AR092365A1 - Derivados de piridopirimidina - Google Patents

Derivados de piridopirimidina

Info

Publication number
AR092365A1
AR092365A1 ARP130102804A ARP130102804A AR092365A1 AR 092365 A1 AR092365 A1 AR 092365A1 AR P130102804 A ARP130102804 A AR P130102804A AR P130102804 A ARP130102804 A AR P130102804A AR 092365 A1 AR092365 A1 AR 092365A1
Authority
AR
Argentina
Prior art keywords
denotes
dihydro
atoms
mono
oxazinyl
Prior art date
Application number
ARP130102804A
Other languages
English (en)
Inventor
Dr Burgdorf Lars
Dr Kuhn Daniel
Dra Ross Tatjana
Dr Deutsch Carl
Original Assignee
Merck Patent Ges Mit Beschränkter Haftung
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 Merck Patent Ges Mit Beschränkter Haftung filed Critical Merck Patent Ges Mit Beschränkter Haftung
Publication of AR092365A1 publication Critical patent/AR092365A1/es

Links

Classifications

    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • 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
    • A61P31/08—Antibacterial agents for leprosy
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Rheumatology (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Biotechnology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)

Abstract

Son inhibidores de Syk (tirosina quinasa del bazo) y se pueden emplear, inter alia, para el tratamiento de cáncer, artritis reumatoidea y/o lupus sistémico. Reivindicación 1: Compuestos de la fórmula (1) en donde R denota H, OH, A o NR⁴R⁴; R¹ denota Ar¹, Het¹, CN, A o -CºC-Ar¹; R² denota Het², NR³Cyc, NR³CR³CON(R³)₂, NR³[C(R³)₂]ₚCR³(NH₂)CH₂OA o NR³[C(R³)₂]ₚN(R³)₂; Ar¹ denota fenilo, que está mono-, di- o trisustituido con A, (CH₂)ₙHet³, [C(R³)₂]ₙOR³, [C(R³)₂]ₙN(R³)₂, NO₂, CN, Hal, COOR³, CON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂ y/O S(O)ₘA; Het¹ denota 3,6-dihidro-2H-piranilo, tetrahidropiridinilo, 1,3-dihidro-bencimidazolilo, pirazolilo, cromanilo, 1,2,3,4-tetrahidro-pirazolo[1,5-a]piridinilo, 6,7-dihidro-4H-pirazolo[5,1-c][1,4]-oxazinilo, 1,4-dihidro-benzo[d][1,3]oxazinilo, 4H-benzo[1,4]oxazinilo, bencimidazolilo, piridilo, pirimidinilo, imidazolilo, pirazolito, furilo, tiazolilo, triazolilo, benzotriazolilo, indolilo, indazolilo, 1,3- ó 2,3-dihidro-indolilo, cada uno de los cuales puede no estar sustituido o puede estar mono-, di-, tri- o tetrasustituido con A, CN, OH, OA, Hal, SO₂NH₂, (CH₂)ₙNH₂, (CH₂)ₙNHA, (CH₂)ₙNA₂ y/u =O; Het² denota piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, tetrahidropiranilo, pirazolilo, indazolilo, azetidinilo u octahidro-bencimidazolilo, cada uno de los cuales está mono-, di- o trisustituido con Hal, A, (CH₂)ₙNH₂, (CH₂)ₙNHA, (CH₂)ₙNA₂, (CH₂)ₙOH y/o (CH₂)ₙOA; Het³ denota piperidinilo, piperazinilo, pirrolidinilo, morfolinilo, imidazolidinilo, piridilo, pirimidinilo, imidazolilo, pirazolilo, furilo, tiazolilo o triazolilo, cada uno de los cuales no está sustituido o está mono- o disustituido con A y/u =O; R³ denota H o alquilo que tiene 1, 2, 3 ó 4 átomos de C; R⁴, R⁴ denotan cada uno, de modo independiente entre sí, H o A; A denota alquilo no ramificado o ramificado que tiene 1 - 10 átomos de C, en donde 1 - 7 átomos de H pueden estar reemplazados por F y/o en donde uno o dos grupos CH₂ no adyacentes pueden estar reemplazados por O y/o NH, o alquilo cíclico que tiene 3 - 7 átomos de C; Cyc denota alquilo cíclico que tiene 3 - 7 átomos de C, que puede no estar sustituido o que puede estar monosustituido con NH₂, CN, CONH₂ u OH; m denota 0, 1 ó 2; n denota 0, 1, 2, 3 ó 4; p denota 1, 2, 3 ó 4; y sus solvatos, sales, enantiómeros, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP130102804A 2012-08-07 2013-08-07 Derivados de piridopirimidina AR092365A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12005716 2012-08-07

Publications (1)

Publication Number Publication Date
AR092365A1 true AR092365A1 (es) 2015-04-15

Family

ID=48782275

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130102804A AR092365A1 (es) 2012-08-07 2013-08-07 Derivados de piridopirimidina

Country Status (10)

Country Link
US (1) US9725462B2 (es)
EP (1) EP2882746B1 (es)
JP (2) JP6374384B2 (es)
CN (1) CN104507942B (es)
AR (1) AR092365A1 (es)
AU (1) AU2013301865B2 (es)
CA (1) CA2881279C (es)
ES (1) ES2618004T3 (es)
IL (1) IL237073A (es)
WO (1) WO2014023385A1 (es)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015511245A (ja) * 2012-02-23 2015-04-16 アッヴィ・インコーポレイテッド ピリドピリミジノン系キナーゼ阻害薬
US9725462B2 (en) * 2012-08-07 2017-08-08 Merck Patent Gmbh Pyridopyrimidine derivatives as protein kinase inhibitors
KR20140027714A (ko) * 2012-08-27 2014-03-07 주식회사 홍인터내셔날 외부 디바이스와 연동하는 다트 게임 장치
AU2016295594B2 (en) * 2015-07-21 2020-04-16 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Fused ring pyrimidine compound, intermediate, and preparation method, composition and use thereof
IL264186B1 (en) 2016-07-12 2024-04-01 Revolution Medicines Inc 2,5-dimutomers of 3-methylpyrazines and 2,5,6-dimutomers of 3-methylpyrazines as allosteric SHP2 inhibitors
LT3559009T (lt) 2016-12-22 2021-06-25 Calithera Biosciences, Inc. Kompozicijos ir būdai, skirti arginazės aktyvumo slopinimui
CN110431134A (zh) 2017-01-23 2019-11-08 锐新医药公司 作为变构shp2抑制剂的吡啶化合物
IL296456A (en) * 2017-01-23 2022-11-01 Revolution Medicines Inc Bicyclics as allosteric shp2 inhibitors
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3652174A4 (en) * 2017-07-13 2021-06-30 Syros Pharmaceuticals, Inc. TAM KINASE INHIBITORS
EP4141005B1 (en) 2017-09-08 2024-04-03 Amgen Inc. Inhibitors of kras g12c and methods of using the same
BR112020007058A2 (pt) 2017-10-12 2020-10-06 Revolution Medicines, Inc. compostos de piridina, pirazina, e triazina como inibidores de shp2 alostéricos
WO2019100106A1 (en) * 2017-11-24 2019-05-31 The University Of Sydney Antibacterial compounds and methods of use thereof
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
MX2020010836A (es) 2018-05-04 2021-01-08 Amgen Inc Inhibidores de kras g12c y métodos para su uso.
JP6995025B2 (ja) 2018-08-09 2022-02-04 株式会社豊田自動織機 太陽熱集熱管
CN110833557A (zh) * 2018-08-15 2020-02-25 广西梧州制药（集团）股份有限公司 吡唑并嘧啶衍生物在治疗肾小管肾炎的用途
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN114144414A (zh) 2019-05-21 2022-03-04 美国安进公司 固态形式
CN112409385A (zh) * 2019-08-22 2021-02-26 上海青煜医药科技有限公司 氮杂芳基化合物及其应用
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN115768750A (zh) * 2020-02-17 2023-03-07 阿莱斯塔治疗公司 Gcn2调节剂化合物
WO2022048684A1 (zh) * 2020-09-07 2022-03-10 武汉朗来科技发展有限公司 Jnk抑制剂、其药物组合物和用途
WO2022079250A1 (en) 2020-10-16 2022-04-21 Merck Patent Gmbh Compounds for the treatment of viral infections
CN117180122B (zh) * 2023-11-02 2024-04-09 杭州湃肽生化科技有限公司 一种舒敏修复组合物及其应用

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1987004928A1 (en) * 1986-02-24 1987-08-27 Mitsui Petrochemical Industries, Ltd. Agents for treating neurophathy
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
SK285141B6 (sk) 1996-02-13 2006-07-07 Astrazeneca Uk Limited Použitie chinazolínového derivátu, chinazolínový derivát, spôsob jeho prípravy a farmaceutická kompozícia, ktorá ho obsahuje
EP0885198B1 (en) 1996-03-05 2001-12-19 AstraZeneca AB 4-anilinoquinazoline derivatives
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
MXPA02011770A (es) 2000-05-31 2003-04-10 Astrazeneca Ab Derivados de indol con actividad de dano vascular.
IL153484A0 (en) 2000-07-07 2003-07-06 Angiogene Pharm Ltd Colchinol derivatives as angiogenesis inhibitors
WO2002008213A1 (en) 2000-07-07 2002-01-31 Angiogene Pharmaceuticals Limited Colchinol derivatives as angiogenesis inhibitors
US7732446B1 (en) 2004-03-11 2010-06-08 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2007125405A2 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
WO2008118823A2 (en) 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20110160232A1 (en) 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
SG2014015085A (en) 2008-04-16 2014-06-27 Portola Pharm Inc 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors
MX2010012010A (es) 2008-05-01 2010-11-30 Sirtris Pharmaceuticals Inc Quinolinas y analogos relacionados como moduladores de sirtuin.
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基***并吡啶，其組合物及使用其之治療方法
CA2745041C (en) 2008-12-01 2017-08-22 Kai Schiemann 2, 5-diamino-substituted pyrido [4, 3-d] pyrimidines as autotaxin inhibitors against cancer
KR101690358B1 (ko) * 2009-10-29 2017-01-09 제노스코 키나아제 억제제
WO2011075699A2 (en) 2009-12-18 2011-06-23 Sunovion Pharmaceuticals Inc. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
US9725462B2 (en) * 2012-08-07 2017-08-08 Merck Patent Gmbh Pyridopyrimidine derivatives as protein kinase inhibitors

Also Published As

Publication number Publication date
ES2618004T3 (es) 2017-06-20
EP2882746A1 (en) 2015-06-17
JP6374384B2 (ja) 2018-08-15
CA2881279C (en) 2020-07-07
CA2881279A1 (en) 2014-02-13
JP2018150307A (ja) 2018-09-27
CN104507942A (zh) 2015-04-08
US20150218186A1 (en) 2015-08-06
WO2014023385A1 (en) 2014-02-13
CN104507942B (zh) 2017-03-22
AU2013301865A1 (en) 2015-03-19
US9725462B2 (en) 2017-08-08
AU2013301865B2 (en) 2017-08-17
EP2882746B1 (en) 2016-12-07
JP2015529657A (ja) 2015-10-08
IL237073A (en) 2016-12-29

Similar Documents

Publication Publication Date Title
AR092365A1 (es) Derivados de piridopirimidina
AR096235A1 (es) Arilquinazolinas
AR093512A1 (es) Derivados heterociclicos como moduladores de la actividad de cinasas
AR097087A1 (es) Derivados de oxoquinazolinil-butanamida
AR090240A1 (es) Derivados de triazolopirazina
AR066543A1 (es) Derivados de piridazinona
AR090105A1 (es) Derivados de furopiridina
AR082726A1 (es) Derivados de triazolopirazina
AR068658A1 (es) Derivados de tiazol
SG10201806965XA (en) 3-(aryl or heteroaryl) methyleneindolin-2-one derivatives as inhibitors of cancer stem cell pathway kinases for the treatment of cancer
AR092211A1 (es) Derivados de hidropirrolopirrol
AR089945A1 (es) DERIVADOS DE FURO[3,2-B] Y TIENO[3,2-B]PIRIDINA COMO MODULADORES DE TBK1 E IKKe
AR095311A1 (es) 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante
AR089944A1 (es) Derivados de tetrahidro-quinazolinona
AR078313A1 (es) Derivados de piridinil-imidazolona inhibidores de quinasas pi3k,composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos en el tratamiento de enfermedades autoinmunes e inflamatorias, entre otras
AR094981A1 (es) Derivados de imidazopirimidinas
AR068749A1 (es) Derivados de n-(pirazol-3-il)-benzamida
AR082728A1 (es) Imidazolonilquinolinas utiles para tratar el cancer, composiciones farmaceuticas que las contienen, proceso de sintesis, intermediarios de dicha sintesis y procedimiento para prepararlos
AR090103A1 (es) Derivados ciclicos de diaminopirimidina
AR082727A1 (es) Derivados de furopiridina, procesos de preparacion y composiciones farmaceuticas que los contienen
AR100333A1 (es) Derivados de heterociclil-butanamida
AR092670A1 (es) Derivados de quinazolinona
AR097866A1 (es) Derivados de 4-azaindol
AR093143A1 (es) Compuestos de 2-aminopiridina
AR097086A1 (es) Derivados 1,3-disustituidos de ciclopentano

Legal Events

Date Code Title Description
FB Suspension of granting procedure