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1. 发明申请

US20160250188A1 METHODS FOR TREATMENT OF MUSCULAR DYSTROPHIES 审中-公开
标题翻译：用于治疗肌肉性状的方法
公开(公告)号：US20160250188A1
公开(公告)日：2016-09-01
申请号：US15031139
申请日：2014-10-24
申请人： Ernest D. Bush , Francois Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanque , Jean-Michel Lefrancois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Burt Paul Wigerinck
发明人： Ernest D. Bush , Francois Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanque , Jean-Michel Lefrancois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Burt Paul Wigerinck
IPC分类号： A61K31/4166 , A61K9/00
CPC分类号： A61K31/4166 , A61K9/0053
摘要： The present invention relates to, inter alia, treatment of muscle dystrophy (e.g., Duchenne Muscular Dystrophy), for example, using a composition, e.g., a composition comprising Compound (I), or a pharmaceutically acceptable salt, prodrug or metabolite thereof.
摘要翻译：本发明尤其涉及治疗肌营养不良症（例如，Duchenne Muscular Dystrophy），例如，使用组合物，例如包含化合物（I）的组合物或其药学上可接受的盐，前药或代谢物。

2. 发明申请

US20100113547A1 NOVEL IMIDAZOLIDINE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS 有权
标题翻译：新型咪唑烷化合物作为雄激素受体调节剂
公开(公告)号：US20100113547A1
公开(公告)日：2010-05-06
申请号：US12557368
申请日：2009-09-10
申请人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
发明人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
IPC分类号： A61K31/4166 , C07D233/40 , A61P35/00 , A61P19/10 , A61P15/00
CPC分类号： C07D233/60 , C07D233/66
摘要： Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3a R3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.
摘要翻译：公开了具有由下式表示的式的新化合物：其中X，R1，R2a，R2b，R2c，R3a R3b，R4a，R4b，R4c和m1如本文所述。化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括非限制性实例，恶病质，骨质疏松症，肌肉减少症，性欲下降和/或性功能障碍。

3. 发明授权

US07968581B2 Imidazolidine compounds as androgen receptor modulators 有权
标题翻译：咪唑烷化合物作为雄激素受体调节剂
公开(公告)号：US07968581B2
公开(公告)日：2011-06-28
申请号：US12557368
申请日：2009-09-10
申请人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
发明人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
IPC分类号： A61K31/4166 , C07D233/40 , A61P35/00
CPC分类号： C07D233/60 , C07D233/66
摘要： Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3a R3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.
摘要翻译：公开了具有由下式表示的式的新化合物：其中X，R1，R2a，R2b，R2c，R3a R3b，R4a，R4b，R4c和m1如本文所述。化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括非限制性实例，恶病质，骨质疏松症，肌肉减少症，性欲下降和/或性功能障碍。

4. 发明申请

US20100210699A1 IMIDAZOLIDINE DERIVATIVES, USES THEREFOR, PREPARATION THEREOF AND COMPOSITIONS COMPRISING SUCH 有权
标题翻译：咪唑啉衍生物，其用途及其制备方法和包含此类化合物的组合物
公开(公告)号：US20100210699A1
公开(公告)日：2010-08-19
申请号：US12751158
申请日：2010-03-31
申请人： Francois NIQUE , Catherine Jagerschmidt , Philippe Clement-Lacroix
发明人： Francois NIQUE , Catherine Jagerschmidt , Philippe Clement-Lacroix
IPC分类号： A61K31/4166 , C07D233/78 , C07D233/86 , C07D409/06 , C07D235/02 , A61P19/10 , A61P15/00 , A61P35/00
CPC分类号： C07D233/78 , A61K31/4166 , C07D233/86 , C07D235/02 , C07D309/10 , C07D409/06
摘要： Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.
摘要翻译：式（I）化合物：其中X为O或S，R1为酰基，醛，环烷基，任选取代的烷基，烯基或炔基，R2为H，烷基，羟基烷基，卤代烷基，烯基或炔基; 取代的烷基; 烷基羰基; R3和R4是H，卤素，烷基，烯基，炔基，烷氧基，烷硫基，羟基烷基，卤代烷基，卤代烯基或卤代炔基; 或R 3和R 4形成任选的芳族或杂环的任选取代的环，R 5是H，卤素，三氟甲基，-CN或-NO 2; 不是所有的R 3，R 4和R 5是H，R 6和R 9是H，卤素，OH; 烷基，羟基烷基，烷氧基，硫代烷基，卤代烷基，烯基或炔基; R7和R8是H，卤素，OH，SH; 任选被OH和/或卤素取代的烷氧基或烷硫基; R7和R8之一不是H或卤素; 或者R 7和R 8中的一个是药学上可接受的酯或硫代酯基团，或者R 6是C 1-3烷基，或者与R 1或R 2一起代表C1-3亚烷基或亚烯基连接基团，任选地被甲基，三氟甲基，OH ，或卤素及其药学上可接受的盐和酯可用作选择性雄激素调节剂。

5. 发明授权

US08383608B2 Imidazolidine compounds as androgen receptor modulators 有权
标题翻译：咪唑烷化合物作为雄激素受体调节剂
公开(公告)号：US08383608B2
公开(公告)日：2013-02-26
申请号：US13167682
申请日：2011-06-23
申请人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
发明人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
IPC分类号： A61K31/4166 , A61K31/675 , A61P15/00
CPC分类号： C07D233/60 , C07D233/66
摘要： Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3a R3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.
摘要翻译：公开了具有由下式表示的式的新化合物：其中X，R1，R2a，R2b，R2c，R3a R3b，R4a，R4b，R4c和m1如本文所述。化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括非限制性实例，恶病质，骨质疏松症，肌肉减少症，性欲下降和/或性功能障碍。

6. 发明申请

US20120178718A1 NOVEL IMIDAZOLIDINE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS 有权
标题翻译：新型咪唑烷化合物作为雄激素受体调节剂
公开(公告)号：US20120178718A1
公开(公告)日：2012-07-12
申请号：US13167682
申请日：2011-06-23
申请人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
发明人： François Nique , Catherine Jagerschmidt , Florence Sylvie Namour , Roland Blanqué , Jean-Michel Lefrançois , Christophe Peixoto , Pierre Deprez , Nicolas Triballeau , Piet Tom Bert Paul Wigerinck
IPC分类号： A61K31/4166 , A61K31/675 , A61P15/00 , A61P21/00 , A61P19/10 , A61P3/00
CPC分类号： C07D233/60 , C07D233/66
摘要： Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3aR3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.
摘要翻译：公开了具有由下式表示的式的新化合物：其中X，R 1，R 2a，R 2b，R 2c，R 3aaR 3b，R 4a，R 4b，R 4c和m 1如本文所述。化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括非限制性实例，恶病质，骨质疏松症，肌肉减少症，性欲下降和/或性功能障碍。

7. 发明授权

US08168667B2 Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such 有权
标题翻译：咪唑烷衍生物，其用途，其制备方法和包含其的组合物
公开(公告)号：US08168667B2
公开(公告)日：2012-05-01
申请号：US12751158
申请日：2010-03-31
申请人： Francois Nique , Catherine Jagerschmidt , Philippe Clement-Lacroix
发明人： Francois Nique , Catherine Jagerschmidt , Philippe Clement-Lacroix
IPC分类号： A61K31/4166 , C07D233/02
CPC分类号： C07D233/78 , A61K31/4166 , C07D233/86 , C07D235/02 , C07D309/10 , C07D409/06
摘要： Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, or halogen, and pharmaceutically acceptable salts and esters thereof, are useful as selective androgen modulators.
摘要翻译：式（I）化合物：其中X为O或S，R1为酰基，醛，环烷基，任选取代的烷基，烯基或炔基，R2为H，烷基，羟基烷基，卤代烷基，烯基或炔基; 取代的烷基; 烷基羰基; R3和R4是H，卤素，烷基，烯基，炔基，烷氧基，烷硫基，羟基烷基，卤代烷基，卤代烯基或卤代炔基; 或R 3和R 4形成任选的芳族或杂环的任选取代的环，R 5是H，卤素，三氟甲基，-CN或-NO 2; 不是所有的R 3，R 4和R 5是H，R 6和R 9是H，卤素，OH; 烷基，羟基烷基，烷氧基，硫代烷基，卤代烷基，烯基或炔基; R7和R8是H，卤素，OH，SH; 任选被OH和/或卤素取代的烷氧基或烷硫基; R7和R8之一不是H或卤素; 或者R 7和R 8中的一个是药学上可接受的酯或硫代酯基团，或者R 6是C 1-3烷基，或者与R 1或R 2一起代表C1-3亚烷基或亚烯基连接基团，任选地被甲基，三氟甲基，OH ，或卤素及其药学上可接受的盐和酯可用作选择性雄激素调节剂。

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