SG11201811515WA - Method for producing a polymorphic form of 3-[5-amino-4-(3- cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide - Google Patents

Method for producing a polymorphic form of 3-[5-amino-4-(3- cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide

Info

Publication number
SG11201811515WA
SG11201811515WA SG11201811515WA SG11201811515WA SG11201811515WA SG 11201811515W A SG11201811515W A SG 11201811515WA SG 11201811515W A SG11201811515W A SG 11201811515WA SG 11201811515W A SG11201811515W A SG 11201811515WA SG 11201811515W A SG11201811515W A SG 11201811515WA
Authority
SG
Singapore
Prior art keywords
international
london
methylbenzamide
amino
pyrazol
Prior art date
Application number
SG11201811515WA
Inventor
Osama Suleiman
Lucia Romero Perez
Cornelius Stephan Harlacher
Stewart Jones
Original Assignee
Mereo Biopharma 1 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 Mereo Biopharma 1 Ltd filed Critical Mereo Biopharma 1 Ltd
Publication of SG11201811515WA publication Critical patent/SG11201811515WA/en

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Classifications

    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C07D231/18One oxygen or sulfur atom
    • 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]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111101111 0 1110101011111 011101 0 011111111111111111001111111011111111111 0111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\" WO 2018/011579 Al 18 January 2018 (18.01.2018) W I P0 I P C T (51) International Patent Classification: MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, A61K 31/415 (2006.01) A61P 29/00 (2006.01) TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, CO7D 231/38 (2006.01) KM, ML, MR, NE, SN, TD, TG). (21) International Application Number: PCT/GB2017/052056 Published: — with international search report (Art. 21(3)) (22) International Filing Date: 13 July 2017 (13.07.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1612240.0 14 July 2016 (14.07.2016) GB (71) Applicant: MEREO BIOPHARMA 1 LIMITED [ /GB]; 1 Cavendish Place, London, Greater London W1G OQF (GB). (72) Inventors: SULEIMAN, Osama; Johnson Matthey Plc., Fine Chemicals Division (Pharmorphix), 250 Cambridge _ Science Park, Milton Road, Cambridge Cambridgeshire CB4 OWE (GB). PEREZ, Lucia Romero; Johnson — Matthey Plc., Johnson Matthey Chemical Product, Or- = - chard Road, Royston, Hertfordshire SG8 5HE (GB). HAR- _ LACHER, Cornelius Stephan; Zihlackerstrasse 60, 4153 =_ Reinach (CH). JONES, Stewart; Mereo Biopharma Group plc, 4th Floor, 1 Cavendish Place, London, Greater London = W1G OQF (GB). Agent: GILL JENNINGS & EVERY LLP et al.; The (74) Broadgate Tower, 20 Primrose Street, London, Greater Lon- don EC2A 2ES (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, 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. Designated States (unless otherwise indicated, for every (84) = kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, — 1-1 01 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, IN 1 1 in ,—, ,-1 (54) Title: METHOD FOR PRODUCING A POLYMORPHIC FORM OF 3-[5-AMINO-4-(3- CYANOBENZOYL)-PYRA- 0 ZOL-1-YL]-N-CYCLOPROPYL-4-METHYLBENZAMIDE --.... , 1 (57) : This invention relates to a process for the preparation of Form A of 3-[5-amino-4-(3- cyanobenzoy1)-pyrazol-1-y1]-N- 0 cyclopropyl-4-methylbenzamide. Also disclosed herein is Form A of 345-amino-4-(3-cyanobenzoy1)-pyrazol-1-y1]-N-cyclopropy1-4- el methylbenzamide, or pharmaceutical compositions thereof, obtainable by the process described herein. C
SG11201811515WA 2016-07-14 2017-07-13 Method for producing a polymorphic form of 3-[5-amino-4-(3- cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide SG11201811515WA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1612240.0A GB201612240D0 (en) 2016-07-14 2016-07-14 Method for producing a polymorphic form of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide
PCT/GB2017/052056 WO2018011579A1 (en) 2016-07-14 2017-07-13 Method for producing a polymorphic form of 3-[5-amino-4-(3- cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide

Publications (1)

Publication Number Publication Date
SG11201811515WA true SG11201811515WA (en) 2019-01-30

Family

ID=56890600

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201811515WA SG11201811515WA (en) 2016-07-14 2017-07-13 Method for producing a polymorphic form of 3-[5-amino-4-(3- cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide

Country Status (18)

Country Link
US (2) US10934260B2 (en)
EP (1) EP3484471B1 (en)
JP (1) JP7094021B2 (en)
KR (1) KR102460529B1 (en)
CN (1) CN109414429B (en)
AU (1) AU2017294643B2 (en)
BR (1) BR112019000460A2 (en)
CA (1) CA3030622A1 (en)
DK (1) DK3484471T3 (en)
ES (1) ES2874661T3 (en)
GB (1) GB201612240D0 (en)
HU (1) HUE054539T2 (en)
IL (1) IL263908B (en)
MX (1) MX2019000385A (en)
PL (1) PL3484471T3 (en)
PT (1) PT3484471T (en)
SG (1) SG11201811515WA (en)
WO (1) WO2018011579A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201612240D0 (en) * 2016-07-14 2016-08-31 Mereo Biopharma 1 Ltd Method for producing a polymorphic form of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1075467B1 (en) 1998-05-05 2005-03-30 F. Hoffmann-La Roche Ag Pyrazole derivatives as p-38 map kinase inhibitors
SI2298743T1 (en) 2003-06-26 2012-12-31 Novartis Ag 5-membered heterocycle-based P38 kinase inhibitors
WO2013139809A1 (en) 2012-03-20 2013-09-26 Novartis Ag Use of a pyrazole derivative in the treatment of acute exacerbations of chronic obstructive pulmonary disease
MX2018010781A (en) 2016-03-08 2018-11-09 Mereo Biopharma 1 Ltd Dosage regimen for the treatment of acute exacerbations of inflammatory conditions.
BR112018067454A2 (en) 2016-03-08 2019-01-15 Mereo Biopharma 1 Ltd Dosage regimen for the treatment of acute exacerbations of chronic obstructive pulmonary disease
GB201612240D0 (en) * 2016-07-14 2016-08-31 Mereo Biopharma 1 Ltd Method for producing a polymorphic form of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide

Also Published As

Publication number Publication date
PT3484471T (en) 2021-06-02
WO2018011579A1 (en) 2018-01-18
RU2019103880A (en) 2020-08-14
US20210206726A1 (en) 2021-07-08
JP2019520420A (en) 2019-07-18
EP3484471A1 (en) 2019-05-22
JP7094021B2 (en) 2022-07-01
US10934260B2 (en) 2021-03-02
PL3484471T3 (en) 2021-09-20
CA3030622A1 (en) 2018-01-18
AU2017294643A1 (en) 2019-01-17
EP3484471B1 (en) 2021-05-05
MX2019000385A (en) 2019-05-23
HUE054539T2 (en) 2021-09-28
CN109414429B (en) 2021-09-14
RU2019103880A3 (en) 2020-09-29
IL263908B (en) 2022-07-01
US11434204B2 (en) 2022-09-06
US20190352269A1 (en) 2019-11-21
KR102460529B1 (en) 2022-10-31
AU2017294643B2 (en) 2021-02-25
ES2874661T3 (en) 2021-11-05
BR112019000460A2 (en) 2019-04-24
KR20190028432A (en) 2019-03-18
CN109414429A (en) 2019-03-01
DK3484471T3 (en) 2021-05-31
IL263908A (en) 2019-01-31
GB201612240D0 (en) 2016-08-31

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