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公开(公告)号：US20210155615A1
公开(公告)日：2021-05-27
申请号：US17045626
申请日：2019-04-05
发明人： Curtis HARWIG , Jeremy D. PETTIGREW , Jennifer CROSS , Jeyaprakashnarayanan SEENISAMY , Mahesh Narayan KEREGADDE , Samir Satish KHER
IPC分类号： C07D413/06 , C07D231/54 , C07D405/12 , C07D401/08 , C07D403/08 , C07D403/04 , C07D241/42 , C07D239/84 , C07D239/74 , C07D209/08 , C07D263/56 , C07D261/20 , A61P29/00
摘要： Compounds of formula (I) wherein, R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.
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![HEXADECAHYDRO-1H-CYCLOPENTA[A]PHENANTHRENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION](/abs-image/US/2021/01/28/US20210024571A1/abs.jpg.150x150.jpg)
22.发明申请公开(公告)号：US20210024571A1
公开(公告)日：2021-01-28
申请号：US17045688
申请日：2019-04-05
发明人： Curtis HARWIG , Jeremy D. PETTIGREW , Jennifer CROSS , Jeyaprakashnarayanan SEENISAMY , Mahesh Narayan KEREGADDE , Samir Satish KHER , Karthikeyan IYANAR
摘要： wherein, R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.
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公开(公告)号：US20190023709A1
公开(公告)日：2019-01-24
申请号：US16129586
申请日：2018-09-12
IPC分类号： C07D473/34 , C07C261/04 , C07D233/60 , C07D213/64 , C07C225/10 , C07C233/23 , C07C233/74 , C07D207/06 , C07D213/38 , C07C35/21 , C07C62/32 , C07C59/46 , C07D307/68 , C07D213/36 , C07D213/30 , C07D213/04 , C07D295/096 , C07C255/31 , C07D209/08 , C07D207/416 , C07D207/335 , C07D207/08 , C07C235/48 , C07C235/46 , C07C235/44 , C07C235/30 , C07C233/60 , C07C233/18 , C07C335/10 , C07D249/08 , C07D241/28 , C07D241/18 , C07C215/52 , C07C215/50 , C07C215/42 , C07D239/34 , C07D235/14 , C07D235/06 , C07C311/04 , C07D233/72 , C07D231/12 , C07C291/04 , C07D317/58 , C07D317/46 , C07C279/08 , C07C275/34 , C07C275/24 , C07C275/10 , C07C35/32 , C07D213/82 , C07D213/81
摘要： Compounds of formula (I): where R1, R2, R3, R4a, R4b, R5, R6 and R7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
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公开(公告)号：US20180290964A1
公开(公告)日：2018-10-11
申请号：US16008952
申请日：2018-06-14
IPC分类号： C07C215/42
摘要： The present invention is generally directed to methods of using novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and pharmaceutical compositions comprising same.
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公开(公告)号：US20180155273A1
公开(公告)日：2018-06-07
申请号：US15885387
申请日：2018-01-31
IPC分类号： C07C215/42
CPC分类号： C07C215/42 , C07B2200/13 , C07C2601/14 , C07C2602/08 , C07C2602/24
摘要： The present invention is generally directed to novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and processes for their preparation.
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公开(公告)号：US09944590B2
公开(公告)日：2018-04-17
申请号：US15191134
申请日：2016-06-23
IPC分类号： C07C215/42
CPC分类号： C07C215/42 , C07B2200/13 , C07C2601/14 , C07C2602/08 , C07C2602/24
摘要： The present invention is generally directed to novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and processes for their preparation.
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公开(公告)号：US20170224682A1
公开(公告)日：2017-08-10
申请号：US15370973
申请日：2016-12-06
发明人： Lloyd F. MACKENZIE , Thomas B. MACRURY , Curtis HARWIG , David BOGUCKI , Jeffery R. RAYMOND , Jeremy D. PETTIGREW , Vladimir KHLEBNIKOV , Rudong SHAN
IPC分类号： A61K31/4965 , A61K31/122 , A61K31/135 , A61K31/085 , A61K31/05 , A61K31/192 , A61K31/09 , A61K31/167 , A61K31/165 , A61K31/277 , A61K31/095 , A61K31/166 , A61K31/4402 , A61K31/4164 , A61K31/4196 , A61K31/495 , A61K31/155 , A61K31/4406 , A61K31/4465 , A61K31/10 , A61K31/443 , A61K31/444 , A61K31/4439 , A61K31/496 , A61K31/12
CPC分类号： A61K31/4965 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/095 , A61K31/10 , A61K31/12 , A61K31/122 , A61K31/135 , A61K31/155 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/192 , A61K31/277 , A61K31/4164 , A61K31/4196 , A61K31/4402 , A61K31/4406 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4465 , A61K31/495 , A61K31/496 , C07B2200/07 , C07C39/17 , C07C43/21 , C07C43/215 , C07C43/23 , C07C49/83 , C07C49/835 , C07C49/84 , C07C62/32 , C07C62/34 , C07C217/84 , C07C225/20 , C07C233/26 , C07C233/28 , C07C233/31 , C07C233/32 , C07C233/60 , C07C233/76 , C07C235/82 , C07C237/08 , C07C255/47 , C07C275/26 , C07C275/64 , C07C279/16 , C07C311/07 , C07C311/17 , C07C311/18 , C07C317/22 , C07C323/20 , C07C2602/28 , C07D211/66 , C07D213/38 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/89 , C07D233/64 , C07D241/24 , C07D249/08 , C07D295/112 , C07D295/215 , C07D401/12 , C07D405/12
摘要： Compounds of formula (I): where n, R1, R4a, R4b, R5, R7 and R8 are defined herein, or pharmaceutically acceptable salts thereof, are described herein. The disclosed compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
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28.发明申请CRYSTALLINE SOLID FORMS OF THE ACETATE SALT OF (1S,3S,4R)-4-((3AS,4R,5S,7AS)-4-(AMINOMETHYL)-7A-METHYL-1-METHYLENEOCTAHYDRO-1H-INDEN-5-YL)-3-(HYDROXYMETHYL)-4-METHYLCYCLOHEXANOL 有权（1S，3S，4R）-4 - （（3AS，4R，5S，7AS）-4-（氨基甲基）-7A-甲基-1-甲基戊酰氧基-1H-吲哚-5-基）乙酸盐的结晶固体形式 ）-3-（羟甲基）-4-甲基环己醇公开(公告)号：US20160376222A1
公开(公告)日：2016-12-29
申请号：US15191134
申请日：2016-06-23
IPC分类号： C07C215/42 , C07C213/00
CPC分类号： C07C215/42 , C07B2200/13 , C07C2601/14 , C07C2602/08 , C07C2602/24
摘要： The present invention is generally directed to novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and processes for their preparation.
摘要翻译： 本发明一般涉及（1S，3S，4R）-4 - （（3aS，4R，5S，7aS）-4-（氨基甲基）-7a-甲基-1-亚甲基八氢 - 1H-茚-5-基）-3-（羟甲基）-4-甲基环己醇，其制备方法。
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公开(公告)号：US20160083387A1
公开(公告)日：2016-03-24
申请号：US14772737
申请日：2014-02-27
IPC分类号： C07D473/34 , C07C215/42 , C07C233/23 , C07D207/335 , C07C311/04 , C07C225/10 , C07D207/06 , C07D213/38 , C07C233/74 , C07D231/12 , C07D249/08 , C07D233/60 , C07D209/08 , C07D317/46 , C07D295/096 , C07D213/64 , C07D239/34 , C07D241/18 , C07C255/31 , C07C275/24 , C07C279/08
CPC分类号： C07D473/34 , C07C35/21 , C07C35/32 , C07C59/46 , C07C62/32 , C07C215/42 , C07C215/50 , C07C215/52 , C07C225/10 , C07C233/18 , C07C233/23 , C07C233/60 , C07C233/74 , C07C235/30 , C07C235/44 , C07C235/46 , C07C235/48 , C07C255/31 , C07C261/04 , C07C275/10 , C07C275/24 , C07C275/34 , C07C279/08 , C07C291/04 , C07C311/04 , C07C335/10 , C07C2602/24 , C07C2603/14 , C07D207/06 , C07D207/08 , C07D207/335 , C07D207/416 , C07D209/08 , C07D213/04 , C07D213/30 , C07D213/36 , C07D213/38 , C07D213/64 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/60 , C07D233/72 , C07D235/06 , C07D235/14 , C07D239/34 , C07D241/18 , C07D241/28 , C07D249/08 , C07D295/096 , C07D307/68 , C07D317/46 , C07D317/58
摘要： Compounds of formula (I): where R1, R2, R3, R4a, R4b, R5, R6 and R7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
摘要翻译： 式（I）化合物：其中R1，R2，R3，R4a，R4b，R5，R6和R7如本文所定义，或其立体异构体或其药学上可接受的盐在本文中描述。 这些化合物具有作为SHIP1调节剂的活性，因此可用于治疗将受益于SHIP1调节的各种疾病，障碍或病症中的任何一种。 还公开了包含式（I）化合物与药学上可接受的载体或稀释剂的组合物，以及通过将这些化合物施用于有此需要的动物的SHIP1调节方法。
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公开(公告)号：US20160031899A1
公开(公告)日：2016-02-04
申请号：US14772731
申请日：2014-02-27
发明人： Lloyd F. Mackenzie , Thomas B. MacRury , Curtis Harwig , David Bogucki , Jeffery R. Raymond , Jeremy D. Pettigrew
IPC分类号： C07D493/10 , C07D211/58 , C07C255/30 , C07D213/75 , C07C275/22 , C07C335/10 , C07D231/54 , C07D215/227 , C07D221/16 , C07C215/38 , C07D307/52 , C07D333/20 , C07D213/38 , C07D277/28 , C07D231/56 , C07D261/20 , C07D277/64 , C07C35/21 , C07C35/23 , C07D307/42 , C07C233/23 , C07D213/82
CPC分类号： C07D493/10 , A61K31/416 , C07C35/21 , C07C35/23 , C07C215/26 , C07C215/38 , C07C233/23 , C07C255/30 , C07C275/22 , C07C335/10 , C07C2601/14 , C07C2602/24 , C07D211/58 , C07D213/30 , C07D213/38 , C07D213/75 , C07D213/82 , C07D215/227 , C07D221/16 , C07D221/18 , C07D231/54 , C07D231/56 , C07D261/20 , C07D277/24 , C07D277/28 , C07D277/64 , C07D307/42 , C07D307/52 , C07D333/16 , C07D333/20
摘要： Compounds of formula (II): wherein A, R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
摘要翻译： 本文描述了其中A，R 1，R 2，R 5和R 13或其立体异构体，对映异构体或互变异构体或其混合物或其药学上可接受的盐或溶剂化物的式（II）化合物，以及其它 化合物。 这些化合物具有作为SHIP1调节剂的活性，因此可用于治疗将受益于SHIP1调节的各种疾病，病症或病症。 还公开了包含本发明化合物的组合物，以及通过将这些化合物施用于有需要的动物的SHIP1调节方法。
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