SG11202000441QA - Process for the preparation of n-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide - Google Patents

Process for the preparation of n-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide

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Publication number
SG11202000441QA
SG11202000441QA SG11202000441QA SG11202000441QA SG11202000441QA SG 11202000441Q A SG11202000441Q A SG 11202000441QA SG 11202000441Q A SG11202000441Q A SG 11202000441QA SG 11202000441Q A SG11202000441Q A SG 11202000441QA SG 11202000441Q A SG11202000441Q A SG 11202000441QA
Authority
SG
Singapore
Prior art keywords
squibb
bristol
drive
new jersey
new
Prior art date
Application number
SG11202000441QA
Inventor
Burcu Selin Aytar
Alina Borovika
Collin Chan
Joerg Deerberg
Nathan R Domagalski
Martin D Eastgate
Yu Fan
Michael David Bengt Fenster
Robert V Forest
Francisco Gonzalez-Bobes
Rebecca A Green
Matthew R Hickey
Nathaniel David Kopp
Cruz Thomas E La
Kathleen Lauser
Hong Geun Lee
David K Leahy
Helen Y Luo
Thomas M Razler
Scott A Savage
Chris Sfouggatakis
Maxime C D Soumeillant
Serge Zaretsky
Bin Zheng
Ye Zhu
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of SG11202000441QA publication Critical patent/SG11202000441QA/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/22—Esters of monothiocarboxylic acids having carbon atoms of esterified thiocarboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-Pyrrolidones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Title: PROCESS FOR THE PREPARATION OF N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRA- ZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-0XOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE (57) : The invention generally relates to an improved process for the preparation of N-((lR,2S,5R)-5-(tert-butylamino)-24(S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2- oxopyrrolidin- 1 -yl)cyclohexyl)acetamide, as well as novel inteiinediates employed in the process, which may be useful for the treatment of cancer. N N N ( N H N O (12) INTERNATIONAL APPLICATION PUBLISHED (19) World Intellectual Property Organization International Bureau UNDER THE PATENT COOPERATION TREATY (PCT) vitivio VIII 00 los OH u oimIE (10) International Publication Number WO 2019/018592 A2 PCT (43) International Publication Date 24 January 2019 (24.01.2019) WIP0 I New Brunswick, New Jersey 08903 (US). GREEN, Rebec- ca A.; c/o Bristol-Myers Squibb Company, 1 Squibb Dri- ve, New Brunswick, New Jersey 08903 (US). HICKEY, Matthew R.; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). KOPP, Nathaniel David; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). LA CRUZ, Thomas E.; c/o Bristol-Myers Squibb Com- pany, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). LAUSER, Kathleen; c/o Bristol-Myers Squibb Com- pany, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). LEE, Hong Geun; Seoul National University, De- partment of Chemistry 503-620, 1 Gwanak-Ro Gwanak-Gu, Seoul 08826 (KR). LEAHY, David K.; 10 Ida Road, Mar- blehead, MA 01945 (US). LUO, Helen Y.; c/o Bristol-My- ers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). RAZLER, Thomas M.; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). SAVAGE, Scott A.; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). SFOUGGATAKIS, Chris; c/o Bristol-Myers Squibb Company, 1 Squibb Dri- ve, New Brunswick, New Jersey 08903 (US). SOUMEIL- LANT, Maxime C.D.; c/o Bristol-Myers Squibb Compa- ny, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). ZARETSKY, Serge; c/o Bristol-Myers Squibb Com- pany, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). ZHENG, Bin; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). ZHU, Ye; 111 Clementi Road, #07-02, Singapore 129792 (SG). (74) Agent: KORSEN, Elliott et al.; Bristol-Myers Squibb Company, Route 206 & Province Line Road, Princeton, New Jersey 08543 (US). (51) International Patent Classification: C07D 235/06 (2006.01) (21) International Application Number: PCT/US2018/042797 (22) International Filing Date: 19 July 2018 (19.07.2018) English English (25) Filing Language: (26) Publication Language: (30) Priority Data: 62/534,908 20 July 2017 (20.07.2017) US (71) Applicant: BRISTOL-MYERS SQUIBB COMPANY [US/US]; Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). (72) Inventors: AYTAR, Burcu Selin; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). BOROVIKA, Anna; c/o Bristol-My- ers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). CHAN, Collin; c/o Bristol-My- ers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). DEERBERG, Joerg; 11 Iron- gate Court, Columbus, New Jersey 08022 (US). DO- MAGALSKI, Nathan R.; 33 Bush Hill Drive, Niantic, Connecticut 0637 (US). EASTGATE, Martin D.; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). FAN, Yu; 603 S. 5th Avenue, Highland Park, New Jersey 08904 (US). FENSTER, Michael David Bengt; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). FOREST, Robert V.; c/o Bristol-My- ers Squibb Company, 1 Squibb Drive, New Brunswick, New Jersey 08903 (US). GONZALEZ-BOBES, Francis- co; c/o Bristol-Myers Squibb Company, 1 Squibb Drive, W O 20 19/0 185 9 2 A2 (I) [Continued on next page] WO 2019/018592 IIIIIIIIIIIIIIIII IIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIII (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) Published: without international search report and to be republished upon receipt of that report (Rule 48.2(g))
SG11202000441QA 2017-07-20 2018-07-19 Process for the preparation of n-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide SG11202000441QA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762534908P 2017-07-20 2017-07-20
PCT/US2018/042797 WO2019018592A2 (en) 2017-07-20 2018-07-19 Process for the preparation of n-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide

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CN (1) CN110933946A (en)
AU (1) AU2018304290B2 (en)
BR (1) BR112020000418A2 (en)
CA (1) CA3070423A1 (en)
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CA3088542A1 (en) * 2018-01-22 2019-07-25 Bristol-Myers Squibb Company Compositions and methods of treating cancer

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* Cited by examiner, † Cited by third party
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JP4546923B2 (en) * 2003-05-30 2010-09-22 チョンウェ ファーマ コーポレーション Beta-strand mimetics and related methods
US7629351B2 (en) * 2006-07-28 2009-12-08 Bristol-Myers Squibb Company N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide and other modulators of chemokine receptor activity, crystalline forms and process
US7671062B2 (en) * 2006-07-28 2010-03-02 Bristol-Myers Squibb Company Modulators of chemokine receptor activity, crystalline forms and process
CN100593536C (en) * 2007-01-09 2010-03-10 吉尔生化（上海）有限公司 Method for synthesizing N-fluorene methoxycarbonyl-N-trityl-D-glutamine
US8383812B2 (en) * 2009-10-13 2013-02-26 Bristol-Myers Squibb Company N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes
EP3974563A1 (en) * 2011-12-28 2022-03-30 Chugai Seiyaku Kabushiki Kaisha Cyclic peptides

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LT3655395T (en) 2022-03-10
IL272034A (en) 2020-03-31
IL272034B (en) 2022-06-01
JP2020527576A (en) 2020-09-10
CN110933946A (en) 2020-03-27
PL3655395T3 (en) 2022-03-07
US11254679B2 (en) 2022-02-22
RS62941B1 (en) 2022-03-31
CY1125023T1 (en) 2023-03-24
EP3655395A2 (en) 2020-05-27
AU2018304290B2 (en) 2022-11-17
DK3655395T3 (en) 2022-03-07
ES2907640T3 (en) 2022-04-25
US20200223852A1 (en) 2020-07-16
AU2018304290A8 (en) 2020-04-02
AU2018304290A1 (en) 2020-03-05
CA3070423A1 (en) 2019-01-24
SI3655395T1 (en) 2022-04-29
HUE058049T2 (en) 2022-06-28
PT3655395T (en) 2022-02-22
HRP20220264T1 (en) 2022-05-13
KR20200031656A (en) 2020-03-24
IL293088A (en) 2022-07-01
WO2019018592A2 (en) 2019-01-24
HRP20220264T8 (en) 2022-05-27
EP3655395B1 (en) 2021-12-01
US20220177482A1 (en) 2022-06-09
WO2019018592A3 (en) 2019-02-28
EA202090346A1 (en) 2020-08-18
BR112020000418A2 (en) 2020-07-14

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