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公开(公告)号:US20170320839A1
公开(公告)日:2017-11-09
申请号:US15406128
申请日:2017-01-13
发明人: Esther Martinborough , Marcus F. Boehm , Adam Richard Yeager , Junko Tamiya , Liming Huang , Enugurthi Brahmachary , Manisha Moorjani , Gregg Alan Timony , Jennifer L. Brooks , Robert Peach , Fiona Lorraine Scott , Michael Allen Hanson
IPC分类号: C07D271/06 , C07D413/14 , C07D413/12 , C07D413/10 , C07C311/13 , C07C245/14 , A61K31/4245 , A61K45/06 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/427 , C07D417/12 , C07C255/58
CPC分类号: C07D271/06 , A61K31/4245 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07C245/14 , C07C255/58 , C07C311/13 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12
摘要: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
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公开(公告)号:US20180021346A1
公开(公告)日:2018-01-25
申请号:US15711858
申请日:2017-09-21
发明人: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs , Daniel Glynn , Mark Mills
IPC分类号: A61K31/551 , C07D417/12 , C07D413/12 , C07D413/04 , C07D409/14 , C07D409/12 , C07D407/12 , C07D405/12 , C07D403/12 , C07D403/10 , C07D403/04 , C07D401/12 , C07D401/06 , C07D401/04 , C07D295/135 , C07D295/084 , C07D285/12 , C07D285/08 , C07D277/30 , C07D271/107 , C07D271/06 , C07D263/32 , C07D253/065 , C07D253/06 , C07D243/08 , C07D241/12 , C07D241/08 , C07D239/74 , C07D239/34 , C07D471/04 , C07D237/08 , C07D231/12 , C07D215/14 , C07D213/55 , C07D211/98 , C07D211/22 , C07D207/08 , A61K38/26 , A61K31/53 , A61K31/506 , A61K31/505 , A61K31/501 , A61K31/50 , A61K31/4965 , A61K31/497 , A61K31/495 , A61K31/4725 , A61K31/4709 , A61K31/4545 , A61K31/454 , A61K31/4468 , A61K31/4439 , A61K31/445 , A61K31/44 , A61K31/433 , A61K31/4245 , A61K31/426 , A61K31/421 , A61K31/4178 , C07D495/04 , A61K31/402 , C07D239/26
CPC分类号: A61K31/551 , A61K31/402 , A61K31/4178 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/53 , A61K38/26 , C07D207/08 , C07D211/22 , C07D211/98 , C07D213/55 , C07D215/14 , C07D231/12 , C07D237/08 , C07D239/26 , C07D239/34 , C07D239/74 , C07D241/08 , C07D241/12 , C07D243/08 , C07D253/06 , C07D253/065 , C07D263/32 , C07D271/06 , C07D271/107 , C07D277/30 , C07D285/08 , C07D285/12 , C07D295/084 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04
摘要: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
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公开(公告)号:US09839664B2
公开(公告)日:2017-12-12
申请号:US15263637
申请日:2016-09-13
发明人: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs
IPC分类号: A61K31/506 , A61K38/05 , C07D401/10 , C07D409/10 , C07D403/10 , C07D403/14 , C07D409/14 , C07D401/14
CPC分类号: A61K38/05 , A61K31/155 , A61K31/4985 , A61K31/506 , A61K31/7004 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/14 , C07D409/10 , C07D409/12 , C07D409/14 , C07D471/08 , C07K5/06139 , A61K2300/00
摘要: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.
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公开(公告)号:US09795613B2
公开(公告)日:2017-10-24
申请号:US14965777
申请日:2015-12-10
发明人: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs , Daniel Glynn , Mark Mills
IPC分类号: C07D403/10 , A61K31/506 , A61K31/551 , C07D403/12 , C07D215/14 , C07D231/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D237/08 , C07D239/26 , C07D407/12 , C07D409/12 , C07D409/14 , C07D239/74 , C07D413/04 , C07D413/12 , C07D241/12 , C07D417/12 , C07D471/04 , C07D253/06 , C07D207/08 , C07D271/06 , C07D495/04 , C07D295/084 , C07D295/135 , C07D213/55 , A61K31/402 , A61K31/4178 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/53 , A61K38/26 , C07D211/22 , C07D211/98 , C07D239/34 , C07D241/08 , C07D243/08 , C07D253/065 , C07D263/32 , C07D271/107 , C07D277/30 , C07D285/08 , C07D285/12 , C07D405/12
CPC分类号: A61K31/551 , A61K31/402 , A61K31/4178 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/53 , A61K38/26 , C07D207/08 , C07D211/22 , C07D211/98 , C07D213/55 , C07D215/14 , C07D231/12 , C07D237/08 , C07D239/26 , C07D239/34 , C07D239/74 , C07D241/08 , C07D241/12 , C07D243/08 , C07D253/06 , C07D253/065 , C07D263/32 , C07D271/06 , C07D271/107 , C07D277/30 , C07D285/08 , C07D285/12 , C07D295/084 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04
摘要: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
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公开(公告)号:US10239846B2
公开(公告)日:2019-03-26
申请号:US15406128
申请日:2017-01-13
发明人: Esther Martinborough , Marcus F. Boehm , Adam Richard Yeager , Junko Tamiya , Liming Huang , Enugurthi Brahmachary , Manisha Moorjani , Gregg Alan Timony , Jennifer L. Brooks , Robert Peach , Fiona Lorraine Scott , Michael Allen Hanson
IPC分类号: A61K31/4245 , A61K45/06 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/427 , C07D271/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12 , C07C245/14 , C07C255/58 , C07C311/13
摘要: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
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公开(公告)号:US10034886B2
公开(公告)日:2018-07-31
申请号:US15711858
申请日:2017-09-21
发明人: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs , Daniel Glynn , Mark Mills
IPC分类号: A61K31/506 , C07D403/10 , A61K31/551 , A61K31/4725 , A61K31/495 , A61K31/4545 , A61K31/454 , A61K31/4468 , A61K31/4439 , A61K31/445 , A61K31/44 , A61K31/433 , A61K31/4245 , A61K31/426 , A61K31/421 , A61K31/4178 , C07D495/04 , C07D471/04 , A61K31/402 , C07D417/12 , C07D413/12 , C07D413/04 , C07D409/14 , C07D409/12 , C07D407/12 , C07D405/12 , C07D403/12 , C07D403/04 , C07D401/12 , C07D401/06 , C07D401/04 , C07D295/135 , C07D295/084 , C07D285/12 , C07D285/08 , C07D277/30 , C07D271/107 , C07D271/06 , C07D263/32 , C07D253/065 , C07D253/06 , C07D243/08 , C07D241/12 , C07D241/08 , C07D239/74 , C07D239/34 , C07D239/26 , C07D237/08 , C07D231/12 , C07D215/14 , C07D213/55 , C07D211/98 , C07D211/22 , C07D207/08 , A61K38/26 , A61K31/53 , A61K31/505 , A61K31/501 , A61K31/50 , A61K31/4965 , A61K31/497 , A61K31/4709
CPC分类号: A61K31/551 , A61K31/402 , A61K31/4178 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/4468 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/53 , A61K38/26 , C07D207/08 , C07D211/22 , C07D211/98 , C07D213/55 , C07D215/14 , C07D231/12 , C07D237/08 , C07D239/26 , C07D239/34 , C07D239/74 , C07D241/08 , C07D241/12 , C07D243/08 , C07D253/06 , C07D253/065 , C07D263/32 , C07D271/06 , C07D271/107 , C07D277/30 , C07D285/08 , C07D285/12 , C07D295/084 , C07D295/135 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04
摘要: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
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公开(公告)号:US20170313717A1
公开(公告)日:2017-11-02
申请号:US15416758
申请日:2017-01-26
发明人: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs
IPC分类号: C07D495/04 , A61K31/155 , C07D417/04 , C07D413/14 , C07D413/12 , C07D413/10 , C07D413/04 , C07D409/14 , C07D409/12 , C07D405/12 , C07D403/14 , C07D403/12 , C07D403/10 , C07D403/04 , C07D401/12 , C07D401/04 , C07D271/06 , C07D243/08 , C07D239/26 , C07D237/04 , C07D233/64 , C07D231/12 , A61K31/551 , A61K31/506 , A61K31/505 , A61K31/4985 , A61K31/4453 , A61K31/4245 , A61K31/4164 , A61K31/415 , C07D417/12 , C07D471/04
CPC分类号: C07D495/04 , A61K31/155 , A61K31/415 , A61K31/4164 , A61K31/4245 , A61K31/4453 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/551 , C07D231/12 , C07D233/64 , C07D237/04 , C07D239/26 , C07D243/08 , C07D271/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D471/04
摘要: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
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公开(公告)号:US10259823B2
公开(公告)日:2019-04-16
申请号:US15416758
申请日:2017-01-26
发明人: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs
IPC分类号: C07D213/24 , C07D495/04 , A61K31/506 , C07D403/12 , C07D401/04 , C07D403/04 , C07D239/26 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D271/06 , C07D231/12 , C07D233/64 , C07D243/08 , C07D403/10 , C07D413/14 , C07D417/04 , C07D471/04 , A61K31/155 , A61K31/415 , A61K31/4164 , A61K31/4245 , A61K31/4453 , A61K31/4985 , A61K31/505 , A61K31/551 , C07D237/04 , C07D401/12 , C07D403/14 , C07D413/10
摘要: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
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公开(公告)号:US20170216392A1
公开(公告)日:2017-08-03
申请号:US15263637
申请日:2016-09-13
发明人: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Adam R. Yeager , Enugurthi Brahmachary , Thomas Fowler , Andrew Novak , Premji Meghani , Michael Knaggs
IPC分类号: A61K38/05 , A61K31/506
CPC分类号: A61K38/05 , A61K31/155 , A61K31/4985 , A61K31/506 , A61K31/7004 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/14 , C07D409/10 , C07D409/12 , C07D409/14 , C07D471/08 , C07K5/06139 , A61K2300/00
摘要: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.
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公开(公告)号:US09700543B2
公开(公告)日:2017-07-11
申请号:US14997364
申请日:2016-01-15
发明人: Marcus F. Boehm , Esther Martinborough , Manisha Moorjani , Junko Tamiya , Liming Huang , Thomas Fowler , Andrew Novak , Premji Meghani , Enugurthi Brahmachary , Adam Richard Yeager
IPC分类号: A61K31/4245 , A61K9/00 , A61K47/20 , A61K47/26 , A61K47/40 , A61K47/48 , A61K45/06 , A61K31/155 , A61K38/26 , C07C255/57 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D309/06 , C07D309/08 , C07D311/16 , C07C271/28 , C07D215/48 , C07D217/02 , C07C275/42 , C07D317/68 , C07D231/12 , C07D333/38 , C07D233/60 , C07C311/08 , C07C311/13 , C07C311/21 , C07D235/06 , C07C311/29 , C07D235/12 , C07D235/18 , C07C311/48 , C07D239/26 , C07D239/28 , C07C317/28 , C07C317/44 , C07D239/74 , C07D413/04 , C07D239/91 , C07D413/12 , C07D241/42 , C07D241/44 , C07D417/12 , C07C323/62 , C07C229/14 , C07D249/08 , C07D257/04 , C07C233/47 , C07C233/51 , C07D261/18 , C07C233/81 , C07C233/83 , C07C235/12 , C07D263/32 , C07C235/38 , C07D263/34 , C07C235/48 , C07D263/48 , C07D263/57 , C07C237/22 , C07C237/36 , C07C237/42 , C07D271/06 , C07D271/07 , C07D271/107 , C07D207/267 , C07D277/30 , C07D209/08 , C07D277/56 , C07D277/66 , C07D279/12 , C07D211/14 , C07D211/34 , C07D211/62 , C07D295/15 , C07D295/155 , C07D295/205 , C07D213/55 , C07D213/65 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/79 , C08B37/16 , C08L5/16 , B82Y5/00 , A61K31/235 , A61K31/341 , A61K31/4406 , A61K31/4465 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K31/54 , C07D295/24 , A61K31/4439 , A61K31/4725
CPC分类号: A61K31/4245 , A61K9/0019 , A61K9/0095 , A61K31/155 , A61K31/235 , A61K31/341 , A61K31/4406 , A61K31/4439 , A61K31/4465 , A61K31/4725 , A61K31/495 , A61K31/505 , A61K31/5375 , A61K31/54 , A61K38/22 , A61K38/26 , A61K45/06 , A61K47/20 , A61K47/26 , A61K47/40 , A61K47/6951 , B82Y5/00 , C07C229/14 , C07C233/47 , C07C233/51 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/38 , C07C235/48 , C07C237/22 , C07C237/36 , C07C237/42 , C07C255/57 , C07C271/28 , C07C275/42 , C07C311/08 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/48 , C07C317/28 , C07C317/44 , C07C323/62 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D209/08 , C07D211/14 , C07D211/34 , C07D211/62 , C07D213/55 , C07D213/65 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D215/48 , C07D217/02 , C07D231/12 , C07D233/60 , C07D235/06 , C07D235/12 , C07D235/18 , C07D239/26 , C07D239/28 , C07D239/74 , C07D239/91 , C07D241/42 , C07D241/44 , C07D249/08 , C07D257/04 , C07D261/18 , C07D263/32 , C07D263/34 , C07D263/48 , C07D263/57 , C07D271/06 , C07D271/07 , C07D271/107 , C07D277/30 , C07D277/56 , C07D277/66 , C07D279/12 , C07D295/15 , C07D295/155 , C07D295/205 , C07D295/24 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/79 , C07D309/06 , C07D309/08 , C07D311/16 , C07D317/68 , C07D333/38 , C07D413/04 , C07D413/12 , C07D417/12 , C08B37/0015 , C08L5/16 , A61K2300/00
摘要: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.
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