SG11201803489SA - 4-(biphen-3-yl)-1h-pyrazolo[3,4-c]pyridazine derivatives of formula (i) as gaba receptor modulators for use in the treatment of epilepsy and pain - Google Patents

4-(biphen-3-yl)-1h-pyrazolo[3,4-c]pyridazine derivatives of formula (i) as gaba receptor modulators for use in the treatment of epilepsy and pain

Info

Publication number
SG11201803489SA
SG11201803489SA SG11201803489SA SG11201803489SA SG11201803489SA SG 11201803489S A SG11201803489S A SG 11201803489SA SG 11201803489S A SG11201803489S A SG 11201803489SA SG 11201803489S A SG11201803489S A SG 11201803489SA SG 11201803489S A SG11201803489S A SG 11201803489SA
Authority
SG
Singapore
Prior art keywords
international
rule
pyrazolo
epilepsy
formula
Prior art date
Application number
SG11201803489SA
Inventor
Robert Mckenzie Owen
David Cameron Pryde
Kevin Neil Dack
Original Assignee
Pfizer Ltd
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 Pfizer Ltd filed Critical Pfizer Ltd
Publication of SG11201803489SA publication Critical patent/SG11201803489SA/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 15 June 2017 (15.06.2017) WIPOIPCT (10) International Publication Number WO 2017/098367 A1 (51) International Patent Classification: C07D 487/04 (2006.01) A61P 25/00 (2006.01) A61K31/5025 (2006.01) (21) International Application Number: PCT/IB2016/05 7049 (22) International Filing Date: (25) Filing Language: (26) Publication Language 22 November 2016 (22.11.2016) English English (30) Priority Data: 62/265,572 10 December 2015 (10.12.2015) US (71) Applicant: PFIZER LIMITED [GB/GB]; 748 Ramsgate Road, Sandwich Kent CT13 9NJ (GB). (72) Inventors: OWEN, Robert McKenzie; c/o Neusentis, Portway Building, Granta Park, Great Abington Cambridge CB21 6GS (GB). PRYDE, David Cameron; c/o Neusentis, Portway Building, Granta Park, Great Abington Cambridge CB21 6GS (GB). DACK, Kevin Neil; c/o Pf­ izer Limited, Ramsgate Road, Sandwich Kent CT13 9NJ (GB). (74) Agent: LANE, Graham M .; Pfizer Limited, 748 Ramsgate Road, Sandwich Kent CT13 9NJ (GB). (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, JP, KE, KG, 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 the identity of the inventor (Rule 4.17(i)) as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: with international search report (Art. 21(3)) < 00 ON n O (54) Title: 4-(BIPHEN-3-YL)-lH-PYRAZOLO[3,4-C]PYRIDAZINE DERIVATIVES OF FORMULA (I) AS GABA RECEPTOR MODULATORS FOR USE IN THE TREATMENT OF EPILEPSY AND PAIN R (I) (57) : The present invention relates to pyrazolopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-lH- pyrazolo[3,4-c]pyridazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined in the description. The pyrazolopyridazine derivatives of the present invention modulate the activity of the GABAA re­ ceptor. They may useful in the treatment of a number of conditions, including pain and epilepsy.
SG11201803489SA 2015-12-10 2016-11-22 4-(biphen-3-yl)-1h-pyrazolo[3,4-c]pyridazine derivatives of formula (i) as gaba receptor modulators for use in the treatment of epilepsy and pain SG11201803489SA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562265572P 2015-12-10 2015-12-10
PCT/IB2016/057049 WO2017098367A1 (en) 2015-12-10 2016-11-22 4-(biphen-3-yl)-1h-pyrazolo[3,4-c]pyridazine derivatives of formula (i) as gaba receptor modulators for use in the treatment of epilepsy and pain

Publications (1)

Publication Number Publication Date
SG11201803489SA true SG11201803489SA (en) 2018-06-28

Family

ID=57485832

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201803489SA SG11201803489SA (en) 2015-12-10 2016-11-22 4-(biphen-3-yl)-1h-pyrazolo[3,4-c]pyridazine derivatives of formula (i) as gaba receptor modulators for use in the treatment of epilepsy and pain

Country Status (6)

Country Link
US (1) US10538523B2 (en)
EP (1) EP3386983A1 (en)
JP (1) JP2018536677A (en)
CA (1) CA3007595C (en)
SG (1) SG11201803489SA (en)
WO (1) WO2017098367A1 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022011091A1 (en) * 2020-07-09 2022-01-13 Usher Iii Initiative, Inc. Treatment of cancer, inflammatory diseases and autoimmune diseases
CN116693555A (en) * 2022-02-25 2023-09-05 上海赛默罗生物科技有限公司 Imidazopyridazine derivative, preparation method, pharmaceutical composition and application thereof

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (en) 1990-01-23 1999-01-15 . Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035298A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing gum containing medicament active agents
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
GB9801210D0 (en) * 1998-01-21 1998-03-18 Merck Sharp & Dohme Therapeutic agents
TWI248936B (en) * 2001-03-21 2006-02-11 Merck Sharp & Dohme Imidazo-pyrimidine derivatives as ligands for GABA receptors
GB0210124D0 (en) * 2002-05-02 2002-06-12 Merck Sharp & Dohme Therapeutic agents
GB0212048D0 (en) * 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
US8357711B2 (en) 2007-03-23 2013-01-22 Pfizer Limited Heterocyclic sulfonamides as inhibitors of ion channels
BRPI1006128A2 (en) 2009-01-12 2016-11-01 Cagen Inc sulfonamide derivatives
UA112028C2 (en) * 2012-12-14 2016-07-11 Пфайзер Лімітед IMIDAZOPYRIDASINE DERIVATIVES AS HAMBA-RECEPTOR MODULATORS
JP6491679B2 (en) 2014-06-12 2019-03-27 ファイザー・リミテッドPfizer Limited Imidazopyridazine derivatives as modulators of GABA A receptor activity

Also Published As

Publication number Publication date
EP3386983A1 (en) 2018-10-17
CA3007595C (en) 2020-08-25
CA3007595A1 (en) 2017-06-15
WO2017098367A1 (en) 2017-06-15
JP2018536677A (en) 2018-12-13
US10538523B2 (en) 2020-01-21
US20180346470A1 (en) 2018-12-06

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