BR9809652A - Derivados de quinolina-4-carboxamida como antagonistas de receptor nk-2 e nk-3 - Google Patents
Derivados de quinolina-4-carboxamida como antagonistas de receptor nk-2 e nk-3Info
- Publication number
- BR9809652A BR9809652A BR9809652-4A BR9809652A BR9809652A BR 9809652 A BR9809652 A BR 9809652A BR 9809652 A BR9809652 A BR 9809652A BR 9809652 A BR9809652 A BR 9809652A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- optionally substituted
- group
- aryl
- cycloalkyl
- Prior art date
Links
- 108010040722 Neurokinin-2 Receptors Proteins 0.000 title abstract 2
- 108010040716 Neurokinin-3 Receptors Proteins 0.000 title abstract 2
- 102100029409 Neuromedin-K receptor Human genes 0.000 title abstract 2
- 102100037342 Substance-K receptor Human genes 0.000 title abstract 2
- 239000002464 receptor antagonist Substances 0.000 title abstract 2
- 229940044551 receptor antagonist Drugs 0.000 title abstract 2
- LEWDKQKVAFOMPI-UHFFFAOYSA-N quinoline-4-carboxamide Chemical class C1=CC=C2C(C(=O)N)=CC=NC2=C1 LEWDKQKVAFOMPI-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- -1 alkyl halogen Chemical class 0.000 abstract 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 125000004945 acylaminoalkyl group Chemical group 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000005518 carboxamido group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 abstract 1
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000005544 phthalimido group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
- C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
- C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
- C07D251/40—Nitrogen atoms
- C07D251/48—Two nitrogen atoms
- C07D251/52—Two nitrogen atoms with an oxygen or sulfur atom attached to the third ring carbon atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
"DERIVADOS DE QUINOLINA-4-CARBOXAMIDA COMO ANTAGONISTAS DE RECEPTOR NK-2 E NK-3". Composto, ou um solvato ou um sal do mesmo, de fórmula (I): em que, Ar é um grupo arila ou um cicloalquidienila C~ 5-7~ opcionalmente substituído, ou um grupo cicloalquila C~ 5-7~ ou um grupo heterocíclico aromático com anel único ou fundido opcionalmente substituído; R é alquila C~ 1-6~, cicloalquila C~ 3-7~, cicloalquilalquila C~ 3-7~, fenila ou fenil-alquila C~ 1-6~ opcionalmente substituída, um anel heteroaromático com cinco membros opcionalmente substituído compreendendo até quatro heteroátomos selecionados dentre O e N, hidroxi alquila C~ 1-6~, amino alquila C~ 1-6~, alquilaminoalquila C~ 1-6~, di-alquilaminoalquila C~ 1-6~, acilaminoalquila C~ 1-6~, alcoxialquila C~ 1-6~, alquilcarbonila C~ 1-6~, carboxi, alcoxicarbonila C~ 1-6~, alcoxicarbonila C~ 1-6~ alquila C~ 1-6~, aminocarbonila, alquilaminocarbonila C~ 1-6~, dialquilaminocarbonila C~ 1-6~, halogênio alquila C~ 1-6~; ou R é um grupo -(CH~ 2~)~ p~- em que p é 2 ou 3, cujo grupo forma um anel com um átomo de carbono de Ar; R~ 1~ representa hidrogênio ou até quatro substituintes opcionais selecionados dentre a lista consistindo de: alquila C~ 1-6~, alquenila C~ 1-6~, arila, alcoxi C~ 1-6~, hidroxi, halogênio, nitro, ciano, carboxi, carboxamido, sulfonamido, alcoxicarbonila C~ 1-6~, trifluorometila, aciloxi, ftalimido, amino ou mono- e di-alquilamino C~ 1-6~; R~ 2~ representa uma porção - (CH~ 2~)~ n~-NY~ 1~Y~ 2~ em que n é um número inteiro na faixa de 1 a 9, Y~ 1~ e Y~ 2~ são independentemente selecionados dentre hidrogênio; alquila C~ 1-6~; alquila C~ 1-6~ substituída com hidroxi, alquilamino C~ 1-6~ ou bis (alquil C~ 1-6~) amino; alquenila C~ 1-6~; arila ou aril-alquila C~ 1-6~ ou Y~ 1~ e Y~ 2~ juntos com o átomo de nitrogênio, em que eles são fixados, representam um grupo heterocíclico com anel único ou fundido N-ligado opcionalmente substituído; R~ 3~ é alquila C~ 1-6~, cicloalquila C~ 3-7~, cicloalquilquila C~ 4-7~ ramificado ou linear, arila opcionalmente substituída, ou um grupo heterocíclico aromático com anel único ou fundido opcionalmente substituído; e R~ 4~ representa hidrogênio ou alquila C~ 1-6~; uma composição farmacêutica compreendendo este composto, processo para preparar este composto e o uso deste composto em remédios.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9710750.2A GB9710750D0 (en) | 1997-05-23 | 1997-05-23 | Novel compounds |
| IT002354 IT1295358B1 (it) | 1997-10-17 | 1997-10-17 | Derivati chinolinici procedimento per la loro preparazione e uso come antagonisti del recettore nk3 |
| ITMI972775 IT1296976B1 (it) | 1997-12-16 | 1997-12-16 | Derivati chinolinici procedimento per la loro preparazione e uso come antagonisti del recettore nk3 |
| PCT/EP1998/003014 WO1998052942A1 (en) | 1997-05-23 | 1998-05-18 | Quinoline-4-carboxamide derivatives as nk-2 and nk-3 receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9809652A true BR9809652A (pt) | 2001-09-11 |
Family
ID=27268859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9809652-4A BR9809652A (pt) | 1997-05-23 | 1998-05-18 | Derivados de quinolina-4-carboxamida como antagonistas de receptor nk-2 e nk-3 |
Country Status (26)
| Country | Link |
|---|---|
| EP (1) | EP0983262B1 (pt) |
| JP (1) | JP2002500645A (pt) |
| CN (1) | CN1264378A (pt) |
| AP (1) | AP9901695A0 (pt) |
| AR (1) | AR012732A1 (pt) |
| AT (1) | ATE244711T1 (pt) |
| AU (1) | AU8209898A (pt) |
| BG (1) | BG104009A (pt) |
| BR (1) | BR9809652A (pt) |
| CA (1) | CA2291111A1 (pt) |
| CO (1) | CO4950515A1 (pt) |
| DE (1) | DE69816290T2 (pt) |
| DZ (1) | DZ2498A1 (pt) |
| EA (1) | EA199901062A1 (pt) |
| ES (1) | ES2201509T3 (pt) |
| HU (1) | HUP0002300A3 (pt) |
| ID (1) | ID22876A (pt) |
| IL (1) | IL133036A0 (pt) |
| MA (1) | MA26501A1 (pt) |
| NO (1) | NO995711L (pt) |
| OA (1) | OA11515A (pt) |
| PE (1) | PE75199A1 (pt) |
| PL (1) | PL336942A1 (pt) |
| SK (1) | SK159299A3 (pt) |
| TR (1) | TR199902883T2 (pt) |
| WO (1) | WO1998052942A1 (pt) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU768708B2 (en) * | 1998-11-20 | 2004-01-08 | Smithkline Beecham Laboratoires Pharmaceutiques | Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists |
| GB9825554D0 (en) * | 1998-11-20 | 1999-01-13 | Smithkline Beecham Spa | Novel Compounds |
| US6780875B2 (en) * | 1998-11-20 | 2004-08-24 | Smithkline Beecham S.P.A. | Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists |
| JP2002540203A (ja) | 1999-03-29 | 2002-11-26 | ニューロゲン コーポレイション | Ｎｋ−３および／またはｇａｂａ（ａ）受容体リガンドとしての４−置換キノリン誘導体 |
| WO2000064877A1 (en) | 1999-04-26 | 2000-11-02 | Neurogen Corporation | 2-aminoquinolinecarboxamides: neurokinin receptor ligands |
| AU2001276556A1 (en) * | 2000-08-11 | 2002-02-25 | Smithkline Beecham P.L.C. | Novel pharmaceutical use of quinnoline derivatives |
| US20040082589A1 (en) * | 2000-11-13 | 2004-04-29 | Carlo Farina | Quinoline derivatives as nk-3 and nk-2 antagonists |
| GB0028964D0 (en) * | 2000-11-28 | 2001-01-10 | Smithkline Beecham Spa | Novel compounds |
| WO2002044165A1 (en) * | 2000-11-28 | 2002-06-06 | Glaxosmithkline Spa | Quinoline derivatives as nk-3 antagonists |
| US6540733B2 (en) | 2000-12-29 | 2003-04-01 | Corazon Technologies, Inc. | Proton generating catheters and methods for their use in enhancing fluid flow through a vascular site occupied by a calcified vascular occlusion |
| GB0109122D0 (en) * | 2001-04-11 | 2001-05-30 | Smithkline Beecham Spa | Novel compounds |
| ES2254688T3 (es) * | 2001-04-11 | 2006-06-16 | Glaxosmithkline S.P.A. | Derivados de quinolina-4-carboxamida como antagonistas de los receptores nk-3 y nk-2. |
| MY134211A (en) * | 2001-05-18 | 2007-11-30 | Smithkline Beecham Corp | Novel use |
| GB0425075D0 (en) * | 2004-11-12 | 2004-12-15 | Smithkline Beecham Corp | Novel compounds |
| GB0425076D0 (en) * | 2004-11-12 | 2004-12-15 | Smithkline Beecham Corp | Novel compounds |
| GB0425077D0 (en) * | 2004-11-12 | 2004-12-15 | Smithkline Beecham Corp | Novel compounds |
| US20080200500A1 (en) * | 2005-06-03 | 2008-08-21 | Astrazeneca Ab | Quinoline Derivatives as Nk3 Antagonists |
| GB0515580D0 (en) | 2005-07-29 | 2005-09-07 | Merck Sharp & Dohme | Therapeutic compounds |
| AR057130A1 (es) | 2005-09-21 | 2007-11-14 | Astrazeneca Ab | Quinolinas de alquilsulfoxido y una composicion farmaceutica |
| DE202007017299U1 (de) * | 2007-12-12 | 2009-04-23 | Drebo Werkzeugfabrik Gmbh | Bohrer |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK0804419T3 (da) * | 1994-05-27 | 2003-11-24 | Glaxosmithkline Spa | Quinolinderivater som tachykinin NK 3-receptor-antagonister |
| 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. |
-
1998
- 1998-05-18 EP EP98932069A patent/EP0983262B1/en not_active Expired - Lifetime
- 1998-05-18 CN CN98807356A patent/CN1264378A/zh active Pending
- 1998-05-18 HU HU0002300A patent/HUP0002300A3/hu unknown
- 1998-05-18 AT AT98932069T patent/ATE244711T1/de not_active IP Right Cessation
- 1998-05-18 WO PCT/EP1998/003014 patent/WO1998052942A1/en not_active Ceased
- 1998-05-18 BR BR9809652-4A patent/BR9809652A/pt not_active IP Right Cessation
- 1998-05-18 AP APAP/P/1999/001695A patent/AP9901695A0/en unknown
- 1998-05-18 IL IL13303698A patent/IL133036A0/xx unknown
- 1998-05-18 ID IDW991432A patent/ID22876A/id unknown
- 1998-05-18 DE DE69816290T patent/DE69816290T2/de not_active Expired - Fee Related
- 1998-05-18 SK SK1592-99A patent/SK159299A3/sk unknown
- 1998-05-18 ES ES98932069T patent/ES2201509T3/es not_active Expired - Lifetime
- 1998-05-18 CA CA002291111A patent/CA2291111A1/en not_active Abandoned
- 1998-05-18 PL PL98336942A patent/PL336942A1/xx unknown
- 1998-05-18 EA EA199901062A patent/EA199901062A1/ru unknown
- 1998-05-18 JP JP54996798A patent/JP2002500645A/ja not_active Ceased
- 1998-05-18 TR TR1999/02883T patent/TR199902883T2/xx unknown
- 1998-05-18 AU AU82098/98A patent/AU8209898A/en not_active Abandoned
- 1998-05-19 DZ DZ980108A patent/DZ2498A1/xx active
- 1998-05-20 PE PE1998000398A patent/PE75199A1/es not_active Application Discontinuation
- 1998-05-21 AR ARP980102363A patent/AR012732A1/es not_active Application Discontinuation
- 1998-05-21 MA MA25086A patent/MA26501A1/fr unknown
- 1998-05-22 CO CO98029024A patent/CO4950515A1/es unknown
-
1999
- 1999-11-22 NO NO995711A patent/NO995711L/no not_active Application Discontinuation
- 1999-11-23 OA OA9900253A patent/OA11515A/en unknown
- 1999-12-14 BG BG104009A patent/BG104009A/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO995711D0 (no) | 1999-11-22 |
| AU8209898A (en) | 1998-12-11 |
| AR012732A1 (es) | 2000-11-08 |
| CO4950515A1 (es) | 2000-09-01 |
| NO995711L (no) | 2000-01-19 |
| EP0983262B1 (en) | 2003-07-09 |
| DZ2498A1 (fr) | 2003-01-25 |
| EP0983262A1 (en) | 2000-03-08 |
| CA2291111A1 (en) | 1998-11-26 |
| CN1264378A (zh) | 2000-08-23 |
| DE69816290D1 (de) | 2003-08-14 |
| JP2002500645A (ja) | 2002-01-08 |
| HUP0002300A2 (hu) | 2001-06-28 |
| SK159299A3 (en) | 2000-06-12 |
| HUP0002300A3 (en) | 2002-01-28 |
| BG104009A (en) | 2000-07-31 |
| WO1998052942A1 (en) | 1998-11-26 |
| ES2201509T3 (es) | 2004-03-16 |
| ID22876A (id) | 1999-12-16 |
| IL133036A0 (en) | 2001-03-19 |
| TR199902883T2 (xx) | 2000-05-22 |
| AP9901695A0 (en) | 1999-12-31 |
| PE75199A1 (es) | 1999-10-22 |
| ATE244711T1 (de) | 2003-07-15 |
| OA11515A (en) | 2004-02-04 |
| PL336942A1 (en) | 2000-07-17 |
| MA26501A1 (fr) | 2004-12-20 |
| EA199901062A1 (ru) | 2000-08-28 |
| DE69816290T2 (de) | 2004-05-27 |
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