cas 1025967-78-5, lifitegrast | Articles data

Articles about 1025967-78-5Total 14 be found

Preparation method of ritast and its intermediate compounds
The present invention relates to a method of preparation of ritast and an intermediate compound thereof. In particular, the present invention relates to a method of synthesis of ritast, a key intermediate for synthesizing tast, a solvate thereof, and a method for hydrolyzing it under alkaline conditions to prepare lithast.
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Paragraph 0130-0135

(2022/01/12)

NOVEL PROCESS FOR THE PREPARATION OF LIFITEGRAST
The present invention relates to a novel process for the preparation of lifitegrast of Formula (I). The present invention further provides a novel process for the purification of lifitegrast of Formula (I).
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Page/Page column 21

(2019/05/02)

A PROCESS FOR THE PREPARATION OF LIFITEGRAST
The present invention provides dibenzylamine salt of Lifitegrast (XV), and diphenylamine salt of Lifitegrast (XVI) and the use of the above salts in the purification process of Lifitegrast (I). The present invention relates to a process for the preparation of Lifitegrast (I).
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(2019/10/23)

AN IMPROVED PROCESS FOR THE PREPARATION OF LIFITEGRAST OR SALTS THEREOF
Disclosed herein is an improved process for the synthesis of lifitegrast or salts thereof with high yields and purity and its use in the therapy.
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Page/Page column 14; 16; 17

(2019/06/13)

PROCESS FOR PREPARATION OF LIFITEGRAST
The present invention relates to a process for the preparation of lifitegrast, a compound of formula I, the process comprising deprotecting a compound of formula III using a Lewis acid. The present invention also relates to lifitegrast organic amine salt, a compound of formula II, process for its preparation and conversion thereof to lifitegrast.
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Paragraph 0211

(2019/04/11)

PROCESSES FOR THE PREPARATION OF (S)-2-(2-(BENZOFURAN-6-CARBONYL)-5,7-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE-6-CARBOXAMIDO)-3-(3-(METHYLSULFONYL)PHENYL) PROPANOIC ACID AND POLYMORPHS THEREOF
The present invention relates to various processes for the preparation of (S)-2-(2- (benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3- (methylsulfonyl)phenyl)propanoic acid represented by the following structural formula-1. The said processes for the preparation of compound of formula-1 proceed through various novel intermediate compounds. The present invention also relates to novel crystalline polymorphs of compound of formula-1 and processes for preparation thereof.
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(2019/03/17)

PROCESS FOR PREPARING AND PURIFYING THE LFA-1 ANTAGONIST LIFITEGRAST
The invention relates to a process for the preparation of lifitegrast (I) comprising a) reacting benzofuran-6-carboxylic acid (II) with a non- chlorinated carboxyl activating agent; and b) reacting the activated compound obtained in step a) with compound (III) or a salt thereof to give lifitegrast. It also relates to a process for the purification of lifitegrast (I) by i) reacting lifitegrast with dicyclohexylamine to give the dicyclohexylamine salt of lifitegrast (la); ii) isolating the salt from the reaction medium; iii) converting the isolated salt into lifitegrast by treatment with an acid; and iv) isolating lifitegrast from the reaction medium. It also relates to the dicyclohexylamine salt of lifitegrast (la) and to a process for its preparation. (Formula I, III)
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Page/Page column 27

(2019/02/13)

PROCESSES FOR PREPARATION OF LIFITEGRAST AND INTERMEDIATES THEREOF
The present invention provides process for preparation of lifitegrast, amine salts of lifitegrast, process for preparation of amine salts of lifitegrast and their use in purification of lifitegrast, and also provided are process for preparation of amorphous lifitegrast and pharmaceutical compositions comprising lifitegrast prepared by the processes of the present invention.
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Page/Page column 20-21

(2019/02/17)

PROCESS FOR PREPARING LIFITEGRAST AND INTERMEDIATES THEREOF
The present disclosure provides efficient, economical, and improved processes for synthesizing lifitegrast and intermediates thereof. The currently discloses processes provide a direct synthetic route, avoiding protection or deprotection steps. The currently disclosed process also provides processes for synthesizing lifitegrast using a reduced number of synthetic steps.
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(2019/01/15)

PROCESS FOR THE PREPARATION OF LIFITEGRAST
The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1- C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.
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(2020/01/08)

Crystal forms of lifitegrast
Crystalline form S1 of lifitegrast characterized by a powder X-ray diffraction pattern with peaks at about 10.7±0.2, 16.2±0.2, 19.9±0.2, 22.1±0.2, 24.7±0.2, and 25.9±0.2 degrees two-theta, crystalline form S2 of lifitegrast characterized by a powder X-ray diffraction pattern with peaks at about 16.4±0.2, 24.9±0.2, and 26.2±0.2 degrees two-theta, and processes of making thereof are provided.
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Page/Page column 4-5

(2019/10/22)

A PROCESS TO OBTAIN A TETRAHYDROISOQUINOLINE DERIVATIVE
The present invention relates to a process for preparing lifitegrast or a salt thereof, wherein the process comprises hydrogenation of compound II in a mixture comprising at least one solvent selected from the group consisting of acetonitrile, a ketone solvent, an ester solvent and a mixture thereof, preferably acetonitrile.
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Page/Page column 14; 15; 16; 17; 18; 19

(2019/06/09)

LFA-1 INHIBITOR AND POLYMORPH THEREOF
Methods of preparation and purification of a compound, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA -1 mediated diseases are also disclosed.
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(2014/02/16)

Discovery and development of potent LFA-1/ICAM-1 antagonist SAR 1118 as an ophthalmic solution for treating dry eye
LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunological synapse, and augmentation of T-cell receptor signaling. The increase of ICAM-1 expression levels in conjunctival epithelial cells and acinar cells was observed in animal models and patients diagnosed with dry eye. Therefore, it has been hypothesized that small molecule LFA-1/ICAM-1 antagonists could be an effective topical treatment for dry eye. In this letter, we describe the discovery of a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist (SAR 1118) and its development as an ophthalmic solution for treating dry eye.
Zhong, Min,Gadek, Thomas R.,Bui, Minna,Shen, Wang,Burnier, John,Barr, Kenneth J.,Hanan, Emily J.,Oslob, Johan D.,Yu, Chul H.,Zhu, Jiang,Arkin, Michelle R.,Evanchik, Marc J.,Flanagan, W. Mike,Hoch, Ute,Hyde, Jennifer,Prabhu, Saileta,Silverman, Jeffrey A.,Wright, Jasmin
p. 203 - 206
(2012/05/04)