BR9916366A - Derivados de 6-azauracila, inibidores de il-5 - Google Patents
Derivados de 6-azauracila, inibidores de il-5Info
- Publication number
- BR9916366A BR9916366A BR9916366-7A BR9916366A BR9916366A BR 9916366 A BR9916366 A BR 9916366A BR 9916366 A BR9916366 A BR 9916366A BR 9916366 A BR9916366 A BR 9916366A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- optionally substituted
- alkylc
- het3
- aryl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- SSPYSWLZOPCOLO-UHFFFAOYSA-N 6-azauracil Chemical class O=C1C=NNC(=O)N1 SSPYSWLZOPCOLO-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- -1 Het ^ 5 ^ Chemical group 0.000 abstract 1
- 108010002616 Interleukin-5 Proteins 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
- C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
- C07D253/06—1,2,4-Triazines
- C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
- C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members 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
- C07D253/075—Two hetero atoms, in positions 3 and 5
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- 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
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
Patente de Invenção: <B>"DERIVADOS DE 6-AZAURACILA, INIBIDORES DE IL-5"<D>. A presente invenção refere-se a compostos de fórmula (I): um N-óxido, um sal de adição farmaceuticamente aceitável, uma amina quaternária ou uma forma estereoquimicamente isomérica do mesmo, em que: p é 0 a 4; q é 0 a 5; X é O, S, NR^ 3^ ou uma ligação direta; ou -X-R² é CN; R¹ é H, OH, halo, NH~ 2~, mono- ou di(C~ 1-4~ alquil)NH~ 2~, C~ 1-6~ alquila, C~ 1-6~ alquilO, C~ 3-7~ cicloalquila, arila, arilC~ 1-6~alquila, NH~ 2~C~ 1-4~ alquila, mono- ou di(C~ 1-4~ alquil) NH~ 2~C~ 1-4~alquila ou mono- ou di(C~ 1-4~ alquil)NH~ 2~C~ 1-4~ alquil NH~ 2~; R² é arila, Het¹, C~ 3-7~ cicloalquila opcionalmente substituída, C~ 1-6~ alquila opcionalmente substituída; R é H ou C~ 1-4~ alquila; R^ 4^ e R^ 5^ são -C(=O)-Z-R^ 14^, C~ 1-6~ alquila, halo, polihalo C~ 1-6~ alquila, OH, mercapto, C~ 1-6~ alquilO, C~ 1-6~ alquiltio, C~ 1-6~ alquilC(=O)O, arila, ciano, nitro, Het³, R^ 6^, NR^ 7^R^ 8^ ou C~ 1-4~ alquila substituída por -C (=O)-Z-R^ 14^, Het³, R^ 6^ ou NR^ 7^R^ 8^; Z é O, S, NH, -CH~ 2~-O- ou -CH~ 2~-S-; R^ 14^ é H, C~ 1-20~ acila, C~ 1-20~ alquila opcionalmente substituída, C~ 3-20~ alquenila opcionalmente substituída, C~ 3-20~ alquinila, C~ 3-7~cicloalquila, polihaloC~ 1-20~alquila, Het^ 5^, fenila ou R^ 14^ é um radical contendo oxigênio; arila é uma fenila opcionalmente substituída; Het¹, Het², Het³ e Het^ 5^ são heterociclos opcionalmente substituídos; Het^ 4^ é um heterociclo monocíclico; desde que, entretanto, R~ 2~ seja diferente de NH~ 2~C(=O), C~ 1-6~alquilOC(=O) C~ 1-6~alquila; e R^ 11^ seja diferente de COOH C~ 1-4~alquilOC(=O), NH~ 2~C(=C), C~ 1-4~ alquilNH~ 2~C(=O), OH C~ 1-4~alquilNH~ 2~C(=O), C~ 1-4~alquilC(=O) NH~ 2~C (-C), C~ 3-7~ cicloalquilNH~ 2~C(=O); e R^ 7^, R^ 8^, R^ 9^, R^ 10^, R^ 12^, R^ 13^, R^ 15^ e R^ 16^ sejam diferentes de C~ 1-4~ alquilC(=O)OC~ 1-4~ alquilC(=O), OH C~ 1-4~alquilC(=O); e Het³ seja diferente de um heterociclo monocíclico substituído por COOH ou C~ 1-4~alquilOC(=O); e os compostos de fórmula (I) contenham pelo menos uma porção -C(=O)-Z-R^ 14^; a processos para sua preparação e composições compreendendo os mesmos. Ela refere-se ainda ao seu uso como um medicamento.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP98204336 | 1998-12-18 | ||
| PCT/EP1999/010169 WO2000037451A1 (en) | 1998-12-18 | 1999-12-16 | Il-5 inhibiting 6-azauracil derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9916366A true BR9916366A (pt) | 2001-09-18 |
Family
ID=8234494
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9916366-7A BR9916366A (pt) | 1998-12-18 | 1999-12-16 | Derivados de 6-azauracila, inibidores de il-5 |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US6803364B1 (pt) |
| EP (1) | EP1140873B1 (pt) |
| JP (1) | JP2002533331A (pt) |
| KR (1) | KR100635721B1 (pt) |
| CN (1) | CN100343239C (pt) |
| AR (1) | AR021887A1 (pt) |
| AT (1) | ATE365723T1 (pt) |
| AU (1) | AU773780B2 (pt) |
| BG (1) | BG105602A (pt) |
| BR (1) | BR9916366A (pt) |
| CA (1) | CA2354511A1 (pt) |
| CO (1) | CO5150147A1 (pt) |
| CZ (1) | CZ20012062A3 (pt) |
| DE (1) | DE69936396T2 (pt) |
| DK (1) | DK1140873T3 (pt) |
| EA (1) | EA004806B1 (pt) |
| EE (1) | EE200100320A (pt) |
| ES (1) | ES2289835T3 (pt) |
| HK (1) | HK1042491A1 (pt) |
| HR (1) | HRP20010455A2 (pt) |
| HU (1) | HUP0104641A3 (pt) |
| ID (1) | ID28880A (pt) |
| IL (1) | IL143766A (pt) |
| MY (1) | MY125808A (pt) |
| NO (1) | NO319814B1 (pt) |
| NZ (1) | NZ512748A (pt) |
| PL (1) | PL198205B1 (pt) |
| PT (1) | PT1140873E (pt) |
| SA (1) | SA00201030B1 (pt) |
| SK (1) | SK8152001A3 (pt) |
| TR (1) | TR200101729T2 (pt) |
| TW (1) | TWI249530B (pt) |
| UA (1) | UA73107C2 (pt) |
| WO (1) | WO2000037451A1 (pt) |
| ZA (1) | ZA200104942B (pt) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8466096B2 (en) * | 2007-04-26 | 2013-06-18 | Afton Chemical Corporation | 1,3,2-dioxaphosphorinane, 2-sulfide derivatives for use as anti-wear additives in lubricant compositions |
| RU2523651C2 (ru) * | 2012-05-22 | 2014-07-20 | Государственное бюджетное образовательное учреждение высшего профессионального образования "Владивостокский государственный медицинский университет" Министерства здравоохранения и социального развития Российской Федерации (ГБОУ ВПО ВГМУ Минздравсоцразвития России) | Способ дифференцированного контроля базисного противовоспалительного лечения бронхиальной астмы у детей и подростков |
| RU2506045C1 (ru) * | 2012-09-05 | 2014-02-10 | Федеральное государственное бюджетное учреждение "Дальневосточный научный центр физиологии и патологии дыхания" Сибирского отделения РАМН | Способ прогнозирования достижения контроля бронхиальной астмы |
| CN119161311B (zh) * | 2024-11-20 | 2025-02-11 | 北京纳百生物科技有限公司 | 一种地克珠利抗原及其合成方法和应用 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2149645A1 (de) | 1970-10-07 | 1972-09-14 | Pfizer | 2-Phenyl-as-triazin-3.5-(2H,4H)-dione und die Verwendung dieser Verbindungen zur Bekaempfung der Coccidiose |
| US3912723A (en) | 1971-03-29 | 1975-10-14 | Pfizer | 2-Phenyl-as-triazine-3,5(2H,4H)diones |
| US3883528A (en) | 1974-04-19 | 1975-05-13 | Pfizer | Preparation of 2(aryl)-as-triazine-3,5(2H,4H)-dione coccidiostats |
| US4631278A (en) | 1984-08-01 | 1986-12-23 | Janssen Pharmaceutica N.V. | Anti-protozoal α-aryl-4-(4,5-dihydro-3,5-dioxo-1,2,4-triazin-2(3H)-yl)-benzeneacetonitrile derivatives, pharmaceutical compositions, and method of use therefor |
| CA1244024A (en) | 1984-08-01 | 1988-11-01 | Gustaaf M. Boeckx | .alpha.- ARYL-4-(4,5-DIHYDRO-3,5-DIOXO-1,2,4-TRIAZIN- 2(3H)-YL)BENZENEACETONITRILES |
| GB8602342D0 (en) | 1986-01-30 | 1986-03-05 | Janssen Pharmaceutica Nv | 5 6-dihydro-2-(substituted phenyl)-1 2 4-triazine-3 5(2h 4h)-diones |
| CA1331757C (en) | 1988-02-29 | 1994-08-30 | Janssen Pharmaceutica Naamloze Vennootschap | 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols |
| EP0476439A1 (de) | 1990-09-18 | 1992-03-25 | Bayer Ag | Substituierte 1,2,4-Triazindione, Verfahren zu ihrer Herstellung, Zwischenprodukte dafür und ihre Verwendung |
| DE4120138A1 (de) | 1991-06-19 | 1992-12-24 | Bayer Ag | Substituierte hexahydro-1,2,4-triazindione, verfahren zu ihrer herstellung, zwischenprodukte dafuer und ihre verwendung |
| TW263495B (pt) | 1992-12-23 | 1995-11-21 | Celltech Ltd | |
| GB9304920D0 (en) | 1993-03-10 | 1993-04-28 | Celltech Ltd | Chemical compounds |
| TW403741B (en) | 1993-10-15 | 2000-09-01 | Takeda Chemical Industries Ltd | Triazine derivative, production and use thereof |
| TW332201B (en) | 1995-04-06 | 1998-05-21 | Janssen Pharmaceutica Nv | 1,3-Dihydro-1-(phenylalkyl)-2H-imidazol-2-one derivatives |
| DE69615601T2 (de) | 1995-04-14 | 2002-07-11 | Takeda Schering-Plough Animal Health K.K., Osaka | Verfahren zur Herstellung von Triazinderivate |
| CN1128141C (zh) * | 1996-08-30 | 2003-11-19 | 武田舍林-普劳动物保健株式会社 | 1,2,4－三嗪－3,5－二酮衍生物,其制备和用途 |
| BR9811678A (pt) * | 1997-07-10 | 2000-09-19 | Janssen Pharmaceutica Nv | Derivados de 6-azauracila de inibição de il-5 |
| HRP990333A2 (en) * | 1997-07-10 | 2000-04-30 | Janssen Pharmaceutica Nv | 6-azauracil derivatives as il-5 inhibitors |
-
1999
- 1999-12-16 PL PL349526A patent/PL198205B1/pl not_active IP Right Cessation
- 1999-12-16 DK DK99965509T patent/DK1140873T3/da active
- 1999-12-16 JP JP2000589523A patent/JP2002533331A/ja not_active Withdrawn
- 1999-12-16 EP EP99965509A patent/EP1140873B1/en not_active Expired - Lifetime
- 1999-12-16 HK HK02104206.0A patent/HK1042491A1/zh unknown
- 1999-12-16 ID IDW00200101295A patent/ID28880A/id unknown
- 1999-12-16 CN CNB998146110A patent/CN100343239C/zh not_active Expired - Fee Related
- 1999-12-16 IL IL14376699A patent/IL143766A/xx not_active IP Right Cessation
- 1999-12-16 EA EA200100677A patent/EA004806B1/ru not_active IP Right Cessation
- 1999-12-16 DE DE69936396T patent/DE69936396T2/de not_active Expired - Fee Related
- 1999-12-16 HR HR20010455A patent/HRP20010455A2/hr not_active Application Discontinuation
- 1999-12-16 BR BR9916366-7A patent/BR9916366A/pt not_active Application Discontinuation
- 1999-12-16 AU AU21001/00A patent/AU773780B2/en not_active Ceased
- 1999-12-16 SK SK815-2001A patent/SK8152001A3/sk unknown
- 1999-12-16 KR KR1020017006666A patent/KR100635721B1/ko not_active Expired - Fee Related
- 1999-12-16 NZ NZ512748A patent/NZ512748A/en unknown
- 1999-12-16 US US09/868,384 patent/US6803364B1/en not_active Expired - Fee Related
- 1999-12-16 CA CA002354511A patent/CA2354511A1/en not_active Abandoned
- 1999-12-16 UA UA2001075132A patent/UA73107C2/uk unknown
- 1999-12-16 AT AT99965509T patent/ATE365723T1/de not_active IP Right Cessation
- 1999-12-16 ES ES99965509T patent/ES2289835T3/es not_active Expired - Lifetime
- 1999-12-16 EE EEP200100320A patent/EE200100320A/xx unknown
- 1999-12-16 PT PT99965509T patent/PT1140873E/pt unknown
- 1999-12-16 CZ CZ20012062A patent/CZ20012062A3/cs unknown
- 1999-12-16 TR TR2001/01729T patent/TR200101729T2/xx unknown
- 1999-12-16 HU HU0104641A patent/HUP0104641A3/hu unknown
- 1999-12-16 WO PCT/EP1999/010169 patent/WO2000037451A1/en not_active Ceased
- 1999-12-17 CO CO99079022A patent/CO5150147A1/es unknown
- 1999-12-17 MY MYPI99005536A patent/MY125808A/en unknown
- 1999-12-17 TW TW088122197A patent/TWI249530B/zh not_active IP Right Cessation
- 1999-12-17 AR ARP990106512A patent/AR021887A1/es not_active Application Discontinuation
-
2000
- 2000-03-05 SA SA00201030A patent/SA00201030B1/ar unknown
-
2001
- 2001-06-14 BG BG105602A patent/BG105602A/xx unknown
- 2001-06-15 NO NO20012987A patent/NO319814B1/no unknown
- 2001-06-15 ZA ZA200104942A patent/ZA200104942B/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B11B | Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements |