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1. 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。

2. 发明授权

US6001844A 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：US6001844A
公开(公告)日：1999-12-14
申请号：US029926
申请日：1998-03-11
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 , C07J73/00 , C07D221/02
CPC分类号： C07J73/005 , A61K31/435
摘要： Compounds of structural Formula (I) ##STR1## and pharmacologically acceptable salts and esters thereof possess 5.alpha.-reductase inhibitory activity. These compounds inhibit 5.alpha.-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： PCT No.PCT / US96 / 14564 Sec。 371日期1998年3月11日 102（e）1998年3月11日PCT PCT 1996年9月11日PCT公布。出版物WO97 / 10217 日期1997年3月20日结构式（I）及其药理学上可接受的盐和酯的化合物具有5种α-还原酶抑制活性。这些化合物抑制1型和2型5型α-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病症，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（也称为雄性激素性脱发），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。

3. 发明授权

US06204273B1 16-substituted-4-aza-androstane 5-&agr;-reductase isozyme 1 inhibitors 失效
标题翻译： 16-取代-4-氮杂 - 雄甾烷5-α-还原酶同功酶1抑制剂
公开(公告)号：US06204273B1
公开(公告)日：2001-03-20
申请号：US09240270
申请日：1999-01-29
申请人： Philippe L. Durette , William K. Hagmann , Thomas J. Lanza, Jr. , Soumya P. Sahoo , Gary H. Rasmusson , Richard L. Tolman , Derek Von Langen
发明人： Philippe L. Durette , William K. Hagmann , Thomas J. Lanza, Jr. , Soumya P. Sahoo , Gary H. Rasmusson , Richard L. Tolman , Derek Von Langen
IPC分类号： A61K3144
CPC分类号： C07J73/005
摘要： Compounds of the Formula I are inhibitors of the 5&agr;-reductase 1 isozyme, and are useful alone, or in combination with a 5&agr;-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
摘要翻译： 5α-还原酶1同功酶的式Iare抑制剂的化合物，并且单独使用或与5α-还原酶2抑制剂组合用于治疗雄激素敏感性疾病，例如寻常痤疮，皮脂溢，女性多毛症，男性型秃发，良性前列腺增生。

4. 发明授权

US5910497A 16-pyrazinyl-substituted-4-aza-androstane 5-.alpha.-reductase isozyme 1 inhibitors 失效
标题翻译： 16-吡嗪基 - 取代-4-氮杂 - 雄甾烷-5-α-还原酶同功酶1抑制剂
公开(公告)号：US5910497A
公开(公告)日：1999-06-08
申请号：US991456
申请日：1997-12-16
申请人： Philippe L. Durette , William K. Hagmann , Thomas J. Lanza, Jr. , Soumya P. Sahoo , Gary H. Rasmusson , Richard L. Tolman , Derek Von Langen
发明人： Philippe L. Durette , William K. Hagmann , Thomas J. Lanza, Jr. , Soumya P. Sahoo , Gary H. Rasmusson , Richard L. Tolman , Derek Von Langen
IPC分类号： A61K31/58 , A61P5/24 , A61P17/14 , A61P29/00 , C07J73/00 , A61K31/50
CPC分类号： C07J73/005
摘要： Compounds of the Formula I ##STR1## are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
摘要翻译：式I的化合物是5α-还原酶1同功酶的抑制剂，并且可单独使用或与5α-还原酶2抑制剂组合用于治疗雄激素敏感性疾病，例如寻常痤疮，皮脂溢，雌性多毛症，男性型秃发和良性前列腺增生。

5. 发明授权

US5763361A 17-alkyl-7-substituted-4-aza steroid derivatives as 5-.alpha.-reductase inhibitors 失效
标题翻译： 17-烷基-7-取代-4-氮杂类固醇衍生物作为5-α-还原酶抑制剂
公开(公告)号：US5763361A
公开(公告)日：1998-06-09
申请号：US734705
申请日：1996-10-21
申请人： Georgianna Harris , Richard L. Tolman , Soumya P. Sahoo
发明人： Georgianna Harris , Richard L. Tolman , Soumya P. Sahoo
IPC分类号： C07J73/00 , A61K31/58
CPC分类号： C07J73/005
摘要： The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase, particularly 5.alpha.-reductase type 1. The compounds of formula I are useful in the systemic, including oral, or parenteral or topical treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia which includes female and male pattern baldness, female hirsutism, benign prostafic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as in the treatment of prostatitis. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis are provided, as well as pharmaceutical compositions for the compounds of formula I. The use of compounds of formula I in combination with other, active agents, for example with a 5.alpha.-reductase type 2 inhibitor such as finasteride or epristeride, or a potassium channel opener, such as minoxidil, or a retinoic acid or a derivative thereof is also taught, wherein such combinations would be useful in one or more of the above-mentioned methods of treatment or pharmaceutical compositions.
摘要翻译：本发明的新化合物是结构式I的化合物：其中（I）化合物或其药学上可接受的盐或立体异构体，其为5α-还原酶，特别是5型α-还原酶1型的抑制剂。式I可用于全身，包括口服或肠胃外或局部治疗高雄性性疾病，如寻常痤疮，皮脂溢，雄激素性脱发，包括女性和男性型秃发，女性多毛症，良性前列腺增生，以及预防和治疗前列腺癌，以及前列腺炎的治疗。使用式I化合物治疗高雄激素病症如寻常痤疮，皮脂溢，雄激素性脱发，男性型秃发，女性多毛症，良性前列腺增生以及预防和治疗前列腺癌的方法，以及治疗提供前列腺炎，以及用于式I化合物的药物组合物。式I化合物与其它活性剂，例如5α-还原酶2抑制剂如非那雄胺或艾美他啶的组合或钾通道开放剂如米诺地尔或视黄酸或其衍生物也被教导，其中这些组合可用于一种或多种上述治疗方法或药物组合物。

6. 发明授权

US5719158A 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors 失效
标题翻译： 16-取代-4-氮杂 - 雄甾烷5-α-还原酶同功酶1抑制剂
公开(公告)号：US5719158A
公开(公告)日：1998-02-17
申请号：US463544
申请日：1995-06-05
申请人： Philippe L. Durette , William K. Hagmann , Thomas J. Lanza, Jr. , Soumya P. Sahoo , Gary H. Rasmusson , Richard L. Tolman , Derek von Langen
发明人： Philippe L. Durette , William K. Hagmann , Thomas J. Lanza, Jr. , Soumya P. Sahoo , Gary H. Rasmusson , Richard L. Tolman , Derek von Langen
IPC分类号： A61K31/58 , A61P5/24 , A61P17/14 , A61P29/00 , C07J73/00 , A61K31/47
CPC分类号： C07J73/005
摘要： Compounds of the Formula I ##STR1## are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
摘要翻译：式I化合物I是5α-还原酶1同功酶的抑制剂，并且可单独使用或与5α-还原酶2抑制剂组合用于治疗雄激素敏感性疾病，例如寻常痤疮，皮脂溢，女性多毛症，男性型秃发和良性前列腺增生。

7. 发明授权

US6143887A Process for the stereoselective synthesis of 16-substituted-4-aza-androstanones 失效
标题翻译： 16取代-4-氮杂 - 雄甾烷酮的立体选择性合成方法
公开(公告)号：US6143887A
公开(公告)日：2000-11-07
申请号：US309833
申请日：1999-05-11
申请人： Dominick F. Gratale , Richard L. Tolman , Soumya P. Sahoo
发明人： Dominick F. Gratale , Richard L. Tolman , Soumya P. Sahoo
IPC分类号： C07J73/00 , C07D401/12 , C07D221/18 , C07D241/08 , C07D253/06 , C07D403/12
CPC分类号： C07J73/005
摘要： The novel process of the present invention involves the stereoselective synthesis of certain 16.beta.-substituted 4-aza-5.alpha.-androstan-3-ones and the useful intermediates obtained therein.
摘要翻译：本发明的新方法涉及某些16β-取代的4-氮杂-5α-雄甾烷-3-酮及其中获得的有用的中间体的立体选择性合成。

8. 发明授权

US06200998B1 Arylthiazolidinedione derivitives 失效
标题翻译：芳基噻唑烷二酮衍生物
公开(公告)号：US06200998B1
公开(公告)日：2001-03-13
申请号：US09448847
申请日：1999-11-23
申请人： Soumya P. Sahoo , Wei Han , Richard L. Tolman , Jeffrey Bergman , Conrad Santini , Ranjit Desai , Victoria K. Lombardo , Julia K. Boueres , Dominick F. Gratale
发明人： Soumya P. Sahoo , Wei Han , Richard L. Tolman , Jeffrey Bergman , Conrad Santini , Ranjit Desai , Victoria K. Lombardo , Julia K. Boueres , Dominick F. Gratale
IPC分类号： A01K31425
CPC分类号： C07D263/44 , C07D277/34 , C07D417/12
摘要： Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr;, &dgr; and/or &ggr; mediated diseases, disorders and conditions.
摘要翻译：取代的5-芳基-2,4-噻唑烷二酮是PPAR的有效激动剂，因此可用于治疗，控制或预防糖尿病，高血糖症，高脂血症（包括高胆固醇血症和高甘油三酯血症），动脉粥样硬化，肥胖症，血管再狭窄和其他PPAR α，δ和/或γ介导的疾病，病症和病症。

9. 发明授权

US06090836A Benzisoxazole-derived antidiabetic compounds 失效
标题翻译：苯并恶唑衍生的抗糖尿病化合物
公开(公告)号：US06090836A
公开(公告)日：2000-07-18
申请号：US791211
申请日：1997-01-31
申请人： Alan D. Adams , Joel P. Berger , Gregory D. Berger , Kenneth J. Fitch , Donald W. Graham , Anthony B. Jones , Derek von Langen , Mark D. Leibowitz , David E. Moller , Arthur A. Patchett , Conrad Santini , Soumya P. Sahoo , Richard L. Tolman , Richard B. Toupence , Thomas F. Walsh
发明人： Alan D. Adams , Joel P. Berger , Gregory D. Berger , Kenneth J. Fitch , Donald W. Graham , Anthony B. Jones , Derek von Langen , Mark D. Leibowitz , David E. Moller , Arthur A. Patchett , Conrad Santini , Soumya P. Sahoo , Richard L. Tolman , Richard B. Toupence , Thomas F. Walsh
IPC分类号： A61K31/192 , A61K31/216 , A61K31/235 , A61K45/06 , C07D209/08 , C07D231/56 , C07D239/74 , C07D249/18 , C07D261/20 , C07D263/56 , C07D263/57 , C07D271/08 , C07D275/04 , C07D307/79 , C07D307/82 , C07D307/91 , C07D311/16 , A61K31/42 , A61K31/41 , C07D413/12
CPC分类号： C07D311/16 , A61K31/192 , A61K31/216 , A61K31/235 , A61K45/06 , C07D209/08 , C07D231/56 , C07D239/74 , C07D249/18 , C07D261/20 , C07D263/57 , C07D271/08 , C07D275/04 , C07D307/79 , C07D307/82 , C07D307/91
摘要： The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.
摘要翻译：本发明涉及可用作抗肥胖和抗糖尿病化合物的乙酰苯酚。还公开了用于治疗糖尿病和肥胖以及用于降低或调节甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或用于增加肠运动性或用于治疗动脉粥样硬化的组合物和方法。

10. 发明授权

US6008237A Arylthiazolidinedione derivatives 失效
标题翻译：芳基噻唑烷二酮衍生物
公开(公告)号：US6008237A
公开(公告)日：1999-12-28
申请号：US213542
申请日：1998-12-17
申请人： Soumya P. Sahoo , Richard L. Tolman , Wei Han , Jeffrey Bergman , Conrad Santini , Victoria K. Lombardo , Ranjit Desai , Julia K. Boueres , Dominick F. Gratale
发明人： Soumya P. Sahoo , Richard L. Tolman , Wei Han , Jeffrey Bergman , Conrad Santini , Victoria K. Lombardo , Ranjit Desai , Julia K. Boueres , Dominick F. Gratale
IPC分类号： C07D263/44 , C07D277/34 , C07D417/12 , A61K31/425
CPC分类号： C07D263/44 , C07D277/34 , C07D417/12
摘要： Substituted 5-aryl-2,4-thiazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR .alpha., .delta. and/or .gamma. mediated diseases, disorders and conditions.
摘要翻译：取代的5-芳基-2,4-噻唑烷二酮是PPAR的有效激动剂，因此可用于治疗，控制或预防糖尿病，高血糖症，高脂血症（包括高胆固醇血症和高甘油三酯血症），动脉粥样硬化，肥胖症，血管再狭窄和其他PPAR α，δ和/或γ介导的疾病，病症和病症。

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