[go: up one dir, main page]

PE20081776A1 - Moduladores 2-aminopirimidina del receptor histamina h4 - Google Patents

Moduladores 2-aminopirimidina del receptor histamina h4

Info

Publication number
PE20081776A1
PE20081776A1 PE2008000324A PE2008000324A PE20081776A1 PE 20081776 A1 PE20081776 A1 PE 20081776A1 PE 2008000324 A PE2008000324 A PE 2008000324A PE 2008000324 A PE2008000324 A PE 2008000324A PE 20081776 A1 PE20081776 A1 PE 20081776A1
Authority
PE
Peru
Prior art keywords
cyclopentil
pyrimidin
aminopyrimidine
histamine
modulators
Prior art date
Application number
PE2008000324A
Other languages
English (en)
Inventor
Hui Cai
Frank Chavez
Anne E Fitzgerald
Danielle K Neff
Brad M Savall
Deborah M Smith
Jennifer D Venable
Jianmei Wei
Ronald L Wolin
Jing Liu
Neelakandha S Mani
Michele C Rizzolio
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PE20081776A1 publication Critical patent/PE20081776A1/es

Links

Classifications

    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • 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
    • 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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 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
    • 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
    • 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
    • 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
    • C07D487/08—Bridged systems
    • 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
    • C07D487/10—Spiro-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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 2-AMINOPIRIMIDINA DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON OH, CF3, ENTRE OTROS SUSTITUYENTES, BENCIL, CICLOALQUILO MONOCICLICO, ADAMANTIL, ENTRE OTROS; R2 ES H, F, METIL O METOXI; -N(R3)R4 ES UNO DE LOS SIGUIENTES SISTEMAS DE ANILLOS ACICLICOS, MONOCICLICOS, ESPIROCICLICOS DE FORMULA (i), (ii), (iii), ENTRE OTROS, DONDE Rb ES H O ALQUILO(C1-C3). SON COMPUESTOS PREFERIDOS: 4-CICLOPENTIL-6-(4-METIL-PIPERAZIN-1-IL)-PIRIMIDIN-2-ILAMINA, (R)-4-(3-AMINO-PIPERIDIN-1-IL)-6-CICLOPENTIL-PIRIMIDIN-2-ILAMINA, 4-CICLOPENTIL-6-(CIS-OCTAHIDRO-PIRROLO[3,4-b]PIRIDIN-6-IL)-PIRIMIDIN-2-ILAMINA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE HISTAMINA H4 SIENDO UTILES EN EL TRATAMIENTO DE ALERGIA, ARTRITIS REUMATOIDEA, ASMA, ENFERMEDADES AUTOINMUNES
PE2008000324A 2007-02-14 2008-02-14 Moduladores 2-aminopirimidina del receptor histamina h4 PE20081776A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88979807P 2007-02-14 2007-02-14

Publications (1)

Publication Number Publication Date
PE20081776A1 true PE20081776A1 (es) 2008-12-18

Family

ID=39686377

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000324A PE20081776A1 (es) 2007-02-14 2008-02-14 Moduladores 2-aminopirimidina del receptor histamina h4

Country Status (23)

Country Link
US (6) US7923451B2 (es)
EP (2) EP2599386A1 (es)
JP (1) JP5281586B2 (es)
KR (1) KR20090110877A (es)
CN (1) CN101668423B (es)
AR (1) AR065354A1 (es)
AU (1) AU2008216727B2 (es)
BR (1) BRPI0807815A2 (es)
CA (1) CA2678077A1 (es)
CL (1) CL2008000467A1 (es)
CO (1) CO6210771A2 (es)
CR (1) CR11027A (es)
EA (1) EA016133B1 (es)
EC (1) ECSP099582A (es)
GT (1) GT200900231A (es)
IL (1) IL200335A0 (es)
MX (1) MX2009008787A (es)
NI (1) NI200900159A (es)
NZ (1) NZ578977A (es)
PE (1) PE20081776A1 (es)
TW (1) TW200904437A (es)
UY (1) UY30917A1 (es)
WO (1) WO2008100565A1 (es)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602007008545D1 (de) 2006-03-31 2010-09-30 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyridine und pyrazine als modulatoren des histamin-h4-rezeptors
TW200904437A (en) * 2007-02-14 2009-02-01 Janssen Pharmaceutica Nv 2-aminopyrimidine modulators of the histamine H4 receptor
WO2009068512A1 (en) * 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
US8436005B2 (en) * 2008-04-03 2013-05-07 Abbott Laboratories Macrocyclic pyrimidine derivatives
US8841287B2 (en) 2008-06-12 2014-09-23 Janssen Pharmaceutica N.V. Diamino-pyridine, pyrimidine, and pyrazine modulators of the histamine H4 receptor
NZ603069A (en) * 2008-06-12 2013-08-30 Janssen Pharmaceutica Nv Use of histamine h4 antagonist for the treatment of post-operative adhesions
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
WO2010064705A1 (ja) * 2008-12-05 2010-06-10 大日本住友製薬株式会社 Ｈ４受容体アンタゴニスト作用を有する新規７位置換ジヒドロピラノピリミジン誘導体
US8436008B2 (en) 2008-12-22 2013-05-07 Incyte Corporation Substituted heterocyclic compounds
EP2201982A1 (en) 2008-12-24 2010-06-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Histamine H4 receptor antagonists for the treatment of vestibular disorders
AR076052A1 (es) 2009-03-20 2011-05-18 Incyte Corp Derivados de pirimidinas sustituidas, composiciones farmaceuticas que los contienen y uso de los mismos en trastornos asociados con receptores de histamina h4, tales como trastornos inflamatorios, prurito y dolor.
US8796297B2 (en) * 2009-06-30 2014-08-05 Abbvie Inc. 4-substituted-2-amino-pyrimidine derivatives
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
AR077999A1 (es) * 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
US8901146B2 (en) 2009-12-23 2014-12-02 Medicis Pharmaceutical Corporation Aminoalkylpyrimidine derivatives as histamine H4 receptor antagonists
CN102260265B (zh) * 2010-05-24 2015-09-02 上海阳帆医药科技有限公司 六氢吡咯[3,4-b]吡咯衍生物、其制备方法及其用途
WO2013182711A1 (en) 2012-06-08 2013-12-12 Sensorion H4 receptor inhibitors for treating tinnitus
MX373786B (es) 2012-11-27 2020-03-23 Thomas Helledays Stiftelse Foer Medicinsk Forskning Derivados de pirimidin-2,4-diamina para el tratamiento de cáncer.
PL2964229T3 (pl) 2013-03-06 2020-05-18 Janssen Pharmaceutica Nv Benzoimidazol-2-ilo pirymidynowe modulatory receptora histaminowego H<sub>4</sub>
WO2015069752A1 (en) * 2013-11-05 2015-05-14 The Regents Of The University Of California Acetylcholine binding protein ligands, cooperative nachr modulators and methods for making and using
AU2015253225B2 (en) 2014-05-01 2017-04-06 Novartis Ag Compounds and compositions as Toll-Like Receptor 7 agonists
CA2949785A1 (en) 2014-06-04 2015-12-10 Thomas Helledays Stiftelse For Medicinsk Forskning Mth1 inhibitors for treatment of cancer
US10064869B2 (en) 2014-06-04 2018-09-04 Thomas Helledays Stiftelse For Medicinsk Forskning MTH1 inhibitors for treatment of inflammatory and autoimmune conditions
NO2721710T3 (es) * 2014-08-21 2018-03-31
GB201416351D0 (en) * 2014-09-16 2014-10-29 Shire Internat Gmbh Heterocyclic derivatives
AU2017289418B2 (en) * 2016-07-01 2021-06-03 Janssen Sciences Ireland Unlimited Company Dihydropyranopyrimidines for the treatment of viral infections
CN109232533A (zh) * 2017-09-28 2019-01-18 北京越之康泰生物医药科技有限公司 氮杂环类衍生物、其制备方法及其医药用途
EP3697776B1 (en) * 2017-10-17 2023-04-19 Palau Pharma, S.L.U. Synthesis of 4-aminopyrimidine compounds
GB201817047D0 (en) * 2018-10-19 2018-12-05 Heptares Therapeutics Ltd H4 antagonist compounds
GB202005858D0 (en) * 2020-04-22 2020-06-03 Heptares Therapeutics Ltd H4 Antagonist compounds
WO2024073502A1 (en) * 2022-09-28 2024-04-04 Accutar Biotechnology Inc. Heterocyclic compounds as e3 ligase inhibitors

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB583815A (en) 1944-05-18 1946-12-31 Francis Henry Swinden Curd New pyrimidine compounds
BE759371A (fr) 1969-11-24 1971-05-24 Bristol Myers Co Azaspirodecanediones heterocycliques et procedes pour leur preparation
US4287338A (en) 1980-03-10 1981-09-01 The Upjohn Company Sulfooxy-pyrimidinium, -pyridinium, and -triazinium hydroxide inner salts
EP0042669A3 (en) 1980-06-23 1982-03-24 The Upjohn Company Compounds and compositions for use in animal feeds
US4393065A (en) 1980-06-23 1983-07-12 The Upjohn Company Animal feed and process
JPS61238784A (ja) 1985-04-17 1986-10-24 Sumitomo Seiyaku Kk コハク酸イミド誘導体及びその酸付加塩
US4980350A (en) 1988-02-25 1990-12-25 Merck & Co., Inc. Piperazinylalkylpyrimidines as hypoglycemic agents
IE63502B1 (en) * 1989-04-21 1995-05-03 Zeneca Ltd Aminopyrimidine derivatives useful for treating cardiovascular disorders
FR2651122B1 (fr) 1989-08-29 1994-10-28 Oreal Compositions destinees a etre utilisees pour freiner la chute des cheveux et pour induire et stimuler leur croissance, contenant des derives de l'amino-2 pyrimidine oxyde-3 et nouveaux composes derives de l'amino-2 pyrimidine oxyde-3.
US5124328A (en) 1990-10-11 1992-06-23 Merck & Co., Inc. Morpholine derivatives compositions and use
US5077290A (en) 1990-10-11 1991-12-31 Merck & Co., Inc. Morpholine derivatives compositions and use
US5328913A (en) 1992-12-11 1994-07-12 Duke University Minoxidil analogs as inhibitors of cell proliferation and lysyl hydroxylase
GB9410031D0 (en) 1994-05-19 1994-07-06 Merck Sharp & Dohme Therapeutic agents
US5470976A (en) 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
DE19517186A1 (de) 1995-05-11 1996-11-14 Bayer Ag Verfahren zur Herstellung substituierter 2-Fluor-pyrimidine
US5760623A (en) 1995-10-13 1998-06-02 Texas Instruments Incorporated Ramp voltage generator for differential switching amplifiers
US5777134A (en) 1995-10-26 1998-07-07 Merck & Co., Inc. 4-oxa and 4-thia steriods
US5998464A (en) 1995-10-26 1999-12-07 Merck & Co., Inc. 4-Oxa and 4-thia steroids
ATE294174T1 (de) 1996-06-10 2005-05-15 Merck & Co Inc Substituierte imidazole mit cytokinin- inhibirender wirkung
CA2260900A1 (en) 1996-07-25 1998-02-05 Merck Sharp & Dohme Limited Substituted triazolo pyridazine derivatives as inverse agonists of the gabaa.alpha.5 receptor subtype
US5880139A (en) 1996-11-20 1999-03-09 Merck & Co., Inc. Triaryl substituted imidazoles as glucagon antagonists
US5955480A (en) 1996-11-20 1999-09-21 Merck & Co., Inc. Triaryl substituted imidazoles, compositions containing such compounds and methods of use
US6632823B1 (en) 1997-12-22 2003-10-14 Merck & Co., Inc. Substituted pyridine compounds useful as modulators of acetylcholine receptors
HUP0302468A2 (hu) 1999-06-02 2003-11-28 Merck & Co., Inc. Alfa V integrin receptor antagonisták és ezeket tartalmazó gyógyszerkészítmények
EP1216238B1 (en) 1999-09-14 2004-02-18 Merck Frosst Canada &amp; Co. Carboxylic acids and acylsulfonamides, compositions containing such compounds and methods of treatment
WO2001047897A1 (en) * 1999-12-28 2001-07-05 Pharmacopeia, Inc. Cytokine, especially tnf-alpha, inhibitors
DE60110391T2 (de) 2000-02-25 2006-01-26 F. Hoffmann-La Roche Ag Adenosin-rezeptor modulatoren
WO2002015902A1 (en) 2000-08-23 2002-02-28 Merck & Co., Inc. Method of treating or preventing urinary incontinence using prostanoid ep1 receptor antagonists
WO2002022584A1 (en) 2000-09-11 2002-03-21 Merck & Co., Inc. Thrombin inhibitors
EP1341773A2 (en) 2000-12-07 2003-09-10 Cv Therapeutics, Inc. Substituted 1,3,5-triazines and pyrimidines as abca-1 elevating compounds against coronary artery disease or atherosclerosis
WO2002053160A1 (en) 2000-12-29 2002-07-11 Alteon, Inc. Method for treating glaucoma ivb
EP1359911A2 (en) 2000-12-29 2003-11-12 Alteon, Inc. Method for treating fibrotic diseases or other indications ivc
US7622117B2 (en) 2002-04-17 2009-11-24 Dynamis Therapeutics, Inc. 3-deoxyglucosone and skin
CA2499497A1 (en) 2002-09-27 2004-04-08 Merck & Co., Inc. Substituted pyrimidines
EP1571146A4 (en) 2002-12-10 2010-09-01 Ono Pharmaceutical Co NITROGENIC HETEROCYCLIC COMPOUNDS AND THEIR MEDICAL USE
EP1437348A1 (fr) 2003-01-13 2004-07-14 L'oreal Dérivés de de la 6-méthyl-pyrimidine-2,4-diamine, procédé de synthèse, compositions les comprenant et utilisations comme agents neutralisants basiques
JP2006521357A (ja) 2003-03-24 2006-09-21 メルク　エンド　カムパニー　インコーポレーテッド ナトリウムチャンネル遮断薬としてのビアリール置換６員複素環化合物
EP1505064A1 (en) 2003-08-05 2005-02-09 Bayer HealthCare AG 2-Aminopyrimidine derivatives
FR2860308B1 (fr) * 2003-09-26 2006-01-13 Inst Nat Rech Inf Automat Modulation de position de curseur dans les donnees video pour ecran d'ordinateur
WO2005054239A1 (en) * 2003-12-05 2005-06-16 Bayer Healthcare Ag 2-aminopyrimidine derivatives
CA2557837A1 (en) 2004-02-17 2005-09-01 Dynamis Therapeutics, Inc. Fructoseamine 3 kinase and the formation of collagen and elastin
AU2005226729B2 (en) 2004-03-25 2010-01-28 Janssen Pharmaceutica N.V. Imidazole compounds
SE0401656D0 (sv) 2004-06-24 2004-06-24 Astrazeneca Ab Chemical compounds
WO2006016014A1 (fr) 2004-07-13 2006-02-16 L'oreal Nouveaux composes de la famille de la 6-methyl-pyrimidine-2,4-diamine, procede de synthese, compositions les comprenant et utilisations
JP4541809B2 (ja) 2004-09-08 2010-09-08 キヤノン株式会社 有機化合物及び有機発光素子
AU2005286653A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridine derivatives for inhibiting human stearoyl-CoA-desaturase
WO2006053109A1 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Heteroaryl compounds
WO2006065590A2 (en) 2004-12-16 2006-06-22 Xtl Biopharmaceuticals Inc. Pyridine and pyrimidine antiviral compositions
EP2049497A2 (en) 2005-05-19 2009-04-22 Astex Therapeutics Limited Pyrimidine derivatives as hsp90 inhibitors
EP1893607A4 (en) 2005-06-09 2010-07-21 Merck Sharp & Dohme CHECKPOINT KINASE INHIBITORS
RU2008114378A (ru) 2005-09-13 2009-10-20 Палау Фарма, С.А. (Es) Производные 2-аминопиримидина как модуляторы активности н4-рецептора гистамина
EP1767537A1 (en) 2005-09-21 2007-03-28 Cellzome (UK) Ltd. Pyrimidine compounds for the treatment of inflammatory disorders
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
WO2007090854A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Azetidine amino pyrimidine compounds for the treatment of inflammatory disorders
EP1829879A1 (en) 2006-02-10 2007-09-05 Cellzome (UK) Ltd. Amino pyrimidine compounds for the treatment of inflammatory disorders
WO2007090853A1 (en) 2006-02-10 2007-08-16 Cellzome (Uk) Ltd. Enantiomers of amino pyrimidine compounds for the treatment of inflammatory disorders
JP2009527508A (ja) 2006-02-24 2009-07-30 メルク フロスト カナダ リミテツド ２−（フェニル又は複素環）−１ｈ−フェナントロ［９，１０−ｄ］イミダゾール
US20090209571A1 (en) 2006-05-18 2009-08-20 Bernard Cote Phenanthrene derivatives as MPGES-1 inhibitors
CN101511190A (zh) 2006-07-11 2009-08-19 詹森药业有限公司 组胺h4受体的苯并呋喃并-和苯并噻吩并嘧啶调节剂
GB0614579D0 (en) 2006-07-21 2006-08-30 Black James Foundation Pyrimidine derivatives
EP2066645A2 (en) 2006-09-12 2009-06-10 UCB Pharma S.A. 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions
US7985745B2 (en) 2006-10-02 2011-07-26 Abbott Laboratories Method for pain treatment
TW200904437A (en) * 2007-02-14 2009-02-01 Janssen Pharmaceutica Nv 2-aminopyrimidine modulators of the histamine H4 receptor
WO2009068512A1 (en) 2007-11-30 2009-06-04 Palau Pharma, S. A. 2 -amino-pyrimidine derivatives as histamine h4 antagonists
PE20091524A1 (es) 2007-12-19 2009-09-25 Palau Pharma Sa Derivados de 2-aminopirimidina

Also Published As

Publication number Publication date
US20130158258A1 (en) 2013-06-20
US20110160451A1 (en) 2011-06-30
US20110218338A1 (en) 2011-09-08
US8686142B2 (en) 2014-04-01
EP2599386A1 (en) 2013-06-05
US8716475B2 (en) 2014-05-06
CO6210771A2 (es) 2010-10-20
JP2010518165A (ja) 2010-05-27
US20110160452A1 (en) 2011-06-30
NI200900159A (es) 2010-03-24
TW200904437A (en) 2009-02-01
AR065354A1 (es) 2009-06-03
EA200970765A1 (ru) 2009-12-30
EP2124560A1 (en) 2009-12-02
KR20090110877A (ko) 2009-10-22
MX2009008787A (es) 2010-02-15
CA2678077A1 (en) 2008-08-21
BRPI0807815A2 (pt) 2014-08-05
ECSP099582A (es) 2009-09-29
CN101668423A (zh) 2010-03-10
US20130158259A1 (en) 2013-06-20
CR11027A (es) 2010-01-21
US7923451B2 (en) 2011-04-12
WO2008100565A1 (en) 2008-08-21
EP2124560A4 (en) 2010-03-31
IL200335A0 (en) 2010-04-29
UY30917A1 (es) 2008-09-02
CL2008000467A1 (es) 2008-08-22
GT200900231A (es) 2011-07-18
US8415366B2 (en) 2013-04-09
JP5281586B2 (ja) 2013-09-04
EA016133B1 (ru) 2012-02-28
AU2008216727B2 (en) 2013-07-11
CN101668423B (zh) 2013-10-30
NZ578977A (en) 2012-04-27
AU2008216727A1 (en) 2008-08-21
US20080194577A1 (en) 2008-08-14

Similar Documents

Publication Publication Date Title
PE20081776A1 (es) Moduladores 2-aminopirimidina del receptor histamina h4
PE20080130A1 (es) Benzoimidazol-2-il pirimidinas y pirazinas como moduladores del receptor h4 de histamina
PE20221628A1 (es) Compuestos inhibidores de rip1 y metodos para hacer y utilizar los mismos
PE20120135A1 (es) Piperidinas sustituidas como antagonistas de ccr3
PE20090775A1 (es) Nuevos derivados de biarilo
PE20071311A1 (es) Compuestos 8-azabiciclo[3.2.1]octano como antagonistas del receptor opioide mu
PE20090183A1 (es) Derivados de 1-oxa-3,9-diaza-espiro-[5.5]undecan-2-ona como moduladores de ccr5
PE20080274A1 (es) Derivados de dioxo-alcanos y dioxo-alquenos sustituidos como moduladores del receptor vanilloide subtipo 1 (trpv1)
MX2009005461A (es) N-oxidos de analogos de 4,5-epoxi-morfinano.
NO20073729L (no) Heterocykliske forbindelser som CCR2B-antagonister
UA98966C2 (ru) Производные бензазепина, пригодные для использования в качестве антагонистов вазопрессина
PE20091734A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PH12013501489A1 (en) Substituted 6,6-fused nitrogenous heterocyclic compounds and uses thereof
MX2009005462A (es) Analogos de 7,8-saturados-4,5-epoxi-morfinano.
MA32175B1 (fr) Oxadiazoanthracènes pour le traitement du diabète
PE20121482A1 (es) Derivados de imidazopiridina como inhibidores de jak
MX2011011661A (es) Compuestos 1-cianoetilheterociclilcarboxamida sustituidos 750.
MX2011010449A (es) Derivados de oxadiazol.
PE20080150A1 (es) Derivados de piridinona n-aril y n-heteroaril sustituidos como antagonistas del receptor de la hormona concentradora de melanina (mch)
PE20142452A1 (es) AMIDAS CICLICAS COMO INHIBIDORES DE MetAP-2
PE20080205A1 (es) DERIVADOS DE PIRAZOLOPIRIDINAS SUSTITUIDAS COMO INHIBIDORES DE LA TIROSIN QUINASA Tie2
PE20110772A1 (es) ESPIRO AZEPAN OXAZOLIDINONAS COMO BLOQUEADORES DEL CANAL DE POTASIO Kv1.3
PE20140868A1 (es) Antagonistas trpm8 y su uso en tratamientos
SV2010003459A (es) Derivados de pirimidina 934
PE20080405A1 (es) COMPUESTOS Y COMPOSICIONES COMO INHIBIDORES DE ITPKb

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed