SG11201903908PA - Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof - Google Patents

Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof

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Publication number
SG11201903908PA
SG11201903908PA SG11201903908PA SG11201903908PA SG11201903908PA SG 11201903908P A SG11201903908P A SG 11201903908PA SG 11201903908P A SG11201903908P A SG 11201903908PA SG 11201903908P A SG11201903908P A SG 11201903908PA SG 11201903908P A SG11201903908P A SG 11201903908PA
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Singapore
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sanofi
boetie
paris
co7d
rue
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SG11201903908PA
Inventor
Monsif Bouaboula
Maurice Brollo
Victor Certal
Youssef El-Ahmad
Bruno Filoche-Romme
Frank Halley
Gary Mccort
Laurent Schio
Michel Tabart
Corinne Terrier
Fabienne Thompson
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Sanofi Sa
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Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of SG11201903908PA publication Critical patent/SG11201903908PA/en

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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
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    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—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 no double bonds between ring members or between ring members and non-ring members 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
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111 IOU 0 11101 010 11111 OIE 10001101111113 OIE 1011 00 111110 HOED Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/091153 Al 24 May 2018 (24.05.2018) WIP0 1 PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every CO7D 403/12 (2006.01) CO7D 411/12 (2006.01) kind of national protection available): AE, AG, AL, AM, CO7D 401/14 (2006.01) CO7D 471/04 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CO7D 405/14 (2006.01) CO7D 207/12 (2006.01) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, CO7D 413/14 (2006.01) A61K 31/4025 (2006.01) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, CO7D 401/12 (2006.01) A61P 35/00 (2006.01) HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, CO7D 405/12 (2006.01) A61P 37/00 (2006.01) KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, CO7D 409/12 (2006.01) A61P 5/32 (2006.01) MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, CO7D 409/14 (2006.01) A61P 19/10 (2006.01) OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (21) International Application Number: SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, PCT/EP2017/068446 TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (22) International Filing Date: (84) Designated States (unless otherwise indicated, for every 21 July 2017 (21.07.2017) kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (25) Filing Language: English UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (26) Publication Language: English 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, (30) Priority Data: MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, 16306506.3 17 November 2016 (17.11.2016) EP TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). — (71) Applicant: SANOFI [FR/FR]; 54 me La Boetie, 75008 PARIS (FR). Declarations under Rule 4.17: = Inventors: BOUABOULA, Monsif; c/o Sanofi, Patent — of inventorship (Rule 4.17(iv)) (72) Department, Mail Stop: 55A-505A, 55 Corporate Drive, Published: Bridgewater, New Jersey 08807 (US). BROLLO, Mau- rice; c/o Sanofi, Patent Department, 54 rue La Boetie, 75008 — with international search report (Art. 21(3)) = _ PARIS (FR). CERTAL, Victor; c/o Sanofi, Patent De- = 54 me La Boetie, 75008 PARIS (FR). EL-AH- _ _ partment, MAD, Youssef; c/o Sanofi, Patent Department, 54 rue La Boetie, 75008 PARIS (FR). FILOCHE-ROMME, Bruno; c/o Sanofi, 54 rue La Boetie, 75008 PARIS (FR). HAL- — _ = LEY, Frank; c/o Sanofi, 54 me La Boetie, 75008 PARIS (FR). MCCORT, Gary; c/o Sanofi, 54 rue La Boetie, 75008 PARIS (FR). SCHIO, Laurent; c/o Sanofi, 54 rue = = La Boetie, 75008 PARIS (FR). TABART, Michel; c/o Sanofi, 54 me La Boetie, 75008 PARIS (FR). TERRIER, Corinne; c/o Sanofi, 54 me La Boetie, 75008 PARIS (FR). = _ THOMPSON, Fabienne; c/o Sanofi, 54 rue La Boetie, 75008 PARIS (FR). = = = Agent: ROMANOWSKI, Caroline; c/o Sanofi, Patent De- (74) = partment, 54 rue La Boetie, 75008 PARIS (FR). = Title: NOVEL SUBSTITUTED N-(3-FLUOROPROPYL)-PYRROLIDINE COMPOUNDS, PROCESSES FOR THEIR — (54) - PREPARATION AND THERAPEUTIC USES THEREOF (57) : The present invention relates to novel substituted N-(3-fluoro- en in propy1)-pyrrolidine compounds of formula (1-A): wherein R1 and R2 represent indepen- R2 R1 1-1 dently a hydrogen atom or a deuterium atom; A represents an oxygen or nitrogen atom; 1-1 N and SERM-F represents a selective estrogen receptor modulator fragment comprising an 01 0 --.... aryl or heteroaryl group linked to the adjacent \"A\" group. The invention also relates to the A preparation and to the therapeutic uses of the compounds of formula (1-A) as inhibitors 1-1 / and degraders of estrogen receptors. cz ei SERM-F (I-A) O
SG11201903908PA 2016-11-17 2017-07-21 Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof SG11201903908PA (en)

Applications Claiming Priority (2)

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EP16306506 2016-11-17
PCT/EP2017/068446 WO2018091153A1 (en) 2016-11-17 2017-07-21 Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof

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US (2) US11149031B2 (en)
EP (1) EP3541809A1 (en)
JP (1) JP6946430B2 (en)
KR (1) KR102477513B1 (en)
CN (1) CN109963848B (en)
AU (1) AU2017362460B2 (en)
BR (1) BR112019009291A2 (en)
CA (1) CA3043646A1 (en)
IL (1) IL266611B2 (en)
MX (1) MX2019005777A (en)
RU (1) RU2742278C2 (en)
SG (1) SG11201903908PA (en)
WO (1) WO2018091153A1 (en)

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AU2017362460B2 (en) 2016-11-17 2021-07-22 Sanofi Novel substituted N-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof
EP3434272A1 (en) 2017-07-25 2019-01-30 Sanofi Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid
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HUE059362T2 (en) * 2018-09-07 2022-11-28 Sanofi Sa Salts of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylate and preparation process thereof
US20230115865A1 (en) * 2019-10-01 2023-04-13 Sanofi Novel Substituted 6,7-Dihydro-5H-Benzo[7]Annulene Compounds, Processes for Their Preparation and Therapeutic Uses Thereof
US20230348459A1 (en) * 2020-05-15 2023-11-02 Simcere Pharmaceutical Co., Ltd. Pyrrolidine compound and use thereof
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