[go: up one dir, main page]

PE20080130A1 - Benzoimidazol-2-il pirimidinas y pirazinas como moduladores del receptor h4 de histamina - Google Patents

Benzoimidazol-2-il pirimidinas y pirazinas como moduladores del receptor h4 de histamina

Info

Publication number
PE20080130A1
PE20080130A1 PE2007000389A PE2007000389A PE20080130A1 PE 20080130 A1 PE20080130 A1 PE 20080130A1 PE 2007000389 A PE2007000389 A PE 2007000389A PE 2007000389 A PE2007000389 A PE 2007000389A PE 20080130 A1 PE20080130 A1 PE 20080130A1
Authority
PE
Peru
Prior art keywords
alkyl
methyl
receptor
pirazines
benzoimidazole
Prior art date
Application number
PE2007000389A
Other languages
English (en)
Inventor
James P Edwards
David E Kindrachuk
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38581554&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20080130(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PE20080130A1 publication Critical patent/PE20080130A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles

Landscapes

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

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1A R4 SON CADA UNO H, ALQUILO C1-C4, ALQUENILO C2-C4, ENTRE OTROS; X1 y X2 SON N y C-Rc; Rc ES H, METILO, ETILO, CF3, ENTRE OTROS; n ES 1-2; Z ES N, CH, C(ALQUILO C1-C4); R6 ES H, ALQUILO C1-C6, CICLOALQUILO MONOCICLICO; R8 ES H, ALQUILO C1-C4; R9 y R10 SON H, ALQUILO C1-C4; R11 ES H, ALQUILO C1-C4. SON COMPUESTOS PREFERIDOS: [5-(5-FLUORO-4-METIL-1H-BENZOIMIDAZOL-2-IL)-4-METIL-PIRIMIDIN-2-IL]-[3-(1-METIL-PIPERIDIN-4-IL)-PROPIL]-AMINA; [5-(4,6-DIMETIL-1H-BENZOIMIDAZOL-2-IL)-4-METIL-PIRIMIDIN-2-IL]-[3-(1-METIL-PIPERIDIN-4-IL)-PROPIL]-AMINA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. LOS COMPUESTOS DESCRITOS ACTUAN A NIVEL DEL RECEPTOR H4 Y SON UTILES EN EL TRATAMIENTO DE ALERGIAS, ASMA, ENFERMEDADES AUTOINMUNES Y PRURITO
PE2007000389A 2006-03-31 2007-03-30 Benzoimidazol-2-il pirimidinas y pirazinas como moduladores del receptor h4 de histamina PE20080130A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US78819006P 2006-03-31 2006-03-31

Publications (1)

Publication Number Publication Date
PE20080130A1 true PE20080130A1 (es) 2008-02-25

Family

ID=38581554

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007000389A PE20080130A1 (es) 2006-03-31 2007-03-30 Benzoimidazol-2-il pirimidinas y pirazinas como moduladores del receptor h4 de histamina

Country Status (34)

Country Link
US (6) US7507737B2 (es)
EP (1) EP2007752B1 (es)
JP (1) JP5066175B2 (es)
KR (1) KR101054325B1 (es)
CN (1) CN101460483B (es)
AR (1) AR059380A1 (es)
AT (1) ATE478067T1 (es)
AU (1) AU2007235576B2 (es)
BR (1) BRPI0710083A2 (es)
CA (1) CA2648036C (es)
CO (1) CO6160328A2 (es)
CR (1) CR10413A (es)
CY (1) CY1111169T1 (es)
DE (1) DE602007008545D1 (es)
DK (1) DK2007752T3 (es)
EA (1) EA016264B1 (es)
EC (1) ECSP088815A (es)
ES (1) ES2348829T3 (es)
IL (2) IL194453A0 (es)
ME (1) ME01143B (es)
MX (1) MX2008012655A (es)
NI (1) NI200800260A (es)
NO (1) NO341523B1 (es)
NZ (1) NZ571691A (es)
PE (1) PE20080130A1 (es)
PL (1) PL2007752T3 (es)
PT (1) PT2007752E (es)
RS (1) RS51423B (es)
SI (1) SI2007752T1 (es)
TW (1) TWI400234B (es)
UA (1) UA95949C2 (es)
UY (1) UY30253A1 (es)
WO (1) WO2007117399A2 (es)
ZA (1) ZA200809328B (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
DE602007008859D1 (de) * 2006-03-31 2010-10-14 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyridine als modulatoren des histamin-h4-rezeptors
EP2010177A2 (en) * 2006-04-10 2009-01-07 Janssen Pharmaceutica N.V. Combination histamine h1r and h4r antagonist therapy for treating pruritus
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US8084466B2 (en) * 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine H4 receptor
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
AU2013204436B2 (en) * 2008-06-30 2014-12-04 Janssen Pharmaceutica Nv Process for the preparation of benzoimidazol-2-yl pyrimidine derivatives
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
CA2729733C (en) * 2008-06-30 2016-10-25 Janssen Pharmaceutica Nv Process for the preparation of substituted pyrimidine derivatives
EP2303869A2 (en) * 2008-06-30 2011-04-06 Janssen Pharmaceutica, N.V. Process for the preparation of benzoimidazol-2-yl pyrimidine derivatives
AR074209A1 (es) 2008-11-24 2010-12-29 Boehringer Ingelheim Int Derivados de pirimidina utiles para el tratamiento del cancer
TWI491605B (zh) 2008-11-24 2015-07-11 Boehringer Ingelheim Int 新穎化合物
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
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
SG174125A1 (en) * 2009-04-02 2011-10-28 Merck Serono Sa Dihydroorotate dehydrogenase inhibitors
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー CRF−1受容体アンタゴニストとしてのピラゾロ[5,1b]オキサゾール誘導体
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
CN102753527B (zh) 2010-02-02 2014-12-24 诺华股份有限公司 用作crf受体拮抗剂的环己基酰胺衍生物
US9133123B2 (en) 2010-04-23 2015-09-15 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
CA2828456C (en) 2011-03-03 2021-05-04 Zalicus Pharmaceuticals Ltd. N-benzl-amino-carboxamide inhibitors of the sodium channel
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013182711A1 (en) 2012-06-08 2013-12-12 Sensorion H4 receptor inhibitors for treating tinnitus
PL2964229T3 (pl) 2013-03-06 2020-05-18 Janssen Pharmaceutica Nv Benzoimidazol-2-ilo pirymidynowe modulatory receptora histaminowego H<sub>4</sub>
GB201504689D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
WO2017076888A1 (en) 2015-11-03 2017-05-11 Janssen Pharmaceutica Nv 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same
HRP20251161T1 (hr) 2021-09-27 2025-11-21 Terns Pharmaceuticals, Inc. Benzimidazol karboksilne kisele kao agonisti glp-1r
AU2022375634A1 (en) 2021-10-25 2024-06-06 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
MX2024010346A (es) 2022-02-23 2024-08-30 Terns Pharmaceuticals Inc Compuestos como agonistas de glp-1r.

Family Cites Families (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3005852A (en) 1959-12-22 1961-10-24 Gen Aniline & Film Corp Production of sulfoxides and sulfones
GB1062357A (en) 1965-03-23 1967-03-22 Pfizer & Co C Quinazolone derivatives
US3931195A (en) 1971-03-03 1976-01-06 Mead Johnson & Company Substituted piperidines
US4191828A (en) 1976-04-14 1980-03-04 Richardson-Merrell Inc. Process for preparing 2-(2,2-dicyclohexylethyl)piperidine
US4337341A (en) 1976-11-02 1982-06-29 Eli Lilly And Company 4a-Aryl-octahydro-1H-2-pyrindines
US4190601A (en) 1978-05-31 1980-02-26 Union Carbide Corporation Production of tertiary amines by reductive alkylation
JPS5942396A (ja) 1982-09-02 1984-03-08 Ishihara Sangyo Kaisha Ltd リン酸アミド誘導体およびそれらを含有する殺虫、殺ダニ、殺線虫剤
JPS6130576A (ja) 1984-07-24 1986-02-12 Ube Ind Ltd 2−アミノ−5−シアノピリミジンの製法
CA2144762A1 (en) 1992-10-14 1994-04-28 George D. Hartman Fibrinogen receptor antagonists
GB9410031D0 (en) 1994-05-19 1994-07-06 Merck Sharp & Dohme Therapeutic agents
GB9422391D0 (en) 1994-11-05 1995-01-04 Solvay Interox Ltd Oxidation of organosulphur compounds
AU4467396A (en) 1994-12-12 1996-07-10 Omeros Medical Systems, Inc. Irrigation solution and method for inhibition of pain, inflammation and spasm
US5883105A (en) 1996-04-03 1999-03-16 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5880140A (en) 1996-04-03 1999-03-09 Merck & Co., Inc. Biheteroaryl inhibitors of farnesyl-protein transferase
WO1997036890A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036898A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5939439A (en) 1996-12-30 1999-08-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU729869B2 (en) 1997-01-17 2001-02-15 Merck & Co., Inc. Integrin antagonists
US5945422A (en) 1997-02-05 1999-08-31 Warner-Lambert Company N-oxides of amino containing pyrido 2,3-D! pyrimidines
EP0973396A4 (en) 1997-04-07 2001-02-07 Merck & Co Inc METHOD FOR TREATING CANCER
GB9801231D0 (en) 1997-06-05 1998-03-18 Merck & Co Inc A method of treating cancer
WO1999018079A1 (en) 1997-10-06 1999-04-15 Warner-Lambert Company Heteroaryl butyric acids and their derivatives as inhibitors of matrix metalloproteinases
KR20010041015A (ko) 1998-02-17 2001-05-15 윌리엄 제이. 리플린 항바이러스성 피리미딘 유도체
WO1999065897A1 (en) 1998-06-19 1999-12-23 Chiron Corporation Inhibitors of glycogen synthase kinase 3
DE69908546T2 (de) 1999-03-25 2004-04-29 Synthon B.V. Imidazopyridinderivate und Verfahren zu ihrer Herstellung
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
NZ516348A (en) 1999-06-23 2003-06-30 Aventis Pharma Gmbh Substituted benzimidazole
TWI279402B (en) 1999-08-20 2007-04-21 Banyu Pharma Co Ltd Spiro compounds having NPY antagonistic activities and agents containing the same
EA200200422A1 (ru) 1999-09-30 2002-10-31 Ньюроджен Корпорейшн НЕКОТОРЫЕ АЛКИЛЕНДИАМИНОЗАМЕЩЕННЫЕ ПИРАЗОЛО[1,5-а]-1,5-ПИРИМИДИНЫ И ПИРАЗОЛО[1,5-а]-1,3,5-ТРИАЗИНЫ
CA2363274A1 (en) 1999-12-27 2001-07-05 Japan Tobacco Inc. Fused-ring compounds and use thereof as drugs for hepatitis c
DE10006453A1 (de) 2000-02-14 2001-08-16 Bayer Ag Piperidylcarbonsäuren als Integrinantagonisten
NZ522015A (en) 2000-04-24 2004-08-27 Teva Pharma Zolpidem hemitartrate
JP2004501913A (ja) 2000-06-23 2004-01-22 ブリストル−マイヤーズ スクイブ ファーマ カンパニー ヘテロアリール−フェニル置換Xa因子阻害剤
IL153662A0 (en) 2000-07-21 2003-07-06 Syngenta Participations Ag Process for the preparation of 4,6-dimethoxy-2- (methylsulfonyl)-1,3-pyrimidine
EP1317433A2 (en) 2000-09-06 2003-06-11 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US6624180B2 (en) 2000-11-20 2003-09-23 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
WO2002064096A2 (en) 2001-02-16 2002-08-22 Tularik Inc. Methods of using pyrimidine-based antiviral agents
MXPA03008143A (es) 2001-03-09 2005-08-16 Johnson & Johnson Compuestos heterociclicos.
AU2002247402A1 (en) 2001-03-23 2002-10-08 Chugai Seiyaku Kabushiki Kaisha Flt-1 ligands and their uses in the treatment of diseases regulatable by angiogenesis
WO2002078701A1 (en) 2001-03-30 2002-10-10 Smithkline Beecham Corporation Use of pyrazolopyridines as therapeutic compounds
CA2446380A1 (en) 2001-05-08 2002-11-14 Yale University Proteomimetic compounds and methods
AR035543A1 (es) 2001-06-26 2004-06-16 Japan Tobacco Inc Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con
EP1441730B1 (en) 2001-11-05 2006-08-09 Merck Patent GmbH Hydrazono-malonitriles
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
EP1472248A1 (en) 2002-01-17 2004-11-03 Eli Lilly And Company Modulators of acetylcholine receptors
TWI270542B (en) 2002-02-07 2007-01-11 Sumitomo Chemical Co Method for preparing sulfone or sulfoxide compound
US7314937B2 (en) * 2002-03-21 2008-01-01 Eli Lilly And Company Non-imidazole aryl alkylamines compounds as histamine H3 receptor antagonists, preparation and therapeutic uses
US7498349B2 (en) 2002-08-02 2009-03-03 Genesoft Pharmaceuticals, Inc. Biaryl compounds having anti-infective activity
AU2003265886A1 (en) 2002-09-06 2004-03-29 Janssen Pharmaceutica N.V. (1H-Benzoimidazol-2-yl)-(piperazinyl)-methanone derivatives and related compounds as histamine H4-receptor antagonists for the treatment of inflammatory and allergic disorders
US20040127395A1 (en) 2002-09-06 2004-07-01 Desai Pragnya J. Use of histamine H4 receptor modulators for the treatment of allergy and asthma
US20040132715A1 (en) 2002-09-06 2004-07-08 Dunford Paul J. Method to treat allergic rhinitis
ES2264534T3 (es) 2002-09-06 2007-01-01 Janssen Pharmaceutica N.V. Compuestos de tienopirrolilo y furanopirrolilo y su utilizacion como ligandos del receptor histaminico h4.
CA2499497A1 (en) 2002-09-27 2004-04-08 Merck & Co., Inc. Substituted pyrimidines
TW200501960A (en) 2002-10-02 2005-01-16 Bristol Myers Squibb Co Synergistic kits and compositions for treating cancer
US20040105856A1 (en) 2002-12-02 2004-06-03 Robin Thurmond Use of histamine H4 receptor antagonist for the treatment of inflammatory responses
DE60329030D1 (de) 2002-12-04 2009-10-08 Ore Pharmaceuticals Inc Melanocortin-rezeptormodulatoren
BRPI0409986A (pt) 2003-05-05 2006-05-09 Hoffmann La Roche derivados de pirimidina fundida com atividade de crf
CA2525547C (en) 2003-05-14 2012-07-03 Torreypines Therapeutics, Inc. Compounds and uses thereof in modulating amyloid beta
SE0302116D0 (sv) 2003-07-21 2003-07-21 Astrazeneca Ab Novel compounds
WO2005039485A2 (en) 2003-08-13 2005-05-06 Chiron Corporation Gsk-3 inhibitors and uses thereof
KR101127201B1 (ko) 2003-09-22 2012-04-12 에스*바이오 피티이 리미티드 벤즈이미다졸 유도체와 그의 제조방법 및 약학적 적용
KR20060111466A (ko) 2003-09-30 2006-10-27 얀센 파마슈티카 엔.브이. 퀴녹살린 화합물
KR20060097024A (ko) * 2003-09-30 2006-09-13 얀센 파마슈티카 엔.브이. 벤조이미다졸 화합물
EP1670739A4 (en) 2003-10-08 2007-08-08 Bristol Myers Squibb Co CYCLIC DIAMINES AND DERIVATIVES AS FACTOR XA INHIBITORS
EP1679309A4 (en) 2003-10-24 2007-03-28 Ono Pharmaceutical Co ANTISTRESS MEDICAMENT AND ITS MEDICAL USE
US8277831B2 (en) 2004-02-17 2012-10-02 Advanced Technologies And Regenerative Medicine, Llc. Drug-enhanced adhesion prevention
AU2005226729B2 (en) * 2004-03-25 2010-01-28 Janssen Pharmaceutica N.V. Imidazole compounds
AU2005247808B2 (en) 2004-05-31 2011-02-10 Msd K.K. Quinazoline derivative
US7250427B2 (en) 2004-06-30 2007-07-31 Janssen Pharmaceutica, N.V. Aryl-substituted benzimidazole and imidazopyridine ethers
CA2577947A1 (en) 2004-08-31 2006-03-09 Banyu Pharmaceutical Co., Ltd. Novel substituted imidazole derivative
WO2006042102A2 (en) * 2004-10-05 2006-04-20 Neurogen Corporation Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
US7381732B2 (en) 2004-10-26 2008-06-03 Bristol-Myers Squibb Company Pyrazolobenzamides and derivatives as factor Xa inhibitors
CN101119973B (zh) 2004-12-17 2011-08-03 默克弗罗斯特加拿大有限公司 作为mPGES-1抑制剂的2-(苯基或者杂环基)-1H-菲并[9,10-d]咪唑类化合物
US7442716B2 (en) 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
AU2006226775A1 (en) 2005-03-24 2006-09-28 Janssen Pharmaceutica, N.V. Biaryl derived amide modulators of vanilloid VR1 receptor
WO2007044085A2 (en) 2005-05-19 2007-04-19 Xenon Pharmaceuticals Inc. Heteroaryl compounds and their uses as therapeutic agents
US8193206B2 (en) 2005-06-14 2012-06-05 Taigen Biotechnology Co., Ltd. Pyrimidine compounds
US20060281712A1 (en) 2005-06-14 2006-12-14 Chi-Feng Yen Pyrimidine compounds
KR101286569B1 (ko) 2005-07-04 2013-07-23 하이 포인트 파마슈티칼스, 엘엘씨 신규 약제
BRPI0612720B1 (pt) 2005-07-06 2016-02-10 Ge Healthcare Bio Sciences Ab método de preparação de uma matriz de separação
RU2008114378A (ru) 2005-09-13 2009-10-20 Палау Фарма, С.А. (Es) Производные 2-аминопиримидина как модуляторы активности н4-рецептора гистамина
JP5301999B2 (ja) 2005-10-31 2013-09-25 メルク・シャープ・アンド・ドーム・コーポレーション Cetp阻害薬
TW200800201A (en) 2005-11-18 2008-01-01 Lilly Co Eli Pyrimidinyl benzothiophene compounds
WO2007063935A1 (ja) 2005-12-02 2007-06-07 Mitsubishi Tanabe Pharma Corporation 芳香族化合物
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
CN101032483B (zh) 2006-03-09 2011-05-04 陈德桂 调节雄激素受体活性的乙内酰脲衍生物及其应用
DE602007008545D1 (de) * 2006-03-31 2010-09-30 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyridine und pyrazine als modulatoren des histamin-h4-rezeptors
DE602007008859D1 (de) 2006-03-31 2010-10-14 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyridine als modulatoren des histamin-h4-rezeptors
JP5132673B2 (ja) 2006-04-07 2013-01-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒスタミンh4受容体のモジュレーターとしてのインドールおよびベンゾイミダゾール
EP2010177A2 (en) 2006-04-10 2009-01-07 Janssen Pharmaceutica N.V. Combination histamine h1r and h4r antagonist therapy for treating pruritus
EP2019675A4 (en) 2006-05-02 2011-03-02 Merck Frosst Canada Ltd METHOD FOR THE TREATMENT OR PREVENTION OF NEOPLASIA
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
US8779154B2 (en) 2006-09-26 2014-07-15 Qinglin Che Fused ring compounds for inflammation and immune-related uses
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
US8084466B2 (en) 2007-12-18 2011-12-27 Janssen Pharmaceutica Nv Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine H4 receptor
US20090181242A1 (en) 2008-01-11 2009-07-16 Enniss James P Exterior window film
NZ603069A (en) 2008-06-12 2013-08-30 Janssen Pharmaceutica Nv Use of histamine h4 antagonist for the treatment of post-operative adhesions
US8841287B2 (en) 2008-06-12 2014-09-23 Janssen Pharmaceutica N.V. Diamino-pyridine, pyrimidine, and pyrazine modulators of the histamine H4 receptor
CA2729733C (en) 2008-06-30 2016-10-25 Janssen Pharmaceutica Nv Process for the preparation of substituted pyrimidine derivatives
EP2303869A2 (en) 2008-06-30 2011-04-06 Janssen Pharmaceutica, N.V. Process for the preparation of benzoimidazol-2-yl pyrimidine derivatives
US8852569B2 (en) 2008-08-28 2014-10-07 The General Hospital Corporation Prevention and treatment of itch with cysteine protease inhibition
TWI519533B (zh) 2010-11-01 2016-02-01 Lg生命科學有限公司 1-{(2S)-2-胺基-4-[2,4-雙(三氟甲基)-5,8-二氫吡啶并[3,4-d]嘧啶-7(6H)-基]-4-側氧丁基}-5,5-二氟哌啶-2-酮酒石酸鹽之水合物
EP2465498A1 (en) 2010-11-23 2012-06-20 Faes Farma, S.A. Diphenyl-amine derivatives: uses, process of synthesis and pharmaceutical compositions
PL2964229T3 (pl) 2013-03-06 2020-05-18 Janssen Pharmaceutica Nv Benzoimidazol-2-ilo pirymidynowe modulatory receptora histaminowego H<sub>4</sub>

Also Published As

Publication number Publication date
WO2007117399A2 (en) 2007-10-18
US9365548B2 (en) 2016-06-14
UY30253A1 (es) 2007-08-31
NO20084540L (no) 2008-10-28
IL194453A0 (en) 2009-08-03
US8343989B2 (en) 2013-01-01
ES2348829T3 (es) 2010-12-15
AR059380A1 (es) 2008-04-09
NI200800260A (es) 2012-01-24
CY1111169T1 (el) 2015-06-11
JP2009532366A (ja) 2009-09-10
KR20080108586A (ko) 2008-12-15
TW200808737A (en) 2008-02-16
CO6160328A2 (es) 2010-05-20
NO341523B1 (no) 2017-11-27
IL244946A0 (en) 2016-05-31
US20090137608A1 (en) 2009-05-28
CN101460483A (zh) 2009-06-17
EA200870400A1 (ru) 2009-04-28
ECSP088815A (es) 2008-11-27
DE602007008545D1 (de) 2010-09-30
CA2648036A1 (en) 2007-10-18
IL244946A (en) 2017-03-30
AU2007235576B2 (en) 2011-11-10
ME01143B (me) 2013-03-20
US20150148361A1 (en) 2015-05-28
SI2007752T1 (sl) 2010-12-31
CR10413A (es) 2009-02-19
PL2007752T3 (pl) 2011-02-28
RS51423B (sr) 2011-02-28
EP2007752A4 (en) 2009-04-22
ATE478067T1 (de) 2010-09-15
KR101054325B1 (ko) 2011-08-04
ZA200809328B (en) 2009-12-30
US20140038995A1 (en) 2014-02-06
EP2007752B1 (en) 2010-08-18
MX2008012655A (es) 2008-12-16
PT2007752E (pt) 2010-10-18
DK2007752T3 (da) 2010-11-15
EA016264B1 (ru) 2012-03-30
BRPI0710083A2 (pt) 2011-08-02
CA2648036C (en) 2012-05-22
US7507737B2 (en) 2009-03-24
TWI400234B (zh) 2013-07-01
UA95949C2 (ru) 2011-09-26
US20130072510A1 (en) 2013-03-21
AU2007235576A1 (en) 2007-10-18
CN101460483B (zh) 2013-05-08
JP5066175B2 (ja) 2012-11-07
EP2007752A2 (en) 2008-12-31
NZ571691A (en) 2011-07-29
US8598189B2 (en) 2013-12-03
US20100256373A1 (en) 2010-10-07
US8962644B2 (en) 2015-02-24
WO2007117399A3 (en) 2008-09-12
US20070244126A1 (en) 2007-10-18

Similar Documents

Publication Publication Date Title
PE20080130A1 (es) Benzoimidazol-2-il pirimidinas y pirazinas como moduladores del receptor h4 de histamina
PE20081776A1 (es) Moduladores 2-aminopirimidina del receptor histamina h4
PE20150041A1 (es) Derivados de aminoacidos funcionalizados en la terminal n capaces de formar microesferas encapsuladoras de farmaco
PE20140011A1 (es) Compuestos y composiciones novedosos para la inhibicion de nampt
PE20080409A1 (es) Compuestos que modulan en el receptor cb2
PE20121148A1 (es) Compuestos heterociclicos y usos de los mismos
PE20160844A1 (es) Compuestos triciclicos como agentes anticancerigenos
PE20130401A1 (es) Heteroaril-ciclohexil-tetraazabenzo[e]azulenos
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PE20121158A1 (es) Derivados de feniletinilo como moduladores alostericos positivos (map)
PE20130402A1 (es) 5-fluoro-1h-pirazolopiridinas sustituidas y su uso
PE20141352A1 (es) Fenil-3-aza-biciclo[3,1,0]hex-3-il-metanonas y su uso como medicamento
AR059957A1 (es) DERIVADOS DE ESPIROINDOLINONA, MÉTODOS PARA SU PREPARACIoN, UNA COMPOSICIoN FARMACÉUTICA QUE LOS CONTIENE Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DEL CÁNCER.
PA8632701A1 (es) Compuestos terapeuticos
PE20121613A1 (es) Derivados de quinolina amida como moduladores alostericos positivos de receptores m1
PE20140250A1 (es) Derivados de piperidina puenteada
PE20060932A1 (es) Derivados de sulfonamidas como moduladores de receptores de glucocorticoides (gr)
PE20080527A1 (es) Derivado de pirimidina como inhibidor de la fosfatidilinositol 3-quinasa (pi3k)
PE20071245A1 (es) COMPUESTOS INDOL SULFONAMIDA COMO MODULADORES DEL RECEPTOR DE PROGESTERONA SELECTIVOS (SPRMs)
PE20120534A1 (es) PIRIMIDINAS FUSIONADAS COMO INHIBIDORES DE Akt
PE20110061A1 (es) Derivados de diamino-piridina, pirimidina y piridazina como moduladores del receptor h4 de histamina
PE20160839A1 (es) Derivados de 4-azaindol
PE20080145A1 (es) Tetrahidro-pirimidoazepinas como moduladores de trpv1
PE20081753A1 (es) Compuestos y composiciones como inhibidores de la proteasa activadora de canal
PE20110196A1 (es) 5-alquinil-pirimidinas

Legal Events

Date Code Title Description
FG Grant, registration