[go: up one dir, main page]

AR056008A1 - Derivados de pirazina antagonistas del receptor a2b de adenosina - Google Patents

Derivados de pirazina antagonistas del receptor a2b de adenosina

Info

Publication number
AR056008A1
AR056008A1 ARP060103279A ARP060103279A AR056008A1 AR 056008 A1 AR056008 A1 AR 056008A1 AR P060103279 A ARP060103279 A AR P060103279A AR P060103279 A ARP060103279 A AR P060103279A AR 056008 A1 AR056008 A1 AR 056008A1
Authority
AR
Argentina
Prior art keywords
alkyl
groups
group
alkylamino
aryl
Prior art date
Application number
ARP060103279A
Other languages
English (en)
Inventor
Trias Cristina Esteve
Pueyo Lidia Soca
Paul Robert Eastwood
Juan Bernat Vidal
Original Assignee
Almirall Lab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35945119&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR056008(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Almirall Lab filed Critical Almirall Lab
Publication of AR056008A1 publication Critical patent/AR056008A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Composiciones farmacéuticas que los contienen u usos para el tratamiento, prevencion o supresion de enfermedades y trastornos que se sabe son susceptibles de mejorar por antagonismo del receptor A2B de adenosina, tales como asma, enfermedad pulmonar obstructiva cronica, fibrosis pulmonar, enfisema, enfermedades alérgicas, inflamacion, dano por reperfusion, isquemia, miocárdica, aterosclerosis, hipertension, retinopatía, diabetes mellitus, trastornos inflamatorios del tracto gastrointestinal y/o enfermedades autoinmunes. Reivindicaciones: Compuesto de la formula (1) en donde: A representa un grupo arilo o heteroarilo monocíclico o policíclico opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que comprende átomos de halogeno, grupos alquilo C1-4, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-4, aril-alcoxi C1-4, alquiltio C1-4, mono- o di-alquilamino C1-4, trifluorometilo, hidroxi y ciano; B representa un grupo heteroarilo monocíclico que contiene nitrogeno opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo que comprende átomos de halogeno, grupos alquilo C1-4, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-4, arilo, alquiltio C1-4, mono o di-alquilamino C1-4, trifluorometilo y ciano; y bien a) R1 representa un grupo de formula: -L-(CR'R'')n-G en donde L representa un grupo de enlace seleccionado del grupo que consiste en un enlace directo, -(CO)-, - (CO)O-, -(CO)NR'-, -SO2- y -SO2NR'-; R'y R'' se seleccionan independientemente del grupo que consiste en átomos de hidrogeno y grupos alquilo C1-4 n es un numero entero de 0 a 6; y G se selecciona del grupo que consiste en átomo de hidrogeno y grupos alquilo C1-4, arilo, heteroarilo, cicloalquilo C3-8 y grupos heterocíclicos saturados o insaturados, en donde los grupos alquilo, cicloalquilo C3-8, arilo o heteroarilo están no sustituidos o sustituidos con uno o más sustituyentes seleccionados de átomos de halogeno, grupos alquilo C1-4, alcoxi C1-4, alquilo C1-4, mono - o di-alquilamino C1-4, trifluorometilo, trifluorometoxi, carbamoílo, carboxi y ciano; y R2 representa un grupo seleccionado de átomos de hidrogeno, átomos de halogeno y grupos alquilo C1-4, alquenilo C2-5, alquinilo C2-5, alcoxi C1-4, alquiltio C1-4, mono o di-alquilamino C1-4, alcoxi C1-4-(CO)-, -NH2, mono o di-alquilamino C1-4-(CO)- y ciano en donde los grupos alquilo, alquenilo y alquinilo pueden estar no sustituidos o sustituidos con un grupo arilo o heteroarilo o bien b) R2, R1 y el grupo -NH-al cual está unido R1, forman un resto seleccionado del resto de las formulas (2) y (3) en donde: Ra se selecciona de átomo de hidrogeno, átomos de halogeno, -OH, -NH2 o grupos seleccionados de alquilo C1-4, cicloalquilo C3-8, cicloalquilo C3-8-alquilo C1-4, arilo, aril-alquilo C1-4, heteroarilo, heteroaril-alquilo C1-4, anillos heterocíclicos saturados, alcoxi C1-4 y alquiltio C1-4, en donde los restos arilo o heteroarilo están no sustituidos o sustituidos con uno o más grupos seleccionados de átomos de halogeno, grupos alquilo C1-4, alquiltio C1-4, alcoxi C1-4, mono o di -alquilamino C1-4, ciano, trifluorometilo, trifluorometoxi, carbamoílo y carboxi; Rb se selecciona de hidrogeno, átomos de halogeno y grupos seleccionados de alquilo C1-4, alquilamino C1-4, aril-alquilamino C1-4 y -NH2; y sus sales y N-oxidos farmacéuticamente aceptables; con la condicion de que el compuesto no se selecciona de N-[6-(1-metil-1H-indol-3-il)-5-piridin-2-ilpirazin-2-il]benzamida, N-[3-etoxicarbonil-6-(1-metil-1H-indol-3-il)-5-piridin-2-il-pirazin-2-il]-benzamida y N-[3-etoxicarbonil-6-(1metil-1H-indol-3-il)-5-pirimidin-2-il-pirazin-2- il]formamida. 0
ARP060103279A 2005-07-29 2006-07-28 Derivados de pirazina antagonistas del receptor a2b de adenosina AR056008A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ES200501876A ES2270715B1 (es) 2005-07-29 2005-07-29 Nuevos derivados de pirazina.

Publications (1)

Publication Number Publication Date
AR056008A1 true AR056008A1 (es) 2007-09-12

Family

ID=35945119

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060103279A AR056008A1 (es) 2005-07-29 2006-07-28 Derivados de pirazina antagonistas del receptor a2b de adenosina

Country Status (22)

Country Link
US (2) US7790728B2 (es)
EP (1) EP1922313A1 (es)
JP (1) JP2009502837A (es)
KR (1) KR20080040681A (es)
CN (1) CN101268064A (es)
AR (1) AR056008A1 (es)
AU (1) AU2006278875A1 (es)
CA (1) CA2616428A1 (es)
EC (1) ECSP088113A (es)
ES (1) ES2270715B1 (es)
IL (1) IL188725A0 (es)
MX (1) MX2008001035A (es)
NO (1) NO20080451L (es)
NZ (1) NZ565150A (es)
PE (1) PE20070407A1 (es)
RU (1) RU2417994C2 (es)
SG (1) SG162805A1 (es)
TW (1) TW200728299A (es)
UA (1) UA93883C2 (es)
UY (1) UY29672A1 (es)
WO (1) WO2007017096A1 (es)
ZA (1) ZA200800353B (es)

Families Citing this family (79)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5307402B2 (ja) * 2005-01-25 2013-10-02 シンタ ファーマシューティカルズ コーポレーション 炎症及び免疫に関連する用途に用いる化合物
ES2274712B1 (es) 2005-10-06 2008-03-01 Laboratorios Almirall S.A. Nuevos derivados imidazopiridina.
BRPI0717767A2 (pt) * 2006-10-19 2013-11-12 Signal Pharm Llc Composto, composição farmacêutica, e, métodos para tratar ou prevenir câncer, uma condição inflamatória, uma condição imunológica ou uma condição metabólica, e para inibir uma quinase em uma célula de expressa a dita quinase
ES2303776B1 (es) * 2006-12-29 2009-08-07 Laboratorios Almirall S.A. Derivados de 5-fenil-6-piridin-4-il-1,3-dihidro-2h-imidazo(4,5-b)piridin-2-ona utiles como antagonistas del receptor de adenosina a2b.
ES2320955B1 (es) 2007-03-02 2010-03-16 Laboratorios Almirall S.A. Nuevos derivados de 3-((1,2,4)triazolo(4,3-a)piridin-7-il)benzamida.
JP5485178B2 (ja) * 2008-02-25 2014-05-07 エフ．ホフマン−ラ ロシュ アーゲー ピロロピラジンキナーゼ阻害剤
CA2718983C (en) 2008-03-26 2015-12-08 Advinus Therapeutics Pvt. Ltd. Heterocyclic compounds as adenosine receptor antagonist
EP2108641A1 (en) 2008-04-11 2009-10-14 Laboratorios Almirall, S.A. New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
EP2113503A1 (en) 2008-04-28 2009-11-04 Laboratorios Almirall, S.A. New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
EP2394999B1 (en) 2009-02-06 2014-01-29 Nippon Shinyaku Co., Ltd. Aminopyrazine derivative and medicine
CN102438624B (zh) 2009-03-13 2016-03-30 阿德维纳斯治疗私人有限公司 取代的稠合嘧啶化合物
US8796290B2 (en) 2009-11-09 2014-08-05 Advinus Therapeutics Limited Substituted fused pyrimidine compounds, its preparation and uses thereof
EP2322176A1 (en) 2009-11-11 2011-05-18 Almirall, S.A. New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
EP2338890A1 (en) 2009-12-22 2011-06-29 Bayer CropScience AG 4,7-Diazaindole derivatives and their use as fungicides
KR101993867B1 (ko) * 2010-02-05 2019-06-27 헵테얼즈 테라퓨틱스 리미티드 1,2,4-트리아진-4-아민 유도체들
CN101817823B (zh) * 2010-03-31 2012-09-12 上海毕得医药科技有限公司 4，7-二氮杂吲哚及其5位取代物的制备方法
SI2593452T1 (sl) 2010-07-14 2017-06-30 Novartis Ag Heterociklične spojine agonisti receptorja IP
US8940751B2 (en) 2010-09-13 2015-01-27 Advinus Therapeutics Private Limited Purine compounds as prodrugs of A2B adenosine receptor antagonists, their process and medicinal applications
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
TWI659030B (zh) * 2011-10-26 2019-05-11 諾華公司 Ｉｐ受體促效劑雜環化合物
UY34572A (es) 2012-01-13 2013-09-02 Novartis Ag Compuestos heterocíclicos agonistas del receptor ip
EP2802582A1 (en) * 2012-01-13 2014-11-19 Novartis AG Fused dihydropyrido [2,3 -b]pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
CN104169282B (zh) * 2012-01-13 2016-04-20 诺华股份有限公司 Ip受体激动剂的盐
WO2013105058A1 (en) * 2012-01-13 2013-07-18 Novartis Ag 7,8- dihydropyrido [3, 4 - b] pyrazines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
EP2802583A1 (en) * 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
US9115129B2 (en) 2012-01-13 2015-08-25 Novartis Ag Substituted pyrido[2,3-B]pyrazines as IP receptor agonists
JP6176244B2 (ja) 2012-05-30 2017-08-09 日本新薬株式会社 芳香族複素環誘導体及び医薬
PH12019502809B1 (en) 2012-06-13 2024-04-24 Incyte Holdings Corp Substituted tricyclic compounds as fgfr inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
WO2014087208A2 (en) * 2012-12-06 2014-06-12 Enaltec Labs Pvt. Ltd. A process of preparing alcaftadine
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9604981B2 (en) 2013-02-13 2017-03-28 Novartis Ag IP receptor agonist heterocyclic compounds
SMT201800127T1 (it) 2013-04-19 2018-05-02 Incyte Holdings Corp Eterocilci biciclici come inibitori di fgfr
CN103364500B (zh) * 2013-06-29 2019-01-22 北京万全德众医药生物技术有限公司 一种用液相色谱法分离测定比拉斯汀原料及其制剂的方法
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CA2967944C (en) * 2014-11-18 2020-11-17 Merck Sharp & Dohme Corp. Aminopyrazine compounds with a2a antagonist properties
CN104447583B (zh) * 2014-11-20 2016-08-24 广东东阳光药业有限公司 含有环丁烷取代基的吡嗪类化合物及其组合物及用途
CN104447585B (zh) * 2014-11-20 2016-08-24 广东东阳光药业有限公司 吡嗪类化合物及其组合物及用途
CN104447584B (zh) * 2014-11-20 2016-08-24 广东东阳光药业有限公司 含有环丁烷取代基的吡嗪类化合物及其组合物及用途
CN104402833B (zh) * 2014-11-20 2016-08-24 广东东阳光药业有限公司 含有环丁烷取代基的吡嗪类化合物及其组合物及用途
CN104496918B (zh) * 2014-12-10 2016-08-24 广东东阳光药业有限公司 吡嗪衍生物及其用途
JP6787899B2 (ja) * 2014-12-23 2020-11-18 ベルゲンビオ アーエスアー 医薬的活性化合物
SG10201913036RA (en) 2015-02-20 2020-02-27 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
ES2580702B1 (es) * 2015-02-25 2017-06-08 Palobiofarma, S.L. Derivados de 2-aminopiridina como antagonistas del receptor A2b de adenosina y ligandos del receptor MT3 de melatonina
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JP7013213B2 (ja) * 2017-05-26 2022-01-31 日本化薬株式会社 ピラジン化合物
US10793561B2 (en) * 2017-07-18 2020-10-06 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
US11028058B2 (en) 2017-07-18 2021-06-08 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
WO2019204813A1 (en) * 2018-04-20 2019-10-24 Virginia Tech Intellectual Properties, Inc. Oxadiazolopyrazines and oxadiazolopyridines useful as mitochondrial uncouplers
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
JP2021523121A (ja) 2018-05-04 2021-09-02 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｆｇｆｒ阻害剤の固体形態及びその調製プロセス
CN109020881B (zh) * 2018-06-28 2020-04-28 新发药业有限公司 一种阿帕替尼的制备方法
CN112279837B (zh) * 2018-08-17 2022-08-09 迪哲(江苏)医药股份有限公司 吡嗪化合物和其用途
EP3870573B1 (en) * 2018-10-24 2023-08-02 LeadXpro AG Functionalized aminotriazines
CN111377873B (zh) * 2018-12-28 2023-03-28 四川科伦博泰生物医药股份有限公司 氨基嘧啶化合物及其制备方法和用途
CN111377906B (zh) * 2018-12-28 2022-09-02 四川科伦博泰生物医药股份有限公司 取代的吡嗪化合物及其制备方法和用途
JP2022515309A (ja) * 2018-12-28 2022-02-18 四川科倫博泰生物医薬股▲フン▼有限公司 置換アリール化合物、その製造方法及び用途
CN113939291A (zh) 2019-01-18 2022-01-14 诺维逊生物股份有限公司 1,8-萘啶酮化合物及其用途
US20220119367A1 (en) * 2019-01-18 2022-04-21 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
US11306071B2 (en) * 2019-01-18 2022-04-19 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
CN110407677B (zh) * 2019-06-17 2022-10-11 南京先进生物材料与过程装备研究院有限公司 二苯乙二酮类化合物的制备方法及应用
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN112479956A (zh) * 2019-07-30 2021-03-12 杭州阿诺生物医药科技有限公司 一种用于制备腺苷受体抑制剂中间体的方法
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JOP20220083A1 (ar) 2019-10-14 2023-01-30 Incyte Corp حلقات غير متجانسة ثنائية الحلقة كمثبطات لـ fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
IL293001A (en) 2019-12-04 2022-07-01 Incyte Corp Derivatives of fgfr repressors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021146631A1 (en) * 2020-01-17 2021-07-22 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
WO2021146629A1 (en) * 2020-01-17 2021-07-22 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
JP2024522188A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN116903634B (zh) * 2023-07-17 2025-07-29 上海美迪西生物医药股份有限公司 一种6-苯基噻吩并[2,3-b]吡嗪的制备方法
WO2025036840A1 (en) * 2023-08-11 2025-02-20 Almirall, S.A. Pyridine or pyrazine derivatives as collagen vii (c7) inducers and their use in therapy

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9309573D0 (en) * 1993-05-10 1993-06-23 Merck Sharp & Dohme Therapeutic agents
US5686470A (en) * 1995-02-10 1997-11-11 Weier; Richard M. 2, 3-substituted pyridines for the treatment of inflammation
US6096748A (en) 1996-03-13 2000-08-01 Smithkline Beecham Corporation Pyrimidine compounds useful in treating cytokine mediated diseases
DE19632549A1 (de) * 1996-08-13 1998-02-19 Merck Patent Gmbh Arylalkanoylpyridazine
TW520362B (en) 1996-12-05 2003-02-11 Amgen Inc Substituted pyrimidine compounds and pharmaceutical composition comprising same
DK1042293T3 (da) 1997-12-19 2008-07-14 Amgen Inc Substituerede pyridin- og pyridazinforbindelser og deres farmaceutiske anvendelse
DE69919707T2 (de) 1998-06-19 2005-09-01 Chiron Corp., Emeryville Glycogen synthase kinase 3 inhibitoren
US6545002B1 (en) 1999-06-01 2003-04-08 University Of Virginia Patent Foundation Substituted 8-phenylxanthines useful as antagonists of A2B adenosine receptors
NZ516260A (en) * 1999-07-02 2004-08-27 Eisai Co Ltd Fused imidazole compounds and remedies for diabetes mellitus
WO2001016134A1 (en) 1999-08-31 2001-03-08 Vanderbilt University Selective antagonists of a2b adenosine receptors
BR0108454A (pt) 2000-02-17 2003-04-01 Cv Therapeutics Inc Métodos para identificação e uso de antagonistas de receptor de adenosina a(2b) papa mediar a proliferação celular em mamìferos
WO2001062233A2 (en) 2000-02-25 2001-08-30 F. Hoffmann La Roche Ag Adenosine receptor modulators
NZ521633A (en) 2000-04-26 2005-01-28 Eisai Co Ltd Use of an adenosine A2 or A2b recpetor antagonist for promoting bowel movement
CN1446202A (zh) 2000-08-11 2003-10-01 卫材株式会社 2－氨基吡啶化合物及其作为药物的用途
KR100860827B1 (ko) 2000-09-06 2008-09-30 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 글리코겐 합성효소 키나아제 3의 억제제
DE60128709T2 (de) 2000-09-15 2007-12-27 Vertex Pharmaceuticals Inc., Cambridge Triazol-verbindungen als protein-kinase-inhibitoren
CN100482793C (zh) 2000-09-19 2009-04-29 诺华疫苗和诊断公司 GSK-3β蛋白质的鉴定及其使用方法
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
JP4335000B2 (ja) 2001-06-29 2009-09-30 シーブイ・セラピューティクス・インコーポレイテッド Ａ２ｂアデノシン・レセプタ拮抗剤
TWI330183B (es) * 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
US7125993B2 (en) * 2001-11-09 2006-10-24 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
IL161867A0 (en) 2001-11-09 2005-11-20 Cv Therapeutics Inc A2b adenosine receptor antagonists
US6977300B2 (en) * 2001-11-09 2005-12-20 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
WO2003057689A1 (en) 2002-01-02 2003-07-17 Fujisawa Pharmaceutical Co., Ltd. Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them
BR0302965A (pt) 2002-02-01 2005-02-09 King Pharmaceuticals Res & Dev Composto e método de tratar doenças mediadas por receptores de adenosina a2b
AU2003245700A1 (en) 2002-02-12 2003-09-04 Glaxo Group Limited Pyrazolopyridine derivatives
AU2003225964B2 (en) 2002-03-28 2008-11-20 Merck Sharp & Dohme Corp. Substituted 2,3-diphenyl pyridines
CA2489179A1 (en) 2002-06-12 2003-12-24 Biogen Idec Ma Inc. Method of treating ischemia reperfusion injury using adenosine receptor antagonists
WO2004022540A2 (en) 2002-09-06 2004-03-18 Fujisawa Pharmaceutical Co., Ltd. Pyridazinone and pyridone derivatives as adenosine antagonists
KR20110050745A (ko) 2002-10-03 2011-05-16 탈자진 인코포레이티드 혈관항상성 유지제 및 그의 사용 방법
MXPA05009069A (es) 2003-02-27 2005-10-19 Uriach Y Compania S A J Derivados de pirazolopiridina.
CA2524778C (en) 2003-05-06 2013-01-29 Cv Therapeutics, Inc. Xanthine derivatives as a2b adenosine receptor antagonists
CN101851238B (zh) 2003-08-25 2012-07-18 卓维斯医药品有限责任公司 取代的8-杂芳基黄嘌呤
ES2229928B1 (es) * 2003-10-02 2006-07-01 Almirall Prodesfarma, S.A. Nuevos derivados de pirimidin-2-amina.
GB0323138D0 (en) 2003-10-03 2003-11-05 Chang Lisa C W Pyrimidines substituted in the 2,4,6 positions and their different uses
KR20060123208A (ko) * 2003-10-27 2006-12-01 아스테라스 세이야쿠 가부시키가이샤 피라진 유도체 및 이의 약학적 용도
BRPI0415888A (pt) 2003-10-31 2007-01-09 Cv Therapeutics Inc antagonistas do receptor de adenosina a2b
GB0401336D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
ES2241496B1 (es) 2004-04-15 2006-12-01 Almirall Prodesfarma, S.A. Nuevos derivados de piridina.
ES2274712B1 (es) * 2005-10-06 2008-03-01 Laboratorios Almirall S.A. Nuevos derivados imidazopiridina.
ES2303776B1 (es) 2006-12-29 2009-08-07 Laboratorios Almirall S.A. Derivados de 5-fenil-6-piridin-4-il-1,3-dihidro-2h-imidazo(4,5-b)piridin-2-ona utiles como antagonistas del receptor de adenosina a2b.

Also Published As

Publication number Publication date
NZ565150A (en) 2011-02-25
US20090042891A1 (en) 2009-02-12
UA93883C2 (ru) 2011-03-25
PE20070407A1 (es) 2007-05-12
TW200728299A (en) 2007-08-01
ES2270715B1 (es) 2008-04-01
ES2270715A1 (es) 2007-04-01
RU2417994C2 (ru) 2011-05-10
MX2008001035A (es) 2008-03-14
SG162805A1 (en) 2010-07-29
CA2616428A1 (en) 2007-02-15
JP2009502837A (ja) 2009-01-29
EP1922313A1 (en) 2008-05-21
WO2007017096A1 (en) 2007-02-15
AU2006278875A1 (en) 2007-02-15
US20100273757A1 (en) 2010-10-28
IL188725A0 (en) 2008-08-07
ZA200800353B (en) 2008-12-31
KR20080040681A (ko) 2008-05-08
RU2008107264A (ru) 2009-09-10
UY29672A1 (es) 2007-01-31
NO20080451L (no) 2008-02-11
CN101268064A (zh) 2008-09-17
ECSP088113A (es) 2008-02-20
US7790728B2 (en) 2010-09-07

Similar Documents

Publication Publication Date Title
AR056008A1 (es) Derivados de pirazina antagonistas del receptor a2b de adenosina
US6716851B2 (en) Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
ES2260318T3 (es) Nuevas sulfamidas y su utilizacion como antagonistas del receptor de endotelina.
AR059622A1 (es) Quinolonas utiles como inhibidores de la sintetasa del oxido nitrico inducibles
PE20070362A1 (es) COMPUESTOS DERIVADOS DE INDAZOL-4-IL-2,4-PIRIMIDINDIAMINA COMO INHIBIDORES DE TIROSINA QUINASA (QUINASA Syk)
AR065874A1 (es) Compuestos de pirimidina hidrazida como inhibidores de pgds
EA200970655A1 (ru) 6-замещенные пиримидины, ингибирующие вич
NO20082719L (no) Aryl-isoksazol-4-yl-oksadiazolderivater
AR059249A1 (es) Compuesto amina trisustituido
PE20060721A1 (es) Serinamidas sustituidas por heteroaroilo
ECSP067058A (es) Nuevos derivados de piridazin-3(2h)-ona
PE20181144A1 (es) Derivados de heteroarilo como inhibidores de parp
AR071323A1 (es) Derivados heterociclicos de piridazinonas activadores de glucoquinasas, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de los mismos en el tratamiento de la diabetes mellitus tipo ii.
AR082887A1 (es) Derivados de piridin-3-il-metil, y composiciones para la inhibicion de nampt
AR070040A1 (es) Tioeteres c-21 como agonistas del receptor de glucocorticoides
ATE496043T1 (de) 3-heteroaryl (amino bzw. amido)-1- (biphenyl bzw. phenylthiazolyl) carbonylpiperdinderivate als orexinrezeptor-inhibitoren
AR027337A1 (es) Derivados de nicotinamida benzocondensada heterocicliclo utiles como inhibidores selectivos de las isozimas pde4.
AR075609A1 (es) Derivados pirazolicos heterociclicos nitrogenados activadores de guanilatociclasas solubles, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares, entre otras.
AR065280A1 (es) Agentes antiparasitarios
ATE530176T1 (de) Verwendung von kaffeesäure und ihren derivaten gegen krebs
UY25904A1 (es) Sulfonamidas heterocíclicas inhibidoras de receptores de endotelina
AR076798A1 (es) Pirazinilpirazoles y composiciones que comprenden dichos compuestos
WO2010103547A3 (en) Substituted fused pyrimidine compounds
AR075583A1 (es) Derivados de isoxazol/o-piridina con eslabon etilo o etenilo
MX2010001338A (es) Derivados de pirimidina y piridina y su uso y composiciones farmaceuticas.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal