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PE20171100A1 - Derivados de hidroxialquil-piperazina como moduladores del receptor cxcr3 - Google Patents

Derivados de hidroxialquil-piperazina como moduladores del receptor cxcr3

Info

Publication number
PE20171100A1
PE20171100A1 PE2017001213A PE2017001213A PE20171100A1 PE 20171100 A1 PE20171100 A1 PE 20171100A1 PE 2017001213 A PE2017001213 A PE 2017001213A PE 2017001213 A PE2017001213 A PE 2017001213A PE 20171100 A1 PE20171100 A1 PE 20171100A1
Authority
PE
Peru
Prior art keywords
trifluoromethyl
ethyl
hydroxialkyl
receptor modulators
piperazine derivatives
Prior art date
Application number
PE2017001213A
Other languages
English (en)
Inventor
Eva Caroff
Emmanuel Meyer
Original Assignee
Idorsia Pharmaceuticals 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 Idorsia Pharmaceuticals Ltd filed Critical Idorsia Pharmaceuticals Ltd
Publication of PE20171100A1 publication Critical patent/PE20171100A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se refiere a un compuesto de formula I, donde: n es 1 o 2; X es N o CH; R1 es un anillo aromatico heteroarilo monociclico o biciclico de 5 a 10 miembros que contiene 1, 2 o 3 heteroatomos, en donde dicho heterarilo se encuentra opcionalmente sustituido; R2 es cicloalquilo C3-C6, alcoxi C1-C4 o fluoroalquilo C1-C2. Son compuestos preferidos: 1{(R)-2-(2-hidroxi-etil)-4-[2-trifluormetil-4(2-trifluormetil-pirimidin-5-il)-tiazol-5-il]-piperazin-1-il}-2-(3-metil-pirazol-1-il)-etanona; 2-(3-etil-pirazol-1-il)-1-{(R)-2-(2-hidroxi-etil)-4-[2-trifluormetil-4-(2-trifluormetil-pirimidin-5-il)-tiazol-5-il]-piperazin-1-il}-etanona; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son moduladores del receptor de quimiocina CXCR3, siendo utiles en el tratamiento de trastornos autoinmunes, fibrosis, entre otros
PE2017001213A 2015-01-15 2016-01-14 Derivados de hidroxialquil-piperazina como moduladores del receptor cxcr3 PE20171100A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP2015050696 2015-01-15

Publications (1)

Publication Number Publication Date
PE20171100A1 true PE20171100A1 (es) 2017-08-07

Family

ID=55129886

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017001213A PE20171100A1 (es) 2015-01-15 2016-01-14 Derivados de hidroxialquil-piperazina como moduladores del receptor cxcr3

Country Status (38)

Country Link
US (1) US10053457B2 (es)
EP (1) EP3245203B1 (es)
JP (1) JP6337218B2 (es)
KR (1) KR101967083B1 (es)
CN (1) CN107250133B (es)
AR (1) AR103414A1 (es)
AU (1) AU2016207988B2 (es)
BR (1) BR112017015093A2 (es)
CA (1) CA2972952C (es)
CL (1) CL2017001831A1 (es)
CO (1) CO2017008156A2 (es)
CY (1) CY1121361T1 (es)
DK (1) DK3245203T3 (es)
EA (1) EA032927B1 (es)
ES (1) ES2709985T3 (es)
HK (1) HK1246789B (es)
HR (1) HRP20190024T1 (es)
HU (1) HUE042559T2 (es)
IL (1) IL253411B (es)
LT (1) LT3245203T (es)
MA (1) MA41337A (es)
MX (1) MX2017009288A (es)
MY (1) MY187614A (es)
NZ (1) NZ734542A (es)
PE (1) PE20171100A1 (es)
PH (1) PH12017501280B1 (es)
PL (1) PL3245203T3 (es)
PT (1) PT3245203T (es)
RS (1) RS58349B1 (es)
SA (1) SA517381905B1 (es)
SG (1) SG11201705617XA (es)
SI (1) SI3245203T1 (es)
TN (1) TN2017000278A1 (es)
TR (1) TR201900680T4 (es)
TW (1) TWI693221B (es)
UA (1) UA119805C2 (es)
WO (1) WO2016113344A1 (es)
ZA (1) ZA201705486B (es)

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* Cited by examiner, † Cited by third party
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MX363432B (es) 2013-07-22 2019-03-22 Idorsia Pharmaceuticals Ltd Derivados 1-(piperazin-1-il)-2-([1,2,4]triazol-1-il)-etanona.
AR099789A1 (es) 2014-03-24 2016-08-17 Actelion Pharmaceuticals Ltd Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina
NZ734542A (en) * 2015-01-15 2023-02-24 Idorsia Pharmaceuticals Ltd Hydroxyalkyl-piperazine derivatives as cxcr3 receptor modulators
AR103399A1 (es) 2015-01-15 2017-05-10 Actelion Pharmaceuticals Ltd Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3
WO2018011265A1 (en) * 2016-07-13 2018-01-18 Idorsia Pharmaceuticals Ltd Hydroxyalkyl-piperazine derivatives as cxcr3 receptor modulators
WO2020060964A1 (en) * 2018-09-18 2020-03-26 Alxerion Biotech Corp. 1, 2, 4-oxadiazole derivatives and uses thereof
WO2022162017A1 (en) 2021-01-28 2022-08-04 Idorsia Pharmaceuticals Ltd Crystalline form of a piperazinyl-thiazole derivative
KR20250067152A (ko) 2022-09-09 2025-05-14 이도르시아 파마슈티컬스 리미티드 항-cd3 항체 및 cxcr3 길항제를 포함하는 약학 병용물

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