cas 75308-46-2, tert-Butyl 2,6-dichloroisonicotinate

Articles about 75308-46-2Total 17 be found

Compounds and methods of use
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.
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Page/Page column 399; 400; 402-404

(2021/08/04)

COMPOUNDS AND METHODS OF USE
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.
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Paragraph 0662-0663

(2021/05/07)

Practical and scalable synthesis of S1P1 receptor agonist ACT-209905
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 A Negishi coupling that was troubled by the use of metal reagents and concomitant metal waste streams has been replaced by a less expensive Guareschi-Thorpe reaction to build up an amino isonicotinic acid.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.
Schmidt, Gunther,Reber, Stefan,Bolli, Martin H.,Abele, Stefan
scheme or table
p. 595 - 604
(2012/07/13)

PYRIDINE AND ISOQUINOLINE DERIVATIVES AS SYK- AND JAK-KINASE INHIBITORS
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.
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Page/Page column 67

(2012/04/17)

Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
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.
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Paragraph 0184

(2013/03/26)

PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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.
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Page/Page column 20

(2011/09/20)

Pyridin-4-yl derivatives as immunomodulating agents
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.
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Page/Page column 15

(2010/04/23)

AMINO-PYRIDINE DERIVATIVES AS S1P1 /EDG1 RECEPTOR AGONISTS
The invention relates to novel amino-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Page/Page column 13

(2010/04/30)

P2X3, RECEPTOR ANTAGONISTS FOR TREATMENT OF PAIN
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.
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Page/Page column 79

(2010/11/18)

PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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.
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Page/Page column 53-54

(2009/04/25)

Development of a scalable synthesis of dipeptidyl peptidase-4 inhibitor ABT-279
A convergent, scalable synthesis of dipeptidyl peptidase-4 inhibitor, ABT-279, has been developed and demonstrated on multikilogram scale. The cis-2,5-disubstituted pyrrolidine is generated by cyclization of a Boc-amine onto an alkynyl ketone followed by stereospecific reduction of the resulting acyliminium intermediate. The amine coupling partner was prepared by a novel Hofmann rearrangement promoted by 1,3-dibromo-5,5-dimethylhydantoin. The final product was isolated as the L-malic acid salt. The scaleup campaign consisted of 15 steps and delivered 42 kg of ABT-279 in 14% overall yield. A second-generation synthesis that addresses some of the issues encountered during scale-up was developed and demonstrated on kilogram scale.
McDermott, Todd S.,Bhagavatula, Lakshmi,Borchardt, Thomas B.,Engstrom, Kenneth M.,Gandarilla, Jorge,Kotecki, Brian J.,Kruger, Albert W.,Rozema, Michael J.,Sheikh, Ahmad Y.,Wagaw, Seble H.,Wittenberger, Steven J.
experimental part
p. 1145 - 1155
(2010/04/22)

PYRIDIN-4-YL DERIVATIVES AS IMMUNOMODULATING AGENTS
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.
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Page/Page column 38-39

(2008/06/13)

AMINO- PYRIDINE DERIVATIVES AS S1P1 /EDG1 RECEPTOR AGONISTS
The invention relates to novel amino-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Page/Page column 31

(2008/12/07)

SYNTHESIS OF (2S,5R)-5-ETHYNYL-1-{N-(4-METHYL-1-(4-CARBOXY-PYRIDIN-2-YL)PIPERIDIN-4-YL)GLYCYL}PYRROLIDINE-2-CARBONITRILE
A process for making (2S,5R)-5-ethynyl-1-{N-(4-methyl-1-(4-carboxy-pyridin-2-yl)piperidin-4-yl)glycyl}pyrrolidine-2-carbonitrile and salts thereof, and intermediates used in the process are disclosed.
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Page/Page column 37-38

(2008/06/13)

BACE INHIBITORS
The present invention provides BACE inhibitors of Formula (I): methods for their use and preparation, and intermediates for their preparation.
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Page/Page column 76

(2008/06/13)

Aminopyrimidine and aminopyridine anti-inflammation agents
Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.
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(2008/06/13)