Bicyclic compounds

Patent metadata

Field	Value
Publication number	US-9359286-B2
Application number	US-201514798498-A
Country	US
Kind code	B2
Filing date	Jul 14, 2015
Priority date	Feb 21, 2013
Publication date	Jun 7, 2016
Grant date	Jun 7, 2016

Abstract

Disclosed are compounds of Formula (I)

and/or a salt thereof; wherein R is —OH or —OP(O)(OH) 2 . Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P 1 , and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

First claim

What is claimed is:

1. A compound having the structure:

wherein said compound is in crystalline Form N-1, which is characterized by one or more of the following:
a) unit cell parameters approximately equal to the following:
Cell dimensions:
a=5.54 Å
b=7.37 Å
c=48.85 Å
α=90.0°
β=90.0°
γ=90.0°

Space group: P2 1 2 1 2 1
Molecules of said compound/asymmetric unit: 1

wherein the unit cell parameters of Form N-1 are measured at a temperature of about −70° C.;
b) a simulated powder x-ray diffraction pattern substantially as shown in FIG. 1 ;
c) an observed powder x-ray diffraction pattern substantially as shown FIG. 1 ;
d) a powder x-ray diffraction pattern comprising four or more 2θ values selected from: 3.6±0.2, 7.2±0.2, 12.5±0.2, 14.0±0.2, 15.0±0.2, 17.5±0.2, 19.4±0.2, 20.4±0.2, and 23.8±0.2, wherein the powder x-ray diffraction pattern of Form N-1 is measured at a temperature of about 25° C.; and/or
e) a powder x-ray diffraction pattern comprising five or more 2θ values selected from: 3.6±0.2, 7.2±0.2, 12.5±0.2, 14.0±0.2, 15.0±0.2, 17.5±0.2, 19.4±0.2, 20.4±0.2, and 23.8±0.2, wherein the powder x-ray diffraction pattern of Form N-1 is measured at a temperature of about 25° C.

2. The compound according to claim 1 , wherein said crystalline Form N-1 is substantially pure.

3. A pharmaceutical composition comprising the compound in crystalline Form N-1 according to claim 1 ; and at least one pharmaceutically acceptable carrier and/or diluent.

Assignees

• Bristol Myers Squibb Co

Inventors

• Xiao Hai-Yun

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P37/02

  Immunomodulators · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title