BRPI0516748A - pirimidinas 5-substituìdas inibidoras de hiv - Google Patents
pirimidinas 5-substituìdas inibidoras de hivInfo
- Publication number
- BRPI0516748A BRPI0516748A BRPI0516748-5A BRPI0516748A BRPI0516748A BR PI0516748 A BRPI0516748 A BR PI0516748A BR PI0516748 A BRPI0516748 A BR PI0516748A BR PI0516748 A BRPI0516748 A BR PI0516748A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- aryl
- amino
- halo
- mono
- Prior art date
Links
- -1 5-substituted pyrimidines Chemical class 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000001475 halogen functional group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl 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
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000003277 amino 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
- 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 Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 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
PIRIMIDINAS 5-SUBSTITUìDAS INIBIDORAS DE HIV. Inibidores de replicação de HIV de fórmula (1), um N-óxido, um sal de adição farmaceuticamente aceitável, uma amina quaternária ou uma forma estereoquimicamente isomérica destes, em que A é CH~ 2~-CH~ 2~, -CH=CH, -C<154>C-; R é hidrogênio, arila, formila, C~ 1-6~ alquilcarbonila, C~ 1-6~ alquila, C~ 1-6~ alquiloxicarbonila, R é hidróxi, halo, C~ 1-6~ alquila, carboxila, ciano, -C(=O)R¬ 6¬, nitro, amino, mono ou di(C~ 1-6~ alquil)amino, polialometila; X~ 1~ é -NR-, -O-, -S-, -S(=O)~ p~-; R é H, C~ 1-6~ alquila, halo; R¬ 4¬ é H, C~ 1-6~ alquila, halo; R¬ 5¬ é nitro, amino, mono e di-C~ 1- 4~ alquilamino, arila, halo, -CHO, -CO-R¬ 6¬, -COOR¬ 7¬, -NH-C(=O)H, -NH-C(=O)R¬ 6¬, -CH=N-O-R¬ 8¬; R¬ 6¬ é C~ 1~-C~ 4~ alquila, amino, mono ou di(C1-4 alquil)amino, ou polialo C~ 1-4~ alquila; R¬ 7¬ é hidrogênio, C~ 1-6~ alquila, aril C~ 1-6~ alquila; R¬ 8¬ é hidrogênio, C~ 1-6~ alquila, arila; cada p é 1 ou 2; arila é opcionalmente substituída por fenila; composições farmacêuticas que contêm esses compostos como ingrediente ativo e processos para preparar os ditos compostos e composições.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04104805 | 2004-09-30 | ||
| PCT/EP2005/054932 WO2006035069A1 (en) | 2004-09-30 | 2005-09-29 | Hiv inhibiting 5-substituted pyrimidines |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0516748A true BRPI0516748A (pt) | 2008-09-23 |
| BRPI0516748B1 BRPI0516748B1 (pt) | 2019-11-19 |
| BRPI0516748B8 BRPI0516748B8 (pt) | 2021-05-25 |
Family
ID=34929637
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0516748A BRPI0516748B8 (pt) | 2004-09-30 | 2005-09-29 | pirimidinas 5-substituídas inibidoras de hiv e composição farmacêutica que as compreende |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8946248B2 (pt) |
| EP (1) | EP1797047B1 (pt) |
| JP (1) | JP5046943B2 (pt) |
| KR (1) | KR20070057837A (pt) |
| CN (1) | CN101027288B (pt) |
| AR (1) | AR051315A1 (pt) |
| AT (1) | ATE542802T1 (pt) |
| AU (1) | AU2005288866B2 (pt) |
| BR (1) | BRPI0516748B8 (pt) |
| CA (1) | CA2575472C (pt) |
| ES (1) | ES2380631T3 (pt) |
| IL (1) | IL181056A (pt) |
| MX (1) | MX2007003796A (pt) |
| RU (1) | RU2410379C2 (pt) |
| TW (1) | TW200626561A (pt) |
| WO (1) | WO2006035069A1 (pt) |
| ZA (1) | ZA200702656B (pt) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5046943B2 (ja) | 2004-09-30 | 2012-10-10 | テイボテク・フアーマシユーチカルズ | Ｈｉｖ阻害性５−置換ピリミジン |
| WO2006035067A2 (en) * | 2004-09-30 | 2006-04-06 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5-heterocyclyl pyrimidines |
| ES2533258T3 (es) * | 2005-02-18 | 2015-04-08 | Janssen Sciences Ireland Uc | Derivados de óxido de 2-(4-cianofenilamino)pirimidina que inhiben el VIH |
| CN101405283B (zh) * | 2006-03-30 | 2014-06-18 | 泰博特克药品有限公司 | Hiv抑制性5-酰氨基取代的嘧啶类化合物 |
| AU2007341227C1 (en) * | 2006-12-29 | 2013-08-29 | Janssen Sciences Ireland Uc | HIV inhibiting 6-substituted pyrimidines |
| AU2007341228B2 (en) * | 2006-12-29 | 2013-04-18 | Janssen Sciences Ireland Uc | HIV inhibiting 5,6-substituted pyrimidines |
| US9139534B2 (en) | 2011-04-22 | 2015-09-22 | Signal Pharmaceuticals, Llc | Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith |
| EP2872492B1 (en) * | 2012-07-12 | 2018-01-31 | Hetero Research Foundation | Process for the preparation of rilpivirine using a novel intermediate |
| ES2648226T3 (es) * | 2012-11-08 | 2017-12-29 | Bristol-Myers Squibb Company | Compuestos de pirimidina sustituidos con alquilamida útiles en la modulación de IL-12, IL-23 y/o IFN |
| 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 |
| US9513297B2 (en) | 2014-12-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-Jun N-terminal kinase in skin |
| CN107108524A (zh) | 2014-12-16 | 2017-08-29 | 西格诺药品有限公司 | 2‑(叔丁基氨基)‑4‑((1r,3r,4r)‑3‑羟基‑4‑甲基环己基氨基)‑嘧啶‑5‑甲酰胺的配制物 |
| EP3250557B1 (en) | 2015-01-29 | 2024-11-20 | Signal Pharmaceuticals, LLC | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| CN107922287B (zh) | 2015-07-24 | 2021-04-09 | 细胞基因公司 | 合成(1r,2r,5r)-5-氨基-2-甲基环己醇盐酸盐的方法和其中可用的中间体 |
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 |
| BR9611562A (pt) | 1995-11-23 | 1999-03-02 | Janssen Pharmaceutica Nv | Misturas sólidas de ciclodextrinas preparadas via extrusão sob fusão |
| 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 |
| EA002973B1 (ru) | 1998-03-27 | 2002-12-26 | Янссен Фармацевтика Н.В. | Производные пиримидина в качестве ингибиторов репликации вируса иммунодефицита человека |
| SK287270B6 (sk) | 1998-11-10 | 2010-05-07 | Janssen Pharmaceutica N. V. | Derivát pyrimidínu |
| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| AU783981C (en) * | 2000-05-08 | 2007-05-03 | Janssen Pharmaceutica N.V. | HIV replication inhibitors |
| US6989385B2 (en) * | 2000-12-21 | 2006-01-24 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| 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 |
| EA009871B1 (ru) | 2002-11-15 | 2008-04-28 | Тиботек Фармасьютикалз Лтд. | Замещённые индолпиридиниевые соединения в качестве противоинфекционного средства |
| US7504396B2 (en) * | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| WO2006035067A2 (en) * | 2004-09-30 | 2006-04-06 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5-heterocyclyl pyrimidines |
| ES2371924T3 (es) * | 2004-09-30 | 2012-01-11 | Tibotec Pharmaceuticals | Pirimidinas 5-carbo o heterociclo- sustituidas que inhiben el hiv. |
| JP5046943B2 (ja) | 2004-09-30 | 2012-10-10 | テイボテク・フアーマシユーチカルズ | Ｈｉｖ阻害性５−置換ピリミジン |
| CN101405283B (zh) | 2006-03-30 | 2014-06-18 | 泰博特克药品有限公司 | Hiv抑制性5-酰氨基取代的嘧啶类化合物 |
| AU2007341227C1 (en) * | 2006-12-29 | 2013-08-29 | Janssen Sciences Ireland Uc | HIV inhibiting 6-substituted pyrimidines |
| AU2007341228B2 (en) * | 2006-12-29 | 2013-04-18 | Janssen Sciences Ireland Uc | HIV inhibiting 5,6-substituted pyrimidines |
-
2005
- 2005-09-29 JP JP2007534028A patent/JP5046943B2/ja not_active Expired - Fee Related
- 2005-09-29 BR BRPI0516748A patent/BRPI0516748B8/pt not_active IP Right Cessation
- 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 CN CN2005800325534A patent/CN101027288B/zh not_active Expired - Fee Related
- 2005-09-29 KR KR1020077006048A patent/KR20070057837A/ko not_active Ceased
- 2005-09-29 AT AT05789686T patent/ATE542802T1/de active
- 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 TW TW094134108A patent/TW200626561A/zh unknown
- 2005-09-29 ES ES05789686T patent/ES2380631T3/es active Active
- 2005-09-29 WO PCT/EP2005/054932 patent/WO2006035069A1/en not_active Ceased
- 2005-09-29 US US11/576,315 patent/US8946248B2/en not_active Expired - Fee Related
- 2005-09-29 RU RU2007116172/04A patent/RU2410379C2/ru active
- 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 |
|---|---|
| US20080262007A1 (en) | 2008-10-23 |
| AU2005288866B2 (en) | 2012-07-26 |
| IL181056A (en) | 2014-02-27 |
| CN101027288A (zh) | 2007-08-29 |
| EP1797047A1 (en) | 2007-06-20 |
| CA2575472A1 (en) | 2006-04-06 |
| ZA200702656B (en) | 2008-08-27 |
| IL181056A0 (en) | 2007-07-04 |
| ES2380631T3 (es) | 2012-05-17 |
| AR051315A1 (es) | 2007-01-03 |
| WO2006035069A1 (en) | 2006-04-06 |
| EP1797047B1 (en) | 2012-01-25 |
| CA2575472C (en) | 2013-07-30 |
| RU2007116172A (ru) | 2008-11-10 |
| AU2005288866A1 (en) | 2006-04-06 |
| KR20070057837A (ko) | 2007-06-07 |
| RU2410379C2 (ru) | 2011-01-27 |
| ATE542802T1 (de) | 2012-02-15 |
| BRPI0516748B1 (pt) | 2019-11-19 |
| CN101027288B (zh) | 2013-04-17 |
| US8946248B2 (en) | 2015-02-03 |
| MX2007003796A (es) | 2007-04-25 |
| JP5046943B2 (ja) | 2012-10-10 |
| BRPI0516748B8 (pt) | 2021-05-25 |
| JP2008514681A (ja) | 2008-05-08 |
| TW200626561A (en) | 2006-08-01 |
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Legal Events
| Date | Code | Title | Description |
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| B25D | Requested change of name of applicant approved |
Owner name: TIBOTEC PHARMACEUTICALS (IE) |
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| B25D | Requested change of name of applicant approved |
Owner name: JANSSEN R AND D IRELAND (IE) |
|
| B25A | Requested transfer of rights approved |
Owner name: JANSSEN SCIENCES IRELAND UC (IE) |
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| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
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| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 19/11/2019, OBSERVADAS AS CONDICOES LEGAIS. (CO) 10 (DEZ) ANOS CONTADOS A PARTIR DE 19/11/2019, OBSERVADAS AS CONDICOES LEGAIS |
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| B16C | Correction of notification of the grant [chapter 16.3 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 29/09/2005 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF |
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| B21F | Lapse acc. art. 78, item iv - on non-payment of the annual fees in time |
Free format text: REFERENTE A 17A ANUIDADE. |
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| B24J | Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12) |
Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2690 DE 26-07-2022 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |