公开(公告)号：US09474755B2

公开(公告)日：2016-10-25

申请号：US14809020

申请日：2015-07-24

Applicant: Receptos, Inc.

Inventor： 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: C07D401/10 ,  C07D403/10 ,  A61K31/506 ,  C07D403/06 ,  C07D403/14 ,  C07D409/12 ,  C07D409/14 ,  A61K38/05 ,  C07D401/14 ,  C07D471/08 ,  C07K5/078

CPC classification number: 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

Abstract: 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.

公开(公告)号：US20150038416A1

公开(公告)日：2015-02-05

申请号：US14296907

申请日：2014-06-05

Applicant: Receptos, Inc.

Inventor： 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: C07K5/072 ,  A61K45/06 ,  A61K31/4245 ,  C07D413/14 ,  A61K31/4545 ,  C07D413/04 ,  A61K31/4439 ,  A61K31/4709 ,  A61K38/05 ,  C07D277/30 ,  A61K31/426 ,  C07D285/08 ,  A61K31/433 ,  C07D239/26 ,  A61K31/505 ,  C07D271/06

CPC classification number: C07K5/06113 ,  A61K31/33 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61K31/551 ,  A61K38/05 ,  A61K38/26 ,  A61K45/06 ,  C07D211/22 ,  C07D233/54 ,  C07D233/60 ,  C07D239/26 ,  C07D239/34 ,  C07D241/08 ,  C07D243/08 ,  C07D255/02 ,  C07D263/32 ,  C07D271/06 ,  C07D271/107 ,  C07D277/24 ,  C07D277/30 ,  C07D285/08 ,  C07D285/12 ,  C07D291/00 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D495/04

Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides 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.

Abstract translation: 本发明涉及调节胰高血糖素样肽1（GLP-1）受体的化合物，其合成方法及其治疗和/或预防用途的方法。 这些化合物独立地用作GLP-1受体的调节剂或增强剂，或者作为受体配体包括GLP-1肽GLP-1（7-36）和GLP-1（9-36）或与基于肽的疗法 ，其中A，B，C，Y 1，Y 2，Z，R 1，R 2，R 3，R 3，R 3，R 3， R4，R5，W1，n，p和q如本文所定义。

公开(公告)号：US20140336185A1

公开(公告)日：2014-11-13

申请号：US14122176

申请日：2012-05-31

Applicant: Receptos, Inc.

Inventor： Marcus F. Boehm ,  Esther Martinborough ,  Manisha Moorjani ,  Junko Tamiya ,  Liming Huang ,  Thomas Fowler ,  Andrew Novak ,  Premji Meghani ,  Enugurthi Brahmachary ,  Adam Richard Yeager

IPC: C07C235/38 ,  C07D307/54 ,  A61K31/341 ,  C07D213/80 ,  A61K31/4406 ,  C07D211/34 ,  A61K31/4465 ,  C07D295/15 ,  A61K31/5375 ,  C07D239/26 ,  A61K31/505 ,  A61K31/495 ,  C07D295/24 ,  A61K31/54 ,  A61K31/235

CPC classification number: 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

Abstract: 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.

Abstract translation: 结合胰高血糖素样肽1（GLP-1）受体的化合物，其合成方法，其治疗和/或预防用途的方法及其在体外稳定GLP-1受体中用于GLP- 1受体。 某些化合物自身或存在受体配体如GIP（1-42），PTH可能具有作为胰高血糖素受体，GIP受体，GLP-1和GLP-2受体以及PTH受体的调节剂或增效剂的活性 （1-34），胰高血糖素（1-29），GLP-2（1-33），GLP-1（7-36），GLP-1（9-36），胃泌酸调节蛋白和毒蜥外泌肽变体。

公开(公告)号：US20130178420A1

公开(公告)日：2013-07-11

申请号：US13712624

申请日：2012-12-12

Applicant: RECEPTOS, INC.

Inventor： 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: C07D413/14 ,  A61K31/4245 ,  C07D413/10 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  C07D239/26 ,  A61K31/505 ,  C07D413/12 ,  A61K31/506 ,  C07D403/12 ,  C07D403/04 ,  C07D243/08 ,  A61K31/551 ,  A61K38/26 ,  C07D271/06

CPC classification number: C07K5/06113 ,  A61K31/33 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61K31/551 ,  A61K38/05 ,  A61K38/26 ,  A61K45/06 ,  C07D211/22 ,  C07D233/54 ,  C07D233/60 ,  C07D239/26 ,  C07D239/34 ,  C07D241/08 ,  C07D243/08 ,  C07D255/02 ,  C07D263/32 ,  C07D271/06 ,  C07D271/107 ,  C07D277/24 ,  C07D277/30 ,  C07D285/08 ,  C07D285/12 ,  C07D291/00 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D495/04

Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides 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.

Abstract translation: 本发明涉及调节胰高血糖素样肽1（GLP-1）受体的化合物，其合成方法及其治疗和/或预防用途的方法。 这些化合物独立地用作GLP-1受体的调节剂或增强剂，或者作为受体配体包括GLP-1肽GLP-1（7-36）和GLP-1（9-36）或与基于肽的疗法 ，其中A，B，C，Y 1，Y 2，Z，R 1，R 2，R 3，R 3，R 3，R 3， R4，R5，W1，n，p和q如本文所定义。

公开(公告)号：US09598430B2

公开(公告)日：2017-03-21

申请号：US14958513

申请日：2015-12-03

Applicant: Receptos, Inc.

Inventor： 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: C07D403/10 ,  A61K31/506 ,  C07D495/04 ,  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 ,  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

CPC classification number: 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

Abstract: 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.

公开(公告)号：US09388147B2

公开(公告)日：2016-07-12

申请号：US14632675

申请日：2015-02-26

Applicant: Receptos, Inc.

Inventor： 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: C07D271/06 ,  C07D413/12 ,  C07D417/12 ,  C07D413/10 ,  C07D413/14 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07C245/14 ,  C07C255/58 ,  C07C311/13

CPC classification number: 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

Abstract: 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.

Abstract translation: 提供了选择性调节鞘氨醇1磷酸受体的化合物，包括调节S1P受体亚型1的化合物。 提供了这些化合物的手性合成方法。 本发明化合物的用途，治疗或预防方法以及制备本发明组合物的方法与治疗或预防医学上指示鞘氨醇1磷酸受体调节的疾病，病症和病症有关。

公开(公告)号：US20160038487A1

公开(公告)日：2016-02-11

申请号：US14809020

申请日：2015-07-24

Applicant: Receptos, Inc.

Inventor： 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: A61K31/506 ,  A61K38/05 ,  C07D409/14 ,  C07D471/08 ,  C07D403/10 ,  C07D403/14 ,  C07D401/14 ,  C07K5/078 ,  C07D409/12

CPC classification number: 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

Abstract: 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.

Abstract translation: 提供调节胰高血糖素样肽1（GLP-1）受体的化合物及其合成方法及其治疗和/或预防用途的方法。 这些化合物可以单独作为GLP-1受体的调节剂或增效剂，或者可以作为GLP-1（7-36），GLP-1（9-36）和胃泌酸调节蛋白的肠降血糖素肽或基于肽的疗法 ，其具有以下一般结构（其中“”表示化合物的R和S形式中的任一者或两者）：其中A，B，C，R 1，R 2，R 3，R 4，R 5，n， p和q如本文所定义。

公开(公告)号：US20150011527A1

公开(公告)日：2015-01-08

申请号：US14302260

申请日：2014-06-11

Applicant: Receptos, Inc.

Inventor： 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: C07D471/04 ,  C07D239/26 ,  C07D409/12 ,  C07D413/04 ,  C07D401/04 ,  C07D243/08 ,  C07D231/12 ,  C07D417/04 ,  C07D403/12 ,  C07D403/10 ,  C07D409/14 ,  C07D413/14 ,  C07D271/06 ,  C07D233/64

CPC classification number: 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

Abstract: 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.

Abstract translation: 提供调节胰高血糖素样肽1（GLP-1）受体的化合物及其合成方法及其治疗和/或预防用途的方法。 这些化合物本身可以作为GLP-1受体的调节剂或增效剂，或者可以作为降解素肽如GLP-1（7-36）和GLP-1（9-36），或者基于肽的疗法，例如 艾塞那肽和利拉鲁肽，具有以下通用结构（其中“”表示化合物的R和S形式中的任一者或两者）：其中A，B，C，Y1，Y2，Z，R1，R2，R3，R4，R5 ，W1，n，p和q如本文所定义。

公开(公告)号：US08778923B2

公开(公告)日：2014-07-15

申请号：US13712624

申请日：2012-12-12

Applicant: Receptos, Inc.

Inventor： 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: A61K31/33 ,  C07D291/00

CPC classification number: C07K5/06113 ,  A61K31/33 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61K31/551 ,  A61K38/05 ,  A61K38/26 ,  A61K45/06 ,  C07D211/22 ,  C07D233/54 ,  C07D233/60 ,  C07D239/26 ,  C07D239/34 ,  C07D241/08 ,  C07D243/08 ,  C07D255/02 ,  C07D263/32 ,  C07D271/06 ,  C07D271/107 ,  C07D277/24 ,  C07D277/30 ,  C07D285/08 ,  C07D285/12 ,  C07D291/00 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D495/04

Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides 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.

Abstract translation: 本发明涉及调节胰高血糖素样肽1（GLP-1）受体的化合物，其合成方法及其治疗和/或预防用途的方法。 这些化合物独立地用作GLP-1受体的调节剂或增强剂，或者作为受体配体包括GLP-1肽GLP-1（7-36）和GLP-1（9-36）或与基于肽的疗法 ，其中A，B，C，Y 1，Y 2，Z，R 1，R 2，R 3，R 3，R 3，R 3， R4，R5，W1，n，p和q如本文所定义。

公开(公告)号：US20130196966A1

公开(公告)日：2013-08-01

申请号：US13740669

申请日：2013-01-14

Applicant: RECEPTOS, INC.

Inventor： Esther Martinborough ,  Marcus F. Boehm ,  Adam Richard Yeager ,  Junko Tamiya ,  Liming Huang ,  Enugurthi Brahmachary ,  Manisha Moorjani

IPC: C07D271/06 ,  A61K45/06 ,  A61K31/454 ,  A61K31/5377 ,  C07D413/12 ,  A61K31/4245

Abstract: 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.