AR043195A1 - Inhibidores no nucleosidos de la transcriptasa inversa derivados de pirazol - Google Patents
Inhibidores no nucleosidos de la transcriptasa inversa derivados de pirazolInfo
- Publication number
- AR043195A1 AR043195A1 ARP040100477A ARP040100477A AR043195A1 AR 043195 A1 AR043195 A1 AR 043195A1 AR P040100477 A ARP040100477 A AR P040100477A AR P040100477 A ARP040100477 A AR P040100477A AR 043195 A1 AR043195 A1 AR 043195A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkoxy
- group
- phenyl
- optionally substituted
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 238000003874 inverse correlation nuclear magnetic resonance spectroscopy Methods 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 10
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Chemical group C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical group C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- 240000007313 Tilia cordata Species 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- -1 pyrimidinyl pyrazinyl Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- 125000004001 thioalkyl group Chemical group 0.000 abstract 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 abstract 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 101100244083 Arabidopsis thaliana PKL gene Proteins 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 235000008733 Citrus aurantifolia Nutrition 0.000 abstract 1
- 102100034343 Integrase Human genes 0.000 abstract 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 abstract 1
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 abstract 1
- 235000011941 Tilia x europaea Nutrition 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000004571 lime Chemical group 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
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003217 pyrazoles Chemical class 0.000 abstract 1
- 125000005017 substituted alkenyl group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
-
- 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
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US44797403P | 2003-02-18 | 2003-02-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR043195A1 true AR043195A1 (es) | 2005-07-20 |
Family
ID=32908518
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040100477A AR043195A1 (es) | 2003-02-18 | 2004-02-17 | Inhibidores no nucleosidos de la transcriptasa inversa derivados de pirazol |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US7241794B2 (https=) |
| EP (1) | EP1597235B1 (https=) |
| JP (1) | JP4608480B2 (https=) |
| KR (1) | KR100776093B1 (https=) |
| CN (1) | CN100389109C (https=) |
| AR (1) | AR043195A1 (https=) |
| AT (1) | ATE370124T1 (https=) |
| BR (1) | BRPI0407591A (https=) |
| CA (1) | CA2515151C (https=) |
| CL (1) | CL2004000270A1 (https=) |
| DE (1) | DE602004008227T2 (https=) |
| ES (1) | ES2291854T3 (https=) |
| MX (1) | MXPA05008748A (https=) |
| PL (1) | PL378556A1 (https=) |
| RU (1) | RU2305680C2 (https=) |
| TW (1) | TW200423930A (https=) |
| WO (1) | WO2004074257A1 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4041153B2 (ja) * | 2003-05-07 | 2008-01-30 | ファイザー・プロダクツ・インク | カンナビノイド受容体リガンドとその使用 |
| US8022225B2 (en) | 2004-08-04 | 2011-09-20 | Taisho Pharmaceutical Co., Ltd | Triazole derivative |
| UA87884C2 (uk) * | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| EP1988083B1 (en) | 2006-02-03 | 2014-04-02 | Taisho Pharmaceutical Co., Ltd. | Triazole derivative |
| JP5218737B2 (ja) * | 2006-02-06 | 2013-06-26 | 大正製薬株式会社 | スフィンゴシン−１−リン酸結合阻害物質 |
| CA2642308C (en) * | 2006-02-14 | 2013-12-17 | Ihara Chemical Industry Co., Ltd. | Process for production of 5-alkoxy-4-hydroxymethylpyrazole compound |
| CL2007002105A1 (es) * | 2006-07-21 | 2008-02-22 | Hoffmann La Roche | Compuestos derivados de 2-[3-(3-cianofenoxi)(fenoxi o fenilsulfanil)]-n-fenil acetamida, inhibidores de la transcriptasa inversa del vih; procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar u |
| CA2658984C (en) | 2006-08-16 | 2014-12-02 | Joshua Kennedy-Smith | Non-nucleoside reverse transcriptase inhibitors |
| BRPI0809617A2 (pt) | 2007-03-29 | 2014-09-16 | Hoffmann La Roche | Inibidores não-nucleosídicos da transcriptase reversa |
| DK2177512T3 (da) | 2007-08-01 | 2012-06-18 | Taisho Pharmaceutical Co Ltd | S1P1-bindingshæmmer |
| RU2495878C2 (ru) * | 2007-12-21 | 2013-10-20 | Ф.Хоффманн-Ля Рош Аг | Гетероциклические антивирусные соединения |
| DE102008015033A1 (de) * | 2008-03-17 | 2009-09-24 | Aicuris Gmbh & Co. Kg | Substituierte (Pyrazolyl-carbonyl)imidazolidinone und ihre Verwendung |
| SI2924034T1 (sl) * | 2010-03-30 | 2017-05-31 | Merck Canada Inc. | Farmacevtski sestavek, ki obsega nenukleozidni inhibitor reverzne transkriptaze |
| CN103097357B (zh) | 2010-07-15 | 2015-01-28 | 大日本住友制药株式会社 | 吡唑化合物 |
| EP2508511A1 (en) * | 2011-04-07 | 2012-10-10 | Laboratoire Biodim | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| WO2013134562A1 (en) | 2012-03-09 | 2013-09-12 | Inception 2, Inc. | Triazolone compounds and uses thereof |
| CN104797255A (zh) | 2012-06-20 | 2015-07-22 | 范德比尔特大学 | 作为mglur5受体变构调节剂的取代的双环烷氧基吡唑类似物 |
| WO2013192343A1 (en) | 2012-06-20 | 2013-12-27 | Vanderbilt University | Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mglur5 receptors |
| JO3470B1 (ar) | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| AU2013363398B2 (en) | 2012-12-20 | 2017-06-01 | Tempest Therapeutics, Inc. | Triazolone compounds and uses thereof |
| US9776976B2 (en) | 2013-09-06 | 2017-10-03 | Inception 2, Inc. | Triazolone compounds and uses thereof |
| WO2015153304A1 (en) | 2014-04-01 | 2015-10-08 | Merck Sharp & Dohme Corp. | Prodrugs of hiv reverse transcriptase inhibitors |
| EP3194386A2 (en) | 2014-09-17 | 2017-07-26 | Ironwood Pharmaceuticals, Inc. | Sgc stimulators |
| US20170298055A1 (en) | 2014-09-17 | 2017-10-19 | Ironwood Pharmaceuticals, Inc. | sGC STIMULATORS |
| CA2978066A1 (en) * | 2015-03-19 | 2016-09-22 | E I Du Pont De Nemours And Company | Fungicidal pyrazoles |
| EP3478665A1 (en) * | 2016-06-29 | 2019-05-08 | Esteve Pharmaceuticals, S.A. | Pyrazole derivatives having activity against pain |
| CN110818636A (zh) * | 2019-11-29 | 2020-02-21 | 河北科技大学 | 一种化合物或其盐及其应用和合成方法 |
| CN115677585B (zh) * | 2022-10-31 | 2024-03-19 | 上海群力化工有限公司 | 一种甲醛吡唑衍生物的合成工艺 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2157368C2 (ru) | 1994-09-26 | 2000-10-10 | Сионоги Энд Ко., Лтд. | Производные имидазола и фармацевтическая композиция на их основе |
| DE19734664A1 (de) * | 1997-08-11 | 1999-02-18 | Bayer Ag | (Hetero)Aryloxypyrazole |
| GB0016787D0 (en) * | 2000-07-07 | 2000-08-30 | Pfizer Ltd | Compounds useful in therapy |
| US20030008841A1 (en) | 2000-08-30 | 2003-01-09 | Rene Devos | Anti-HCV nucleoside derivatives |
| GB0024795D0 (en) | 2000-10-10 | 2000-11-22 | Hoffmann La Roche | Pyrazole derivatives for the treatment of viral diseases |
| GB0028484D0 (en) | 2000-11-22 | 2001-01-10 | Hoffmann La Roche | Imidazolone derivatives for the treatment of viral diseases |
| RS51166B (sr) * | 2001-04-10 | 2010-10-31 | Pfizer Inc. | Derivati pirazola za tretiranje hiv |
| GB0113524D0 (en) * | 2001-06-04 | 2001-07-25 | Hoffmann La Roche | Pyrazole derivatives |
-
2004
- 2004-02-12 TW TW093103358A patent/TW200423930A/zh unknown
- 2004-02-16 CL CL200400270A patent/CL2004000270A1/es unknown
- 2004-02-17 WO PCT/EP2004/001477 patent/WO2004074257A1/en not_active Ceased
- 2004-02-17 ES ES04711607T patent/ES2291854T3/es not_active Expired - Lifetime
- 2004-02-17 BR BRPI0407591-9A patent/BRPI0407591A/pt not_active IP Right Cessation
- 2004-02-17 CN CNB2004800044061A patent/CN100389109C/zh not_active Expired - Fee Related
- 2004-02-17 KR KR1020057015085A patent/KR100776093B1/ko not_active Expired - Fee Related
- 2004-02-17 MX MXPA05008748A patent/MXPA05008748A/es active IP Right Grant
- 2004-02-17 DE DE602004008227T patent/DE602004008227T2/de not_active Expired - Lifetime
- 2004-02-17 CA CA2515151A patent/CA2515151C/en not_active Expired - Fee Related
- 2004-02-17 JP JP2006500034A patent/JP4608480B2/ja not_active Expired - Fee Related
- 2004-02-17 AT AT04711607T patent/ATE370124T1/de not_active IP Right Cessation
- 2004-02-17 PL PL378556A patent/PL378556A1/pl not_active Application Discontinuation
- 2004-02-17 RU RU2005128832/04A patent/RU2305680C2/ru active
- 2004-02-17 EP EP04711607A patent/EP1597235B1/en not_active Expired - Lifetime
- 2004-02-17 AR ARP040100477A patent/AR043195A1/es not_active Application Discontinuation
- 2004-02-18 US US10/781,373 patent/US7241794B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| KR20050105471A (ko) | 2005-11-04 |
| US7241794B2 (en) | 2007-07-10 |
| AU2004213134A1 (en) | 2004-09-02 |
| CN100389109C (zh) | 2008-05-21 |
| RU2005128832A (ru) | 2006-04-27 |
| CN1751028A (zh) | 2006-03-22 |
| KR100776093B1 (ko) | 2007-11-15 |
| DE602004008227D1 (de) | 2007-09-27 |
| DE602004008227T2 (de) | 2008-05-15 |
| CA2515151C (en) | 2010-11-30 |
| BRPI0407591A (pt) | 2006-02-14 |
| ATE370124T1 (de) | 2007-09-15 |
| WO2004074257A1 (en) | 2004-09-02 |
| MXPA05008748A (es) | 2005-09-20 |
| TW200423930A (en) | 2004-11-16 |
| EP1597235A1 (en) | 2005-11-23 |
| EP1597235B1 (en) | 2007-08-15 |
| RU2305680C2 (ru) | 2007-09-10 |
| ES2291854T3 (es) | 2008-03-01 |
| CA2515151A1 (en) | 2004-09-02 |
| CL2004000270A1 (es) | 2005-02-04 |
| PL378556A1 (pl) | 2006-05-02 |
| JP2006515339A (ja) | 2006-05-25 |
| JP4608480B2 (ja) | 2011-01-12 |
| US20040192666A1 (en) | 2004-09-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |