SG11201807540UA - Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis - Google Patents

Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis

Info

Publication number
SG11201807540UA
SG11201807540UA SG11201807540UA SG11201807540UA SG11201807540UA SG 11201807540U A SG11201807540U A SG 11201807540UA SG 11201807540U A SG11201807540U A SG 11201807540UA SG 11201807540U A SG11201807540U A SG 11201807540UA SG 11201807540U A SG11201807540U A SG 11201807540UA
Authority
SG
Singapore
Prior art keywords
wittelaan
mechelen
galapagos
generaal
international
Prior art date
Application number
SG11201807540UA
Inventor
Oscar Mammoliti
Koen Jansen
Adeline Palisse
Caroline Joannesse
Christel Menet
Brigitte Allart
Bkassiny Sandy El
Original Assignee
Galapagos Nv
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 Galapagos Nv filed Critical Galapagos Nv
Publication of SG11201807540UA publication Critical patent/SG11201807540UA/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
    • A61K31/495Heterocyclic 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
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

WO 17 / 1487 87 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/148787 Al 8 September 2017 (08.09.2017) WIPO I PCT 1111111111111101110111111111110101111101110101111111101111111101111111111111110111111 (51) International Patent Classification: C07D 401/14 (2006.01) A61P 35/00 (2006.01) C07D 403/04 (2006.01) (21) International Application Number: PCT/EP2017/054139 (22) International Filing Date: 23 February 2017 (23.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1603745.9 4 March 2016 (04.03.2016) GB (71) Applicant: GALAPAGOS NV [BE/BE]; Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (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, 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). arations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(11)) of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 21(3)) (72) Inventors: MAMMOLITI, Oscar; Galapagos NV Gener- aal De Wittelaan Ll l/A3, 2800 Mechelen (BE). JANSEN, Koen, Karel; Galapagos NV Generaal De Wittelaan Ll l/A3, 2800 Mechelen (BE). PALISSE, Adeline, Marie, Elise; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). JOANNESSE, Caroline, Martine, An- Decl dree-Marie; Galapagos NV Generaal De Wittelaan Ll l/A3, 2800 Mechelen (BE). MENET, Christel, Jeanne, Marie; Confo Therapeutics Pleinlaan 2, Building E, 7th floor, E7.6, 1050 Brussels (BE). ALLART, Brigitte; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). EL BKASSINY, Sandy; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (74) Agent: BAR, Gregory, Louis, Joseph; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (54) Title: NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROSIS Ia (R 5 ) rin (57) : The present invention discloses compounds according to Formula I, wherein Rla, R 1b , R 2a , R 2b , R, R 3 4 , R 5 , R6a , c yl, Cy2, and the subscript n and m are as defined herein. The present invention relates to antagonists compounds of sphingosine 1-phos- phate (SIP) receptor, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment us - ing the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, inflammatory diseases, autoimmune dis - eases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering the compound of the invention.
SG11201807540UA 2016-03-04 2017-02-23 Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis SG11201807540UA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1603745.9A GB201603745D0 (en) 2016-03-04 2016-03-04 Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis
PCT/EP2017/054139 WO2017148787A1 (en) 2016-03-04 2017-02-23 Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis

Publications (1)

Publication Number Publication Date
SG11201807540UA true SG11201807540UA (en) 2018-09-27

Family

ID=55858990

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201807540UA SG11201807540UA (en) 2016-03-04 2017-02-23 Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis

Country Status (19)

Country Link
US (1) US20190388421A1 (en)
EP (1) EP3423445B1 (en)
JP (1) JP2019507766A (en)
KR (1) KR20180118752A (en)
CN (1) CN108699037A (en)
AR (1) AR107798A1 (en)
AU (1) AU2017227900A1 (en)
BR (1) BR112018067312A2 (en)
CA (1) CA3016185A1 (en)
CO (1) CO2018009876A2 (en)
GB (1) GB201603745D0 (en)
IL (1) IL261444A (en)
MX (1) MX2018010218A (en)
PH (1) PH12018501849A1 (en)
RU (1) RU2018134780A (en)
SG (1) SG11201807540UA (en)
TW (1) TW201734005A (en)
WO (1) WO2017148787A1 (en)
ZA (1) ZA201805601B (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019091999A1 (en) 2017-11-08 2019-05-16 INSERM (Institut National de la Santé et de la Recherche Médicale) S1pr2 antagonists for treating diseases involving abnormal immune responses
KR20200088844A (en) 2017-11-15 2020-07-23 갈라파고스 엔.브이. Compounds for use in the treatment of fibrotic diseases and pharmaceutical compositions thereof
US12024500B2 (en) * 2018-02-02 2024-07-02 Qingdao Kingagroot Chemical Compound Co., Ltd. Five-membered ring-substituted pyridazinol compounds and derivatives, preparation methods, herbicidal compositions and applications thereof
WO2019148850A1 (en) 2018-02-02 2019-08-08 青岛清原化合物有限公司 Pyridine ring-substituted pyridazinol compound and derivatives thereof, preparation method, herbicidal composition, and application
CN110878086B (en) * 2018-09-06 2024-06-07 青岛清原化合物有限公司 Five-membered ring substituted pyridazinol compound and derivative, preparation method, weeding composition and application thereof
CN109053693B (en) * 2018-09-20 2021-02-05 顺毅股份有限公司 Preparation and application of pyridazine amine compound
JP2022510691A (en) * 2018-12-05 2022-01-27 バイキング・セラピューティクス・インコーポレイテッド Compositions for the treatment of fibrosis and inflammation
CN110128457B (en) * 2019-05-24 2022-05-03 宁波瑞奇医药科技有限公司 Preparation method of heterocyclic small molecule compound
US11465982B2 (en) * 2019-07-22 2022-10-11 Boehringer Ingelheim International Gmbh Pyridazines
US11485727B2 (en) 2019-07-22 2022-11-01 Boehringer Ingelheim International Gmbh N-methyl, n-(6-(methoxy)pyridazin-3-yl) amine derivatives as autotaxin (ATX) modulators
CN111777549A (en) * 2020-07-07 2020-10-16 中瀚(齐河县)生物医药科技有限公司 Synthesis process of 2-methoxy-3-bromo-5-fluoropyridine
EP4419508A2 (en) * 2021-10-22 2024-08-28 Carmot Therapeutics, Inc. Oxazole, oxadiazole, and indole derivatives for the inhibition of usp28

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2360305A1 (en) * 1999-02-09 2000-08-17 Bristol-Myers Squibb Company Lactam inhibitors of fxa and method
BRPI0817397A2 (en) * 2007-09-24 2015-04-07 Allergan Inc Indole compounds containing aryl or heteroaryl groups with sphingosine-1-phosphate receptor (sip) biological activity

Also Published As

Publication number Publication date
EP3423445B1 (en) 2020-04-01
KR20180118752A (en) 2018-10-31
JP2019507766A (en) 2019-03-22
US20190388421A1 (en) 2019-12-26
PH12018501849A1 (en) 2019-01-28
MX2018010218A (en) 2018-11-09
TW201734005A (en) 2017-10-01
CO2018009876A2 (en) 2018-10-10
CN108699037A (en) 2018-10-23
GB201603745D0 (en) 2016-04-20
WO2017148787A1 (en) 2017-09-08
AR107798A1 (en) 2018-06-06
EP3423445A1 (en) 2019-01-09
IL261444A (en) 2018-10-31
ZA201805601B (en) 2019-06-26
RU2018134780A (en) 2020-04-06
AU2017227900A1 (en) 2018-10-25
BR112018067312A2 (en) 2018-12-26
CA3016185A1 (en) 2017-09-08

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