AR082109A1 - Derivados de bipiridilo - Google Patents

Derivados de bipiridilo

Info

Publication number
AR082109A1
AR082109A1 ARP110102395A ARP110102395A AR082109A1 AR 082109 A1 AR082109 A1 AR 082109A1 AR P110102395 A ARP110102395 A AR P110102395A AR P110102395 A ARP110102395 A AR P110102395A AR 082109 A1 AR082109 A1 AR 082109A1
Authority
AR
Argentina
Prior art keywords
cyy
denotes
nyy
atoms
het3
Prior art date
Application number
ARP110102395A
Other languages
English (en)
Inventor
Dipl-Chem Dorsch Dieter Dr
Jonczyk Alfred Dr
Amendt Christiane Dr
Zenke Frank Dr
Heolzemann Guenter Dr
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 AR082109A1 publication Critical patent/AR082109A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • 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
    • 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
    • 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
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • AIDS & HIV (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

La presente se refiere a derivados de bipiridilo de la fórmula (1) y al uso de tales compuestos, en donde la inhibición, regulación y/o modulación de la transducción de señales por proteínas que consumen ATP como quinasas desempeña un papel importante, en particular a inhibidores de las quinasas TGF-b receptoras y al uso de tales compuestos para el tratamiento de enfermedades inducidas por quinasas, en particular para el tratamiento de tumores.Reivindicación 1: Compuestos de la fórmula (1) en donde: W1, W2, W3 denotan de modo independiente entre sí, N o CR3; R1 denota arilo monocíclico que tiene 5, 6, 7, 8, 9 ó 10 átomos de C o un heteroarilo monocíclico que tiene 5, 6, 7, 8, 9, 10, 11, 12, 13 ó 14 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, cada uno de los cuales puede estar sustituido, de modo independiente entre sí, con al menos un sustituyente seleccionado del grupo que consiste en Y, Hal, CN, CF3, OY; R2 denota Ar, Het1, Het2, NY-Het1 o NY-Het2, con preferencia, denota Ar, Het1 o Het2, cada uno de los cuales puede estar sustituido, de modo independiente entre sí, con R4; R3 denota H, NYY o NY-COY; R4 denota Hal, A, -(CYY)n-OY, -(CYY)n-NYY, (CYY)n-Het3, (CYY)n-O-Het3, SY, NO2, CF3, CN, COOY, -CO-NYY, -NY-COA, -NY-SO2A, -SO2-NYY, S(O)mA, -CO-Het3, -O(CYY)n-NYY, -O(CYY)n-Het3, -NH-COOA, -NH-CO-NYY, -NH-COO-(CYY)n-NYY, -NH-COO-(CYY)n-Het3, -NH-CO-NH-(CYY)n-NYY, -NH-CO-NH(CYY)n-Het3,-OCO-NH-(CYY)n-NYY, -OCO-NH-(CYY)n-Het3, CHO, COA, =S, =NY, =O; Y denota H o A; A denota alquilo no ramificado o ramificado que tiene 1, 2, 3, 4, 5, 6, 7, 8, 9 ó 10 átomos de C, en donde 1, 2, 3,4, 5, 6 ó 7 átomos de H pueden estar reemplazados, de modo independiente entre sí, por Hal y/o en donde uno o dos grupos CH2 pueden estar reemplazados, de modo independiente entre sí, con O, S, SO, SO2, un grupo -CY=CY- y/o un grupo -CºC-; Ar denota un carbociclo mono- o bicíclico saturado, insaturado o aromático que tiene 5, 6, 7, 8, 9 ó 10 átomos de C; Het1 denota un heterociclo mono, bi- o tricíclico saturado o insaturado que tiene 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 ó 20 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S; Het2 denota un heteroarilo mono-, bi- o tricíclico que tiene 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 ó 20 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S; Het3 denota un heterociclo mono, bi- o tricíclico saturado o insaturado que tiene 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 ó 20 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, que puede estar sustituido, de modo independiente entre sí, con al menos un sustituyente seleccionado del grupo de Hal, A, -(CYY)n-OY, -(CYY)n-NYY, SY, NO2, CN, CF3, COOY, -CO-NYY, -NY-COA, -NY-SO2A, -SO2-NYY, S(O)mA, -NH-COOA, -NH-CO-NYY, CHO, COA, =S, =NY, =O; Hal denota F, Cl, Br o I; m denota 0, 1 ó 2; n denota 0, 1, 2, 3 ó 4; y sus sales, solvatos, tautómeros y estereoisómeros fisiológicamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP110102395A 2010-07-05 2011-07-05 Derivados de bipiridilo AR082109A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10006927 2010-07-05

Publications (1)

Publication Number Publication Date
AR082109A1 true AR082109A1 (es) 2012-11-14

Family

ID=44259587

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110102395A AR082109A1 (es) 2010-07-05 2011-07-05 Derivados de bipiridilo

Country Status (15)

Country Link
US (2) US8846931B2 (es)
EP (1) EP2590946B1 (es)
JP (1) JP5886842B2 (es)
KR (1) KR20130131293A (es)
CN (1) CN102971293A (es)
AR (1) AR082109A1 (es)
AU (1) AU2011276193B2 (es)
BR (1) BR112012033658A2 (es)
CA (1) CA2804285C (es)
EA (1) EA201300080A1 (es)
ES (1) ES2535656T3 (es)
IL (1) IL223978A (es)
MX (1) MX2012014537A (es)
SG (1) SG186871A1 (es)
WO (1) WO2012003912A1 (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2711558C (en) 2008-01-04 2016-12-13 Intellikine, Inc. Phosphatidyl inositol-3 kinase inhibiting compounds
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
AU2012205669B2 (en) 2011-01-10 2015-08-20 Infinity Pharmaceuticals Inc. Processes for preparing isoquinolinones and solid forms of isoquinolinones
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
AU2013326867B2 (en) * 2012-10-05 2018-03-08 Rigel Pharmaceuticals, Inc. GDF-8 inhibitors
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
GB201312800D0 (en) 2013-07-17 2013-08-28 Heptares Therapeutics Ltd mGlu5 modulators
WO2015108881A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2015108861A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
CN104004762B (zh) * 2014-05-20 2016-03-30 南京医科大学附属南京儿童医院 Tgf-r反义序列及其在制备抗气道炎症反应药物中的应用
CN107531666A (zh) * 2015-02-20 2018-01-02 里格尔药品股份有限公司 Gdf‑8抑制剂
MX391135B (es) 2016-06-24 2025-03-21 Infinity Pharmaceuticals Inc Terapias de combinacion.
JP7132937B2 (ja) 2017-03-15 2022-09-07 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト Ｈｐｋ１の阻害剤としてのアザインドール
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
WO2019071144A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. USE OF P38 INHIBITORS TO REDUCE DUX4 EXPRESSION
MD3762368T2 (ro) 2018-03-08 2022-07-31 Incyte Corp Compuși diol aminopirazină ca inhibitori ai PI3K-Y
CA3093851A1 (en) 2018-03-29 2019-10-03 Arbutus Biopharma Corporation Substituted 1,1'-biphenyl compounds, analogues thereof, and methods using same
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
EP4087657A1 (en) 2020-01-08 2022-11-16 Synthis Therapeutics, Inc. Alk5 inhibitor conjugates and uses thereof
CN117412959A (zh) * 2021-03-29 2024-01-16 爱彼特生物制药公司 经取代的1-芳基-1'-杂芳基化合物、经取代的1,1'-联杂芳基化合物和其使用方法
MX2023011552A (es) * 2021-03-29 2024-01-03 Arbutus Biopharma Corp Compuestos de 1-arilo-1'-heteroarilo sustituido, compuestos de 1,1'-biheteroarilo sustituido, y métodos de uso de estos.
EP4727586A1 (en) 2023-06-13 2026-04-22 Synthis Therapeutics, Inc. Anti-cd5 antibodies and their uses

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
AU4972900A (en) 1999-04-08 2000-11-14 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
AU2003260345A1 (en) * 2002-07-31 2004-02-23 Smithkline Beecham Corporation 2-phenylpyridin-4-yl derivatives as alk5 inhibitors
GB0218876D0 (en) * 2002-08-13 2002-09-25 Merck Sharp & Dohme Therapeutic agents
US20060293339A1 (en) 2003-03-24 2006-12-28 Chakravarty Prasun K Biaryl substituted 6-membered heterocycles as sodium channel blockers
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US7504401B2 (en) 2003-08-29 2009-03-17 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
BRPI0519424B8 (pt) 2004-12-28 2021-05-25 Athenex Inc compostos, composição e uso dos ditos compostos para a preparação de um medicamento para prevenção ou tratamento de um distúrbio de proliferação celular ou infecção microbiana
BRPI0619424B1 (pt) 2005-12-05 2022-02-08 Pfizer Products Inc Uso de inibidores c-met/hgfrs para a fabricação de medicamentos
US20070191371A1 (en) 2006-02-14 2007-08-16 Kalypsys, Inc. Heterocyclic modulators of ppar
US20080280891A1 (en) 2006-06-27 2008-11-13 Locus Pharmaceuticals, Inc. Anti-cancer agents and uses thereof
CN101595084B (zh) 2006-06-29 2013-01-02 金克斯医药品有限公司 用于调整激酶级联的二芳基组合物和方法
ES2500165T3 (es) 2006-06-29 2014-09-30 Kinex Pharmaceuticals, Llc Composiciones de biarilo y métodos para modular una cascada de quinasas
WO2008008059A1 (en) 2006-07-12 2008-01-17 Locus Pharmaceuticals, Inc. Anti-cancer agents ans uses thereof
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
JP4751856B2 (ja) 2007-07-03 2011-08-17 本田技研工業株式会社 車体側部構造
US20090069288A1 (en) 2007-07-16 2009-03-12 Breinlinger Eric C Novel therapeutic compounds
WO2009024825A1 (en) 2007-08-21 2009-02-26 Astrazeneca Ab 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors
EP2231642B1 (en) * 2008-01-11 2013-10-23 Novartis AG Pyrimidines as kinase inhibitors
US8343966B2 (en) 2008-01-11 2013-01-01 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
EA201300080A1 (ru) 2013-06-28
EP2590946A1 (en) 2013-05-15
AU2011276193B2 (en) 2015-01-22
US9051307B2 (en) 2015-06-09
SG186871A1 (en) 2013-02-28
BR112012033658A2 (pt) 2016-11-29
US20130102608A1 (en) 2013-04-25
CA2804285C (en) 2019-05-14
US20140336201A1 (en) 2014-11-13
US8846931B2 (en) 2014-09-30
ES2535656T3 (es) 2015-05-13
AU2011276193A1 (en) 2013-02-21
JP2013530192A (ja) 2013-07-25
KR20130131293A (ko) 2013-12-03
CN102971293A (zh) 2013-03-13
IL223978A (en) 2017-10-31
CA2804285A1 (en) 2012-01-12
WO2012003912A8 (en) 2012-03-08
JP5886842B2 (ja) 2016-03-16
EP2590946B1 (en) 2015-02-18
AU2011276193A8 (en) 2013-05-02
WO2012003912A1 (en) 2012-01-12
MX2012014537A (es) 2013-02-21

Similar Documents

Publication Publication Date Title
AR085637A1 (es) Derivados de pirido[2,3-b]pirazina
AR081994A1 (es) Derivados de [1,8]naftiridina, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para el tratamiento de enfermedades inducidas por quinasas, en particular diferentes tipos de canceres
AR113818A2 (es) Pirazolo-quinazolinas como inhibidores de proteína quinasa
AR096246A1 (es) Derivados de benzimidazol como inhibidores de bromodominio
AR072622A1 (es) Derivados de imidazo[2,1-b][1,3,4]tiadiazol, composiciones farmaceuticas que los comprenden, metodo para prepararlos, y uso de los mismos para el tratamiento de tumores y otras enfermedades inducidas por quinasas
ES2570127T3 (es) Compuestos y composiciones como inhibidores de la proteína quinasa
AR068658A1 (es) Derivados de tiazol
PE20070832A1 (es) Derivados de piridazinona como inhibidores de la tirosina quinasa
AR067478A1 (es) Compuestos derivados de morfolina pirimidina
AR085283A1 (es) Antagonistas de hepcidina a base de sulfonaminoquinolina
AR095311A1 (es) 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante
AR066543A1 (es) Derivados de piridazinona
AR079205A1 (es) Morfolinotiazoles como moduladores alostericos positivos alfa 7
AR089774A1 (es) Derivados de indolizina, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
AR087841A1 (es) Derivados de tetrahidrotriazolopirimidina
AR057109A1 (es) Benzimidazoles sustituidos y metodos para usarlos como inhibidores de las quinasas asociadas con la tumorigenesis
AR093077A1 (es) ANTAGONISTAS DE mGlu2/3 PARA EL TRATAMIENTO DE LOS TRASTORNOS AUTISTAS
AR094116A1 (es) Imidazopiridinas sustituidas como inhibidores de hdm2
AR068872A1 (es) 5- ciano- tienopiridinas. procesos de obtencion y composiciones farmaceuticas.
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
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
AR071208A1 (es) Derivados de piridazinona
AR100418A1 (es) Compuestos y composiciones para inducir condrogénesis
CO6420344A2 (es) Derivados de triazolopiridina como inhibidores de proteínas cinasas activadas por mitogeno p38 (map)
AR097087A1 (es) Derivados de oxoquinazolinil-butanamida

Legal Events

Date Code Title Description
FA Abandonment or withdrawal
FB Suspension of granting procedure