SK2162000A3 - Substituted 4-oxo-napthyridine-3-carboxamides as gaba brain receptor ligands - Google Patents
Substituted 4-oxo-napthyridine-3-carboxamides as gaba brain receptor ligands Download PDFInfo
- Publication number
- SK2162000A3 SK2162000A3 SK216-2000A SK2162000A SK2162000A3 SK 2162000 A3 SK2162000 A3 SK 2162000A3 SK 2162000 A SK2162000 A SK 2162000A SK 2162000 A3 SK2162000 A3 SK 2162000A3
- Authority
- SK
- Slovakia
- Prior art keywords
- oxo
- naphthyridine
- carboxamide
- tetrahydro
- compound
- Prior art date
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- 239000003446 ligand Substances 0.000 title description 5
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- 150000002431 hydrogen Chemical group 0.000 claims abstract description 35
- 125000003118 aryl group Chemical group 0.000 claims abstract description 19
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract description 13
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- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 210000001640 nerve ending Anatomy 0.000 description 1
- 239000002858 neurotransmitter agent Substances 0.000 description 1
- 231100000344 non-irritating Toxicity 0.000 description 1
- 230000009871 nonspecific binding Effects 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 230000035764 nutrition Effects 0.000 description 1
- GYCKQBWUSACYIF-UHFFFAOYSA-N o-hydroxybenzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1O GYCKQBWUSACYIF-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- PIDFDZJZLOTZTM-KHVQSSSXSA-N ombitasvir Chemical compound COC(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)NC1=CC=C([C@H]2N([C@@H](CC2)C=2C=CC(NC(=O)[C@H]3N(CCC3)C(=O)[C@@H](NC(=O)OC)C(C)C)=CC=2)C=2C=CC(=CC=2)C(C)(C)C)C=C1 PIDFDZJZLOTZTM-KHVQSSSXSA-N 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 description 1
- 125000005561 phenanthryl group Chemical group 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 230000001242 postsynaptic effect Effects 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 239000002287 radioligand Substances 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 230000004799 sedative–hypnotic effect Effects 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 229910001467 sodium calcium phosphate Inorganic materials 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000012258 stirred mixture Substances 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000001424 substituent group Chemical group 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 210000000225 synapse Anatomy 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 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
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 238000000844 transformation Methods 0.000 description 1
- 125000004953 trihalomethyl group Chemical group 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91818097A | 1997-08-25 | 1997-08-25 | |
| PCT/US1998/017513 WO1999010347A1 (en) | 1997-08-25 | 1998-08-24 | Substituted 4-oxo-napthyridine-3-carboxamides as gaba brain receptor ligands |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SK2162000A3 true SK2162000A3 (en) | 2001-03-12 |
Family
ID=25439933
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK216-2000A SK2162000A3 (en) | 1997-08-25 | 1998-08-24 | Substituted 4-oxo-napthyridine-3-carboxamides as gaba brain receptor ligands |
Country Status (24)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1177177B1 (en) * | 1999-05-06 | 2005-02-23 | Neurogen Corporation | Substituted 4-oxo-quinoline-3-carboxamides: gaba brain receptor ligands |
| US6448246B1 (en) | 1999-05-25 | 2002-09-10 | Neurogen Corporation | Substituted 4H-1,4-benzothiazine-2-carboxamide: GABA brain receptor ligands |
| US6559145B2 (en) | 2000-07-12 | 2003-05-06 | Pharmacia & Upjohn Company | Heterocycle carboxamides as antiviral agents |
| US6730682B2 (en) | 2000-07-12 | 2004-05-04 | Pharmacia & Upjohn Company | Heterocycle carboxamides as antiviral agents |
| US6562822B2 (en) | 2000-07-12 | 2003-05-13 | Pharmacia & Upjohn Company | Heterocyle carboxamides as antiviral agents |
| ATE345129T1 (de) | 2000-10-12 | 2006-12-15 | Merck & Co Inc | Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer |
| SK4322003A3 (en) | 2000-10-12 | 2003-09-11 | Merck & Co Inc | Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors |
| ATE364385T1 (de) | 2000-10-12 | 2007-07-15 | Merck & Co Inc | Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer |
| US20020151591A1 (en) * | 2000-10-17 | 2002-10-17 | Anabella Villalobos | Combination use of acetylcholinesterase inhibitors and GABAa inverse agonists for the treatment of cognitive disorders |
| OA12554A (en) * | 2001-03-01 | 2006-06-07 | Pfizer Prod Inc | Use of GABA a inverse agonists in combination withnicotine receptor partial agonists, estrogen, sel ective estrogen modulators, or bitamin E for the treatment of cognitive disorders. |
| AR036256A1 (es) | 2001-08-17 | 2004-08-25 | Merck & Co Inc | Sal sodica de un inhibidor de integrasa del vih, procesos para su preparacion, composiciones farmaceuticas que lo contienen y su uso para la manufactura de un medicamento |
| CA2472372C (en) | 2002-01-17 | 2010-08-17 | Melissa Egbertson | Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors |
| WO2003077850A2 (en) | 2002-03-15 | 2003-09-25 | Merck & Co., Inc. | N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors |
| WO2004106336A1 (en) * | 2003-05-27 | 2004-12-09 | Pfizer Products Inc. | Process for the preparation and purification of 1,5-naphthyridine-3-carboxyamides |
| WO2004106334A2 (en) * | 2003-05-28 | 2004-12-09 | Pfizer Products Inc. | Process for the preparation of 1,5-naphthyridine-3-carboxy amides by direct ester amidation |
| CA2954376C (en) * | 2006-10-16 | 2019-06-11 | Bionomics Limited | Novel anxiolytic compounds |
| SI2083811T1 (sl) * | 2006-11-22 | 2017-02-28 | Clinical Research Associates, Llc | Postopki zdravljenja Downovega sindroma, sindroma krhkega X in avtizma |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR204162A1 (es) * | 1972-05-08 | 1975-11-28 | Yamanouchi Pharma Co Ltd | Proceso para la preparacion de derivados de ampicilina |
| GB1433774A (en) * | 1973-02-26 | 1976-04-28 | Allen & Hanburys Ltd | Heterocyclic compounds apparatus for conveying articles |
| US4374138A (en) * | 1981-11-13 | 1983-02-15 | Warner-Lambert Company | Antibacterial amide compounds, compositions, and methods of use |
| DD279887A1 (de) * | 1987-07-03 | 1990-06-20 | Inst Pharmakologische Forschun | Verfahren zur herstellung von d-alpha-(4(1h)-1,5-naphthyridon-3-carboxamido)-benzylpenicillin und anderen beta-lactamantibiotika |
| DD279875A1 (de) * | 1987-07-03 | 1990-06-20 | Inst Pharmakologische Forschun | Verfahren zur herstellung von aktivierten carbonsaeureestern |
| DD295360A5 (de) * | 1987-07-03 | 1991-10-31 | Akad Wissenschaften | Verfahren zur Herstellung von aktivierten Carbonsäureestern |
| JPS6461461A (en) * | 1987-09-01 | 1989-03-08 | Otsuka Pharma Co Ltd | Benzohetero ring derivative |
-
1998
- 1998-08-24 IL IL13429198A patent/IL134291A0/xx unknown
- 1998-08-24 AU AU91173/98A patent/AU753800B2/en not_active Ceased
- 1998-08-24 WO PCT/US1998/017513 patent/WO1999010347A1/en not_active Application Discontinuation
- 1998-08-24 KR KR1020007001948A patent/KR20010023313A/ko not_active Withdrawn
- 1998-08-24 JP JP2000507675A patent/JP2001514181A/ja active Pending
- 1998-08-24 NZ NZ502548A patent/NZ502548A/en unknown
- 1998-08-24 SK SK216-2000A patent/SK2162000A3/sk unknown
- 1998-08-24 PL PL98338783A patent/PL338783A1/xx unknown
- 1998-08-24 HU HU0003258A patent/HUP0003258A3/hu unknown
- 1998-08-24 YU YU10500A patent/YU10500A/sh unknown
- 1998-08-24 EP EP98943352A patent/EP1007526A1/en not_active Withdrawn
- 1998-08-24 SI SI9820055A patent/SI20270A/sl unknown
- 1998-08-24 BR BR9811362-3A patent/BR9811362A/pt not_active Application Discontinuation
- 1998-08-24 CN CN98808578A patent/CN1268136A/zh active Pending
- 1998-08-24 CA CA002301599A patent/CA2301599C/en not_active Expired - Fee Related
- 1998-09-29 EG EG118098A patent/EG21717A/xx active
- 1998-10-23 TW TW87117597A patent/TW574221B/zh active
- 1998-11-13 PE PE1998001100A patent/PE130999A1/es not_active Application Discontinuation
-
2000
- 2000-02-01 AP APAP/P/2000/001742A patent/AP2000001742A0/en unknown
- 2000-02-18 NO NO20000822A patent/NO20000822L/no not_active Application Discontinuation
- 2000-02-18 OA OA1200000044A patent/OA11293A/en unknown
- 2000-02-22 IS IS5382A patent/IS5382A/is unknown
- 2000-02-25 BG BG104192A patent/BG104192A/xx unknown
- 2000-03-16 LV LVP-00-29A patent/LV12539B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2001514181A (ja) | 2001-09-11 |
| OA11293A (en) | 2002-11-19 |
| PL338783A1 (en) | 2000-11-20 |
| LV12539A (en) | 2000-10-20 |
| BR9811362A (pt) | 2000-08-22 |
| CA2301599C (en) | 2003-03-25 |
| EP1007526A1 (en) | 2000-06-14 |
| AU9117398A (en) | 1999-03-16 |
| SI20270A (sl) | 2000-12-31 |
| LV12539B (en) | 2001-01-20 |
| AP2000001742A0 (en) | 2000-02-24 |
| NZ502548A (en) | 2002-06-28 |
| PE130999A1 (es) | 1999-12-16 |
| EG21717A (en) | 2002-02-27 |
| HUP0003258A2 (en) | 2001-03-28 |
| WO1999010347A1 (en) | 1999-03-04 |
| BG104192A (en) | 2001-05-31 |
| TW574221B (en) | 2004-02-01 |
| NO20000822L (no) | 2000-04-13 |
| KR20010023313A (ko) | 2001-03-26 |
| IS5382A (is) | 2000-02-22 |
| CN1268136A (zh) | 2000-09-27 |
| NO20000822D0 (no) | 2000-02-18 |
| AU753800B2 (en) | 2002-10-31 |
| CA2301599A1 (en) | 1999-03-04 |
| IL134291A0 (en) | 2001-04-30 |
| YU10500A (sh) | 2002-10-18 |
| HUP0003258A3 (en) | 2001-05-28 |
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