SG11201806383TA - 6,7-dihydro-5h-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds - Google Patents

6,7-dihydro-5h-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds

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Publication number
SG11201806383TA
SG11201806383TA SG11201806383TA SG11201806383TA SG11201806383TA SG 11201806383T A SG11201806383T A SG 11201806383TA SG 11201806383T A SG11201806383T A SG 11201806383TA SG 11201806383T A SG11201806383T A SG 11201806383TA SG 11201806383T A SG11201806383T A SG 11201806383TA
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Singapore
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international
street
massachusetts
compounds
rule
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SG11201806383TA
Inventor
Thomas Allen Chappie
Nandini Chaturbhai Patel
Patrick Robert Verhoest
Christopher John Helal
Simone Sciabola
Erik Alphie Lachapelle
Travis T Wager
Matthew Merrill Hayward
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Pfizer
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Publication of SG11201806383TA publication Critical patent/SG11201806383TA/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00Drugs for dermatological disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Addiction (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 11M1111101110101011111 HO 111110111010 11111 10011111011100111110111011# International Bureau (43) International Publication Date .......,./ (10) International Publication Number WO 2017/145013 Al 31 August 2017 (31.08.2017) WIPO I PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C07D 498/04 (2006.01) A61K 31/5365 (2006.01) kind CO7D 519/00 (2006.01) A61P 25/00 (2006.01) AO, of national protection available): AE, AG, AL, AM, 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/IB2017/050844 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, 15 February 2017 (15.02.2017) 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: 62/298,657 23 February 2016 (23.02.2016) US (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, New York, New York 10017 (US). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (72) Inventors: CHAPPIE, Thomas Allen; 59 Hemlock Hill TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, Road, Carlisle, Massachusetts 01741 (US). PATEL, DK, LV, Nandini Chaturbhai; 34 Mary Ellen Road, Waban, Mas- EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, sachusetts 02468 (US). VERHOEST, Patrick Robert; 23 TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, Calvin Road, Newton, Massachusetts 02460 (US). GW, KM, ML, MR, NE, SN, TD, TG). HELAL, Christopher John; 18 Elm Street, Mystic, Con- Declarations under Rule 4.17: necticut 06355 (US). SCIABOLA, Simone; 109 River as to Street, Cambridge, Massachusetts 02139 (US). the identity of the inventor (Rule 4.170) LACHAPELLE, Erik Alphie; 69 Richard Brown Drive, — as to applicant's entitlement to apply for and be granted a Uncasville, Connecticut 06382 (US). WAGER, Travis T.; patent (Rule 4. 1700) 465 Washington Street, Apt. 6, Brookline, Massachusetts as to the applicant's entitlement to claim the priority of the 02446 (US). HAYWARD, Matthew Merrill; 3 Pyrus earlier application (Rule 4.17(iii)) Court, Old Lyme, Connecticut 06371 (US). Published: . (74) Agent: WALDRON, Roy F.; Pfizer Inc., 235 East 42nd Street, MS 235/9/S20, New York, NY 10017 (US). — with international search report (Art. 21(3)) Title: 6,7-DIHYDRO-5H-PYRAZOLO[5,1-B][1,3]0XAZINE-2-CARBOXAMIDE COMPOUNDS = (54) R 1 i 0 NO N N — R 2 en ,—, © ir) ii- / R3 ,-1 IN 1-1 (57) : The present invention is directed to PDE4B inhibitors of Formula I: (I) or a pharmaceutically acceptable salt thereof, 0 wherein the substituents R', R 2 , R 3 , and R 'are as defined herein. The invention is also directed to pharmaceutical compositions com- \" prising the compounds, methods of treatment using the compounds, and methods of preparing the compounds.
SG11201806383TA 2016-02-23 2017-02-15 6,7-dihydro-5h-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds SG11201806383TA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662298657P 2016-02-23 2016-02-23
PCT/IB2017/050844 WO2017145013A1 (en) 2016-02-23 2017-02-15 6,7-dihydro-5h-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds

Publications (1)

Publication Number Publication Date
SG11201806383TA true SG11201806383TA (en) 2018-09-27

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SG11201806383TA SG11201806383TA (en) 2016-02-23 2017-02-15 6,7-dihydro-5h-pyrazolo[5,1-b][1,3]oxazine-2-carboxamide compounds

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US (2) US10323042B2 (en)
EP (1) EP3419979B1 (en)
JP (1) JP6837072B2 (en)
KR (1) KR102148587B1 (en)
CN (2) CN108699080B (en)
AU (1) AU2017223132B2 (en)
BR (1) BR112018015191B1 (en)
CA (1) CA3015166C (en)
DK (1) DK3419979T3 (en)
ES (1) ES2775674T3 (en)
HU (1) HUE048658T2 (en)
IL (1) IL260536B (en)
MX (1) MX2018010177A (en)
PL (1) PL3419979T3 (en)
PT (1) PT3419979T (en)
RU (1) RU2719599C2 (en)
SG (1) SG11201806383TA (en)
WO (1) WO2017145013A1 (en)
ZA (1) ZA201804619B (en)

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CN108699080B (en) 2021-05-14
AU2017223132A1 (en) 2018-07-26
WO2017145013A1 (en) 2017-08-31
BR112018015191A2 (en) 2018-12-18
EP3419979B1 (en) 2020-01-29
US10738063B2 (en) 2020-08-11
JP2019505558A (en) 2019-02-28
CA3015166A1 (en) 2018-08-31
HUE048658T2 (en) 2020-07-28
CN113332292A (en) 2021-09-03
DK3419979T3 (en) 2020-03-23
ZA201804619B (en) 2020-12-23
US20190055262A1 (en) 2019-02-21
MX2018010177A (en) 2019-01-21
BR112018015191B1 (en) 2023-10-17
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