ZA200410213B - Indole derivatives useful as histamine H3 antagonists. - Google Patents
Indole derivatives useful as histamine H3 antagonists. Download PDFInfo
- Publication number
- ZA200410213B ZA200410213B ZA200410213A ZA200410213A ZA200410213B ZA 200410213 B ZA200410213 B ZA 200410213B ZA 200410213 A ZA200410213 A ZA 200410213A ZA 200410213 A ZA200410213 A ZA 200410213A ZA 200410213 B ZA200410213 B ZA 200410213B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- aryl
- compound
- alkoxy
- independently selected
- Prior art date
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- 150000002475 indoles Chemical class 0.000 title description 3
- 229940054051 antipsychotic indole derivative Drugs 0.000 title description 2
- 239000003395 histamine H3 receptor antagonist Substances 0.000 title description 2
- 125000000217 alkyl group Chemical group 0.000 claims description 98
- 150000001875 compounds Chemical class 0.000 claims description 47
- 125000003545 alkoxy group Chemical group 0.000 claims description 26
- 229910052799 carbon Inorganic materials 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 150000002367 halogens Chemical class 0.000 claims description 20
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 18
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- 208000026935 allergic disease Diseases 0.000 claims description 18
- 229940044551 receptor antagonist Drugs 0.000 claims description 18
- 239000002464 receptor antagonist Substances 0.000 claims description 18
- 230000007815 allergy Effects 0.000 claims description 17
- 229910052757 nitrogen Inorganic materials 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 16
- -1 piperidinoethyl Chemical group 0.000 claims description 16
- 125000001072 heteroaryl group Chemical group 0.000 claims description 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 125000005843 halogen group Chemical group 0.000 claims description 14
- 238000000034 method Methods 0.000 claims description 14
- 125000001424 substituent group Chemical group 0.000 claims description 14
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- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 6
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 6
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- 230000002057 chronotropic effect Effects 0.000 description 1
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- 150000002169 ethanolamines Chemical class 0.000 description 1
- 150000002171 ethylene diamines Chemical class 0.000 description 1
- 125000003838 furazanyl group Chemical group 0.000 description 1
- 230000027119 gastric acid secretion Effects 0.000 description 1
- 125000004438 haloalkoxy group Chemical group 0.000 description 1
- 125000001188 haloalkyl group Chemical group 0.000 description 1
- 210000002837 heart atrium Anatomy 0.000 description 1
- 239000000938 histamine H1 antagonist Substances 0.000 description 1
- 206010020765 hypersomnia Diseases 0.000 description 1
- 125000001041 indolyl group Chemical group 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 125000002346 iodo group Chemical group I* 0.000 description 1
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- 239000003446 ligand Substances 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 235000010755 mineral Nutrition 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 description 1
- 201000003631 narcolepsy Diseases 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
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- 150000007524 organic acids Chemical class 0.000 description 1
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- AHHWIHXENZJRFG-UHFFFAOYSA-N oxetane Chemical compound C1COC1 AHHWIHXENZJRFG-UHFFFAOYSA-N 0.000 description 1
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- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
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- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
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Classifications
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- 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
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- A61P25/06—Antimigraine agents
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- A—HUMAN NECESSITIES
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- A61P25/08—Antiepileptics; Anticonvulsants
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
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- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Neurosurgery (AREA)
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- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
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- Pulmonology (AREA)
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- Pain & Pain Management (AREA)
- Hematology (AREA)
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- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Anesthesiology (AREA)
- Ophthalmology & Optometry (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| US39098702P | 2002-06-24 | 2002-06-24 |
Publications (1)
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| ZA200410213B true ZA200410213B (en) | 2005-10-20 |
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| ZA200410213A ZA200410213B (en) | 2002-06-24 | 2004-12-17 | Indole derivatives useful as histamine H3 antagonists. |
Country Status (22)
| Country | Link |
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| EP (2) | EP1777223A1 (zh) |
| JP (1) | JP4326468B2 (zh) |
| KR (1) | KR20050009757A (zh) |
| CN (1) | CN100497334C (zh) |
| AR (1) | AR039718A1 (zh) |
| AT (1) | ATE344798T1 (zh) |
| AU (1) | AU2003243709B2 (zh) |
| CA (1) | CA2489337C (zh) |
| CY (1) | CY1105986T1 (zh) |
| DE (1) | DE60309598T2 (zh) |
| DK (1) | DK1539742T3 (zh) |
| ES (1) | ES2271644T3 (zh) |
| HK (1) | HK1072259A1 (zh) |
| IL (1) | IL165863A0 (zh) |
| MX (1) | MXPA05000193A (zh) |
| MY (1) | MY135686A (zh) |
| NZ (1) | NZ537200A (zh) |
| PT (1) | PT1539742E (zh) |
| TW (1) | TW200400031A (zh) |
| WO (1) | WO2004000831A1 (zh) |
| ZA (1) | ZA200410213B (zh) |
Families Citing this family (45)
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| PE20020507A1 (es) * | 2000-10-17 | 2002-06-25 | Schering Corp | Compuestos no-imidazoles como antagonistas del receptor histamina h3 |
| WO2004002983A2 (en) * | 2002-06-28 | 2004-01-08 | Euro-Celtique, S.A. | Therapeutic piperazine derivatives useful for treating pain |
| MXPA05007513A (es) | 2003-01-14 | 2005-09-21 | Cytokinetics Inc | Compuestos, composiciones y metodos. |
| BRPI0512193B8 (pt) | 2004-06-17 | 2021-05-25 | Cytokinetics Inc | composto ou sal farmaceuticamente aceitável, composição farmacêutica, e, uso do composto ou sal |
| NZ551663A (en) | 2004-06-21 | 2009-09-25 | Hoffmann La Roche | Indole derivatives as histamine receptor antagonists |
| US7176222B2 (en) | 2004-07-27 | 2007-02-13 | Cytokinetics, Inc. | Syntheses of ureas |
| FR2878849B1 (fr) | 2004-12-06 | 2008-09-12 | Aventis Pharma Sa | Indoles substitues, compositions les contenant, procede de fabrication et utilisation |
| JP2008532926A (ja) * | 2004-12-06 | 2008-08-21 | アバンテイス・フアルマ・エス・アー | 置換インドール化合物、それを含有する組成物、この製造方法およびこの使用 |
| BRPI0606502A2 (pt) | 2005-01-19 | 2009-06-30 | Hoffmann La Roche | compostos; processo para a fabricação de compostos; composições farmacêuticas; método para o tratamento ou prevenção de doenças que são associadas com a modulação de receptores h3; método para o tratamento ou prevenção de obesidade em um ser humano ou animal; método de tratamento ou prevenção de diabetes tipo ii em um ser humano ou animal e usos de compostos |
| AU2006262441A1 (en) | 2005-06-20 | 2007-01-04 | Schering Corporation | Piperidine derivatives useful as histamine H3 antagonists |
| EP1896453B1 (en) * | 2005-06-20 | 2009-12-02 | Schering Corporation | Carbon-linked substituted piperidines and derivatives thereof useful as histamine h3 antagonists |
| EP1909797A4 (en) * | 2005-08-02 | 2013-02-27 | Neurogen Corp | DIPIPERAZINYL KETONE AND RELATED ANALOG |
| US7538223B2 (en) | 2005-08-04 | 2009-05-26 | Cytokinetics, Inc. | Compounds, compositions and methods |
| US7332604B2 (en) * | 2005-09-20 | 2008-02-19 | Schering Corporation | 1-[[1-[(2-Amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-b]pyridin-3-yl]piperidine |
| GB2431927B (en) * | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
| US7977359B2 (en) | 2005-11-04 | 2011-07-12 | Amira Pharmaceuticals, Inc. | 5-lipdxygenase-activating protein (FLAP) inhibitors |
| ATE485294T1 (de) | 2005-11-18 | 2010-11-15 | Hoffmann La Roche | Azaindol-2-carboxamid-derivate |
| DE602006014022D1 (de) | 2005-11-30 | 2010-06-10 | Hoffmann La Roche | 5-substituierte indol-2-carbonsäureamidderivate |
| US7825120B2 (en) | 2005-12-15 | 2010-11-02 | Cytokinetics, Inc. | Certain substituted ((piperazin-1-ylmethyl)benzyl)ureas |
| TW200808321A (en) | 2005-12-15 | 2008-02-16 | Cytokinetics Inc | Certain chemical entities, compositions and methods |
| WO2007078815A2 (en) | 2005-12-16 | 2007-07-12 | Cytokinetics, Inc. | Certain chemical entities, compositions, and methods |
| EP1962852B1 (en) | 2005-12-19 | 2017-01-25 | Cytokinetics, Inc. | Compounds, compositions and methods |
| BRPI0620386A2 (pt) * | 2005-12-21 | 2011-12-20 | Schering Corp | composição compreendendo a combinação de um antagonista de h3/agonista inverso e um supressor de apetite e uso da referida composição |
| AR058558A1 (es) * | 2005-12-21 | 2008-02-13 | Schering Corp | Derivados de anilina sustituida utiles como antagonistas de la histamina h3 |
| AU2006331882A1 (en) * | 2005-12-21 | 2007-07-05 | Schering Corporation | Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists |
| JP2010519171A (ja) * | 2006-02-17 | 2010-06-03 | メモリー・ファーマシューティカルズ・コーポレイション | ５−ｈｔ６受容体親和性を有する化合物 |
| US7514433B2 (en) * | 2006-08-03 | 2009-04-07 | Hoffmann-La Roche Inc. | 1H-indole-6-yl-piperazin-1-yl-methanone derivatives |
| CA2667548C (en) * | 2006-10-27 | 2015-02-03 | Boehringer Ingelheim International Gmbh | Substituted piperidyl-propane-thiols |
| JP5581055B2 (ja) * | 2006-10-27 | 2014-08-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ピペリジル−プロパン−チオールｃｃｒ３モジュレーター |
| CA2695456A1 (en) * | 2007-08-15 | 2009-02-19 | Robert Dunn | 3' substituted compounds having 5-ht6 receptor affinity |
| NZ587202A (en) * | 2008-01-04 | 2013-03-28 | Schabar Res Associates Llc | Methods for measuring a patient response upon administration of a drug and compositions thereof |
| AU2009325091A1 (en) | 2008-05-23 | 2010-06-17 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein inhibitor |
| US20100016297A1 (en) * | 2008-06-24 | 2010-01-21 | Memory Pharmaceuticals Corporation | Alkyl-substituted 3' compounds having 5-ht6 receptor affinity |
| US20100035862A1 (en) * | 2008-06-25 | 2010-02-11 | Abbott Laboratories | Novel aza-cyclic indole-2-carboxamides and methods of use thereof |
| AR072297A1 (es) | 2008-06-27 | 2010-08-18 | Novartis Ag | Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona. |
| WO2010011657A1 (en) * | 2008-07-23 | 2010-01-28 | Schering Corporation | Bicyclic heterocycle derivatives as histamine h3 receptor antagonists |
| US20100029629A1 (en) * | 2008-07-25 | 2010-02-04 | Memory Pharmaceuticals Corporation | Acyclic compounds having 5-ht6 receptor affinity |
| US20100056531A1 (en) * | 2008-08-22 | 2010-03-04 | Memory Pharmaceuticals Corporation | Alkyl-substituted 3' compounds having 5-ht6 receptor affinity |
| US9024041B2 (en) | 2010-04-08 | 2015-05-05 | Respivert Ltd. | P38 MAP kinase inhibitors |
| WO2011153359A1 (en) | 2010-06-04 | 2011-12-08 | Albany Molecular Research, Inc. | Glycine transporter-1 inhibitors, methods of making them, and uses thereof |
| WO2013151982A1 (en) | 2012-04-03 | 2013-10-10 | Arena Pharmaceuticals, Inc. | Methods and compounds useful in treating pruritus, and methods for identifying such compounds |
| TWI748194B (zh) | 2018-06-28 | 2021-12-01 | 德商菲尼克斯 Ｆｘｒ有限責任公司 | 含有雙環核心部分之新穎lxr調節劑 |
| EP3797769A1 (fr) | 2019-09-25 | 2021-03-31 | Fontès, M. Michel | Composition a usage therapeutique |
| US11331307B2 (en) | 2020-07-15 | 2022-05-17 | Schabar Research Associates, Llc | Unit oral dose compositions composed of ibuprofen and famotidine for the treatment of acute pain and the reduction of the severity and/or risk of heartburn |
| US11324727B2 (en) | 2020-07-15 | 2022-05-10 | Schabar Research Associates, Llc | Unit oral dose compositions composed of naproxen sodium and famotidine for the treatment of acute pain and the reduction of the severity of heartburn and/or the risk of heartburn |
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| JPH0730037B2 (ja) | 1987-03-13 | 1995-04-05 | 第一製薬株式会社 | ピリミジニルプロピオン酸誘導体 |
| DK181190D0 (da) | 1990-07-30 | 1990-07-30 | Lundbeck & Co As H | 3-aryl-indol- eller 3-aryl-indazolderivater |
| US5352707A (en) * | 1992-03-26 | 1994-10-04 | Harbor Branch Oceanographic Institution, Inc. | Method for treating airway congestion |
| US5217986A (en) * | 1992-03-26 | 1993-06-08 | Harbor Branch Oceanographic Institution, Inc. | Anti-allergy agent |
| US5846982A (en) * | 1996-06-14 | 1998-12-08 | Eli Lilly And Company | Inhibition of serotonin reuptake |
| SK20099A3 (en) | 1996-08-16 | 2000-08-14 | Schering Corp | Treatment of upper airway allergic responses with a combination of histamine receptor antagonists |
| CZ180599A3 (cs) * | 1996-11-25 | 1999-11-17 | The Procter & Gamble Company | 2-Imidazolinylaminoindolová sloučenina, farmaceutický prostředek ji obsahující a její použití |
| US5869479A (en) * | 1997-08-14 | 1999-02-09 | Schering Corporation | Treatment of upper airway allergic responses |
| ATE319709T1 (de) | 1999-12-20 | 2006-03-15 | Lilly Co Eli | Indolderivate zur behandlung von depression und angstzuständen |
| PE20020507A1 (es) * | 2000-10-17 | 2002-06-25 | Schering Corp | Compuestos no-imidazoles como antagonistas del receptor histamina h3 |
| ES2172436B1 (es) | 2000-10-31 | 2004-01-16 | Almirall Prodesfarma Sa | Derivados de indolilpiperidina como agentes antihistaminicos y antialergicos. |
| WO2002072093A2 (en) | 2001-02-08 | 2002-09-19 | Schering Corporation | Use of dual h3/m2 antagonists with a bipiperidinic structure in the treatment of cognition deficit disorders |
| CA2440559C (en) | 2001-03-13 | 2010-09-21 | Schering Corporation | Novel non-imidazole compounds |
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- 2003-06-20 DE DE60309598T patent/DE60309598T2/de not_active Expired - Lifetime
- 2003-06-20 KR KR10-2004-7020914A patent/KR20050009757A/ko not_active Application Discontinuation
- 2003-06-20 EP EP06020215A patent/EP1777223A1/en not_active Withdrawn
- 2003-06-20 IL IL16586303A patent/IL165863A0/xx unknown
- 2003-06-20 WO PCT/US2003/019619 patent/WO2004000831A1/en active IP Right Grant
- 2003-06-20 AU AU2003243709A patent/AU2003243709B2/en not_active Ceased
- 2003-06-20 NZ NZ537200A patent/NZ537200A/en unknown
- 2003-06-20 ES ES03761216T patent/ES2271644T3/es not_active Expired - Lifetime
- 2003-06-20 DK DK03761216T patent/DK1539742T3/da active
- 2003-06-20 PT PT03761216T patent/PT1539742E/pt unknown
- 2003-06-20 AT AT03761216T patent/ATE344798T1/de not_active IP Right Cessation
- 2003-06-20 EP EP03761216A patent/EP1539742B1/en not_active Expired - Lifetime
- 2003-06-20 CN CNB038147173A patent/CN100497334C/zh not_active Expired - Fee Related
- 2003-06-20 TW TW092116874A patent/TW200400031A/zh unknown
- 2003-06-20 MY MYPI20032323A patent/MY135686A/en unknown
- 2003-06-20 US US10/600,674 patent/US6951871B2/en not_active Expired - Fee Related
- 2003-06-20 CA CA2489337A patent/CA2489337C/en not_active Expired - Fee Related
-
2004
- 2004-12-17 ZA ZA200410213A patent/ZA200410213B/en unknown
-
2005
- 2005-06-18 HK HK05105092A patent/HK1072259A1/xx not_active IP Right Cessation
-
2007
- 2007-02-05 CY CY20071100153T patent/CY1105986T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN100497334C (zh) | 2009-06-10 |
| WO2004000831A1 (en) | 2003-12-31 |
| EP1539742B1 (en) | 2006-11-08 |
| AR039718A1 (es) | 2005-03-09 |
| US6951871B2 (en) | 2005-10-04 |
| JP4326468B2 (ja) | 2009-09-09 |
| ES2271644T3 (es) | 2007-04-16 |
| KR20050009757A (ko) | 2005-01-25 |
| EP1539742A1 (en) | 2005-06-15 |
| CA2489337C (en) | 2010-05-25 |
| AU2003243709A1 (en) | 2004-01-06 |
| DK1539742T3 (da) | 2006-12-27 |
| NZ537200A (en) | 2007-09-28 |
| IL165863A0 (en) | 2006-01-15 |
| JP2005531615A (ja) | 2005-10-20 |
| CA2489337A1 (en) | 2003-12-31 |
| US20040019099A1 (en) | 2004-01-29 |
| AU2003243709B2 (en) | 2007-01-18 |
| ATE344798T1 (de) | 2006-11-15 |
| PT1539742E (pt) | 2007-01-31 |
| EP1777223A1 (en) | 2007-04-25 |
| HK1072259A1 (en) | 2005-08-19 |
| MY135686A (en) | 2008-06-30 |
| DE60309598T2 (de) | 2007-09-13 |
| DE60309598D1 (de) | 2006-12-21 |
| MXPA05000193A (es) | 2005-04-08 |
| CN1662524A (zh) | 2005-08-31 |
| TW200400031A (en) | 2004-01-01 |
| CY1105986T1 (el) | 2011-04-06 |
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