NO312292B1 - Acylaminoalkenylen-amidderivater som NK1- og NK2- antagonister, anvendelse derav, farmasöytiske preparater samtfremgangsmåte for fremstilling av derivatene - Google Patents
Acylaminoalkenylen-amidderivater som NK1- og NK2- antagonister, anvendelse derav, farmasöytiske preparater samtfremgangsmåte for fremstilling av derivatene Download PDFInfo
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- NO312292B1 NO312292B1 NO19990786A NO990786A NO312292B1 NO 312292 B1 NO312292 B1 NO 312292B1 NO 19990786 A NO19990786 A NO 19990786A NO 990786 A NO990786 A NO 990786A NO 312292 B1 NO312292 B1 NO 312292B1
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- Prior art keywords
- methyl
- compound
- hydrogen
- formula
- amino
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- -1 their use Substances 0.000 title claims description 43
- 239000000825 pharmaceutical preparation Substances 0.000 title claims description 15
- 238000002360 preparation method Methods 0.000 title claims description 14
- 238000000034 method Methods 0.000 title description 35
- 239000005557 antagonist Substances 0.000 title description 6
- 150000001408 amides Chemical class 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims description 133
- 239000000203 mixture Substances 0.000 claims description 54
- 239000001257 hydrogen Substances 0.000 claims description 41
- 229910052739 hydrogen Inorganic materials 0.000 claims description 41
- 150000003839 salts Chemical class 0.000 claims description 36
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 32
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 28
- 125000000217 alkyl group Chemical group 0.000 claims description 19
- 201000010099 disease Diseases 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims description 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 10
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims description 8
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 8
- 125000000814 indol-3-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C([*])C2=C1[H] 0.000 claims description 8
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims description 7
- 108010040722 Neurokinin-2 Receptors Proteins 0.000 claims description 7
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 7
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 7
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- 108010040718 Neurokinin-1 Receptors Proteins 0.000 claims description 6
- 102100037342 Substance-K receptor Human genes 0.000 claims description 5
- 102100037346 Substance-P receptor Human genes 0.000 claims description 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
- 125000005809 3,4,5-trimethoxyphenyl group Chemical group [H]C1=C(OC([H])([H])[H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims description 4
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 4
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- 230000008485 antagonism Effects 0.000 claims description 4
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- 125000001424 substituent group Chemical group 0.000 claims description 4
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- 125000003545 alkoxy group Chemical group 0.000 claims description 2
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Classifications
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- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
- C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D223/12—Nitrogen atoms not forming part of a nitro radical
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Hydrogenated Pyridines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH206196 | 1996-08-22 | ||
| PCT/EP1997/004436 WO1998007694A1 (en) | 1996-08-22 | 1997-08-13 | Acylaminoalkenylene-amide derivatives as nk1 and nk2 antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NO990786D0 NO990786D0 (no) | 1999-02-19 |
| NO990786L NO990786L (no) | 1999-03-25 |
| NO312292B1 true NO312292B1 (no) | 2002-04-22 |
Family
ID=4225003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO19990786A NO312292B1 (no) | 1996-08-22 | 1999-02-19 | Acylaminoalkenylen-amidderivater som NK1- og NK2- antagonister, anvendelse derav, farmasöytiske preparater samtfremgangsmåte for fremstilling av derivatene |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US6319917B1 (cs) |
| EP (1) | EP0923550B1 (cs) |
| JP (1) | JP3654908B2 (cs) |
| KR (1) | KR100467402B1 (cs) |
| CN (1) | CN1119328C (cs) |
| AR (1) | AR009266A1 (cs) |
| AT (1) | ATE224875T1 (cs) |
| AU (1) | AU721850B2 (cs) |
| BR (1) | BR9711350A (cs) |
| CA (1) | CA2264065C (cs) |
| CO (1) | CO4900047A1 (cs) |
| CZ (1) | CZ294233B6 (cs) |
| DE (1) | DE69715886T2 (cs) |
| DK (1) | DK0923550T3 (cs) |
| ES (1) | ES2184083T3 (cs) |
| HU (1) | HU226395B1 (cs) |
| ID (1) | ID18059A (cs) |
| IL (1) | IL128631A (cs) |
| MY (1) | MY132550A (cs) |
| NO (1) | NO312292B1 (cs) |
| NZ (1) | NZ334736A (cs) |
| PE (1) | PE107498A1 (cs) |
| PL (1) | PL193731B1 (cs) |
| PT (1) | PT923550E (cs) |
| RU (1) | RU2185375C2 (cs) |
| SI (1) | SI0923550T1 (cs) |
| SK (1) | SK283991B6 (cs) |
| TR (1) | TR199900363T2 (cs) |
| TW (1) | TW438777B (cs) |
| WO (1) | WO1998007694A1 (cs) |
| ZA (1) | ZA977493B (cs) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6281300B1 (en) * | 1998-03-20 | 2001-08-28 | Exxon Chemical Patents, Inc. | Continuous slurry polymerization volatile removal |
| GB0010958D0 (en) * | 2000-05-05 | 2000-06-28 | Novartis Ag | Organic compounds |
| GB0203061D0 (en) * | 2002-02-08 | 2002-03-27 | Novartis Ag | Organic compounds |
| GB0224788D0 (en) * | 2002-10-24 | 2002-12-04 | Novartis Ag | Organic compounds |
| GB2394417A (en) * | 2002-10-24 | 2004-04-28 | Novartis Ag | Solid dispersion comprising a piperidine substance P antagonist and a carrier |
| EP2158910A1 (en) | 2003-10-27 | 2010-03-03 | Novartis Ag | Use of neurokinin antagonists in the treatment of urinary incontinence |
| US20080227724A1 (en) * | 2003-12-01 | 2008-09-18 | Cambridge University Technical Services Limited | Anti-Inflammatory Agents |
| RU2365585C2 (ru) * | 2003-12-01 | 2009-08-27 | Кембридж Энтерпрайз Лимитед | Противовоспалительные средства |
| GB0402679D0 (en) * | 2004-02-06 | 2004-03-10 | Novartis Ag | Organic compounds |
| GB0607532D0 (en) * | 2006-04-13 | 2006-05-24 | Novartis Ag | Organic compounds |
| JO2630B1 (en) * | 2006-04-13 | 2012-06-17 | نوفارتيس ايه جي | Organic compounds |
| EP1938804A1 (en) * | 2006-12-22 | 2008-07-02 | Novartis AG | Pharmaceutical formulation comprising neurokinin antagonist |
| EP2117538A1 (en) | 2007-01-24 | 2009-11-18 | Glaxo Group Limited | Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-) |
| UA105182C2 (ru) | 2008-07-03 | 2014-04-25 | Ньюрексон, Інк. | Бензоксазины, бензотиазины и родственные соединения, которые имеют ингибирующую nos активность |
| CN102395358A (zh) * | 2009-02-24 | 2012-03-28 | 诺瓦提斯公司 | Nk受体拮抗剂的用途 |
| RU2697414C1 (ru) * | 2018-05-11 | 2019-08-14 | Общество с ограниченной ответственностью "АЙ БИ ДИ Терапевтикс" | Новый антагонист тахикининовых рецепторов и его применение |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI97540C (fi) * | 1989-11-06 | 1997-01-10 | Sanofi Sa | Menetelmä terapeuttisesti käyttökelpoisten, aromaattisesti substituoitujen piperidiini- ja piperatsiinijohdannaisten valmistamiseksi |
| JPH06509087A (ja) | 1991-07-05 | 1994-10-13 | メルク シヤープ エンド ドーム リミテツド | 芳香族化合物、それらを含む医薬組成物、及び治療におけるそれらの使用 |
| MY110227A (en) * | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
| US5217996A (en) | 1992-01-22 | 1993-06-08 | Ciba-Geigy Corporation | Biaryl substituted 4-amino-butyric acid amides |
| EP0716077A1 (de) * | 1994-12-08 | 1996-06-12 | Ciba-Geigy Ag | Aromatisch substituierte Omega-Aminoalkansäureamide und Alkansäurediamide und ihre Verwendung als Renininhibitoren |
| CA2213080C (en) | 1995-02-22 | 2007-11-13 | Novartis Ag | 1-aryl-2-acylamino-ethane compounds and their use as neurokinin especially neurokinin 1 antagonists |
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