SG11201808221QA - 1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4h-pyrazolo[4,3-c]pyridin-4-ones as pde1 inhibitors - Google Patents

1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4h-pyrazolo[4,3-c]pyridin-4-ones as pde1 inhibitors

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Publication number
SG11201808221QA
SG11201808221QA SG11201808221QA SG11201808221QA SG11201808221QA SG 11201808221Q A SG11201808221Q A SG 11201808221QA SG 11201808221Q A SG11201808221Q A SG 11201808221QA SG 11201808221Q A SG11201808221Q A SG 11201808221QA SG 11201808221Q A SG11201808221Q A SG 11201808221QA
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Singapore
Prior art keywords
valby
lundbeck
ottiliavej
pyrazolo
ones
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SG11201808221QA
Inventor
Karsten Juhl
Mikkel Jessing
Morten Langgård
Paulo Vital
Mauro Marigo
Jan Kehler
Lars Rasmussen
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H Lundbeck As
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Publication of SG11201808221QA publication Critical patent/SG11201808221QA/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
    • A61K31/435—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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization M1111101110101011111 HO 11111 0111010 HE 11111 I 1001101111101111011# 11 International Bureau 0.. .... .. ...... ... (10) International Publication Number (43) International Publication Date WO 2017/178350 Al 19 October 2017(19.10.2017) WIPO I PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C07D 487/04 (2006.01) A61K 31/519 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 31/437 (2006.01) 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, (21) International Application Number: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, PCT/EP2017/058332 HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (22) International Filing Date: KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, 7 April 2017 (07.04.2017) MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (25) Filing Language: English RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, (26) Publication Language: English TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: PA201600221 12 April 2016 (12.04.2016) DK (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (71) Applicant: H. LUNDBECK A/S [DK/DK]; Ottiliavej 9, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, 2500 Valby (DK). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (72) Inventors: JUHL, Karsten; H. Lundbeck A/S Ottiliavej 9, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, 2500 Valby (DK). JESSING, Mikkel; H. Lundbeck A/S DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, L Ottiliavej 9, 2500 Valby (DK). LANGGARD, Morten; H. V, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, Lundbeck A/S Ottiliavej 9, 2500 Valby (DK). VITAL, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, Paulo, Jorge, Vieira; H. Lundbeck A/S Ottiliavej 9, 2500 GW, KM, ML, MR, NE, SN, TD, TG). Valby (DK). MARIGO, Mauro; H. Lundbeck A/S Ot- Published: tiliavej 9, 2500 Valby (DK). KEHLER, Jan; H. Lundbeck — with international search report (Art. 21(3)) A/S Ottiliavej 9, 2500 Valby (DK). RASMUSSEN, Lars, Kyhn; H. Lundbeck A/S Ottiliavej 9, 2500 Valby (DK). (54) © ir) M GO IN 11 IN 11 0 ei IN-4-ONES AS PDE1 INHIBITORS R 2 R 3 ....„..„ N ( 0 Y I ) Title: 1,5-DIHYDRO-4H-PYRAZOLO[3,4-D]PYRIMIDIN-4-ONES \ N\" hi . AND 1,5-DIHYDRO-4H-PYRAZOLO[4,3-C]PYRID- (57) : The present invention provides 1,5-di- hydro-4H-pyrazolo [3,4-d]pyrimidin-4-ones and 1,5-di- hydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particu- lar for the treatment of neurodegenerative disorders and psychiatric disorders. O
SG11201808221QA 2016-04-12 2017-04-07 1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4h-pyrazolo[4,3-c]pyridin-4-ones as pde1 inhibitors SG11201808221QA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA201600221 2016-04-12
PCT/EP2017/058332 WO2017178350A1 (en) 2016-04-12 2017-04-07 1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4h-pyrazolo[4,3-c]pyridin-4-ones as pde1 inhibitors

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EP (1) EP3442975B1 (en)
JP (1) JP7093306B2 (en)
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CN (1) CN109071549B (en)
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AU (1) AU2017250431B2 (en)
BR (1) BR112017026278A2 (en)
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CR (1) CR20180470A (en)
CY (1) CY1123269T1 (en)
DK (1) DK3442975T3 (en)
DO (1) DOP2018000201A (en)
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MA (1) MA44656B1 (en)
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NI (1) NI201800092A (en)
PE (1) PE20181853A1 (en)
PH (1) PH12018502168A1 (en)
PL (1) PL3442975T3 (en)
PT (1) PT3442975T (en)
RS (1) RS60714B1 (en)
RU (1) RU2018133391A (en)
SG (1) SG11201808221QA (en)
SI (1) SI3442975T1 (en)
SV (1) SV2018005753A (en)
TN (1) TN2018000321A1 (en)
TW (1) TWI729109B (en)
UA (1) UA121925C2 (en)
WO (1) WO2017178350A1 (en)
ZA (1) ZA201806407B (en)

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SI3442975T1 (en) 2020-10-30
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EP3442975A1 (en) 2019-02-20
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US20190194204A1 (en) 2019-06-27
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UA121925C2 (en) 2020-08-10
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TW201738242A (en) 2017-11-01
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