AR111801A1 - Inhibidores y antagonistas de gpr84 para el tratamiento de endometriosis - Google Patents

Inhibidores y antagonistas de gpr84 para el tratamiento de endometriosis

Info

Publication number
AR111801A1
AR111801A1 ARP180101292A ARP180101292A AR111801A1 AR 111801 A1 AR111801 A1 AR 111801A1 AR P180101292 A ARP180101292 A AR P180101292A AR P180101292 A ARP180101292 A AR P180101292A AR 111801 A1 AR111801 A1 AR 111801A1
Authority
AR
Argentina
Prior art keywords
gpr84
endometriosis
antagonist
inhibitor
patient
Prior art date
Application number
ARP180101292A
Other languages
English (en)
Inventor
Shang Catherine Dr
Oppermann Udo Dr
Martinez Estrada Fernando Dr
Langer Gernot Dr
Obendorf Maik Dr
Sacher Frank Dr
Original Assignee
Bayer Pharma AG
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 Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of AR111801A1 publication Critical patent/AR111801A1/es

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/689—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to pregnancy or the gonads
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Biochemistry (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Biophysics (AREA)
  • General Physics & Mathematics (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Cell Biology (AREA)
  • Analytical Chemistry (AREA)
  • Pathology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se refiere a un antagonista o inhibidor del receptor 84 acoplado a proteína G (GPR84) para utilizar en el tratamiento y/o prevención de un paciente que padece endometriosis, que está en riesgo de desarrollar dicha enfermedad, y/o que está siendo diagnosticado para endometriosis, así como también métodos de selección de dicho antagonista o inhibidor así como también métodos para el diagnóstico, composiciones farmacéuticas. Reivindicación 1: Un antagonista o inhibidor del receptor acoplado a proteína G 84 (GPR84) caracterizado por ser para utilizar en el tratamiento y/o prevención de la endometriosis en un paciente que sufre de, que está en riesgo de desarrollar, y/o que está siendo diagnosticado para endometriosis. Reivindicación 2: El antagonista o inhibidor de acuerdo con la reivindicación 1, caracterizado por ser un anticuerpo, preferentemente un anticuerpo monoclonal, que se une específicamente a GPR84, o por ser un fragmento de unión al antígeno o derivado del mismo. Reivindicación 9: El antagonista o inhibidor de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizado por inhibir la activación de GPR84 inducida por embelina con un valor IC₅₀ de 5 mM o más bajo, preferentemente 10 mM o más bajo, más preferentemente 9,4 nM o más bajo, y/o la activación de GPR84 inducida por 2-OH ácido decanoico con un valor IC₅₀ de 5 mM o más bajo, preferentemente 10 mM o más bajo, más preferentemente de 16 nM o más bajo, y/o la activación de GPR84 inducida por 6-n-octilaminouracilo con un valor IC₅₀ de 5 mM o más bajo, preferentemente 10 mM o más bajo, más preferentemente 20 nM o más bajo, según lo determinado en un ensayo de liberación de cAMP de GPR84. Reivindicación 10: El antagonista o inhibidor de acuerdo con cualquiera de las reivindicaciones 1, y 7 a 9, caracterizado por ser un miembro de uno de los grupos seleccionados de la lista que comprende: dihidropiridoisoquinolinona; dihidropirimidinoisoquinolinona. Reivindicación 11: El antagonista de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizado porque la endometriosis se caracteriza por presencia de ácidos grasos libres de cadena media (AGLCM), y/o enzimas acil-CoA tioesterasa (ACOT) y/o sintasas de ácido graso (FASN) en lesiones ectópicas, en comparación con endometrio eutópico; y/o aumento de la expresión de GPR84 en macrófagos tomados de un paciente con endometriosis, en comparación con macrófagos tomados de un paciente control; y/o fracción más grande de células GPR84 positivas en monocitos y/o macrófagos tomados de un paciente con endometriosis, en comparación con monocitos y/o macrófagos tomados de un paciente control.
ARP180101292A 2017-05-16 2018-05-16 Inhibidores y antagonistas de gpr84 para el tratamiento de endometriosis AR111801A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP17171351.4A EP3403649A1 (en) 2017-05-16 2017-05-16 Inhibitors and antagonists of gpr84 for the treatment of endometriosis

Publications (1)

Publication Number Publication Date
AR111801A1 true AR111801A1 (es) 2019-08-21

Family

ID=58745052

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP180101292A AR111801A1 (es) 2017-05-16 2018-05-16 Inhibidores y antagonistas de gpr84 para el tratamiento de endometriosis

Country Status (14)

Country Link
US (1) US20210401823A1 (es)
EP (2) EP3403649A1 (es)
JP (1) JP2020519662A (es)
KR (1) KR20200003830A (es)
CN (1) CN110573146A (es)
AR (1) AR111801A1 (es)
AU (1) AU2018269328A1 (es)
BR (1) BR112019023999A2 (es)
CA (1) CA3063489A1 (es)
MX (1) MX2019013734A (es)
PE (1) PE20191746A1 (es)
SG (1) SG11201909783VA (es)
TW (1) TW201900214A (es)
WO (1) WO2018210822A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111012782B (zh) * 2019-12-27 2023-08-04 郑州大学第一附属医院 一种g蛋白偶联受体gpr84抑制剂及其应用
EP4110056A4 (en) * 2020-02-25 2024-05-01 Texas A & M Univ Sys METHODS OF TREATING ENDOMETRIOSIS

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US6548640B1 (en) 1986-03-27 2003-04-15 Btg International Limited Altered antibodies
US5223409A (en) 1988-09-02 1993-06-29 Protein Engineering Corp. Directed evolution of novel binding proteins
ATE102631T1 (de) 1988-11-11 1994-03-15 Medical Res Council Klonierung von immunglobulin sequenzen aus den variabelen domaenen.
US5859205A (en) 1989-12-21 1999-01-12 Celltech Limited Humanised antibodies
CA2229043C (en) 1995-08-18 2016-06-07 Morphosys Gesellschaft Fur Proteinoptimierung Mbh Protein/(poly)peptide libraries
US7053202B2 (en) 2001-10-19 2006-05-30 Millennium Pharmaceuticals, Inc. Immunoglobulin DNA cassette molecules, monobody constructs, methods of production, and methods of use therefor
WO2003073843A2 (en) 2002-03-05 2003-09-12 Artemis Pharmaceuticals Gmbh Inbred embryonic stem-cell derived mice
GB0414798D0 (en) * 2004-07-01 2004-08-04 Paradigm Therapeutics Ltd Receptor
US8691498B2 (en) 2005-09-02 2014-04-08 Arena Pharmaceuticals, Inc. Methods of screening for a compound that reduces atherogenesis
TW200732350A (en) 2005-10-21 2007-09-01 Amgen Inc Methods for generating monovalent IgG
AR089284A1 (es) * 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
GB201122146D0 (en) 2011-12-22 2012-02-01 Galapagos Nv Screening methods to identify compounds useful in the prevention and/or treatment of inflammatory conditions
CN104870445B (zh) * 2012-12-20 2017-09-15 加拉帕戈斯股份有限公司 用于治疗炎性疾病的新二氢嘧啶并异喹啉酮类及其药物组合物(gpr84拮抗剂)
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

Also Published As

Publication number Publication date
PE20191746A1 (es) 2019-12-12
SG11201909783VA (en) 2019-11-28
BR112019023999A2 (pt) 2020-06-30
MX2019013734A (es) 2020-01-15
AU2018269328A1 (en) 2019-11-07
KR20200003830A (ko) 2020-01-10
CN110573146A (zh) 2019-12-13
TW201900214A (zh) 2019-01-01
US20210401823A1 (en) 2021-12-30
CA3063489A1 (en) 2018-11-22
EP3403649A1 (en) 2018-11-21
EP3624781A1 (en) 2020-03-25
JP2020519662A (ja) 2020-07-02
WO2018210822A1 (en) 2018-11-22

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