/06 , A61P31/10 , C07D257/04
CPC分类号： C07D257/04 , A61K31/165 , A61K31/41 , A61K31/415 , A61K31/4196 , A61K45/06 , A61K2300/00
摘要： The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

63. 发明申请

US20120283225A1 Combination Therapy for Skin Disorders 有权
标题翻译：皮肤疾病组合治疗
公开(公告)号：US20120283225A1
公开(公告)日：2012-11-08
申请号：US13518818
申请日：2011-04-11
申请人： Howard Fein , Mindy B. Berlin
发明人： Howard Fein , Mindy B. Berlin
IPC分类号： A61K31/353 , A61P5/28 , A61P31/00 , A61K31/65 , A61P17/00
CPC分类号： A61K31/65 , A61K9/0014 , A61K9/0053 , A61K9/127 , A61K9/48 , A61K9/7023 , A61K31/135 , A61K31/353 , A61K31/496 , A61K31/565 , A61K45/06 , A61K2300/00
摘要： The present invention provides a novel therapeutic combination comprising one or more anti-androgen agents and one or more antibiotic/anti-inflammatory agents or pharmaceutically acceptable salts or hydrates thereof, useful for the treatment of a dermatological disorder.
摘要翻译：本发明提供了一种新颖的治疗组合，其包含一种或多种抗雄激素剂和一种或多种可用于治疗皮肤病的抗生素/抗炎剂或其药学上可接受的盐或水合物。

64. 发明申请

US20120178678A1 DERIVATIVES OF 2H PYRIDAZIN- 3 -ONES, THEIR PREPARATION AND THEIR USE AS SCD-1 INHIBITORS 有权
标题翻译： 2H吡啶-3-酮的衍生物，其制备及其作为SCD-1抑制剂的用途
公开(公告)号：US20120178678A1
公开(公告)日：2012-07-12
申请号：US13388884
申请日：2010-08-05
申请人： Elisabeth Dupont-Passelaigue , Samuel Mialhe , Jean-Pierre Rieu , Didier Junquero , Karine Valeille
发明人： Elisabeth Dupont-Passelaigue , Samuel Mialhe , Jean-Pierre Rieu , Didier Junquero , Karine Valeille
IPC分类号： A61K31/501 , C07D403/12 , C07D401/06 , A61P3/04 , A61P3/10 , A61P3/06 , A61P3/00 , A61P9/10 , A61P1/16 , A61P9/00 , A61P35/00 , A61P17/00 , A61P17/10 , A61P17/06 , A61P17/08 , A61K38/28 , A61K38/26 , A61K31/513 , A61K38/22 , A61P31/04 , A61P5/28 , A61P35/02 , C12N9/99 , C07D401/12
CPC分类号： C07D237/22 , C07D401/12 , C07D403/12
摘要： The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: —R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, —when n=m=1, W represents CH then Y represents oxygen, —U represents: either —(C═O)CH2NH— and is branched at position 4 of pyridazinone, then R2 represents H, or —(C═O)NH— and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, —R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders.
摘要翻译：本发明涉及通式（I）的化合物，其特征在于（式1）其中特别地：-R 1表示一个或多个基团，例如三氟甲基，卤素如F，Cl， - 当n = m = 1时， W表示CH，Y表示氧，-U表示： - （C = O）CH 2 NH-，并且在哒嗪酮的4位具有支链，则R2表示H或 - （C = O）NH-，U在（4），（5）或（6），则R2表示H，-R3表示氢或甲基，加成盐与药学上可接受的碱和酸和不同的异构体，以及它们的混合物以任何比例用作用于治疗肥胖症，2型糖尿病和脂质疾病的SCD-1酶抑制剂。

65. 发明申请

US20120129773A1 METHODS OF TREATING AUTISM AND AUTISM SPECTRUM DISORDERS 审中-公开
标题翻译：治疗原发性和异常性疾病的方法
公开(公告)号：US20120129773A1
公开(公告)日：2012-05-24
申请号：US13338008
申请日：2011-12-27
申请人： Mark R. GEIER , David A. GEIER
发明人： Mark R. GEIER , David A. GEIER
IPC分类号： A61K38/09 , A61P15/00 , A61P5/30 , A61P25/00 , A61P5/28
CPC分类号： A61K38/02 , G01N2333/59 , G01N2800/28 , G01N2800/38
摘要： The present invention relates to methods of treating a subject diagnosed with autism or an autism spectrum disorder, lowering the level of mercury in a subject determined to contain a high level of mercury, methods of lowering the level of mercury in a child diagnosed with autism, lowering the level of at least one androgen in a subject diagnosed with autism, lowering the level of mercury and the level of at least one androgen in a subject diagnosed with autism and methods of assessing the risk of whether a child is susceptible of developing autism.
摘要翻译：本发明涉及治疗患有自闭症或自闭症谱系障碍的受试者，降低被测定为含有高水平汞的受试者的汞水平的方法，降低诊断为自闭症的儿童中的汞水平的方法，降低诊断为自闭症的受试者中至少一种雄激素的水平，降低汞诊断患儿的汞水平和至少一种雄激素水平，以及评估儿童是否容易发展自闭症的风险的方法。

66. 发明申请

US20110223214A1 USE OF CARBOXYMETHYLCELLULOSE TO CONTROL EJECTABILITY AND SOLIDIFICATION TIME OF COMPOSITIONS COMPRISING ONE OR MORE BIORESORBABLE CERAMICS 有权
标题翻译：使用羧甲基纤维素来控制包含一种或多种可生物陶瓷的组合物的可回收性和固化时间
公开(公告)号：US20110223214A1
公开(公告)日：2011-09-15
申请号：US13127331
申请日：2009-11-27
申请人： Lars Åke Malmsten , Niklas Axén , Hans Lennernäs , Anders Carlsson
发明人： Lars Åke Malmsten , Niklas Axén , Hans Lennernäs , Anders Carlsson
IPC分类号： A61K9/14 , A61K31/167 , A61K31/57 , A61K31/277 , A61P35/00 , A61P29/00 , A61P5/28
CPC分类号： A61K31/167 , A61K9/0019 , A61K31/57 , A61K47/02 , A61K47/38 , A61L27/446 , A61L27/58 , A61L2400/06 , C08L1/28
摘要： Carboxymethylcellulose, notably sodium carboxymethylcellulose or other alkali metal or alkaline earth metal salts of carboxymethylcellulose, are employed to control solidification time of compositions comprising one or more bioresorbable ceramics, notably a hydratable calcium sulphate, in order to facilitate preparation of a ready-to-use composition for inserting into the body by injection.
摘要翻译：使用羧甲基纤维素，特别是羧甲基纤维素钠或羧甲基纤维素的其它碱金属或碱土金属盐来控制包含一种或多种生物可再吸收陶瓷，特别是可水合硫酸钙的组合物的固化时间，以便于制备即用型用于通过注射插入体内的组合物。

67. 发明申请

US20100292201A1 NOVEL STEROIDAL ESTERS OF 17-OXIMINO-5-ANDROSTEN-3BETA-OL 有权
标题翻译： 17-OXIMINO-5-ANDROSTEN-3BETA-OL的新型甾体酯
公开(公告)号：US20100292201A1
公开(公告)日：2010-11-18
申请号：US12733415
申请日：2008-08-14
申请人： Tilak Raj Bhardwaj , Manoj Kumar , Neelima Dhingra , Neeraj Mehta
发明人： Tilak Raj Bhardwaj , Manoj Kumar , Neelima Dhingra , Neeraj Mehta
IPC分类号： A61K31/568 , C07J41/00 , A61P5/28 , A61P13/08
CPC分类号： C07J41/0016
摘要： The present invention relates to steroidal esters of 17-oximino-5-androsten-3-ol, of compound of general formula (A) wherein R is selected from a group consisting of arylalkyl, aryl, substituted aryl. The ester derivatives are synthesized starting from Dehydroandrosterone acetate. The compounds were tested for their antiproliferative activity and 5α-reductase inhibitory activity in comparison to Finasteride. Decreased androgen level have been found in serum of animal treated with newly synthesized compounds. These compounds have also shown better cytotoxicity in comparison to reference drug Finasteride. Thus such compounds can be useful in treatment of androgen dependent disorder of prostate alone or by synergistic effect they can decrease the size of prostate due to their antiproliferative activity.
摘要翻译：本发明涉及通式（A）化合物，其中R选自芳烷基，芳基，取代芳基的17-肟基-5-雄甾-3-醇类甾体酯。酯衍生物是从乙酸脱氢睾酮开始合成的。与非那雄胺相比，测试了这些化合物的抗增殖活性和5α-还原酶抑制活性。在新合成的化合物处理的动物血清中发现雄激素水平降低。与参考药物非那雄胺相比，这些化合物也显示出更好的细胞毒性。因此，这样的化合物可用于治疗前列腺单独的雄激素依赖性病症或通过协同作用，由于它们的抗增殖活性，它们可以减少前列腺的大小。

68. 再颁专利

USRE39056E1 4-Azasteroids for treatment of hyperandrogenic conditions 失效
标题翻译： 4-Azasteroids用于治疗雄激素过多的病症
公开(公告)号：USRE39056E1
公开(公告)日：2006-04-04
申请号：US10020740
申请日：1996-09-11
申请人： Raman K. Bakshi , Soumya P. Sahoo , Richard L. Tolman
发明人： Raman K. Bakshi , Soumya P. Sahoo , Richard L. Tolman
IPC分类号： A61K31/435 , A61K31/44 , A61P5/28 , C07D221/02 , C07D221/18
CPC分类号： C07J73/005 , A61K31/435
摘要： Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.
摘要翻译：结构式（I）的化合物及其药理学上可接受的盐和酯具有5α-还原酶抑制活性。这些化合物抑制1型和2型5α-还原酶。结构式I的化合物可用于全身，包括口服和肠胃外，包括局部治疗和预防高雄激素症状，包括前列腺癌，良性前列腺增生症，寻常痤疮，皮脂溢，雄激素性脱发（也称雄激素性脱发），包括男性和女性型秃发，女性多毛症和前列腺炎。一类本发明的化合物也是有效的抗雄激素。本发明还涉及含有这些化合物的新型组合物，其用途及其制备方法。

69. 发明申请

US20050261303A1 N-phenyl-(2r,5s) dimethylpiperadine derivative 有权
标题翻译： N-苯基 - （2r，5s）二甲基哌啶衍生物
公开(公告)号：US20050261303A1
公开(公告)日：2005-11-24
申请号：US10521119
申请日：2003-07-11
申请人： Nobuaki Taniguchi , Masakazu Imamura , Masahiko Hayakawa , Kenichi Kawaguchi , Takenori Kimura , Isao Kinoyama , Hiroyuki Kaizawa , Minoru Okada , Takashi Furutani
发明人： Nobuaki Taniguchi , Masakazu Imamura , Masahiko Hayakawa , Kenichi Kawaguchi , Takenori Kimura , Isao Kinoyama , Hiroyuki Kaizawa , Minoru Okada , Takashi Furutani
IPC分类号： A61P5/28 , A61P13/08 , A61P17/08 , A61P17/14 , A61P35/00 , C07D213/75 , C07D213/84 , C07D239/42 , C07D295/215 , A61K31/496 , A61K31/506 , C07D43/02
CPC分类号： C07D213/75 , C07D213/84 , C07D239/42 , C07D295/215
摘要： The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.
摘要翻译：本发明涉及用作抗雄激素剂的新型N-苯基 - （2R，5S）二甲基哌嗪衍生物，其与常规化合物相比表现出足够的前列腺减少效果，口服活性优异。本申请的化合物可用于预防或治疗前列腺癌，良性前列腺增生等。本发明还提供了可用于制备本发明化合物的新型中间体。

70. 发明申请

US20050256048A1 Selective androgen receptor modulators and methods for their identification, design and use 审中-公开
标题翻译：选择性雄激素受体调节剂及其鉴定，设计和使用方法
公开(公告)号：US20050256048A1
公开(公告)日：2005-11-17
申请号：US11130935
申请日：2005-05-17
申请人： Mark Salvati , Marco Gottardis , Ricardo Attar , Stanley Krystek , John Sack
发明人： Mark Salvati , Marco Gottardis , Ricardo Attar , Stanley Krystek , John Sack
IPC分类号： G01N33/483 , A61K31/00 , A61K31/407 , A61K31/4155 , A61K31/416 , A61K31/4196 , A61K31/42 , A61K31/433 , A61K31/4439 , A61K31/4709 , A61K31/4995 , A61K31/506 , A61K31/655 , A61K31/675 , A61K45/00 , A61P5/28 , A61P13/08 , A61P35/00 , C07D471/18 , C07D487/08 , C07D487/18 , C07D491/08 , C07D491/18 , C07D491/22 , C07D493/18 , C07D495/18 , C07D519/00 , C07K14/72 , C12Q1/02 , G01N33/15 , G01N33/50 , G01N33/53 , A61K38/17 , A61K31/56 , G01N33/48 , G06F19/00
CPC分类号： C07D487/08 , A61K31/00 , A61K31/407 , A61K31/655 , A61K31/675 , A61K2300/00
摘要： Selective androgen receptor modulators (SARMs) having antagonist activity in hormone-dependent tumors while exhibiting no activity or agonist activity against other nontumor tissues containing the androgen receptor as well as methods for identifying, designing and using SARMs are provided.
摘要翻译：提供了在激素依赖性肿瘤中具有拮抗剂活性的选择性雄激素受体调节剂（SARM），同时对包含雄激素受体的其它非肿瘤组织没有活性或激动剂活性以及鉴定，设计和使用SARMs的方法。

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