SG11201903305XA - Substituted 6-(1h-pyrazol-1-yl)pyrimidin-4-amine derivatives and uses thereof - Google Patents

Substituted 6-(1h-pyrazol-1-yl)pyrimidin-4-amine derivatives and uses thereof

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Publication number
SG11201903305XA
SG11201903305XA SG11201903305XA SG11201903305XA SG11201903305XA SG 11201903305X A SG11201903305X A SG 11201903305XA SG 11201903305X A SG11201903305X A SG 11201903305XA SG 11201903305X A SG11201903305X A SG 11201903305XA SG 11201903305X A SG11201903305X A SG 11201903305XA
Authority
SG
Singapore
Prior art keywords
wuppertal
international
compounds
strabe
pyrazol
Prior art date
Application number
SG11201903305XA
Inventor
Anja Giese
Jürgen Klar
Alexander Ehrmann
Jens Willwacher
David Engel
Andre Philippe Dieskau
Antje Kahnert
Alexey Gromov
Carsten Schmeck
Niels Lindner
Thomas Müller
Anna Lena Andreevski
Jan Dreher
Karl Collins
Original Assignee
Bayer Ag
Bayer Pharma AG
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 Bayer Ag, Bayer Pharma AG filed Critical Bayer Ag
Publication of SG11201903305XA publication Critical patent/SG11201903305XA/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • A61K31/495—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
    • 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
    • A61K31/535—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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • 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

Abstract

Oco O O () INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 19 April 2018 (19.04.2018) WIPO I PCT (51) International Patent Classification: CO7D 403/14 (2006.01) A61K 31/506 (2006.01) CO7D 471/04 (2006.01) A61K 31/5377 (2006.01) C07D 487/04 (2006.01) A61P 13/12 (2006.01) CO7D 413/14 (2006.01) (21) International Application Number: PCT/EP2017/075630 (22) International Filing Date: 09 October 2017 (09.10.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 16193953.3 14 October 2016 (14.10.2016) EP (71) Applicants: BAYER AKTIENGESELLSCHAFT [DE/DE]; Kaiser-Wilhelm-Allee 1, 51373 Leverkusen (DE). BAYER PHARMA AKTIENGESELLSCHAFT [DE/DE]; Miillerstr. 178, 13353 Berlin (DE). (72) Inventors: GIESE, Anja; Horst-Kohl StraBe 15a, 12157 Berlin (DE). KLAR, Jurgen; Leipziger StraBe 6, 42109 Wuppertal (DE). EHRMANN, Alexander; Am Hausberg 2, 45219 Essen (DE). WILLWACHER, Jens; In den Birken 32, 42113 Wuppertal (DE). ENGEL, David; Schone Aussicht 15, 42369 Wuppertal (DE). DIESKAU, An- dre Philippe; Dr.-Tigges-Weg 19, 42115 Wuppertal (DE). KAHNERT, Antje; Paul-Ehrlich-Str. 10, 42113 Wup- pertal (DE). GROMOV, Alexey; Fuhlrottstr. 9, 40699 Erkrath (DE). SCHMECK, Carsten; Carl-Friedrich-Go- erdeler-StraBe 24, 45472 Millheim (DE). LINDNER, Niels; Bodelschwinghweg 4, 42115 Wuppertal (DE). MULLER, Thomas; Parkstr. 24, 40764 Langenfeld (DE). AN- DREEVSKI, Anna Lena; Altenhofer StraBe 123, 42719 Solingen (DE). DREHER, Jan; Ottenbrucher Str. 24, 42105 Wuppertal (DE). COLLINS, Karl; Fiirstenwall 135, 40215 Diisseldorf (DE). (74) Agent: BIP PATENTS; Alfred-Nobel-Str. 10, 40789 Mon- heim am Rhein NRW (DE). (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: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) Published: — with international search report (Art. 21(3)) (54) Title: SUBSTITUTED 6-(1H-PYRAZOL-1-YL)PYRIMIDIN-4-AMINE DERIVATIVES AND USES THEREOF (57) : The present invention covers substituted 6-(1H-pyrazol-1-yl)pyrimidin-4-amine compounds of general formula (I) as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing phar- maceutical compositions for the treatment or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular and renal diseases, as a sole agent or in combination with other active ingredients. olimion °nolo omoionolomommio oimIE (10) International Publication Number WO 2018/069222 Al
SG11201903305XA 2016-10-14 2017-10-09 Substituted 6-(1h-pyrazol-1-yl)pyrimidin-4-amine derivatives and uses thereof SG11201903305XA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16193953 2016-10-14
PCT/EP2017/075630 WO2018069222A1 (en) 2016-10-14 2017-10-09 Substituted 6-(1h-pyrazol-1-yl)pyrimidin-4-amine derivatives and uses thereof

Publications (1)

Publication Number Publication Date
SG11201903305XA true SG11201903305XA (en) 2019-05-30

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Country Status (28)

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US (2) US11208400B2 (en)
EP (1) EP3526212B1 (en)
JP (1) JP2019532961A (en)
KR (1) KR20190065402A (en)
CN (1) CN110191884A (en)
AR (1) AR109947A1 (en)
AU (1) AU2017341324A1 (en)
BR (1) BR112019007496A2 (en)
CA (1) CA3040166A1 (en)
CL (1) CL2019001004A1 (en)
CO (1) CO2019003761A2 (en)
CR (1) CR20190192A (en)
CU (1) CU24518B1 (en)
DO (1) DOP2019000099A (en)
EA (1) EA201990947A1 (en)
EC (1) ECSP19026563A (en)
GE (1) GEP20217269B (en)
IL (1) IL265923A (en)
JO (1) JOP20190080A1 (en)
MA (1) MA46514A (en)
MX (1) MX2019004347A (en)
PE (1) PE20191549A1 (en)
PH (1) PH12019500808A1 (en)
SG (1) SG11201903305XA (en)
TN (1) TN2019000114A1 (en)
TW (1) TW201825477A (en)
UY (1) UY37444A (en)
WO (1) WO2018069222A1 (en)

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CN115403524A (en) * 2021-05-26 2022-11-29 浙江省化工研究院有限公司 Preparation method of 3-fluoro-pyrazole carboxylate and 3-fluoroalkyl-1-substituted pyrazole-4-carboxylic acid
WO2024061768A1 (en) 2022-09-19 2024-03-28 Basf Se Azole pesticidal compounds

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ECSP19026563A (en) 2019-04-30
CN110191884A (en) 2019-08-30
KR20190065402A (en) 2019-06-11
US11208400B2 (en) 2021-12-28
CO2019003761A2 (en) 2019-04-30
CU20190035A7 (en) 2019-11-04
EA201990947A1 (en) 2019-08-30
PE20191549A1 (en) 2019-10-24
MX2019004347A (en) 2019-07-01
JOP20190080A1 (en) 2019-04-11
WO2018069222A1 (en) 2018-04-19
AR109947A1 (en) 2019-02-06
IL265923A (en) 2019-06-30
PH12019500808A1 (en) 2020-01-20
UY37444A (en) 2018-05-31
BR112019007496A2 (en) 2019-09-10
TW201825477A (en) 2018-07-16
CL2019001004A1 (en) 2019-08-30
AU2017341324A1 (en) 2019-05-02
US20230065629A1 (en) 2023-03-02
CR20190192A (en) 2019-09-02
JP2019532961A (en) 2019-11-14
GEP20217269B (en) 2021-06-25
MA46514A (en) 2019-08-21
TN2019000114A1 (en) 2020-10-05
DOP2019000099A (en) 2019-07-15
EP3526212A1 (en) 2019-08-21
EP3526212B1 (en) 2021-12-22
CU24518B1 (en) 2021-06-08
US20200055842A1 (en) 2020-02-20
CA3040166A1 (en) 2018-04-19

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