AR074688A1 - Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores. - Google Patents

Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores.

Info

Publication number
AR074688A1
AR074688A1 ARP090104911A ARP090104911A AR074688A1 AR 074688 A1 AR074688 A1 AR 074688A1 AR P090104911 A ARP090104911 A AR P090104911A AR P090104911 A ARP090104911 A AR P090104911A AR 074688 A1 AR074688 A1 AR 074688A1
Authority
AR
Argentina
Prior art keywords
piperidin
nhet
nhet1
hal
nor2
Prior art date
Application number
ARP090104911A
Other languages
English (en)
Inventor
Dieter Dorsch
Andree Blaukat
Frank Stieber
Oliver Schadt
Original Assignee
Merck Patent Gmbh
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 Gmbh filed Critical Merck Patent Gmbh
Publication of AR074688A1 publication Critical patent/AR074688A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
    • A61K31/505—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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/282—Organic compounds, e.g. fats
    • A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof

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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Los compuestos de la fórmula (1) en donde R1 es Ar, Het, A, OR2, O[C(R2)2]nAr, O[C(R2)2]nHet, N(R2)2, NR2[C(R2)2]nAr o NR2[C(R2)2]nHet; R2 es H o A'; R3, R3' son, en cada caso de modo independiente entre sí, H, Hal, A, OR2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, SO2N(R2)2 o S(O)mA, Y es [C(R2)2]nNR2COZ, [C(R2)2]nNR2COHet1, [C(R2)2]nCyc[C(R2)2]nN(R2)2, [C(R2)2]nCyc[C(R2)2]nOR2, [C(R2)2]nCyc[C(R2)2]nHet1, [C(R2)2]n-C(CH2)-((CH2)p)-[C(R2)2]nN(R2)2, [C(R2)2]n-C(CH2-(CH2)p)[C(R2)2]nOR2, [C(R2)2]n-C(CH2-(CH2)p)-[C(R2)2]nHet, [C(R2)2]nHet2, [C(R2)2]nCR2(NR2)2COOR2, [C(R2)2]nNR2CO[C(R2)2]nNR2COA, [C(R2)2]nNR2COOA, [C(R2)2]nCO-NR2-A, [C(R2)2]nCO-NR2-[C(R2)2]nHet1, [C(R2)2]nCONH2, [C(R2)2]nCONHA, [C(R2)2]nCONA2, [C(R2)2]nCO-NR2-[C(R2)2]nN(R2)2 o COOA; ; Z es CR2(NR2)2CR2(OR2)A, Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, [C(R2)2]nOR2, [C(R2)2]nN(R2)2, SR2, NO2, CN, CO-OR2, CON(R2)2, NR2COA, NR2SO2A, SO2N(R2)2, S(O)mA, CO-Het, Het, O[C(R2)2]nN(R2)2, O[C(R2)2]nHet, NHCOOA, NHCON(R2)2, NHCOO[C(R2)2]nN(R2)2, NHCOO[C(R2)2]nHet, NHCONH[C(R2)2]nN(R2)2, NHCONH[C(R2)2]nHet, OCONH[C(R2)2]nN(R2)2, OCONH[C(R2)2]nHet, CONR2[C(R2)2]nN(R2)2, CONR2[C(R2)2]nHet, y/o COA, Het es un heterociclo mono-, bi- o tricíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar mono-, di- o trisustituido con Hal, A, [C(R2)2]nOR2, [C(R2)2]n(R2)2, SR2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, SO2N(R2)2, S(O)mA, CO-Het1, [C(R2)2]nHet1, O[C(R2)2]nN(R2)2, O[C(R2)2]nHet1, NHCOOA, NHCON(R2)2, NHCOO[C(R2)2]nN(R2)2, NHCOO[C(R2)2]nHet1, NHCONH[C(R2)2]nN(R2)2, NHCONH[C(R2)2]nHet1, OCONH[C(R2)2]nN(R2)2, OCONH[C(R2)2]nHet1, CO-Het1, CHO, COA, =S, =NH, =NA y/u =O (oxígeno del carbonilo), Het1 es un heterociclo saturado monocíclico con 1 a 2 átomos de N y/u O, que puede estar mono- o disustituido con A, OA, OH, COOH, COOA, Hal y/u =O (oxígeno del carbonilo), Het2 es 2-metoxicarbonil-pirrolidin-4-ilo, 2-carboxi-pirrolidin-4-ilo, 1-ciclopropilmetil-piperidin-4-ilo, piperidin-4-ilo, morfolin-2-o 4-ilo, 1-isopropil-piperidin-4-ilo, 1-metil-piperidin-4-ilo, 4-piperazinilo, 1-metil-pirrolidin-2-ilo, 1-ter.-butoxicarbonil-piperidin-4-ilo, 1-etil-piperidin-2-ilo, 1-(2-metoxi-etil)-piperidin-4-ilo, 1-[2-(N,N-dimetilamino)-etil]-piperidin-4-ilo, 1,2,2,6,6-pentametil-piperidin-4-ilo, 1-aza-biciclo[2,2,2]oct-3-ilo, tetrahidropiran-4-ilo, 1-formil-piperidin-4-ilo o 1-metil-1-oxi-piperidin-4-ilo, A es alquilo no ramificado o ramificado C1-10, 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, NH, S, SO, SO2 y/o grupos CH=CH, o es alquilo cíclico C3-7, A' es alquilo no ramificado o ramificado C1-6 en donde 1-5 átomos de H pueden estar reemplazados por F; CyC es cicloalquileno C3-7; Hal es F, Cl, Br o I; m es 0, 1 o 2, n es 1, 2, 3 o 4, p es 1, 2, 3, 4, o 5; así como sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de las tirosina quinasas, en especial de la Met-quinasa, y pueden utilizarse, por ejemplo, para el tratamiento de tumores.
ARP090104911A 2008-12-23 2009-12-16 Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores. AR074688A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102008062826A DE102008062826A1 (de) 2008-12-23 2008-12-23 Pyridazinonderivate

Publications (1)

Publication Number Publication Date
AR074688A1 true AR074688A1 (es) 2011-02-02

Family

ID=41628227

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090104911A AR074688A1 (es) 2008-12-23 2009-12-16 Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores.

Country Status (22)

Country Link
US (1) US8637518B2 (es)
EP (1) EP2367815B1 (es)
JP (1) JP5592395B2 (es)
KR (1) KR20110098854A (es)
CN (1) CN102264727B (es)
AR (1) AR074688A1 (es)
AU (1) AU2009331991B2 (es)
BR (1) BRPI0923497A2 (es)
CA (1) CA2747863C (es)
CY (1) CY1116191T1 (es)
DE (1) DE102008062826A1 (es)
DK (1) DK2367815T3 (es)
EA (1) EA201100966A1 (es)
ES (1) ES2532139T3 (es)
HR (1) HRP20150375T1 (es)
HU (1) HUE025138T2 (es)
MX (1) MX2011006652A (es)
PL (1) PL2367815T3 (es)
PT (1) PT2367815E (es)
SI (1) SI2367815T1 (es)
WO (1) WO2010072296A1 (es)
ZA (1) ZA201105440B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102009003954A1 (de) * 2009-01-07 2010-07-08 Merck Patent Gmbh Pyridazinonderivate
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
MX2015007921A (es) * 2012-12-21 2016-03-03 Zenith Epigenetics Corp Compuestos heterociclicos novedosos como inhibidores de bromodominio.
SG11201506100XA (en) * 2013-02-07 2015-09-29 Merck Patent Gmbh Pyridazinone-amides derivatives
WO2015004534A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
WO2015002754A2 (en) 2013-06-21 2015-01-08 Zenith Epigenetics Corp. Novel bicyclic bromodomain inhibitors
US9855271B2 (en) 2013-07-31 2018-01-02 Zenith Epigenetics Ltd. Quinazolinones as bromodomain inhibitors
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
JP2017537946A (ja) 2014-12-11 2017-12-21 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． ブロモドメイン阻害剤としての置換複素環
CA2966450A1 (en) 2014-12-17 2016-06-23 Olesya KHARENKO Inhibitors of bromodomains
HUE051734T2 (hu) * 2016-10-27 2021-03-29 Fujian Cosunter Pharmaceutical Co Ltd Piridon-vegyület, mint C-Met inhibitor
US11465986B2 (en) 2018-04-26 2022-10-11 Fujian Akeylink Biotechnology Co., Ltd. Crystal form of c-MET inhibitor and salt form thereof and preparation method therefor
CN108752322A (zh) * 2018-09-12 2018-11-06 广州新民培林医药科技有限公司 一种新型Tepotinib衍生物和制备方法及其在抗肿瘤药物中的应用
WO2020191056A1 (en) * 2019-03-20 2020-09-24 Goldfinch Bio, Inc. Pyridazinones and methods of use thereof
WO2022063869A2 (en) * 2020-09-24 2022-03-31 Merck Patent Gmbh Compounds for the treatment of viral infections
CN114736191B (zh) * 2022-04-01 2023-08-08 上海工程技术大学 特普替尼中间体及其制备方法和应用
CN115583939A (zh) * 2022-11-04 2023-01-10 苏州莱安医药化学技术有限公司 一种特泊替尼中间体的合成方法
CN116768868B (zh) * 2023-08-15 2023-12-08 云南省药物研究所 一种哒嗪酮硫代衍生物及其制备方法和应用

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5795964A (en) 1980-12-04 1982-06-15 Morishita Seiyaku Kk Preparation of 2-substituted-3(2h)-pyridazinone derivative
US4397854A (en) 1981-05-14 1983-08-09 Warner-Lambert Company Substituted 6-phenyl-3(2H)-pyridazinones useful as cardiotonic agents
IL115889A0 (en) 1994-11-14 1996-01-31 Rohm & Haas Pyridazinones and their use as fungicides
US5635494A (en) 1995-04-21 1997-06-03 Rohm And Haas Company Dihydropyridazinones and pyridazinones and their use as fungicides and insecticides
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
DE19604388A1 (de) 1996-02-07 1997-08-14 Merck Patent Gmbh Arylalkyl-diazinone
BR9707495A (pt) 1996-02-13 1999-07-27 Zeneca Ltd Derivado de quinazolina processo para a preparação do mesmo composição farmacêutica e processo para a produç o de um efeito antiangiogênico e/ou de redução de permeabilidade vascular em um animal de sangue quente
KR100489174B1 (ko) 1996-03-05 2005-09-30 제네카-파마 소시에떼아노님 4-아닐리노퀴나졸린유도체
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
PT1043317E (pt) 1997-11-19 2009-05-11 Kowa Co Novos derivados de piridazina e fármacos que os contêm como ingrediente activo
TWI241295B (en) 1998-03-02 2005-10-11 Kowa Co Pyridazine derivative and medicine containing the same as effect component
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
IL152682A0 (en) 2000-05-31 2003-06-24 Astrazeneca Ab Indole derivatives with vascular damaging activity
US20050277627A1 (en) 2000-07-07 2005-12-15 Arnould Jean C Colchinol derivatives as vascular damaging agents
KR20030022264A (ko) 2000-07-07 2003-03-15 앤지오젠 파마슈티칼스 리미티드 신생 혈관 형성 억제제인 콜치놀 유도체
MXPA04003668A (es) 2001-10-31 2004-07-22 Merck Patent Gmbh Inhibidores de fosfodiesteresa de tipo 4 y usos de los mismos.
DE102005042742A1 (de) * 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
DE102005055355A1 (de) 2005-11-21 2007-10-31 Merck Patent Gmbh 3,6-Dihydro-2-oxo-6H-[1,3,4]thiadiazinderivate
DE102005055354A1 (de) 2005-11-21 2007-10-31 Merck Patent Gmbh Substituierte 5-Phenyl-3,6-dihydro-2-oxo-6H-[1,3,4]thiadiazine
DE102005057924A1 (de) 2005-12-05 2007-06-06 Merck Patent Gmbh Pyridazinonderivate
DE102006037478A1 (de) * 2006-08-10 2008-02-14 Merck Patent Gmbh 2-(Heterocyclylbenzyl)-pyridazinonderivate
GB0619753D0 (en) 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
DE102007025718A1 (de) * 2007-06-01 2008-12-04 Merck Patent Gmbh Pyridazinonderivate
DE102007025717A1 (de) * 2007-06-01 2008-12-11 Merck Patent Gmbh Arylether-pyridazinonderivate
DE102007032507A1 (de) * 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
DE102007061963A1 (de) * 2007-12-21 2009-06-25 Merck Patent Gmbh Pyridazinonderivate
BRPI0923480B8 (pt) * 2008-12-22 2021-05-25 Merck Patent Gmbh formas polimórficas de di-hidrogenofosfato de 6-(1-metil-1h-pirazol-4-il)-2-{3-[5-(2-morfolin-4-il-etóxi)-pirimidin-2-il]-benzil}-2h-piridazin-3-ona, seus processos de fabricação, composição farmacêutica, medicamento, e kit
WO2010113986A1 (ja) * 2009-03-30 2010-10-07 住友化学株式会社 ピリダジノン化合物の有害節足動物防除用途

Also Published As

Publication number Publication date
JP5592395B2 (ja) 2014-09-17
AU2009331991A1 (en) 2011-08-11
US20110257181A1 (en) 2011-10-20
MX2011006652A (es) 2011-07-12
DK2367815T3 (en) 2015-03-09
CN102264727B (zh) 2014-11-05
EP2367815B1 (de) 2015-01-14
DE102008062826A1 (de) 2010-07-01
BRPI0923497A2 (pt) 2019-09-24
CN102264727A (zh) 2011-11-30
CY1116191T1 (el) 2017-02-08
CA2747863A1 (en) 2010-07-01
SI2367815T1 (sl) 2015-05-29
AU2009331991B2 (en) 2015-10-22
EP2367815A1 (de) 2011-09-28
JP2012513418A (ja) 2012-06-14
ES2532139T3 (es) 2015-03-24
KR20110098854A (ko) 2011-09-01
CA2747863C (en) 2016-08-23
PL2367815T3 (pl) 2015-04-30
EA201100966A1 (ru) 2012-01-30
PT2367815E (pt) 2015-02-20
WO2010072296A1 (de) 2010-07-01
HUE025138T2 (en) 2016-03-29
HRP20150375T1 (hr) 2015-05-22
US8637518B2 (en) 2014-01-28
ZA201105440B (en) 2012-03-28

Similar Documents

Publication Publication Date Title
AR074688A1 (es) Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores.
AR066543A1 (es) Derivados de piridazinona
AR071208A1 (es) Derivados de piridazinona
AR057214A1 (es) Derivados de piridazinona como inhibidores, reguladores o moduladores de quinasas.
AR069843A1 (es) Derivados de piridazinona, procedimiento para preparar dichos compuestos, composiciones farmaceuticas y usos de los mismos para preparar un medicamento
AR072860A1 (es) Derivados de 3-(3-pirimidin-2-il-bencil)-[1,2,4]triazolo[4,3-b]piridazina
AR083670A1 (es) DERIVADOS DE 7-([1,2,3]TRIAZOL-4-IL)-PIRROLO[2,3-b]PIRAZINA UTILES COMO INHIBIDORES DE LA PROLIFERACION CELULAR, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y PROCEDIMIENTO PARA PREPARARLOS
AR073055A1 (es) Derivados biciclicos de triazol
AR094313A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR090220A1 (es) Inhibidores de serina/treonina cinasa
AR075122A1 (es) Derivados de piridazinona
PE20141370A1 (es) Inhibidores de quinasa
AR070828A1 (es) Derivados de azetidina y ciclobutano como inhibidores de jak
AR108388A2 (es) Compuestos de oxazol sustituidos con indazol como inhibidores de pi3-quinasas
AR092211A1 (es) Derivados de hidropirrolopirrol
AR066892A1 (es) Derivados de benzoxazolona, proceso, medicamento, uso para tratar tumores y kit
AR082109A1 (es) Derivados de bipiridilo
AR094214A1 (es) Inhibidores de la quinasa que regula la señal de la apoptosis
AR057109A1 (es) Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis
AR055376A1 (es) Derivados de 1-acildihidropirazol
AR089945A1 (es) DERIVADOS DE FURO[3,2-B] Y TIENO[3,2-B]PIRIDINA COMO MODULADORES DE TBK1 E IKKe
AR067081A1 (es) Derivados de pirrolo[2,3-b]piridin-pirimidina,proceso de preparacion, medicamentos que los contienen y usos de los mismos para el tratamiento de tumores cancerigenos y metastasis tumorales.
AR074418A1 (es) Compuestos de benzonaftiridina, procedimiento de preparacion y su uso en el tratamiento de tumores
AR077567A1 (es) Derivados de aminopiridina
AR077488A1 (es) Compuestos heterociclicos nitrogenados inhibidores de autotaxina, medicamentos que los contienen y uso de los mismos para el tratamiento y/o prevencion de cancer y enfermedades tumorales.

Legal Events

Date Code Title Description
FB Suspension of granting procedure