75308-46-2Relevant academic research and scientific papers
Compounds and methods of use
-
Page/Page column 399; 400; 402-404, (2021/08/04)
Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X1, X2, X3, X4, Y, A, L1, L2, R1, R2, R5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
COMPOUNDS AND METHODS OF USE
-
Paragraph 0662-0663, (2021/05/07)
Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X1, X2, X3, X4, X5, A, L, R1, R2, R5, m and n are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
Practical and scalable synthesis of S1P1 receptor agonist ACT-209905
Schmidt, Gunther,Reber, Stefan,Bolli, Martin H.,Abele, Stefan
scheme or table, p. 595 - 604 (2012/07/13)
A practical and scalable route for the fast delivery of 12 kg of S1P 1 agonist (ACT-209905) has been developed. ACT-209905 is composed of an amino pyridine group, an oxadiazole spacer, a 2-ethyl-5-methylphenol moiety and a chiral 1-amino-2-propanol side chain. The convergent synthesis consists of 16 steps with 9 isolated intermediates and is chromatography-free. Key building blocks are accessed from low-cost starting materials, such as acetone, diethyl oxalate, cyanoacetamide, and 2-ethyl-5-methyl aniline. A Negishi coupling that was troubled by the use of metal reagents and concomitant metal waste streams has been replaced by a less expensive Guareschi-Thorpe reaction to build up an amino isonicotinic acid. The chiral 1-amino-2-propanol moiety was secured by selective ring-opening of an epoxide with lithium hexamethyldisilazide as an ammonia surrogate, thus omitting the notorious double alkylated byproduct.
PYRIDINE AND ISOQUINOLINE DERIVATIVES AS SYK- AND JAK-KINASE INHIBITORS
-
Page/Page column 67, (2012/04/17)
The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase and/or Janus kinases.
Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
-
Paragraph 0184, (2013/03/26)
The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by inhibition of Syk kinase and/or Janus kinases.
PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
-
Page/Page column 20, (2011/09/20)
The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituents are as defined in the claims.
Pyridin-4-yl derivatives as immunomodulating agents
-
Page/Page column 15, (2010/04/23)
The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
AMINO-PYRIDINE DERIVATIVES AS S1P1 /EDG1 RECEPTOR AGONISTS
-
Page/Page column 13, (2010/04/30)
The invention relates to novel amino-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
P2X3, RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN
-
Page/Page column 79, (2010/11/18)
The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
-
Page/Page column 53-54, (2009/04/25)
The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituants are as defined in the claims.
