CN101952274A - 非核苷逆转录酶抑制剂 - Google Patents
非核苷逆转录酶抑制剂 Download PDFInfo
- Publication number
- CN101952274A CN101952274A CN2008801168055A CN200880116805A CN101952274A CN 101952274 A CN101952274 A CN 101952274A CN 2008801168055 A CN2008801168055 A CN 2008801168055A CN 200880116805 A CN200880116805 A CN 200880116805A CN 101952274 A CN101952274 A CN 101952274A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- independently
- compound
- chloro
- haloalkyl
- 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.)
- Pending
Links
- 0 C[C@@](*)(C=C(C)*)C=NC(N1C)=C(*)OC1=O Chemical compound C[C@@](*)(C=C(C)*)C=NC(N1C)=C(*)OC1=O 0.000 description 16
- JUBXTBVKELTJEX-UHFFFAOYSA-N C(C1)C1N1CCCCC1 Chemical compound C(C1)C1N1CCCCC1 JUBXTBVKELTJEX-UHFFFAOYSA-N 0.000 description 1
- DQMVYRXJWHHQTR-VOTSOKGWSA-N CC(C)(C)OC([n]1nc(/C=C/c(nc2)cc(Oc3cc(Cl)cc(C#N)c3)c2Cl)c2cccnc12)=O Chemical compound CC(C)(C)OC([n]1nc(/C=C/c(nc2)cc(Oc3cc(Cl)cc(C#N)c3)c2Cl)c2cccnc12)=O DQMVYRXJWHHQTR-VOTSOKGWSA-N 0.000 description 1
- NKKVZRZVEKUQGZ-UHFFFAOYSA-N CC(C)(C)OC([n]1nc(CCc(nc(c(Cl)c2Oc3cc(Cl)cc(C#N)c3)OC)c2Cl)c2cccnc12)=O Chemical compound CC(C)(C)OC([n]1nc(CCc(nc(c(Cl)c2Oc3cc(Cl)cc(C#N)c3)OC)c2Cl)c2cccnc12)=O NKKVZRZVEKUQGZ-UHFFFAOYSA-N 0.000 description 1
- AQNJVUMOINBHAG-UHFFFAOYSA-N CC(C=CN(Cc1n[nH]c2c1cccn2)C1=O)=C1Oc1cc(Br)cc(Cl)c1 Chemical compound CC(C=CN(Cc1n[nH]c2c1cccn2)C1=O)=C1Oc1cc(Br)cc(Cl)c1 AQNJVUMOINBHAG-UHFFFAOYSA-N 0.000 description 1
- YMRUCOCNLHJFRC-UHFFFAOYSA-N CC(C=CN(Cc1n[nH]c2c1cccn2)C1=O)=C1Oc1cc(C#N)cc(Cl)c1 Chemical compound CC(C=CN(Cc1n[nH]c2c1cccn2)C1=O)=C1Oc1cc(C#N)cc(Cl)c1 YMRUCOCNLHJFRC-UHFFFAOYSA-N 0.000 description 1
- NPVPXUFRPFPGTQ-UHFFFAOYSA-N CN(CC1)CCS1(=O)=[O]=C Chemical compound CN(CC1)CCS1(=O)=[O]=C NPVPXUFRPFPGTQ-UHFFFAOYSA-N 0.000 description 1
- AVFZOVWCLRSYKC-UHFFFAOYSA-N CN1CCCC1 Chemical compound CN1CCCC1 AVFZOVWCLRSYKC-UHFFFAOYSA-N 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- KDTVWEHAAISPNW-UHFFFAOYSA-N CN1CCSCC1 Chemical compound CN1CCSCC1 KDTVWEHAAISPNW-UHFFFAOYSA-N 0.000 description 1
- NRQMZHMCEUJCCS-UHFFFAOYSA-N COc(nc(C(c1n[nH]c2ncccc12)O)cc1Oc2cc(Cl)cc(C#N)c2)c1Cl Chemical compound COc(nc(C(c1n[nH]c2ncccc12)O)cc1Oc2cc(Cl)cc(C#N)c2)c1Cl NRQMZHMCEUJCCS-UHFFFAOYSA-N 0.000 description 1
- YQELOHGDMCGRAY-UHFFFAOYSA-N COc1nc(Cc2n[nH]c3ncccc23)cc(Oc2cc(Cl)cc(Br)c2)c1Cl Chemical compound COc1nc(Cc2n[nH]c3ncccc23)cc(Oc2cc(Cl)cc(Br)c2)c1Cl YQELOHGDMCGRAY-UHFFFAOYSA-N 0.000 description 1
- NCPJKBVDFNPLLG-UHFFFAOYSA-N N#Cc1cc(Cl)cc(OC(C=C(CCc2n[nH]c3ncccc23)NC2=O)=C2Cl)c1 Chemical compound N#Cc1cc(Cl)cc(OC(C=C(CCc2n[nH]c3ncccc23)NC2=O)=C2Cl)c1 NCPJKBVDFNPLLG-UHFFFAOYSA-N 0.000 description 1
- DZUHNBJTDWFYCJ-UHFFFAOYSA-N Nc1ccc(c(CNc(c(Cl)c2)nc(Oc3cc(Cl)cc(C#N)c3)c2F)n[nH]2)c2n1 Chemical compound Nc1ccc(c(CNc(c(Cl)c2)nc(Oc3cc(Cl)cc(C#N)c3)c2F)n[nH]2)c2n1 DZUHNBJTDWFYCJ-UHFFFAOYSA-N 0.000 description 1
- DWGIQXKNNRPSKU-UHFFFAOYSA-O [NH3+]c(cc1)nc2c1c(CN(C=CC(C(F)(F)F)=C1Oc3cc(Cl)cc(Cl)c3)C1=O)n[nH]2 Chemical compound [NH3+]c(cc1)nc2c1c(CN(C=CC(C(F)(F)F)=C1Oc3cc(Cl)cc(Cl)c3)C1=O)n[nH]2 DWGIQXKNNRPSKU-UHFFFAOYSA-O 0.000 description 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
- 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
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US376907P | 2007-11-20 | 2007-11-20 | |
| US61/003769 | 2007-11-20 | ||
| PCT/US2008/012774 WO2009067166A2 (en) | 2007-11-20 | 2008-11-14 | Non-nucleoside reverse transcriptase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101952274A true CN101952274A (zh) | 2011-01-19 |
Family
ID=40336474
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008801168055A Pending CN101952274A (zh) | 2007-11-20 | 2008-11-14 | 非核苷逆转录酶抑制剂 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8404856B2 (enExample) |
| EP (1) | EP2222661B1 (enExample) |
| JP (1) | JP5539216B2 (enExample) |
| KR (1) | KR20100088142A (enExample) |
| CN (1) | CN101952274A (enExample) |
| AU (1) | AU2008326784B2 (enExample) |
| BR (1) | BRPI0820162A2 (enExample) |
| CA (1) | CA2705834A1 (enExample) |
| IL (1) | IL205386A0 (enExample) |
| MX (1) | MX2010005483A (enExample) |
| RU (1) | RU2010125220A (enExample) |
| WO (1) | WO2009067166A2 (enExample) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108289931A (zh) * | 2015-09-23 | 2018-07-17 | 默沙东公司 | 4’-取代的核苷逆转录酶抑制剂及其制备 |
| CN110066273A (zh) * | 2019-06-05 | 2019-07-30 | 山东大学 | 一种含三氮唑环的单芳基嘧啶类hiv-1逆转录酶抑制剂及其制备方法与应用 |
| CN112876409A (zh) * | 2021-01-20 | 2021-06-01 | 都创(上海)医药科技股份有限公司 | 一种2-(5-溴-6-甲氧基吡啶-2-基)乙腈及其衍生物的合成方法 |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010026075A1 (en) * | 2008-09-04 | 2010-03-11 | F. Hoffmann-La Roche Ag | Pyridine derivatives as inhibitors of hiv-i reverse transcriptase |
| US20120232062A1 (en) * | 2009-10-20 | 2012-09-13 | Eiger Biopharmaceuticals, Inc. | Azaindazoles to treat flaviviridae virus infection |
| CN102971308B (zh) | 2010-03-30 | 2015-02-04 | 默克加拿大有限公司 | 非核苷类逆转录酶抑制剂 |
| US20130040914A1 (en) * | 2010-04-08 | 2013-02-14 | Samson M. Jolly | Prodrugs of an hiv reverse transcriptase inhibitor |
| EP2900240B1 (en) * | 2012-09-26 | 2020-01-08 | Merck Sharp & Dohme Corp. | Crystalline form of a reverse transcriptase inhibitor |
| JO3470B1 (ar) | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| MX355439B (es) * | 2012-12-05 | 2018-04-18 | Merck Sharp & Dohme | Proceso para preparar inhibidores de la transcriptasa inversa. |
| CA2930585A1 (en) * | 2013-12-04 | 2015-06-11 | Merck Sharp & Dohme Corp. | Process for making reverse transcriptase inhibitors |
| RU2693622C2 (ru) | 2014-04-01 | 2019-07-03 | Мерк Шарп И Доум Корп. | Пролекарственные средства ингибиторов обратной транскриптазы вич |
| DK3180335T3 (da) | 2014-08-11 | 2021-08-09 | Angion Biomedica Corp | Cytokrom-p450-inhibitorer og anvendelser deraf |
| EP3240778A4 (en) | 2014-12-31 | 2018-07-11 | Angion Biomedica Corp. | Methods and agents for treating disease |
| RU2750151C2 (ru) | 2015-11-20 | 2021-06-22 | Форма Терапьютикс, Инк. | Гипоксантины в качестве ингибиторов убиквитин-специфической протеазы 1 |
| KR102590848B1 (ko) | 2016-12-28 | 2023-10-19 | 다트 뉴로사이언스, 엘엘씨 | Pde2 억제제로서 치환된 피라졸로피리미디논 화합물 |
| JP7254078B2 (ja) | 2017-11-27 | 2023-04-07 | ダート・ニューロサイエンス・エルエルシー | Pde1阻害剤としての置換フラノピリミジン化合物 |
| MA54549A (fr) | 2018-12-18 | 2022-03-30 | Merck Sharp & Dohme | Dérivés de pyrimidone en tant qu'agents cytotoxiques sélectifs contre des cellules infectées par le vih |
| CN114026081B (zh) * | 2019-05-22 | 2025-02-11 | 默沙东有限责任公司 | 作为针对hiv感染的细胞的选择性细胞毒性剂的吡啶酮衍生物 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999055676A1 (en) * | 1998-04-27 | 1999-11-04 | Centre National De La Recherche Scientifique | 3-(amino- or aminoalkyl)pyridinone derivatives and their use for the treatment of hiv related diseases |
| WO2007015809A2 (en) * | 2005-07-22 | 2007-02-08 | Merck & Co., Inc. | Hiv reverse transcriptase inhibitors |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL99731A0 (en) | 1990-10-18 | 1992-08-18 | Merck & Co Inc | Hydroxylated pyridine derivatives,their preparation and pharmaceutical compositions containing them |
| WO1995004045A1 (en) * | 1993-07-28 | 1995-02-09 | Rhone-Poulenc Rorer Limited | Compounds as pde iv and tnf inhibitors |
| GB9910577D0 (en) | 1999-05-08 | 1999-07-07 | Zeneca Ltd | Chemical compounds |
| SE9904045D0 (sv) | 1999-11-09 | 1999-11-09 | Astra Ab | Compounds |
| US6800651B2 (en) * | 2000-02-03 | 2004-10-05 | Eli Lilly And Company | Potentiators of glutamate receptors |
| DK1318997T3 (da) | 2000-09-15 | 2006-09-25 | Vertex Pharma | Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer |
| WO2002024650A2 (en) * | 2000-09-19 | 2002-03-28 | Centre National De La Recherche Scientifique (Cnrs) | Pyridinone and pyridinethione derivatives having hiv inhibiting properties |
| GB0129260D0 (en) | 2001-12-06 | 2002-01-23 | Eisai London Res Lab Ltd | Pharmaceutical compositions and their uses |
| ES2334990T3 (es) * | 2002-02-14 | 2010-03-18 | Pharmacia Corporation | Piridinonas sustituidas como moduladores de p38 map quinasa. |
| CL2004000192A1 (es) | 2003-02-07 | 2005-03-18 | Janssen Pharmaceutica Nv | Uso de compuestos derivados de 2-aminopirimidina para preparar un medicamento para la prevencion de una infeccion por vih relaciones sexuales o un contacto intimo en la pareja. |
| EP1608629A1 (en) * | 2003-03-24 | 2005-12-28 | F. Hoffmann-La Roche Ag | Benzyl-pyridazinons as reverse transcriptase inhibitors |
| WO2004096147A2 (en) * | 2003-04-28 | 2004-11-11 | Idenix (Cayman) Limited | Oxo-pyrimidine compounds |
| US7166738B2 (en) * | 2004-04-23 | 2007-01-23 | Roche Palo Alto Llc | Non-nucleoside reverse transcriptase inhibitors |
| DK1742908T3 (da) | 2004-04-23 | 2010-01-18 | Hoffmann La Roche | Ikke nukleosid revers transkriptase inhibitorer |
| TWI360539B (en) * | 2004-10-28 | 2012-03-21 | Shionogi & Co | 3-carbamoyl-2-pyridone derivatives |
| EP1831157A2 (en) * | 2004-12-22 | 2007-09-12 | Pfizer Limited | Nonnucleoside inhibitors of hiv-1 reverse transcriptase |
| BRPI0617720A2 (pt) * | 2005-10-19 | 2011-08-02 | Hoffmann La Roche | compostos inibidores de nnrt de fenil-acetamida, usos dos referidos compostos e composição farmacêutica que os contém |
| ES2320042T3 (es) | 2005-10-19 | 2009-05-18 | F. Hoffmann-La Roche Ag | Inhibidores de transcriptasa reversa con nucleosidos de n-fenil fenilacetamida. |
| EP2038272B8 (en) * | 2006-06-30 | 2013-10-23 | Sunesis Pharmaceuticals, Inc. | Pyridinonyl pdk1 inhibitors |
| US8314119B2 (en) * | 2006-11-06 | 2012-11-20 | Abbvie Inc. | Azaadamantane derivatives and methods of use |
| TW200831085A (en) * | 2006-12-13 | 2008-08-01 | Merck & Co Inc | Non-nucleoside reverse transcriptase inhibitors |
| WO2008098143A2 (en) * | 2007-02-08 | 2008-08-14 | Trius Therapeutics | Antimicrobial compounds and methods of use |
-
2008
- 2008-11-14 AU AU2008326784A patent/AU2008326784B2/en not_active Ceased
- 2008-11-14 MX MX2010005483A patent/MX2010005483A/es not_active Application Discontinuation
- 2008-11-14 CA CA2705834A patent/CA2705834A1/en active Pending
- 2008-11-14 US US12/742,159 patent/US8404856B2/en active Active
- 2008-11-14 WO PCT/US2008/012774 patent/WO2009067166A2/en not_active Ceased
- 2008-11-14 CN CN2008801168055A patent/CN101952274A/zh active Pending
- 2008-11-14 KR KR1020107011127A patent/KR20100088142A/ko not_active Withdrawn
- 2008-11-14 EP EP08851089.6A patent/EP2222661B1/en not_active Not-in-force
- 2008-11-14 BR BRPI0820162A patent/BRPI0820162A2/pt not_active IP Right Cessation
- 2008-11-14 RU RU2010125220/04A patent/RU2010125220A/ru unknown
- 2008-11-14 JP JP2010534947A patent/JP5539216B2/ja not_active Expired - Fee Related
-
2010
- 2010-04-27 IL IL205386A patent/IL205386A0/en unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999055676A1 (en) * | 1998-04-27 | 1999-11-04 | Centre National De La Recherche Scientifique | 3-(amino- or aminoalkyl)pyridinone derivatives and their use for the treatment of hiv related diseases |
| WO2007015809A2 (en) * | 2005-07-22 | 2007-02-08 | Merck & Co., Inc. | Hiv reverse transcriptase inhibitors |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108289931A (zh) * | 2015-09-23 | 2018-07-17 | 默沙东公司 | 4’-取代的核苷逆转录酶抑制剂及其制备 |
| CN108289931B (zh) * | 2015-09-23 | 2022-10-11 | 默沙东公司 | 4’-取代的核苷逆转录酶抑制剂及其制备 |
| CN110066273A (zh) * | 2019-06-05 | 2019-07-30 | 山东大学 | 一种含三氮唑环的单芳基嘧啶类hiv-1逆转录酶抑制剂及其制备方法与应用 |
| CN112876409A (zh) * | 2021-01-20 | 2021-06-01 | 都创(上海)医药科技股份有限公司 | 一种2-(5-溴-6-甲氧基吡啶-2-基)乙腈及其衍生物的合成方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2008326784B2 (en) | 2014-04-24 |
| WO2009067166A2 (en) | 2009-05-28 |
| EP2222661B1 (en) | 2016-04-20 |
| CA2705834A1 (en) | 2009-05-28 |
| RU2010125220A (ru) | 2011-12-27 |
| IL205386A0 (en) | 2010-12-30 |
| JP5539216B2 (ja) | 2014-07-02 |
| KR20100088142A (ko) | 2010-08-06 |
| WO2009067166A3 (en) | 2009-07-16 |
| US20100256181A1 (en) | 2010-10-07 |
| AU2008326784A1 (en) | 2009-05-28 |
| JP2011503230A (ja) | 2011-01-27 |
| BRPI0820162A2 (pt) | 2019-09-24 |
| US8404856B2 (en) | 2013-03-26 |
| EP2222661A2 (en) | 2010-09-01 |
| MX2010005483A (es) | 2010-06-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20110119 |