MX2014007363A - Novedosas dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios. - Google Patents

Novedosas dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios.

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Publication number
MX2014007363A
MX2014007363A MX2014007363A MX2014007363A MX2014007363A MX 2014007363 A MX2014007363 A MX 2014007363A MX 2014007363 A MX2014007363 A MX 2014007363A MX 2014007363 A MX2014007363 A MX 2014007363A MX 2014007363 A MX2014007363 A MX 2014007363A
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MX
Mexico
Prior art keywords
diseases
treatment
pharmaceutical compositions
formula
methods
Prior art date
Application number
MX2014007363A
Other languages
English (en)
Other versions
MX351681B (es
Inventor
Frédéric Gilbert Labéguére
Gregory John Robert Newsome
Luke Jonathan Alvey
Laurent Raymond Maurice Sanière
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.)
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Publication date
Application filed by Galapagos Nv filed Critical Galapagos Nv
Publication of MX2014007363A publication Critical patent/MX2014007363A/es
Publication of MX351681B publication Critical patent/MX351681B/es

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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un compuesto según la Fórmula la en donde L1 y G, y R1 son según lo descrito en la presente invención. La presente invención se refiere a compuestos novedosos según la Fórmula I que antagonizan el GPR84, un receptor acoplado a la proteína G que está involucrado en afecciones inflamatorias, y métodos para la producción de estos compuestos novedosos, composiciones farmacéuticas que comprenden estos compuestos, y métodos para la prevención y/o tratamiento de afecciones inflamatorias (por ejemplo enfermedades intestinales inflamatorias (IBID), artritis reumatoide, vasculitis, enfermedades pulmonares (por ejemplo enfermedad pulmonar obstructiva crónica (COPD) y enfermedades intersticiales pulmonares (por ejemplo fibrosis pulmonar idiopática (IPF))), afecciones neuroinflamatorias, enfermedades infecciosas, enfermedades autoinmunes, enfermedades endocrinas y/o metabólicas, y/o enfermedades que involucran el deterioro de las funciones de células inmunes mediante la administración de un compuesto de la invención.
MX2014007363A 2011-12-22 2012-12-20 Novedosas dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios. MX351681B (es)

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
MX2014007363A true MX2014007363A (es) 2014-08-01
MX351681B MX351681B (es) 2017-10-25

Family

ID=47520068

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014007363A MX351681B (es) 2011-12-22 2012-12-20 Novedosas dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios.

Country Status (35)

Country Link
US (5) US8927543B2 (es)
EP (3) EP2794604B1 (es)
JP (1) JP6062453B2 (es)
KR (1) KR102012268B1 (es)
CN (1) CN103998448B (es)
AR (1) AR089284A1 (es)
AU (1) AU2012357067B2 (es)
BR (1) BR112014015142B1 (es)
CA (1) CA2859578C (es)
CL (1) CL2014001664A1 (es)
CO (1) CO7010835A2 (es)
CR (1) CR20140305A (es)
CY (1) CY1119434T1 (es)
DK (2) DK3378862T3 (es)
EA (1) EA023826B1 (es)
ES (2) ES2643379T3 (es)
HK (1) HK1201528A1 (es)
HR (2) HRP20220456T1 (es)
HU (1) HUE12812237T4 (es)
IL (2) IL233212B (es)
IN (1) IN2014MN01033A (es)
LT (2) LT3378862T (es)
MX (1) MX351681B (es)
NI (1) NI201400060A (es)
PE (1) PE20141685A1 (es)
PH (1) PH12014501178A1 (es)
PL (2) PL3378862T3 (es)
PT (2) PT2794604T (es)
SG (1) SG11201403169PA (es)
SI (2) SI3378862T1 (es)
TW (1) TWI567073B (es)
UA (1) UA111767C2 (es)
UY (1) UY34545A (es)
WO (1) WO2013092791A1 (es)
ZA (1) ZA201404607B (es)

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AP2014007796A0 (en) 2011-12-22 2014-07-31 Alios Biopharma Inc Substituted nucleosides, nucleotides and analogs thereof
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
WO2014095798A1 (en) * 2012-12-20 2014-06-26 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
KR102305710B1 (ko) * 2017-03-06 2021-09-30 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 Gpr84 수용체 길항제 및 이의 용도
EP3403649A1 (en) 2017-05-16 2018-11-21 Bayer Pharma Aktiengesellschaft Inhibitors and antagonists of gpr84 for the treatment of endometriosis
CN111343986A (zh) 2017-11-15 2020-06-26 加拉帕戈斯股份有限公司 用于治疗纤维化疾病的化合物及其药物组合物
JP2023508908A (ja) 2019-12-19 2023-03-06 バイエル、アクチエンゲゼルシャフト フロインダゾール誘導体
WO2021123394A1 (en) 2019-12-20 2021-06-24 University Of Copenhagen G protein-coupled receptor modulators and a pharmaceutical composition
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WO2022179940A1 (en) 2021-02-23 2022-09-01 Bayer Aktiengesellschaft Furoindazole derivatives as gpr84 antagonists
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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
EP4330260A1 (en) 2021-04-29 2024-03-06 Bayer Aktiengesellschaft Furoindazole derivatives as antagonists or inhibitors of gpr84
WO2022263676A1 (en) 2021-06-18 2022-12-22 University Of Copenhagen Polysubstituted 4-hydroxypyridine and 4-hydroxyquinoline derivatives as gpr84 antagonists
CN115572293A (zh) * 2021-06-21 2023-01-06 武汉人福创新药物研发中心有限公司 用于gpr84拮抗剂的三环化合物
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
WO2024083705A1 (en) 2022-10-18 2024-04-25 Bayer Aktiengesellschaft Furoindazole derivatives for the treatment of pain

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WO2014095798A1 (en) 2012-12-20 2014-06-26 Galapagos Nv Novel dihydropyrimidinoisoquinolinones and pharmaceutical compositions thereof for the treatment of inflammatory disorders (gpr84 antagonists)

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Publication number Publication date
BR112014015142B1 (pt) 2022-03-29
CN103998448A (zh) 2014-08-20
UA111767C2 (uk) 2016-06-10
IL233212B (en) 2018-03-29
US20160244442A1 (en) 2016-08-25
NI201400060A (es) 2015-04-27
TW201331201A (zh) 2013-08-01
LT3378862T (lt) 2022-04-25
PT2794604T (pt) 2017-10-23
AR089284A1 (es) 2014-08-13
HUE12812237T4 (hu) 2017-12-28
BR112014015142A2 (pt) 2017-06-13
PH12014501178B1 (en) 2014-10-20
PT3378862T (pt) 2022-04-11
CN103998448B (zh) 2016-04-20
IL257581A (en) 2018-04-30
AU2012357067B2 (en) 2017-01-05
CR20140305A (es) 2014-07-23
PL2794604T3 (pl) 2017-12-29
SG11201403169PA (en) 2014-07-30
CL2014001664A1 (es) 2014-10-03
EP2794604A1 (en) 2014-10-29
ES2643379T3 (es) 2017-11-22
NZ626473A (en) 2016-03-31
US9255095B2 (en) 2016-02-09
EA023826B1 (ru) 2016-07-29
US8927543B2 (en) 2015-01-06
US20190002458A1 (en) 2019-01-03
CA2859578A1 (en) 2013-06-27
US20140121204A1 (en) 2014-05-01
KR102012268B1 (ko) 2019-08-21
IN2014MN01033A (es) 2015-05-01
TWI567073B (zh) 2017-01-21
US11220499B2 (en) 2022-01-11
KR20140117427A (ko) 2014-10-07
UY34545A (es) 2013-07-31
LT2794604T (lt) 2017-10-25
IL233212A0 (en) 2014-08-31
PE20141685A1 (es) 2014-11-25
CY1119434T1 (el) 2018-03-07
HRP20171404T1 (hr) 2017-11-17
US10047083B2 (en) 2018-08-14
HRP20220456T1 (hr) 2022-05-27
EP3378862A1 (en) 2018-09-26
MX351681B (es) 2017-10-25
EA201491245A1 (ru) 2014-10-30
EP3378862B1 (en) 2022-03-16
ES2911449T3 (es) 2022-05-19
US20130165437A1 (en) 2013-06-27
WO2013092791A1 (en) 2013-06-27
SI3378862T1 (sl) 2022-05-31
AU2012357067A1 (en) 2014-07-10
US20220227751A1 (en) 2022-07-21
JP6062453B2 (ja) 2017-01-18
CA2859578C (en) 2020-03-10
ES2643379T9 (es) 2018-01-05
DK3378862T3 (da) 2022-04-11
EP4019519A1 (en) 2022-06-29
SI2794604T1 (sl) 2017-12-29
DK2794604T3 (da) 2017-11-06
CO7010835A2 (es) 2014-07-31
EP2794604B1 (en) 2017-09-13
PL3378862T3 (pl) 2022-05-16
PH12014501178A1 (en) 2014-10-20
JP2015500861A (ja) 2015-01-08
ZA201404607B (en) 2020-02-26
HK1201528A1 (en) 2015-09-04

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