1213591-14-0Relevant articles and documents
Preparation method of ozanimod intermediate
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, (2021/11/27)
The invention discloses a preparation method of an ozanimod intermediate, which comprises the following four steps: synthesis of 4-cyanoindene oxime, synthesis of N-(4-cyano-3H-indene-1-yl)-acetamide, synthesis of N-(4-cyanoindan-1-yl)-acetamide, and synthesis of (S)-1-amino-2, 3-dihydro-1H-indene-4-formonitrile. The method has the advantages of easily available and cheap raw materials, mild reaction conditions, free of dangerous intermediates and unstable intermediates, and high chiral selectivity.
INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
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, (2021/09/11)
The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
SUBSTITUTED AMINO-PYRIMIDINES
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Page/Page column 26; 28-29, (2021/12/31)
The invention provides novel compounds having the general formula (I), wherein R1, R2, and R3 are as defined herein, compositions including the compounds and methods of using the compounds.
AMINO-PYRIMIDINE CYCLO-AMIDES
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Page/Page column 26; 29, (2021/12/31)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and n are as defined herein, compositions including the compounds and methods of using the compounds.
Enantioselective Synthesis of Ozanimod, the Active Pharmaceutical Ingredient of a New Drug for Multiple Sclerosis
Cianferotti, Claudio,Barreca, Giuseppe,Bollabathini, Venkatesh,Carcone, Luca,Grainger, Damian,Staniland, Samantha,Taddei, Maurizio
, p. 1924 - 1930 (2021/04/05)
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.
AMINO-PYRIMIDINE AMIDES
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Page/Page column 28; 31, (2021/12/31)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein, compositions including the compounds and methods of using the compounds.
A PROCESS FOR THE PREPARATION OF OZANIMOD AND ITS INTERMEDIATE (S)-1-AMINO-2,3-DIHYDRO-1H-INDENE-4-CARBONITRILE
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Page/Page column 19-21, (2020/05/07)
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.
PD-1/PD-L1 INHIBITORS
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Paragraph 0725; 0727, (2020/02/05)
Compounds and methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
IMPROVED PROCESS FOR PREPARING OZANIMOD
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Page/Page column 17, (2020/07/04)
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.
PROCESS FOR THE PREPARATION OF SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST
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, (2020/05/13)
Industrially viable and advantageous processes for the preparation of Ozanimod are described. The invention also discloses the intermediates obtained in the process.