PH12014501178B1 - Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders - Google Patents

Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders

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Publication number
PH12014501178B1
PH12014501178B1 PH12014501178A PH12014501178A PH12014501178B1 PH 12014501178 B1 PH12014501178 B1 PH 12014501178B1 PH 12014501178 A PH12014501178 A PH 12014501178A PH 12014501178 A PH12014501178 A PH 12014501178A PH 12014501178 B1 PH12014501178 B1 PH 12014501178B1
Authority
PH
Philippines
Prior art keywords
diseases
treatment
pharmaceutical compositions
formula
methods
Prior art date
Application number
PH12014501178A
Other languages
English (en)
Other versions
PH12014501178A1 (en
Inventor
Fr‚D‚Ric Gilbert LabGuere
Gregory John Robert Newsome
Luke Jonathan Alvey
Laurent Raymond Maurice Saniere
Stephen Robert Fletcher
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 PH12014501178A1 publication Critical patent/PH12014501178A1/en
Publication of PH12014501178B1 publication Critical patent/PH12014501178B1/en

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Classifications

    • 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
PH12014501178A 2011-12-22 2014-05-26 Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders PH12014501178B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161578979P 2011-12-22 2011-12-22
PCT/EP2012/076275 WO2013092791A1 (en) 2011-12-22 2012-12-20 Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Publications (2)

Publication Number Publication Date
PH12014501178A1 PH12014501178A1 (en) 2014-10-20
PH12014501178B1 true PH12014501178B1 (en) 2014-10-20

Family

ID=47520068

Family Applications (1)

Application Number Title Priority Date Filing Date
PH12014501178A PH12014501178B1 (en) 2011-12-22 2014-05-26 Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders

Country Status (34)

Country Link
US (5) US8927543B2 (enExample)
EP (3) EP2794604B1 (enExample)
JP (1) JP6062453B2 (enExample)
KR (1) KR102012268B1 (enExample)
CN (1) CN103998448B (enExample)
AR (1) AR089284A1 (enExample)
AU (1) AU2012357067B2 (enExample)
BR (1) BR112014015142B1 (enExample)
CA (1) CA2859578C (enExample)
CL (1) CL2014001664A1 (enExample)
CO (1) CO7010835A2 (enExample)
CR (1) CR20140305A (enExample)
CY (2) CY1119434T1 (enExample)
DK (2) DK2794604T3 (enExample)
EA (1) EA023826B1 (enExample)
ES (2) ES2911449T3 (enExample)
HR (2) HRP20220456T1 (enExample)
HU (1) HUE12812237T4 (enExample)
IL (2) IL233212B (enExample)
IN (1) IN2014MN01033A (enExample)
LT (2) LT2794604T (enExample)
MX (1) MX351681B (enExample)
NI (1) NI201400060A (enExample)
PE (1) PE20141685A1 (enExample)
PH (1) PH12014501178B1 (enExample)
PL (2) PL3378862T3 (enExample)
PT (2) PT3378862T (enExample)
SG (1) SG11201403169PA (enExample)
SI (2) SI3378862T1 (enExample)
TW (1) TWI567073B (enExample)
UA (1) UA111767C2 (enExample)
UY (1) UY34545A (enExample)
WO (1) WO2013092791A1 (enExample)
ZA (1) ZA201404607B (enExample)

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AR089284A1 (es) 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
USRE48171E1 (en) 2012-03-21 2020-08-25 Janssen Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
US9441007B2 (en) 2012-03-21 2016-09-13 Alios Biopharma, Inc. Substituted nucleosides, nucleotides and analogs thereof
EP2935262B1 (en) 2012-12-20 2017-03-15 Galapagos NV Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)
GB201319677D0 (en) * 2013-11-07 2013-12-25 Eth Z Rich Cyclopropanation
GB201411241D0 (en) * 2014-06-25 2014-08-06 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
GB201506894D0 (en) * 2015-04-23 2015-06-10 Galapagos Nv Novel dihydropyridoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders
JP6918957B2 (ja) * 2017-03-06 2021-08-11 上海 インスティテュート オブ マテリア メディカ、チャイニーズ アカデミー オブ サイエンシーズShanghai Institute Of Materia Medica, Chinese Academy Of Sciences Gpr84受容体拮抗剤およびその使用
EP3403649A1 (en) 2017-05-16 2018-11-21 Bayer Pharma Aktiengesellschaft Inhibitors and antagonists of gpr84 for the treatment of endometriosis
WO2019096944A1 (en) 2017-11-15 2019-05-23 Galapagos Nv Compounds and pharmaceutical compositions thereof for use in the treatment of fibrotic diseases
JOP20220156A1 (ar) 2019-12-19 2023-01-30 Bayer Ag مشتقات فوروإندازول
WO2021123394A1 (en) 2019-12-20 2021-06-24 University Of Copenhagen G protein-coupled receptor modulators and a pharmaceutical composition
JP2023553295A (ja) 2020-11-24 2023-12-21 ガラパゴス・ナムローゼ・フェンノートシャップ 線維性疾患の治療における使用のための化合物及び線維性疾患の治療方法
CA3206499A1 (en) 2021-02-02 2022-08-11 Liminal Biosciences Limited Gpr84 antagonists and uses thereof
WO2022179940A1 (en) 2021-02-23 2022-09-01 Bayer Aktiengesellschaft Furoindazole derivatives as gpr84 antagonists
CN115109072A (zh) * 2021-03-18 2022-09-27 武汉人福创新药物研发中心有限公司 一种gpr84拮抗剂及其制备方法和用途
WO2022218372A1 (zh) * 2021-04-14 2022-10-20 武汉人福创新药物研发中心有限公司 一种二氢嘧啶并异喹啉酮类衍生物及用途
CA3218018A1 (en) 2021-04-29 2022-11-03 Bayer Aktiengesellschaft Furoindazole derivatives as antagonists or inhibitors of gpr84
US20250066335A1 (en) 2021-06-18 2025-02-27 University Of Copenhagen Polysubstituted 4-hydroxypyridine and 4-hydroxyquinoline derivatives as gpr84 antagonists
EP4361151A4 (en) 2021-06-21 2025-06-11 Wuhan Humanwell Innovative Drug Research and Development Center Limited Company Tricyclic compound as a GPR84 antagonist
CN115611944A (zh) 2021-07-15 2023-01-17 中国科学院上海药物研究所 不对称gpr84拮抗剂及其用途
WO2023076668A1 (en) * 2021-10-29 2023-05-04 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Compositions and methods for treatment of cancer
GB202202297D0 (en) 2022-02-21 2022-04-06 Verona Pharma Plc Formulation production process
WO2024083705A1 (en) 2022-10-18 2024-04-25 Bayer Aktiengesellschaft Furoindazole derivatives for the treatment of pain
CN120569392A (zh) * 2022-12-30 2025-08-29 广州市联瑞制药有限公司 三环类化合物及其制备方法和应用
WO2024220480A2 (en) * 2023-04-17 2024-10-24 The Board Of Trustees Of The Leland Stanford Junior University Method for detecting innate immune action in vivo using gpr84-pet
US12194045B1 (en) 2023-06-26 2025-01-14 Verona Pharma Plc Particulate composition

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JP2011088847A (ja) * 2009-10-21 2011-05-06 Takeda Chem Ind Ltd 三環性化合物およびその用途
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AR089284A1 (es) 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
EP2935262B1 (en) 2012-12-20 2017-03-15 Galapagos NV Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)

Also Published As

Publication number Publication date
CO7010835A2 (es) 2014-07-31
WO2013092791A1 (en) 2013-06-27
BR112014015142A2 (pt) 2017-06-13
ES2643379T3 (es) 2017-11-22
NZ626473A (en) 2016-03-31
JP6062453B2 (ja) 2017-01-18
NI201400060A (es) 2015-04-27
EA201491245A1 (ru) 2014-10-30
MX351681B (es) 2017-10-25
TWI567073B (zh) 2017-01-21
KR20140117427A (ko) 2014-10-07
CY1119434T1 (el) 2018-03-07
HRP20171404T1 (hr) 2017-11-17
US20220227751A1 (en) 2022-07-21
SI3378862T1 (sl) 2022-05-31
PH12014501178A1 (en) 2014-10-20
CA2859578A1 (en) 2013-06-27
PL2794604T3 (pl) 2017-12-29
DK3378862T3 (da) 2022-04-11
US20130165437A1 (en) 2013-06-27
ES2643379T9 (es) 2018-01-05
HUE12812237T4 (hu) 2017-12-28
ZA201404607B (en) 2020-02-26
AU2012357067A1 (en) 2014-07-10
KR102012268B1 (ko) 2019-08-21
US10047083B2 (en) 2018-08-14
CY1125167T1 (el) 2024-09-20
US8927543B2 (en) 2015-01-06
EA023826B1 (ru) 2016-07-29
IL233212B (en) 2018-03-29
AR089284A1 (es) 2014-08-13
TW201331201A (zh) 2013-08-01
IL257581A (en) 2018-04-30
US20160244442A1 (en) 2016-08-25
LT2794604T (lt) 2017-10-25
PT3378862T (pt) 2022-04-11
CR20140305A (es) 2014-07-23
IN2014MN01033A (enExample) 2015-05-01
UA111767C2 (uk) 2016-06-10
ES2911449T3 (es) 2022-05-19
EP4019519A1 (en) 2022-06-29
HRP20220456T1 (hr) 2022-05-27
HK1201528A1 (en) 2015-09-04
AU2012357067B2 (en) 2017-01-05
US20190002458A1 (en) 2019-01-03
PT2794604T (pt) 2017-10-23
EP3378862A1 (en) 2018-09-26
SI2794604T1 (sl) 2017-12-29
EP2794604A1 (en) 2014-10-29
LT3378862T (lt) 2022-04-25
JP2015500861A (ja) 2015-01-08
CN103998448A (zh) 2014-08-20
CL2014001664A1 (es) 2014-10-03
IL233212A0 (en) 2014-08-31
DK2794604T3 (da) 2017-11-06
MX2014007363A (es) 2014-08-01
CA2859578C (en) 2020-03-10
PL3378862T3 (pl) 2022-05-16
SG11201403169PA (en) 2014-07-30
PE20141685A1 (es) 2014-11-25
BR112014015142B1 (pt) 2022-03-29
EP2794604B1 (en) 2017-09-13
CN103998448B (zh) 2016-04-20
US20140121204A1 (en) 2014-05-01
UY34545A (es) 2013-07-31
US11220499B2 (en) 2022-01-11
US9255095B2 (en) 2016-02-09
EP3378862B1 (en) 2022-03-16

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