PE20141685A1 - Novedosas dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de transtornos inflamatorios - Google Patents

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

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Publication number
PE20141685A1
PE20141685A1 PE2014000988A PE2014000988A PE20141685A1 PE 20141685 A1 PE20141685 A1 PE 20141685A1 PE 2014000988 A PE2014000988 A PE 2014000988A PE 2014000988 A PE2014000988 A PE 2014000988A PE 20141685 A1 PE20141685 A1 PE 20141685A1
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PE
Peru
Prior art keywords
treatment
pharmaceutical compositions
inflammatory disorders
alkyl
dihydropyrimidinoisoquinolinones
Prior art date
Application number
PE2014000988A
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English (en)
Inventor
Frederic Gilbert Labeguere
Gregory John Robert Newsome
Luke Jonathan Alvey
Laurent Raymond Maurice Saniere
Stephan Robert Fletcher
Original Assignee
Galapagos Nv
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Publication date
Application filed by Galapagos Nv filed Critical Galapagos Nv
Publication of PE20141685A1 publication Critical patent/PE20141685A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (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

SE REFIERE A UN COMPUESTO DE FORMULA IA, DONDE: R1 ES H, HALO; L1 ESTA AUSENTE O ES -O-, -S-, ENTRE OTROS; G ES R2, -W-L2-R2, O -W-L3-R3; W ES ALQUILENO C1-C4, ALQUENILENO 2C-4C ENTRE OTROS; L2 ESTA AUSENTE O ES -O-; R2 ES H, ALQUILO 1C-8C, ENTRE OTROS; L3 ES NR4B; R3 ES ALQUILO 1C-4C SUSTITUIDO; HETEROARILO O ARILO; R4B ES H, ALQUILO 1C-4C O CICLOALQUILO 3C-7C. SON COMPUESTOS PREFERIDOS: 9-ALILOXI-2-([1,4] DIOXAN-2-ILMETOXI)-6,7-DIHIDRO-PIRIMIDO[6,1-A]ISOQUINOLIN-4-ONA; 2-([1,4]DIOXAN-2-ILMETOXI)-9-PIRIDIN-4-IL-6,7-DIHIDRO-PIRIMIDO[6,1-A]ISOQUINOLIN-4-ONA; ENTRE OTROS. DICHO COMPUESTO ES ANTAGONISTA DEL GPR84 (PROBABLE RECEPTOR ACOPLADO A PROTEINA G 84). TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN METODO PARA SU OBTENCION, SIENDO UTIL EN EL TRATAMIENTO DE AFECCIONES INFLAMATORIAS.
PE2014000988A 2011-12-22 2012-12-20 Novedosas dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de transtornos inflamatorios PE20141685A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161578979P 2011-12-22 2011-12-22

Publications (1)

Publication Number Publication Date
PE20141685A1 true PE20141685A1 (es) 2014-11-25

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PE2014000988A PE20141685A1 (es) 2011-12-22 2012-12-20 Novedosas dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de transtornos inflamatorios

Country Status (34)

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US (5) US8927543B2 (es)
EP (3) EP3378862B1 (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 (2) CY1119434T1 (es)
DK (2) DK2794604T3 (es)
EA (1) EA023826B1 (es)
ES (2) ES2911449T3 (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) PL2794604T3 (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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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
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UA111767C2 (uk) 2016-06-10
NI201400060A (es) 2015-04-27
EP3378862B1 (en) 2022-03-16
AR089284A1 (es) 2014-08-13
HK1201528A1 (en) 2015-09-04
CL2014001664A1 (es) 2014-10-03
US20160244442A1 (en) 2016-08-25
US11220499B2 (en) 2022-01-11
TWI567073B (zh) 2017-01-21
PH12014501178B1 (en) 2014-10-20
PT3378862T (pt) 2022-04-11
UY34545A (es) 2013-07-31
ZA201404607B (en) 2020-02-26
IL233212A0 (en) 2014-08-31
EP4019519A1 (en) 2022-06-29
KR102012268B1 (ko) 2019-08-21
JP6062453B2 (ja) 2017-01-18
CR20140305A (es) 2014-07-23
US10047083B2 (en) 2018-08-14
CA2859578A1 (en) 2013-06-27
EA201491245A1 (ru) 2014-10-30
IL233212B (en) 2018-03-29
IL257581A (en) 2018-04-30
EP2794604A1 (en) 2014-10-29
BR112014015142A2 (pt) 2017-06-13
WO2013092791A1 (en) 2013-06-27
ES2643379T9 (es) 2018-01-05
DK3378862T3 (da) 2022-04-11
US20220227751A1 (en) 2022-07-21
IN2014MN01033A (es) 2015-05-01
AU2012357067B2 (en) 2017-01-05
ES2911449T3 (es) 2022-05-19
HUE12812237T4 (hu) 2017-12-28
CY1125167T1 (el) 2024-09-20
BR112014015142B1 (pt) 2022-03-29
LT3378862T (lt) 2022-04-25
US20130165437A1 (en) 2013-06-27
CO7010835A2 (es) 2014-07-31
HRP20171404T1 (hr) 2017-11-17
SI3378862T1 (sl) 2022-05-31
EP2794604B1 (en) 2017-09-13
CA2859578C (en) 2020-03-10
SI2794604T1 (sl) 2017-12-29
MX351681B (es) 2017-10-25
HRP20220456T1 (hr) 2022-05-27
CN103998448A (zh) 2014-08-20
PL2794604T3 (pl) 2017-12-29
US20190002458A1 (en) 2019-01-03
PH12014501178A1 (en) 2014-10-20
CY1119434T1 (el) 2018-03-07
TW201331201A (zh) 2013-08-01
NZ626473A (en) 2016-03-31
MX2014007363A (es) 2014-08-01
PL3378862T3 (pl) 2022-05-16
DK2794604T3 (da) 2017-11-06
SG11201403169PA (en) 2014-07-30
CN103998448B (zh) 2016-04-20
EA023826B1 (ru) 2016-07-29
US20140121204A1 (en) 2014-05-01
US9255095B2 (en) 2016-02-09
JP2015500861A (ja) 2015-01-08
PT2794604T (pt) 2017-10-23
US8927543B2 (en) 2015-01-06
KR20140117427A (ko) 2014-10-07
ES2643379T3 (es) 2017-11-22
LT2794604T (lt) 2017-10-25
AU2012357067A1 (en) 2014-07-10
EP3378862A1 (en) 2018-09-26

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