DE69939749D1 - Aromatische heterocyclen mit hiv integrase inhibierenden eigenschaften - Google Patents
Aromatische heterocyclen mit hiv integrase inhibierenden eigenschaftenInfo
- Publication number
- DE69939749D1 DE69939749D1 DE69939749T DE69939749T DE69939749D1 DE 69939749 D1 DE69939749 D1 DE 69939749D1 DE 69939749 T DE69939749 T DE 69939749T DE 69939749 T DE69939749 T DE 69939749T DE 69939749 D1 DE69939749 D1 DE 69939749D1
- Authority
- DE
- Germany
- Prior art keywords
- aromatic heterocycles
- hiv integrase
- inhibiting properties
- integrase inhibiting
- properties
- 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.)
- Expired - Lifetime
Links
Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
- C07D333/30—Hetero atoms other than halogen
- C07D333/34—Sulfur atoms
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP37127098 | 1998-12-25 | ||
JP24747999 | 1999-09-01 | ||
PCT/JP1999/007101 WO2000039086A1 (fr) | 1998-12-25 | 1999-12-17 | Composes heterocycliques aromatiques possedant des activites inhibitrices de l'integrase du vih |
Publications (1)
Publication Number | Publication Date |
---|---|
DE69939749D1 true DE69939749D1 (de) | 2008-11-27 |
Family
ID=26538287
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE69939749T Expired - Lifetime DE69939749D1 (de) | 1998-12-25 | 1999-12-17 | Aromatische heterocyclen mit hiv integrase inhibierenden eigenschaften |
Country Status (22)
Country | Link |
---|---|
US (3) | US6620841B1 (de) |
EP (1) | EP1142872B1 (de) |
JP (1) | JP3929244B2 (de) |
KR (1) | KR20010089708A (de) |
CN (1) | CN1178913C (de) |
AP (1) | AP2001002169A0 (de) |
AT (1) | ATE411286T1 (de) |
AU (1) | AU763040B2 (de) |
BR (1) | BR9916583A (de) |
CA (1) | CA2353961A1 (de) |
CZ (1) | CZ20012160A3 (de) |
DE (1) | DE69939749D1 (de) |
HK (1) | HK1042701A1 (de) |
HU (1) | HUP0201472A3 (de) |
ID (1) | ID29027A (de) |
IL (1) | IL143958A0 (de) |
NO (1) | NO20013179L (de) |
NZ (1) | NZ512184A (de) |
PL (1) | PL348596A1 (de) |
RU (1) | RU2225860C2 (de) |
TR (1) | TR200101886T2 (de) |
WO (1) | WO2000039086A1 (de) |
Families Citing this family (47)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6262055B1 (en) | 1998-06-03 | 2001-07-17 | Merck & Co., Inc. | HIV integrase inhibitors |
US6306891B1 (en) | 1998-06-03 | 2001-10-23 | Merck & Co., Inc. | HIV integrase inhibitors |
US6380249B1 (en) | 1998-06-03 | 2002-04-30 | Merck & Co., Inc. | HIV integrase inhibitors |
CA2338490A1 (en) | 1998-07-27 | 2000-02-10 | Sergio Altamura | Diketoacid-derivatives as inhibitors of polymerases |
GB9816358D0 (en) * | 1998-07-27 | 1998-09-23 | Angeletti P Ist Richerche Bio | Enzyme inhibitors |
AU763231B2 (en) * | 1999-06-02 | 2003-07-17 | Shionogi & Co., Ltd. | Novel processes for the preparation of substituted propenone derivatives |
WO2001000578A1 (en) * | 1999-06-25 | 2001-01-04 | Merck & Co., Inc. | 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof |
US20030171406A1 (en) * | 2000-06-13 | 2003-09-11 | Akihiko Sato | Medicinal compositions containing propenone derivatives |
EP1297834A4 (de) * | 2000-06-14 | 2007-05-09 | Shionogi & Co | Enzyminhibitor mit zwei divalenten metallionen als aktiven zentren |
WO2002038771A1 (fr) * | 2000-11-09 | 2002-05-16 | Shionogi & Co., Ltd. | Integrases du hiv tolerantes aux medicaments |
WO2003016275A1 (en) | 2001-08-10 | 2003-02-27 | Shionogi & Co., Ltd. | Antiviral agent |
CN102229605B (zh) * | 2001-10-26 | 2015-01-14 | Msd意大利有限公司 | 关于hiv整合酶的n-取代的羟基嘧啶酮甲酰胺抑制剂 |
TW200407132A (en) * | 2001-11-15 | 2004-05-16 | Shionogi & Co | Process for producing 1-H-1,2,4-triazole-3-carboxylic acid ester |
WO2003047564A1 (fr) * | 2001-12-05 | 2003-06-12 | Shionogi & Co., Ltd. | Dérivé ayant une activité d'inhibition de l'intégrase du vih |
WO2004024693A1 (ja) | 2002-08-13 | 2004-03-25 | Shionogi & Co., Ltd. | Hivインテグラーゼ阻害活性を有するヘテロ環化合物 |
AU2003301439A1 (en) | 2002-10-16 | 2004-05-04 | Gilead Sciences, Inc. | Pre-organized tricyclic integrase inhibitor compounds |
CN1569803B (zh) * | 2003-07-16 | 2011-04-13 | 中国科学院上海药物研究所 | 芳基β-二酮酸的新制备方法 |
US20060019952A1 (en) * | 2004-01-29 | 2006-01-26 | Elixir Pharmaceuticals, Inc. | Anti-viral therapeutics |
EA015846B1 (ru) * | 2004-08-25 | 2011-12-30 | Ардеа Байосайенсиз, Инк. | 2-[5-бром-4-(4-циклопропилнафталин-1-ил)-4н-[1,2,4]триазол-3-илсульфанил]уксусная кислота и ее метиловый эфир |
CN101014572B (zh) * | 2004-09-15 | 2011-07-06 | 盐野义制药株式会社 | 具有hiv整合酶抑制活性的氨基甲酰基吡啶酮衍生物 |
UA87884C2 (uk) * | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
TR201907729T4 (tr) * | 2004-12-03 | 2019-06-21 | Merck Sharp & Dohme | Bir anti-çekirdekleştirici ajan içeren farmasötik bileşim. |
US7250421B2 (en) * | 2005-01-31 | 2007-07-31 | University Of Georgia Research Foundation, Inc. | Diketo acids with nucleobase scaffolds: anti-HIV replication inhibitors targeted at HIV integrase |
JP2008542352A (ja) * | 2005-06-01 | 2008-11-27 | ビオアリアンス ファルマ | キノリン化合物及び他のhiv感染治療薬を含む相乗作用のコンビネーション |
EP2066670A2 (de) * | 2006-05-16 | 2009-06-10 | Gilead Sciences, Inc. | Integraseinhibitoren |
AU2007275805A1 (en) * | 2006-07-19 | 2008-01-24 | University Of Georgia Research Foundation, Inc. | Pyridinone diketo acids: Inhibitors of HIV replication in combination therapy |
WO2008041882A1 (fr) * | 2006-10-03 | 2008-04-10 | Viktor Veniaminovich Tets | Procédé pour agir sur les virus au moyen d'une substance à base de 2,8-dithioxo-1h- pyrano[2,3-d;6,5-d'] dipyrimidine et de leurs analogues 10-aza (et variantes) |
JP5562255B2 (ja) | 2008-01-25 | 2014-07-30 | キメリクス,インコーポレイテッド | ウイルス感染を治療する方法 |
US8664255B2 (en) | 2008-10-20 | 2014-03-04 | The Texas A&M University System | Inhibitors of mycobacterium tuberculosis malate synthase, methods of making and uses thereof |
WO2011071849A2 (en) | 2009-12-07 | 2011-06-16 | University Of Georgia Research Foundation, Inc. | Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications |
HUE032860T2 (en) | 2010-02-12 | 2017-11-28 | Chimerix Inc | A method for treating a virus infection |
WO2011119920A2 (en) | 2010-03-25 | 2011-09-29 | Oregon Health & Science University | Cmv glycoproteins and recombinant vectors |
CN101928258B (zh) * | 2010-08-18 | 2014-10-29 | 杭州民生药业有限公司 | 1-(2-取代苯胺基-4-甲基-噻唑-5)-3-取代苯基-丙烯酮衍生物、制备方法及其制药用途 |
CA2832109C (en) | 2011-06-10 | 2021-07-06 | Oregon Health & Science University | Cmv glycoproteins and recombinant vectors |
WO2014026033A1 (en) | 2012-08-08 | 2014-02-13 | University Of Florida Research Foundation, Inc. | Cross-reactive t cell epitopes of hiv, siv, and fiv for vaccines in humans and cats |
LT3608325T (lt) | 2012-12-21 | 2022-09-12 | Gilead Sciences, Inc. | Policikliniai karbamoilpiridono junginiai ir jų farmacinis naudojimas |
NO2865735T3 (de) | 2013-07-12 | 2018-07-21 | ||
ES2859102T3 (es) | 2013-07-12 | 2021-10-01 | Gilead Sciences Inc | Compuestos de carbamoilpiridona policíclica y su uso para el tratamiento de infecciones por VIH |
NO2717902T3 (de) | 2014-06-20 | 2018-06-23 | ||
TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
TR201905009T4 (tr) | 2015-04-02 | 2019-05-21 | Gilead Sciences Inc | Polisiklik-karbamoilpiridon bileşikleri ve bunların farmasötik kullanımları. |
CN106905244B (zh) * | 2017-02-27 | 2019-08-16 | 武汉工程大学 | 二芳基嘧啶-二酮酸类杂合型hiv-1抑制剂及其制备方法 |
CN114829357A (zh) * | 2019-10-28 | 2022-07-29 | 中国科学院上海药物研究所 | 五元杂环氧代羧酸类化合物及其医药用途 |
CN111943899B (zh) * | 2020-09-08 | 2023-04-21 | 河北凯诺中星科技有限公司 | 一种5-甲酸乙酯四氮唑的合成方法 |
CN113683574B (zh) * | 2021-09-06 | 2023-11-17 | 上海晋鲁医药科技有限公司 | 一种合成1-甲基-1h-1,2,4-三唑-3-甲酸甲酯的方法 |
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US3899508A (en) | 1974-04-12 | 1975-08-12 | Lilly Co Eli | 5-(2-Aminophenyl)pyrazole-3-carboxylic acids and esters thereof |
US3931247A (en) | 1974-12-11 | 1976-01-06 | Morton-Norwich Products, Inc. | 5-(Substituted)phenylfurfuryl alcohols |
JPS5811878B2 (ja) | 1974-12-19 | 1983-03-04 | 大正製薬株式会社 | フロ ( 3 2−b ) インド−ルルイノ セイホウ |
JPS56100784A (en) | 1980-01-16 | 1981-08-12 | Yoshitomi Pharmaceut Ind Ltd | Indolizine derivative |
US4273776A (en) | 1980-01-30 | 1981-06-16 | E. R. Squibb & Sons, Inc. | Antibacterial and antifungal derivatives of 3-(1H-imidazol-1-yl)-2-propen-1-ones |
US4423063A (en) | 1980-12-29 | 1983-12-27 | Merck & Co., Inc. | 2,4-Dioxo-4-substituted-1-butaoic acid derivatives useful in treating urinary track calcium oxalate lithiasis |
US4336397A (en) | 1980-12-29 | 1982-06-22 | Merck & Co., Inc. | 2,4-Dioxo-4-substituted-1-butanoic acid derivatives useful in treating urinary tract calcium oxalate lithiasis |
US4332735A (en) | 1981-07-06 | 1982-06-01 | Morton-Norwich Products, Inc. | Antifungal compound |
US4637829A (en) | 1984-04-27 | 1987-01-20 | Ciba-Geigy Corporation | Sulfonylureas |
JPS61134346A (ja) | 1984-12-03 | 1986-06-21 | Shionogi & Co Ltd | 4−オキソカルボン酸誘導体および抗潰瘍剤 |
CA1334975C (en) * | 1987-11-13 | 1995-03-28 | James H. Holms | Furan and pyrrole containing lipoxygenase inhibiting compounds |
JPH0238403A (ja) | 1988-07-28 | 1990-02-07 | Canon Inc | 光重合性組成物および記録媒体 |
PH27357A (en) | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
US5192773A (en) * | 1990-07-02 | 1993-03-09 | Vertex Pharmaceuticals, Inc. | Immunosuppressive compounds |
TW224974B (de) | 1991-07-02 | 1994-06-11 | Hoffmann La Roche | |
EP0658559A1 (de) * | 1993-12-14 | 1995-06-21 | Chemisch Pharmazeutische Forschungsgesellschaft m.b.H. | Thienothiazinderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als 5-dipoxygenase und Cyclooxygenaseinhibitoren |
US5475109A (en) | 1994-10-17 | 1995-12-12 | Merck & Co., Inc. | Dioxobutanoic acid derivatives as inhibitors of influenza endonuclease |
US5693804A (en) * | 1994-11-17 | 1997-12-02 | Molecular Geriatrics Corporation | Substituted 1-aryl-3-piperazin-1'-yl propanones |
EP0971894A1 (de) | 1997-04-04 | 2000-01-19 | Pfizer Products Inc. | Nicotinamid-derivate |
IL122591A0 (en) | 1997-12-14 | 1998-06-15 | Arad Dorit | Pharmaceutical compositions comprising cystein protease inhibitors |
HUP0103460A3 (en) | 1998-03-26 | 2002-11-28 | Shionogi & Co | Indole derivatives with antiviral activity and pharmaceutical compositions containing them |
WO1999048371A1 (en) | 1998-03-27 | 1999-09-30 | The Regents Of The University Of California | Novel hiv integrase inhibitors and hiv therapy based on drug combinations including integrase inhibitors |
WO1999062513A1 (en) | 1998-06-03 | 1999-12-09 | Merck & Co., Inc. | Hiv integrase inhibitors |
CA2333771A1 (en) | 1998-06-03 | 1999-12-09 | Mark W. Embrey | Hiv integrase inhibitors |
EP1082121A4 (de) * | 1998-06-03 | 2003-02-05 | Merck & Co Inc | Hiv-integraseinhibitoren |
WO2001000578A1 (en) | 1999-06-25 | 2001-01-04 | Merck & Co., Inc. | 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof |
-
1999
- 1999-12-17 AT AT99961299T patent/ATE411286T1/de not_active IP Right Cessation
- 1999-12-17 HU HU0201472A patent/HUP0201472A3/hu unknown
- 1999-12-17 US US09/857,632 patent/US6620841B1/en not_active Expired - Fee Related
- 1999-12-17 ID IDW00200101355A patent/ID29027A/id unknown
- 1999-12-17 CZ CZ20012160A patent/CZ20012160A3/cs unknown
- 1999-12-17 PL PL99348596A patent/PL348596A1/xx not_active Application Discontinuation
- 1999-12-17 NZ NZ512184A patent/NZ512184A/xx unknown
- 1999-12-17 WO PCT/JP1999/007101 patent/WO2000039086A1/ja not_active Application Discontinuation
- 1999-12-17 JP JP2000590998A patent/JP3929244B2/ja not_active Expired - Fee Related
- 1999-12-17 KR KR1020017008150A patent/KR20010089708A/ko not_active Application Discontinuation
- 1999-12-17 CN CNB99816285XA patent/CN1178913C/zh not_active Expired - Fee Related
- 1999-12-17 RU RU2001120016/04A patent/RU2225860C2/ru not_active IP Right Cessation
- 1999-12-17 IL IL14395899A patent/IL143958A0/xx unknown
- 1999-12-17 EP EP99961299A patent/EP1142872B1/de not_active Expired - Lifetime
- 1999-12-17 AU AU17979/00A patent/AU763040B2/en not_active Ceased
- 1999-12-17 BR BR9916583-0A patent/BR9916583A/pt not_active IP Right Cessation
- 1999-12-17 TR TR2001/01886T patent/TR200101886T2/xx unknown
- 1999-12-17 CA CA002353961A patent/CA2353961A1/en not_active Abandoned
- 1999-12-17 AP APAP/P/2001/002169A patent/AP2001002169A0/en unknown
- 1999-12-17 DE DE69939749T patent/DE69939749D1/de not_active Expired - Lifetime
-
2001
- 2001-06-22 NO NO20013179A patent/NO20013179L/no not_active Application Discontinuation
-
2002
- 2002-06-04 HK HK02104241.7A patent/HK1042701A1/zh unknown
- 2002-11-06 US US10/288,380 patent/US6645956B1/en not_active Expired - Fee Related
-
2003
- 2003-06-18 US US10/463,816 patent/US7098201B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
HUP0201472A3 (en) | 2006-03-28 |
PL348596A1 (en) | 2002-06-03 |
CA2353961A1 (en) | 2000-07-06 |
NO20013179L (no) | 2001-08-27 |
US20040002485A1 (en) | 2004-01-01 |
CZ20012160A3 (cs) | 2001-10-17 |
HK1042701A1 (zh) | 2002-08-23 |
NZ512184A (en) | 2003-08-29 |
TR200101886T2 (tr) | 2001-12-21 |
EP1142872A1 (de) | 2001-10-10 |
RU2225860C2 (ru) | 2004-03-20 |
ATE411286T1 (de) | 2008-10-15 |
CN1335834A (zh) | 2002-02-13 |
EP1142872A4 (de) | 2002-04-17 |
AU763040B2 (en) | 2003-07-10 |
BR9916583A (pt) | 2001-09-25 |
CN1178913C (zh) | 2004-12-08 |
AU1797900A (en) | 2000-07-31 |
HUP0201472A2 (hu) | 2003-10-28 |
EP1142872B1 (de) | 2008-10-15 |
WO2000039086A1 (fr) | 2000-07-06 |
US7098201B2 (en) | 2006-08-29 |
ID29027A (id) | 2001-07-26 |
RU2001120016A (ru) | 2003-12-10 |
US6645956B1 (en) | 2003-11-11 |
US6620841B1 (en) | 2003-09-16 |
KR20010089708A (ko) | 2001-10-08 |
NO20013179D0 (no) | 2001-06-22 |
AP2001002169A0 (en) | 2001-06-30 |
IL143958A0 (en) | 2002-04-21 |
JP3929244B2 (ja) | 2007-06-13 |
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