AR051315A1 - Pirimidinas 5-sustituidas inhibidoras del vih - Google Patents
Pirimidinas 5-sustituidas inhibidoras del vihInfo
- Publication number
- AR051315A1 AR051315A1 ARP050104155A ARP050104155A AR051315A1 AR 051315 A1 AR051315 A1 AR 051315A1 AR P050104155 A ARP050104155 A AR P050104155A AR P050104155 A ARP050104155 A AR P050104155A AR 051315 A1 AR051315 A1 AR 051315A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- halo
- aryl
- mono
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- -1 nitro, amino Chemical group 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 1
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000006684 polyhaloalkyl group Polymers 0.000 abstract 1
- 230000010076 replication Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/50—Three nitrogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Inhibidores de la replicacion del VIH de formula (1), un N-oxido, una sal de adicion aceptable desde el punto de vista farmacéutico, una amina cuaternaria o una forma estereoquímicamente isomérica de los mismos, en los cuales A es -CH2-CH2-, -CH=CH- , C:::C-; R1 es H, arilo, formilo, alquil C1-6carbonilo, alquilo C1-6, alquiloxi C1-6carbonilo, R2 es hidroxi, halo, alquilo C1-6, carboxilo, ciano, -C(=O)R6, nitro, amino, mono- o di(alquil C1-6)amino, polihalometilo; X1 es -NR1-, -O-, -S-, -S(=O)p- ; R3 es H, alquilo C1-6, halo; R4 es H, alquilo C1-6, halo; R5 es nitro, amino, mono- y dialquilamino C1-4, arilo, halo, -CHO, -CO-R6, -COOR7, -NH-C(=O)H, -NH-C(=O)R6, -CH=N-O-R8; R6 es alquilo C1-4, amino, mono- o di(alquil C1-4)amino o polihaloalquilo C1-4; R7 es H, alquilo C1-6, arilalquilo C1-6; R8 es H, alquilo C1-6, arilo; p es 1 o 2; arilo es fenilo sustituido en forma opcional, composiciones farmacéuticas que contienen estos compuestos como componente activo y procesos para preparar dichos compuestos y composiciones.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04104805 | 2004-09-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR051315A1 true AR051315A1 (es) | 2007-01-03 |
Family
ID=34929637
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050104155A AR051315A1 (es) | 2004-09-30 | 2005-09-30 | Pirimidinas 5-sustituidas inhibidoras del vih |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8946248B2 (es) |
| EP (1) | EP1797047B1 (es) |
| JP (1) | JP5046943B2 (es) |
| KR (1) | KR20070057837A (es) |
| CN (1) | CN101027288B (es) |
| AR (1) | AR051315A1 (es) |
| AT (1) | ATE542802T1 (es) |
| AU (1) | AU2005288866B2 (es) |
| BR (1) | BRPI0516748B8 (es) |
| CA (1) | CA2575472C (es) |
| ES (1) | ES2380631T3 (es) |
| IL (1) | IL181056A (es) |
| MX (1) | MX2007003796A (es) |
| RU (1) | RU2410379C2 (es) |
| TW (1) | TW200626561A (es) |
| WO (1) | WO2006035069A1 (es) |
| ZA (1) | ZA200702656B (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE542802T1 (de) | 2004-09-30 | 2012-02-15 | Tibotec Pharm Ltd | Hiv-inhibierende 5-substituierte pyrimidine |
| ATE520680T1 (de) * | 2004-09-30 | 2011-09-15 | Tibotec Pharm Ltd | Hiv-hemmende 5-heterocyclylpyrimidine |
| JP5247154B2 (ja) * | 2005-02-18 | 2013-07-24 | テイボテク・フアーマシユーチカルズ | Ｈｉｖ阻害性２−（４−シアノフェニルアミノ）ピリミジンオキシド誘導体 |
| AU2007233737B2 (en) * | 2006-03-30 | 2012-11-29 | Janssen Sciences Ireland Uc | HIV inhibiting 5-amido substituted pyrimidines |
| BRPI0722079B8 (pt) * | 2006-12-29 | 2021-05-25 | Janssen R & D Ireland | pirimidinas 5,6-substituídas inibidoras de hiv e composição farmacêutica que as compreende |
| JP5185283B2 (ja) * | 2006-12-29 | 2013-04-17 | テイボテク・フアーマシユーチカルズ | Ｈｉｖ阻害６−置換ピリミジン |
| SG10201702654VA (en) | 2011-04-22 | 2017-06-29 | Signal Pharm Llc | Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith |
| ES2664094T3 (es) * | 2012-07-12 | 2018-04-18 | Hetero Research Foundation | Procedimiento de preparación de rilpivirina utilizando un intermedio nuevo |
| US9540333B2 (en) * | 2012-11-08 | 2017-01-10 | Bristol-Myers Squibb Company | Alkyl amide-substituted pyrimidine compounds useful in the modulation of IL-12, IL-23 and/or IFNα |
| NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| SG11201704827UA (en) | 2014-12-16 | 2017-07-28 | Signal Pharm Llc | Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide |
| EP3233808B1 (en) | 2014-12-16 | 2021-07-14 | Signal Pharmaceuticals, LLC | Medical uses comprising methods for measurement of inhibition of c-jun n-terminal kinase in skin |
| WO2016123291A1 (en) | 2015-01-29 | 2016-08-04 | Signal Pharmaceuticals, Llc | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| MX2018001004A (es) | 2015-07-24 | 2018-06-07 | Celgene Corp | Metodos de sintesis de clorhidrato de (1r,2r,5r)-5-amino-2-metilci clohexanol e intermedios utiles en este. |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3459731A (en) * | 1966-12-16 | 1969-08-05 | Corn Products Co | Cyclodextrin polyethers and their production |
| EP0310550B1 (de) * | 1987-09-28 | 1993-05-26 | Ciba-Geigy Ag | Schädlingsbekämpfungsmittel |
| PL189122B1 (pl) | 1995-11-23 | 2005-06-30 | Janssen Pharmaceutica Nv | Sposób wytwarzania mieszaniny stałej zawierającejjedną lub wiele cyklodekstryn, mieszanina stała ikompozycja farmaceutyczna |
| NO311614B1 (no) | 1996-10-01 | 2001-12-17 | Janssen Pharmaceutica Nv | Substituerte diamino-1,3,5-triazinderivater |
| EP0945447A1 (en) | 1998-03-27 | 1999-09-29 | Janssen Pharmaceutica N.V. | Trisubstituted 1,3,5-triazine derivatives for treatment of HIV infections |
| ATE232521T1 (de) | 1998-03-27 | 2003-02-15 | Janssen Pharmaceutica Nv | Hiv hemmende pyrimidin derivate |
| EA004049B1 (ru) | 1998-11-10 | 2003-12-25 | Янссен Фармацевтика Н.В. | Пиримидины, ингибирующие репликацию вич |
| GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| CA2406562C (en) * | 2000-05-08 | 2009-09-15 | Janssen Pharmaceutica N.V. | Hiv replication inhibiting pyrimidines and triazines |
| CN102250071A (zh) * | 2000-12-21 | 2011-11-23 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的吡唑化合物 |
| JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| NZ540321A (en) | 2002-11-15 | 2007-09-28 | Tibotec Pharm Ltd | Substituted indolepyridinium as anti-infective compounds |
| US7504396B2 (en) * | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| WO2006035068A2 (en) * | 2004-09-30 | 2006-04-06 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines |
| ATE520680T1 (de) | 2004-09-30 | 2011-09-15 | Tibotec Pharm Ltd | Hiv-hemmende 5-heterocyclylpyrimidine |
| ATE542802T1 (de) | 2004-09-30 | 2012-02-15 | Tibotec Pharm Ltd | Hiv-inhibierende 5-substituierte pyrimidine |
| AU2007233737B2 (en) | 2006-03-30 | 2012-11-29 | Janssen Sciences Ireland Uc | HIV inhibiting 5-amido substituted pyrimidines |
| JP5185283B2 (ja) * | 2006-12-29 | 2013-04-17 | テイボテク・フアーマシユーチカルズ | Ｈｉｖ阻害６−置換ピリミジン |
| BRPI0722079B8 (pt) | 2006-12-29 | 2021-05-25 | Janssen R & D Ireland | pirimidinas 5,6-substituídas inibidoras de hiv e composição farmacêutica que as compreende |
-
2005
- 2005-09-29 AT AT05789686T patent/ATE542802T1/de active
- 2005-09-29 ES ES05789686T patent/ES2380631T3/es active Active
- 2005-09-29 RU RU2007116172/04A patent/RU2410379C2/ru active
- 2005-09-29 KR KR1020077006048A patent/KR20070057837A/ko not_active Ceased
- 2005-09-29 EP EP05789686A patent/EP1797047B1/en not_active Expired - Lifetime
- 2005-09-29 AU AU2005288866A patent/AU2005288866B2/en not_active Ceased
- 2005-09-29 US US11/576,315 patent/US8946248B2/en not_active Expired - Fee Related
- 2005-09-29 JP JP2007534028A patent/JP5046943B2/ja not_active Expired - Fee Related
- 2005-09-29 TW TW094134108A patent/TW200626561A/zh unknown
- 2005-09-29 BR BRPI0516748A patent/BRPI0516748B8/pt not_active IP Right Cessation
- 2005-09-29 CN CN2005800325534A patent/CN101027288B/zh not_active Expired - Fee Related
- 2005-09-29 MX MX2007003796A patent/MX2007003796A/es active IP Right Grant
- 2005-09-29 CA CA2575472A patent/CA2575472C/en not_active Expired - Fee Related
- 2005-09-29 WO PCT/EP2005/054932 patent/WO2006035069A1/en not_active Ceased
- 2005-09-30 AR ARP050104155A patent/AR051315A1/es not_active Application Discontinuation
-
2007
- 2007-01-30 IL IL181056A patent/IL181056A/en active IP Right Grant
- 2007-03-29 ZA ZA200702656A patent/ZA200702656B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2410379C2 (ru) | 2011-01-27 |
| ES2380631T3 (es) | 2012-05-17 |
| WO2006035069A1 (en) | 2006-04-06 |
| EP1797047B1 (en) | 2012-01-25 |
| AU2005288866B2 (en) | 2012-07-26 |
| IL181056A (en) | 2014-02-27 |
| JP5046943B2 (ja) | 2012-10-10 |
| BRPI0516748B1 (pt) | 2019-11-19 |
| IL181056A0 (en) | 2007-07-04 |
| ATE542802T1 (de) | 2012-02-15 |
| MX2007003796A (es) | 2007-04-25 |
| CA2575472C (en) | 2013-07-30 |
| CA2575472A1 (en) | 2006-04-06 |
| US20080262007A1 (en) | 2008-10-23 |
| RU2007116172A (ru) | 2008-11-10 |
| TW200626561A (en) | 2006-08-01 |
| US8946248B2 (en) | 2015-02-03 |
| AU2005288866A1 (en) | 2006-04-06 |
| ZA200702656B (en) | 2008-08-27 |
| BRPI0516748B8 (pt) | 2021-05-25 |
| JP2008514681A (ja) | 2008-05-08 |
| BRPI0516748A (pt) | 2008-09-23 |
| KR20070057837A (ko) | 2007-06-07 |
| CN101027288A (zh) | 2007-08-29 |
| EP1797047A1 (en) | 2007-06-20 |
| CN101027288B (zh) | 2013-04-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |