cas 1306760-87-1, Benzonitrile, 5-[3-[(1S)-2,3-dihydro-1-[(2-hydroxyethyl)aMino]-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-(1-Methylethoxy)- (free base)

Articles about 1306760-87-1Total 13 be found

Enantioselective Synthesis of Ozanimod, the Active Pharmaceutical Ingredient of a New Drug for Multiple Sclerosis
We report here a short enantioselective synthesis of Ozanimod, a potent modulator of the enzyme Sphingosine-1-phosphate receptor (S1PR), recently approved by FDA and EMA for the treatment of relapsing-remitting multiple sclerosis. Amongst different synthetic approaches explored, we achieved the best result introducing the stereogenic centre in the last step through imine asymmetric transfer hydrogenation (ATH) using Wills’ catalysts. Besides the reduced numbers of enantiomeric purity controls required, this process culminates in an exceptionally high enantioselective reductive amination obtained with commercially available tethered Ru catalysts. Starting from commercially available 4-cyano-indanone, enantiomerically pure Ozanimod was obtained in 5 steps in 62 % overall yield and 99 % ee.
Cianferotti, Claudio,Barreca, Giuseppe,Bollabathini, Venkatesh,Carcone, Luca,Grainger, Damian,Staniland, Samantha,Taddei, Maurizio
p. 1924 - 1930
(2021/04/05)

IMPROVED PROCESS FOR PREPARING OZANIMOD
The present invention relates to the process of preparation of compound of formula (I) or a salt thereof. Further it relates to the solid form of compound (I).
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Page/Page column 9-10

(2021/02/12)

PROCESS FOR THE PREPARATION OF SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST
Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process.
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Page/Page column 61-63

(2020/05/13)

A PROCESS FOR THE PREPARATION OF OZANIMOD AND ITS INTERMEDIATE (S)-1-AMINO-2,3-DIHYDRO-1H-INDENE-4-CARBONITRILE
The present invention relates to an improved process for preparation of Ozanimod (I) or pharmaceutically acceptable salts thereof. The present invention also relates to an improved process for preparation of (S)-l-amino-2,3-dihydro- 1H-indene-4-carbonitrile (II) or its optically active acid salts.
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Page/Page column 18-20

(2020/05/07)

IMPROVED PROCESS FOR PREPARING OZANIMOD
The presented invention relates to a process for preparation of compound of formula (1) or a salt thereof (i.e.) ozanimod : (1). The invention also relates to intermediates used in the process.
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(2020/07/04)

IMPROVED PROCESS FOR THE PREPARATION OF OZANIMOD Α-AMINO COMPOUND
The present invention relates to an improved process for the preparation of optically chiral amino compound. The present invention particularly relates to the improved process for the preparation of (S)-1-amino-2,3-dihydro-1H-indene-4-carbonitrile, an important intermediate for the synthesis of ozanimod. The present invention more particularly relates to preparation of (S)-1-amino-2,3-dihydro-1H-indene-4- carbonitrile using 4-cyano-1-indanone and α-methylbenzylamine derivatives as starting materials. The present invention specifically relates to preparation of (S)-1- amino-2,3-dihydro-1H-indene-4-carbonitrile comprising diastereoselective chiral amine synthesis by protection with chiral auxiliary ?-methyl benzylamine derivatives followed by reduction and debenzylation.
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(2019/04/16)

SALTS AND SOLID STATE FORMS OF OZANIMOD
Disclosed are Ozanimod solid state forms, salts including hydrochloride and solid state thereof, processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
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Paragraph 00115

(2019/05/30)

CRYSTALLINE FORMS OF OZANIMOD AND OZANIMOD HYDROCHLORIDE, AND PROCESSES FOR PREPARATION THEREOF
The present disclosure is directed to novel crystalline forms of ozanimod and ozanimod hydrochloride, as well as preparation method thereof. Said crystalline forms of ozanimod and ozanimod hydrochloride can be used for treating autoimmune diseases, partic
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Paragraph 0178; 0180

(2019/11/19)

PROCESS FOR THE PRODUCTION OF OZANIMOD
The present invetion relates a new process for the preparation of ozanimod of the formula and acid addition salts, via new intermediates and a new polimop form of ozanimod base.
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Page/Page column 31; 32

(2018/12/13)

COMPOUNDS AND METHODS FOR TREATING LUPUS
Methods for treatment of systemic lupus erythematosus (SLE" or "Lupus") by administration of a modulator of sphingosine-1-phosphate receptor subtype 1 (S1P1), as well as compositions and methods related to the same, wherein such S1P1 modulators have the f
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Page/Page column 70; 71; 72; 73

(2018/04/17)

DEUTERIUM-SUBSTITUTED OXADIAZOLES
Described are deuterated modulators of S1P1 receptors, pharmaceutical compositions thereof, and methods of use thereof.
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(2016/10/31)

SELECTIVE SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND COMBINATION THERAPY THEREWITH
Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided, including compounds which modulate subtype 1 of the S1P receptor, and methods of their therapeutic and/or prophylactic use in combination with at least one other medicament adapted for treatement of a malcondition for which activation of S1P1 is medically indicated, such as multiple sclerosis.
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Page/Page column 97-99

(2015/05/19)

NOVEL MODULATORS OF SPHINGOSINE PHOSPHATE RECEPTORS
Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds
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Page/Page column 170-171

(2010/01/07)