JP2008542367A - Ｎｋ−３アンタゴニストとしてのキノリン誘導体 - Google Patents
Ｎｋ−３アンタゴニストとしてのキノリン誘導体 Download PDFInfo
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- JP2008542367A JP2008542367A JP2008514588A JP2008514588A JP2008542367A JP 2008542367 A JP2008542367 A JP 2008542367A JP 2008514588 A JP2008514588 A JP 2008514588A JP 2008514588 A JP2008514588 A JP 2008514588A JP 2008542367 A JP2008542367 A JP 2008542367A
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- Prior art keywords
- alkyl
- cyanomethyl
- phenyl
- pharmaceutically acceptable
- disease
- Prior art date
- Legal status (The legal status 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 status listed.)
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- 229940027991 antiseptic and disinfectant quinoline derivative Drugs 0.000 title description 3
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 31
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- 125000000217 alkyl group Chemical group 0.000 claims description 25
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- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide Chemical compound CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims description 14
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- NGIJJOHATIDYHC-QHCPKHFHSA-N 3-(cyanomethyl)-2-phenyl-n-[(1s)-1-phenylpropyl]quinoline-4-carboxamide Chemical compound N([C@@H](CC)C=1C=CC=CC=1)C(=O)C(C1=CC=CC=C1N=1)=C(CC#N)C=1C1=CC=CC=C1 NGIJJOHATIDYHC-QHCPKHFHSA-N 0.000 claims description 3
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- RDZTWEVXRGYCFV-UHFFFAOYSA-M sodium 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonate Chemical compound [Na+].OCCN1CCN(CCS([O-])(=O)=O)CC1 RDZTWEVXRGYCFV-UHFFFAOYSA-M 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 201000009032 substance abuse Diseases 0.000 description 1
- 231100000736 substance abuse Toxicity 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000035900 sweating Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 239000003104 tissue culture media Substances 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 239000002753 trypsin inhibitor Substances 0.000 description 1
- 238000003828 vacuum filtration Methods 0.000 description 1
- 210000005166 vasculature Anatomy 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 230000001755 vocal effect Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/50—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
- C07D215/52—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4 with aryl radicals attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/50—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- 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
-
- 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
- A61P1/12—Antidiarrhoeals
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Reproductive Health (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US68741805P | 2005-06-03 | 2005-06-03 | |
| PCT/SE2006/000630 WO2006130080A2 (en) | 2005-06-03 | 2006-05-30 | Quinoline derivatives as nk3 anatgonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008542367A true JP2008542367A (ja) | 2008-11-27 |
| JP2008542367A5 JP2008542367A5 (enExample) | 2009-07-16 |
Family
ID=37482086
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008514588A Pending JP2008542367A (ja) | 2005-06-03 | 2006-05-30 | Ｎｋ−３アンタゴニストとしてのキノリン誘導体 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20080200500A1 (enExample) |
| EP (1) | EP1891012A2 (enExample) |
| JP (1) | JP2008542367A (enExample) |
| KR (1) | KR20080016591A (enExample) |
| CN (1) | CN101189211A (enExample) |
| AU (1) | AU2006253054A1 (enExample) |
| CA (1) | CA2611060A1 (enExample) |
| IL (1) | IL187410A0 (enExample) |
| MX (1) | MX2007014831A (enExample) |
| NO (1) | NO20080033L (enExample) |
| WO (1) | WO2006130080A2 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008131779A1 (en) | 2007-04-26 | 2008-11-06 | H. Lundbeck A/S | Isoquinolinone derivatives as nk3 antagonists |
| US8173639B2 (en) | 2007-04-26 | 2012-05-08 | H. Lundbeck A/S | Isoquinolinone derivatives as NK3 antagonists |
| KR20110026429A (ko) | 2008-06-23 | 2011-03-15 | 하. 룬드벡 아크티에셀스카브 | Ｎｋ3 길항제로서의 이소퀴놀리논 유도체 |
| US8242134B2 (en) | 2008-09-15 | 2012-08-14 | H. Lundbeck A/S | Isoquinolinone derivatives as NK3 antagonists |
| AU2009306819A1 (en) | 2008-10-20 | 2010-04-29 | H. Lundbeck A/S | Isoquinolinone derivatives as NK3 antagonists |
| TW201143768A (en) | 2009-12-15 | 2011-12-16 | Lundbeck & Co As H | Pyridone derivatives as NK3 antagonists |
| TW201144311A (en) | 2010-03-12 | 2011-12-16 | Lundbeck & Co As H | Azaisoquionolinone derivatives as NK3 antagonists |
| EP3915560A1 (en) | 2014-06-25 | 2021-12-01 | Emory University | Methods of managing conditioned fear with neurokinin receptor antagonists |
| KR20160069683A (ko) | 2014-12-09 | 2016-06-17 | 백찬욱 | 콤비보트 및 그 제작 방법 |
| EP3704271B1 (en) | 2017-11-02 | 2026-01-28 | California Institute of Technology | Neurokinin antagonists and uses thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RO114445B1 (ro) * | 1994-05-27 | 1999-04-30 | Smithkline Beecham S.P.A. | Derivaţi de chinolină antagonişti ai receptorului nk3 tachichinină,procedeu de preparare,compoziţii farmaceutice pe baza acestora şi metodă de tratament |
| IT1270615B (it) * | 1994-07-14 | 1997-05-07 | Smithkline Beecham Farma | Uso di derivati di chinolina |
| GB9524137D0 (en) * | 1995-11-24 | 1996-01-24 | Smithkline Beecham Spa | Novel compounds |
| AR004735A1 (es) * | 1995-11-24 | 1999-03-10 | Smithkline Beecham Spa | Quinoleina 4-amido sustituida, un procedimiento para su preparacion, una composicion farmaceutica que los contiene y el uso de los mismos para lapreparacion de un medicamento. |
| ES2201509T3 (es) * | 1997-05-23 | 2004-03-16 | Glaxosmithkline S.P.A. | Derivados de quinolina-4-carboxamida como antagonista de los receptores nk-2 y nk-3. |
| AP1201A (en) * | 1997-09-17 | 2003-09-01 | Smithkline Beecham Corp | Method for the synthesis of quinoline derivatives. |
| CN1406225A (zh) * | 1998-11-20 | 2003-03-26 | 葛兰素史密丝克莱恩有限公司 | 用作nk－3和nk－2受体拮抗剂的喹啉－4－甲酰胺衍生物 |
| US20040152726A1 (en) * | 2001-04-11 | 2004-08-05 | Carlo Farina | Quinoline-4-carboxamide derivatives as nk-3 and nk-2 receptor antagonists |
| EP1915363A1 (en) * | 2005-08-11 | 2008-04-30 | AstraZeneca AB | Oxopyridyl quinoline amides as nk3 receptor modulators |
| AR058051A1 (es) * | 2005-09-21 | 2008-01-23 | Astrazeneca Ab | Quinolinas de alquilnitrilo.proceso de obtencion y composiciones farmaceuticas. |
| WO2007086799A1 (en) * | 2006-01-27 | 2007-08-02 | Astrazeneca Ab | Amide substituted quinolines |
-
2006
- 2006-05-30 AU AU2006253054A patent/AU2006253054A1/en not_active Abandoned
- 2006-05-30 MX MX2007014831A patent/MX2007014831A/es not_active Application Discontinuation
- 2006-05-30 EP EP06747824A patent/EP1891012A2/en not_active Withdrawn
- 2006-05-30 JP JP2008514588A patent/JP2008542367A/ja active Pending
- 2006-05-30 KR KR1020077027965A patent/KR20080016591A/ko not_active Withdrawn
- 2006-05-30 WO PCT/SE2006/000630 patent/WO2006130080A2/en not_active Ceased
- 2006-05-30 CA CA002611060A patent/CA2611060A1/en not_active Abandoned
- 2006-05-30 CN CNA2006800196735A patent/CN101189211A/zh active Pending
- 2006-05-30 US US11/914,583 patent/US20080200500A1/en not_active Abandoned
-
2007
- 2007-11-15 IL IL187410A patent/IL187410A0/en unknown
-
2008
- 2008-01-03 NO NO20080033A patent/NO20080033L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2006130080A3 (en) | 2007-01-25 |
| KR20080016591A (ko) | 2008-02-21 |
| NO20080033L (no) | 2008-01-03 |
| MX2007014831A (es) | 2008-02-15 |
| US20080200500A1 (en) | 2008-08-21 |
| WO2006130080A2 (en) | 2006-12-07 |
| IL187410A0 (en) | 2008-02-09 |
| CA2611060A1 (en) | 2006-12-07 |
| CN101189211A (zh) | 2008-05-28 |
| EP1891012A2 (en) | 2008-02-27 |
| AU2006253054A1 (en) | 2006-12-07 |
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