TW213462B - - Google Patents
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- TW213462B TW213462B TW081102762A TW81102762A TW213462B TW 213462 B TW213462 B TW 213462B TW 081102762 A TW081102762 A TW 081102762A TW 81102762 A TW81102762 A TW 81102762A TW 213462 B TW213462 B TW 213462B
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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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- 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
- 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
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (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)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Saccharide Compounds (AREA)
- Steroid Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Description
213462 A7 B7 C7 D7 經濟部中央標準局員工消費合作社印製 六、申請專利範圍 Z 代表一個具有化學式NR7RS之基，其中， 1^及1^分別代表氫、c2-6烯基、c3-e環烷基、金剛烷 基或苯基烷基 該基後來可能搞有一値或更多 値取代物，該等取代物傺選自：由鹵素、羥基、烷 基、烷氣基、胺基及硝基所組成之族群；（C：L-4烷 基）-胺基-(C：L-6烷基 -二-《Ci—烷基卜胺基-(Cpe 烷基）或Ci-6烷基，該基後來可能被下列之基取代：羥 基、胺基、羧基、嗎啉羰基、[4-<2-羥基-乙基 >-六氫毗 阱-卜基]-鑛基、（C^-4烷氯基）-羰基或5-或6-節飽和或 非飽和雜環基（該雜環基含有一値或更多値氮及/ 或氣原子，而且可能與一苯環産生縮合作用；或 R7及^3共同形成一値具有化學式<CH2b-W-(CH2^,其中 ,j及k分別代表1、2或3, W代表氣或CH2或CHOH基 或具有化學式之基，其中，代表氫、烷 氣基羰基或烷基，該基後來可能攜有一種取代物， 該等取代物傺選自：由羥基或苯基所組成之族群； 或具有化學式SR9之基，其中， R"代表被烷氯基）_羰基取代之烷基， 但若Q代表氫或具有化學式S(0>pR3之基時，R1及R2則不得 為氫或院基。 2. 如申請專利範圍第1項之嘧啶衍生物，其中，Q代表 一個6-節雜環基，該雜環基含有一個氮原子及/或一個（ 或更多個）氣原子或一値烷基卜硫基，Ri及R2分別代表 氫或直鏈型或支鏈型C：L-4烷基，或共同形成一個（_CH2>4基， (請先閲讀背面之注意事項再場寫本頁) •丨裝· 訂· 本紙張尺度遑用中國國家樣準（CNS>甲4规格（210 X 297公釐> 213462 A7 B7 C7 _____ D7 經濟部中央標準局R工消費合作社印製 六、申請專利範園z代表一個具有化學式NR7R8之基，其中，R7及Rs分別 代表直鏈型或支鍵型烷基，該基可能攥有一値含有氮原子 及/或氣原子之6-節雜環基。 3·如申請專利範圍第1項之哺啶衍生物，2-(甲基硫）-5 -{N-(3-嗎啉丙基）}-胺基-6,7,8,9-四氫-1,2,4-三唑[5,1 -互]DI唑啉， 5-(二乙胺基）-7-甲基-2-嗎啉·1,2,4-三唑[1,5-!]-嘧啶， 2 - (1-甲基乙基硫卜5-{Ν-(3-嗎啉丙基））-胺基-6, 7,8,9-四氫-1,2,4-三唑[5,1-互]暗唑啉， 2-(乙基硫）-5-(N-(2-q|啉乙基）卜胺基-6,7,8,9-四氫-1, 2,4-三唑[1,5-上]-¾唑琳， 2-(甲基硫）-5-(1<-(2-嗎啉乙基）}-胺基-6,7,8,9,10,11，12 ,13,14 ,15-十氫一環十二2,4-三唑[1,5-立卜嘧啶 及其可供藥用之盏。 4. 一種製備具有如申請專利範圍第1項所述之嘧啶衍生 物之方法，其僳使具有化學通式（I)之三唑衍生物與具有 化學通式（M)之胺或硫醚反應，以製備該嘧啶衍生物。
其中，Q, Ri及R2代表之意義如申請專利範圍第1項所述，L 代表一個脱離基《以鹵素、〇-三烷基矽烷基、〇-院基磺醛
本紙張尺度適用中國國家標準（CNS)甲4规格（210 X 297么D (請先閲讀背面之注意事項再填寫本頁) 丨裝. 訂· i線」 213462 A7 B7 C7 _______ D7 經濟部中央標準局8工消費合作社印製 六、申請專利範園 基或〇-芳基磺醛基較佳）， H-Z (I ) 其中，Z代表之意義如申請專利範圍第1項所述， 以及必要時，包括：將該嘧啶衍生物變成其可供藥用之酸 -加成鹽、自其酸-加成鹽釋出具有化學式（I)之鹼基、或 將該嘧啶衍生物之鹼基之酸-加成鹽變成另一酸-加成鹽等 方法。 5. 如申請專利範圍第4項之方法，其中，化學反應係在 有超量胺（具有化學通式U),其中，Z代表具有化學式 NR7Re之基，R7及Re代表之意義通式⑴對R7及…的定義） 之情況下進行。 6· 如申請專利範圍第4項之方法，其中，具有化學通式 U)(其中，L代表鹵素、0-烷基磺醯基或〇-芳基磺醛基， 餘均與通式（I)所定義者相同）之化合物之反應，係在有一 驗性酸-結合劑存在之情況下，在一質子性、極性非質子性 或非極性非質子性溶劑内進行。 7· 如申請專利範圍第6項之方法，其中，所用質子性溶 劑是：脂肪醇或二元醇，極性非質子性溶劑是：乙腈、二 甲基甲醛胺或四氫呋喃，非極性非質子性溶劑是：苯、或 其同条物，1,2-二氛乙烷、氛苯或氯仿。 8· 如申請專利範圍第6項之方法，其中，使用第三级鹼 (以三乙基胺較佳）作為酸-結合劑。 -67 - (請先閲讀背面之注意事項再填寫本頁) 本紙張尺度適用中國國家標準（CNS)甲4規格（210 X 297公釐> 213462 A7 B7 C7 _______ D7 六、申請專利範圍 9·如申請專利範圍第4項之方法，其中，具有化學通式 U)(其中，L代表0-三烷基矽烷基，餘均與通式（I)所定 義者相同）之化合物之反應，像在有一）之化合物之反應， 偽在一極性非質子性或非極性非質子性溶劑内進行。 10·如申請專利範圍第9項之方法，其中，使用乙腈、二 甲基甲醯胺或四氫呋喃作為極性非質子性溶劑，及苯或其 同条物1,2-二氣乙烷、氯仿或六甲基二矽氮烷作為非極性 非質子性溶劑。 11. 如申請專利範圍第4項之方法，其中，具有化學通式 (E ) (L代表0-三烷基矽烷基，餘均與通式（I)所定義者相 同）之化合物（在原處製得）與具有化學通式（1)(其中，Ζ 之定義與通式（I)所定義之Ζ相同）之胺或硫醚反應。 12. 如申請專利範圍第4、5、6、7、8、9、10或11項之方 法，其中，化學反應係在介於室溫至所用溶劑或超量使用 、具有化學通式（m )(其中，Ζ之定義與通式（I)所定義之 Z相同）之胺之沸點間之溫度下進行。 13. —種主要用於增強肌肉收縮力及抗绞痛之醫藥組合物 ，其傺包括至少如申諳專利範圍第1項之嘧啶衍生物作為 有效成分或其與適當惰性固體或液體藥物載體摻和可供藥 用之鹽。 (請先閲讀背面之注意事項再璜寫本頁) 丨裝· 訂· .線」
經濟部中央標準局R工消費合作社印K -6 8- 本紙張又度適用中國國家標準（CNS)甲4规格（210 X 297公釐）
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU91587A HU208693B (en) | 1991-02-22 | 1991-02-22 | Process for producing 1,2,4-triazolo (1,5-a) pyrimidinis derivatives and their carbicycli-tetrahydro-thiofurane-tetrahydrothiopyrane-, or tetrahydropyridine- condensated derivatives or medical preparatives containing them |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW213462B true TW213462B (zh) | 1993-09-21 |
Family
ID=10950293
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW081102762A TW213462B (zh) | 1991-02-22 | 1992-04-09 |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP0500136B1 (zh) |
| JP (1) | JPH05148267A (zh) |
| KR (1) | KR920016456A (zh) |
| CN (1) | CN1033585C (zh) |
| AT (1) | ATE138067T1 (zh) |
| AU (1) | AU642073B2 (zh) |
| CA (1) | CA2061629A1 (zh) |
| CS (1) | CS51592A3 (zh) |
| DE (1) | DE69210647T2 (zh) |
| ES (1) | ES2089258T3 (zh) |
| FI (1) | FI100401B (zh) |
| GB (1) | GB2254611B (zh) |
| HU (1) | HU208693B (zh) |
| IL (1) | IL101033A (zh) |
| PL (1) | PL170050B1 (zh) |
| RU (1) | RU2097382C1 (zh) |
| TW (1) | TW213462B (zh) |
| YU (1) | YU17592A (zh) |
| ZA (1) | ZA921269B (zh) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW224044B (zh) * | 1991-12-30 | 1994-05-21 | Shell Internat Res Schappej B V | |
| IL108731A (en) * | 1993-03-04 | 1997-03-18 | Shell Int Research | 6, N-DISUBSTITUTED-£1, 2, 4| TRIAZOLO-£1, 5-a| PYRIMIDINE- 7-AMINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS FUNGICIDES |
| US5571813A (en) * | 1993-06-10 | 1996-11-05 | Beiersdorf-Lilly Gmbh | Fused pyrimidine compounds and their use as pharmaceuticals |
| EP0628559B1 (en) * | 1993-06-10 | 2002-04-03 | Beiersdorf-Lilly GmbH | Pyrimidine compounds and their use as pharmaceuticals |
| US8508469B1 (en) | 1995-12-01 | 2013-08-13 | Immersion Corporation | Networked applications including haptic feedback |
| WO2005037837A1 (ja) * | 2003-10-17 | 2005-04-28 | Nippon Kayaku Kabushiki Kaisha | 置換２−アミノ−[１，２，４]トリアゾロ[１，５−a]ピリミジン誘導体及びその用途 |
| RU2378278C2 (ru) * | 2008-01-24 | 2010-01-10 | Андрей Александрович Иващенко | ЗАМЕЩЕННЫЕ 3-СУЛЬФОНИЛ-[1,2,3]ТРИАЗОЛО[1,5-a]ПИРИМИДИНЫ-АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6 РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ |
| US9238653B2 (en) * | 2009-09-29 | 2016-01-19 | Board Of Regents, The University Of Texas System | Antimalarial agents that are inhibitors of dihydroorotate dehydrogenase |
| DK3597649T3 (da) * | 2014-04-23 | 2022-01-10 | Dart Neuroscience Llc | Sammensætninger indeholdende substituerede [1,2,4]triazolo[1,5-a]pyrimidin-7-yl-forbindelser som pde2-inhibitorer |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1792811C2 (de) * | 1966-10-03 | 1982-12-30 | VEB Deutsches Hydrierwerk Rodleben, DDR 4530 Roßlau | "Arzneimittel mit koronargefäßerweiternder Wirkung" |
| DE2327133A1 (de) * | 1972-06-07 | 1974-01-03 | Icn Pharmaceuticals | 2-subst.-thio-s-triazolo eckige klammer auf 1,5a eckige klammer zu -pyrimidine |
| US4497814A (en) * | 1982-08-16 | 1985-02-05 | Schering Corporation | 2-(Pyridinyl)-1,2,4-triazolo[1,5-a]pyrimidines and derivatives useful in increasing cardiac contractility |
| DD280111A1 (de) * | 1986-01-09 | 1990-06-27 | Hydrierwerk Rodleben Veb | Verfahren zur herstellung neuer triazolo-pyrimidine |
-
1991
- 1991-02-22 HU HU91587A patent/HU208693B/hu not_active IP Right Cessation
-
1992
- 1992-02-21 PL PL92293564A patent/PL170050B1/pl unknown
- 1992-02-21 CA CA002061629A patent/CA2061629A1/en not_active Abandoned
- 1992-02-21 GB GB9203736A patent/GB2254611B/en not_active Expired - Fee Related
- 1992-02-21 FI FI920776A patent/FI100401B/fi active
- 1992-02-21 JP JP4070092A patent/JPH05148267A/ja active Pending
- 1992-02-21 IL IL10103392A patent/IL101033A/en not_active IP Right Cessation
- 1992-02-21 YU YU17592A patent/YU17592A/sh unknown
- 1992-02-21 KR KR1019920002616A patent/KR920016456A/ko active IP Right Grant
- 1992-02-21 RU SU925011062A patent/RU2097382C1/ru active
- 1992-02-21 ZA ZA921269A patent/ZA921269B/xx unknown
- 1992-02-21 AU AU11175/92A patent/AU642073B2/en not_active Ceased
- 1992-02-21 CS CS92515A patent/CS51592A3/cs unknown
- 1992-02-22 CN CN92101158A patent/CN1033585C/zh not_active Expired - Fee Related
- 1992-02-24 DE DE69210647T patent/DE69210647T2/de not_active Expired - Fee Related
- 1992-02-24 EP EP92102981A patent/EP0500136B1/en not_active Expired - Lifetime
- 1992-02-24 ES ES92102981T patent/ES2089258T3/es not_active Expired - Lifetime
- 1992-02-24 AT AT92102981T patent/ATE138067T1/de not_active IP Right Cessation
- 1992-04-09 TW TW081102762A patent/TW213462B/zh active
Also Published As
| Publication number | Publication date |
|---|---|
| GB9203736D0 (en) | 1992-04-08 |
| GB2254611A (en) | 1992-10-14 |
| DE69210647T2 (de) | 1997-01-09 |
| EP0500136B1 (en) | 1996-05-15 |
| HU910587D0 (en) | 1991-09-30 |
| IL101033A (en) | 1996-07-23 |
| ATE138067T1 (de) | 1996-06-15 |
| JPH05148267A (ja) | 1993-06-15 |
| FI920776A0 (fi) | 1992-02-21 |
| EP0500136A1 (en) | 1992-08-26 |
| HUT61308A (en) | 1992-12-28 |
| AU1117592A (en) | 1992-08-27 |
| IL101033A0 (en) | 1992-11-15 |
| FI100401B (fi) | 1997-11-28 |
| CN1064277A (zh) | 1992-09-09 |
| GB2254611B (en) | 1995-04-26 |
| CN1033585C (zh) | 1996-12-18 |
| AU642073B2 (en) | 1993-10-07 |
| DE69210647D1 (de) | 1996-06-20 |
| CS51592A3 (en) | 1992-10-14 |
| PL170050B1 (pl) | 1996-10-31 |
| YU17592A (sh) | 1995-03-27 |
| RU2097382C1 (ru) | 1997-11-27 |
| ES2089258T3 (es) | 1996-10-01 |
| CA2061629A1 (en) | 1992-08-23 |
| PL293564A1 (en) | 1992-11-02 |
| ZA921269B (en) | 1993-08-26 |
| FI920776A (fi) | 1992-08-23 |
| HU208693B (en) | 1993-12-28 |
| KR920016456A (ko) | 1992-09-24 |
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