CO6160328A2 - 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 histaminaInfo
- Publication number
- CO6160328A2 CO6160328A2 CO08109912A CO08109912A CO6160328A2 CO 6160328 A2 CO6160328 A2 CO 6160328A2 CO 08109912 A CO08109912 A CO 08109912A CO 08109912 A CO08109912 A CO 08109912A CO 6160328 A2 CO6160328 A2 CO 6160328A2
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- chemical entity
- further characterized
- methyl
- independently
- Prior art date
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- 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
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- 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
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- 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
- A61P11/02—Nasal agents, e.g. decongestants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- A61P17/00—Drugs for dermatological disorders
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
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- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/14—Decongestants or antiallergics
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- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A61P7/06—Antianaemics
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- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
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- 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
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- 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
- A61K31/41—Heterocyclic 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Virology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Biotechnology (AREA)
- Communicable Diseases (AREA)
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- Urology & Nephrology (AREA)
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Abstract
1.- Una entidad química que es un compuesto de fórmula (I):en donde cada uno de R1-4 es independientemente H, alquilo de C1-4, alquenilo de C2-4, alquinilo de C2-4, fenilo, -CF3, -OCF3, -CN, halo, -NO2, -Oalquilo de C1-4, -Salquilo de C1-4, -S(O)alquilo de C1-4, -SO2alquiIo de C1-4, -C(O)alquilo de C1-4, -C(O)fenilo, C(O)NRaRb, -CO2aIquiIo de C1-4, -CO2H, -C(O)NRaRd, en donde Ra y Rb son cada uno independientemente H, alquilo de C1-4, o cicloalquilo de C3-7, uno de X1 y X2 es N y el otro es C-Rc; donde Rc es H, metilo, hidroximetilo, dimetilaminometilo, etilo, propilo, isopropilo, -CF3, ciclopropilo o ciclobutilo; n es 1 o 2; Z es N, CH, o C(alquilo de C1-4; R6 es H, alquilo de C1-6, o cicloalquiio monocíclico; R8 es H o alquilo de C1-4; R9 y R10 son cada uno independientemente H o alquilo de C1-4; y R11 es H o alquilo de C1-4; una sal farmacéuticamente aceptable de compuesto de la fórmula (I), un profármaco farmacéuticamente aceptable de compuesto de fórmula (I), o un metabolito activo farmacéuticamente de compuesto de fórmula (I). 2.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque cada uno de R1-4 es independientemente H, metilo, terc-butilo, metoxi, -CF3, -CN, fluoro, metoxicarbonilo, o benzoilo. 3.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque X2 es N. 4.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque X1 es N. 5.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque Rc es H, metilo, etilo, -CF3, ciclopropilo, o ciclobutilo. 6.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque Rc es H o metilo. 7.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque n es 1. 8.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque Z es N o CH. 9.- La entidad química de conformidad con la reivindicación 1, caracterizada además porque Z es CH.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US78819006P | 2006-03-31 | 2006-03-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6160328A2 true CO6160328A2 (es) | 2010-05-20 |
Family
ID=38581554
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO08109912A CO6160328A2 (es) | 2006-03-31 | 2008-10-15 | 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 (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009532367A (ja) * | 2006-03-31 | 2009-09-10 | 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ベンゾイミダゾール−２−イルピリジン |
| KR101054325B1 (ko) * | 2006-03-31 | 2011-08-04 | 얀센 파마슈티카 엔.브이. | 히스타민 ｈ４ 수용체 조절제로서의 벤조이미다졸―２―일 피리미딘 및 피라진 |
| 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 |
| WO2009079001A1 (en) * | 2007-12-18 | 2009-06-25 | Janssen Pharmaceutica N.V. | Bicyclic heteroaryl-substituted imidazoles as modulators of the histamine h4 receptor |
| MX2010013726A (es) | 2008-06-12 | 2011-01-14 | Janssen Pharmaceutica Nv | Moduladores de diamino-piridina, pirimidina, y piridazina del receptor h4 de histamina. |
| KR101631644B1 (ko) | 2008-06-12 | 2016-06-20 | 얀센 파마슈티카 엔.브이. | 수술후 접착의 치료를 위한, 히스타민 ｈ4 길항제의 용도 |
| US20100029942A1 (en) * | 2008-06-30 | 2010-02-04 | Sergio Cesco-Cancian | Process for the preparation of benzoimidazol-2-yl pyrimidine derivatives |
| AU2013204436B2 (en) * | 2008-06-30 | 2014-12-04 | Janssen Pharmaceutica Nv | Process for the preparation of benzoimidazol-2-yl pyrimidine derivatives |
| PL2310012T3 (pl) | 2008-06-30 | 2015-08-31 | Janssen Pharmaceutica Nv | Sposób wytwarzania podstawionych pochodnych pirymidyny |
| US9371311B2 (en) | 2008-06-30 | 2016-06-21 | Janssen Pharmaceutica Nv | 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 |
| AR074210A1 (es) | 2008-11-24 | 2010-12-29 | Boehringer Ingelheim Int | Derivados de pirimidina como inhibidores de ptk2-quinasa |
| 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 |
| SG10201401169QA (en) * | 2009-04-02 | 2014-05-29 | Merck Serono Sa | Dihydroorotate dehydrogenase inhibitors |
| WO2011092293A2 (en) | 2010-02-01 | 2011-08-04 | Novartis Ag | Cyclohexyl amide derivatives as crf receptor antagonists |
| 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 |
| JP5748777B2 (ja) | 2010-02-02 | 2015-07-15 | ノバルティス アーゲー | Ｃｒｆ受容体アンタゴニストとしてのシクロヘキシルアミド誘導体 |
| AR081331A1 (es) | 2010-04-23 | 2012-08-08 | Cytokinetics Inc | Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos |
| 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 |
| EP2560488B1 (en) | 2010-04-23 | 2015-10-28 | Cytokinetics, Inc. | Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use |
| EP3009427B1 (en) | 2011-03-03 | 2019-12-18 | Zalicus Pharmaceuticals Ltd. | Benzimidazole 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 |
| JP6185574B2 (ja) | 2012-06-08 | 2017-08-23 | センソリオン | 耳鳴りを治療するためのｈ４受容体阻害剤 |
| MY180726A (en) | 2013-03-06 | 2020-12-08 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor |
| 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 |
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