Patents by Inventor Alexei Kalinin
Alexei Kalinin has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 11649243Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.Type: GrantFiled: August 11, 2021Date of Patent: May 16, 2023Assignee: Merck Sharp & Dohme Corp.Inventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
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Publication number: 20220073523Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.Type: ApplicationFiled: August 11, 2021Publication date: March 10, 2022Inventors: Feng XU, Zhuqing LIU, Richard DESMOND, Jeonghan PARK, Alexei KALININ, Birgit KOSJEK, Hallena STROTMAN, Hongmei LI, Johannah MONCECCHI
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Patent number: 11091493Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KED) biocatalyst enzymes and methods of using the biocatalysts.Type: GrantFiled: June 26, 2020Date of Patent: August 17, 2021Assignee: Merck Sharp & Dohme Corp.Inventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
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Publication number: 20200392141Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.Type: ApplicationFiled: June 26, 2020Publication date: December 17, 2020Inventors: Feng XU, Zhuqing LIU, Richard Desmond, Jeonghan PARK, Alexei KALININ, Birgit KOSJEK, Hallena STROTMAN, Hongmei LI, Johannah MONCECCHI
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Patent number: 10696681Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.Type: GrantFiled: March 11, 2019Date of Patent: June 30, 2020Assignee: MERCK SHARP & DOHME CORPORATIONInventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
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Patent number: 10457690Abstract: The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.Type: GrantFiled: June 3, 2016Date of Patent: October 29, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Jingjun Yin, Tetsuji Itoh, Jianguo Yin, Bangping Xiang, Kevin R. Campos, Alexei Kalinin, Zhuqing Liu, Melodie Deniz Christensen, Kevin M. Belyk, Richard J. Varsolona, Andrew Brunskill
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Publication number: 20190194211Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.Type: ApplicationFiled: March 11, 2019Publication date: June 27, 2019Inventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
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Patent number: 10287289Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of I-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.Type: GrantFiled: March 12, 2014Date of Patent: May 14, 2019Assignee: MERCK SHARP & DOHME CORP.Inventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
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Publication number: 20180179223Abstract: The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.Type: ApplicationFiled: June 3, 2016Publication date: June 28, 2018Applicant: MERCK SHARP & DOHME CORP.Inventors: Jingjun Yin, Tetsuji Itoh, Jianguo Yin, Bangping Xiang, Kevin R. Campos, Alexei Kalinin, Zhuqing Liu, Melodie Deniz Christensen, Kevin M. Belyk, Richard J. Varsolona, Andrew Brunskill
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Publication number: 20170145014Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of 1-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.Type: ApplicationFiled: March 12, 2014Publication date: May 25, 2017Applicant: MERCK SHARP & DOHME CORP.Inventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
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Patent number: 7897777Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride which includes (i) resolving a racemic mixture of racemic threo-methylphenidate hydrochloride with a less than stoichiometric amount of tertiary amine base to obtain a methylphenidate-chiral acid salt, (ii) basifying the methylphenidate-chiral acid salt to obtain methylphenidate free base, and (iii) converting the methylphenidate free base into d-threo-methylphenidate hydrochloride.Type: GrantFiled: January 5, 2007Date of Patent: March 1, 2011Assignee: Archimica, Inc.Inventors: Alexei Kalinin, Guofang Qiu, Thomas J. Marren, James E. Aldred, Jr., Yu Ji
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Publication number: 20080167470Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride which includes (i) resolving a racemic mixture of racemic threo-methylphenidate hydrochloride with a less than stoichiometric amount of tertiary amine base to obtain a methylphenidate-chiral acid salt, (ii) basifying the methylphenidate-chiral acid salt to obtain methylphenidate free base, and (iii) converting the methylphenidate free base into d-threo-methylphenidate hydrochloride.Type: ApplicationFiled: January 5, 2007Publication date: July 10, 2008Inventors: Alexei Kalinin, Guofang Qiu, Thomas J. Marren, James E. Aldred, Yu Ji
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Patent number: 7196219Abstract: A process for preparing anilineboronic acid derivative of the formula I, by converting an aniline to a diprotected aniline by introducing two protecting groups, metalating the diprotected aniline with a metalating agent and simultaneously or subsequently reacting with a boronic ester B(OR1,2,3)3 to form a protected anilineboronic ester, which is converted, by detaching the protecting groups, to the anilineboronic esters of the formula (I).Type: GrantFiled: May 14, 2004Date of Patent: March 27, 2007Assignee: Archimica GmbHInventors: Stefan Scherer, Andreas Meudt, Bernd Lehnemann, Alexei Kalinin, Victor Snieckus
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Publication number: 20050038287Abstract: A process for preparing anilineboronic acid derivatives of the formula I, by converting an aniline (II) to a diprotected aniline (III) by introducing two protecting groups PG, metalating (III) and simultaneously or subsequently reacting with a boronic ester B(OR1,2,3)3 (IV) to a protected anilineboronic ester of the formula (V), which is converted, by detaching the protecting groups PG, to the anilineboronic esters of the formula (I) Step 1: Protection of the Aniline by Dibenzylation Step 2: Metalation of the Protected Aniline, Conversion to Boronic Acid Derivative Step 3: Detachment of the Protecting Group where R is for example, H, F, Cl, Br, I, a, C1-C20—,alkyl or -alkoxy radical, a C6-C12-aryl or -aryloxy radical, a heteroaryl or heteroaryloxy radical, a C3-C8-cycloalkyl radical; X is H, Cl, Br, I or F; R1, R2, R3 are each independently H, a C1-C20-alkyl group, and two R1-3 radicals together may optionally form a ring, or are each further B(OR)3 radicals.Type: ApplicationFiled: May 14, 2004Publication date: February 17, 2005Inventors: Stefan Scherer, Andreas Meudt, Bernd Lehnemann, Alexei Kalinin, Victor Snieckus
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Patent number: 6855848Abstract: A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant: in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents R1 to R6 having the following meanings: R114 R6 are H, aryl or substituted or unsubstituted C1-C4-alkyl or two radicals R may be closed to form a cyclic system. As oxidant, it is possible to use, for example, alkyl halides or dialkyl sulfates. In a particularly preferred embodiment, the diene used is 2,5-dimethylhexa-2,4-diene (R1, R2, R5, R6=methyl, R3, R4=H).Type: GrantFiled: August 28, 2003Date of Patent: February 15, 2005Assignee: Clariant GmbHInventors: Stefan Scherer, Alexei Kalinin, Victor Snieckus
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Patent number: 6706925Abstract: A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents R1 to R6 having the following meanings: R1-R6 are H, aryl or substituted or unsubstituted C1-C4-alkyl or two radicals R may be closed to form a cyclic system. As oxidant, it is possible to use, for example, alkyl halides or dialkyl sulfates. In a particularly preferred embodiment, the diene used is 2,5-dimethylhexa-2,4-diene (R1, R2, R5, R6=methyl, R3, R4=H).Type: GrantFiled: September 6, 2002Date of Patent: March 16, 2004Assignee: Clariant GmbHInventors: Stefan Scherer, Alexei Kalinin, Victor Snieckus
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Publication number: 20040039233Abstract: A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant 1Type: ApplicationFiled: August 28, 2003Publication date: February 26, 2004Applicant: Clariant GmbHInventors: Stefan Scherer, Alexei Kalinin, Victor Snieckus
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Publication number: 20030096995Abstract: A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant 1Type: ApplicationFiled: September 6, 2002Publication date: May 22, 2003Applicant: Clariant GmbHInventors: Stefan Scherer, Alexei Kalinin, Victor Snieckus