BRPI0516748A - pirimidinas 5-substituìdas inibidoras de hiv - Google Patents

pirimidinas 5-substituìdas inibidoras de hiv

Info

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
Application number
BRPI0516748-5A
Other languages
English (en)
Inventor
Jerome Emile Georges Guillemont
Jan Heeres
Paulus Joannes Lewi
Original Assignee
Tibotec Pharm Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34929637&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0516748(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of BRPI0516748A publication Critical patent/BRPI0516748A/pt
Publication of BRPI0516748B1 publication Critical patent/BRPI0516748B1/pt
Publication of BRPI0516748B8 publication Critical patent/BRPI0516748B8/pt

Links

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)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • General Chemical & Material Sciences (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (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.
BRPI0516748A 2004-09-30 2005-09-29 pirimidinas 5-substituídas inibidoras de hiv e composição farmacêutica que as compreende BRPI0516748B8 (pt)

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005288864B2 (en) * 2004-09-30 2012-08-23 Janssen Sciences Ireland Uc HIV inhibiting 5-heterocyclyl pyrimidines
CN101027288B (zh) 2004-09-30 2013-04-17 泰博特克药品有限公司 抑制hiv的5-取代嘧啶
BRPI0607811B8 (pt) * 2005-02-18 2021-05-25 Janssen R & D Ireland derivados de óxido de pirimidina de 2-(4-cianofenilamino) inibidores de hiv, composição farmacêutica compreendendo os mesmos, processo para preparar a referida composição e uso
EP2004632B1 (en) * 2006-03-30 2014-03-12 Janssen R&D Ireland Hiv inhibiting 5-amido substituted pyrimidines
AU2007341228B2 (en) * 2006-12-29 2013-04-18 Janssen Sciences Ireland Uc HIV inhibiting 5,6-substituted pyrimidines
BRPI0720858B8 (pt) * 2006-12-29 2021-05-25 Janssen R & D Ireland pirimidinas 6-substituídas inibidoras de hiv e composição farmacêutica que as compreende
TWI548621B (zh) 2011-04-22 2016-09-11 標誌製藥公司 經取代之二胺基甲醯胺及二胺基甲腈嘧啶、其組合物、及以該等治療之方法
US9139535B2 (en) * 2012-07-12 2015-09-22 Hetero Research Foundation Process for rilpivirine using novel intermediate
EP2917186B1 (en) * 2012-11-08 2017-10-18 Bristol-Myers Squibb Company Alkyl amide-substituted pyrimidine compounds useful in the modulation of il-12, il-23 and/or 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
EA033530B1 (ru) 2014-12-16 2019-10-31 Signal Pharm Llc Композиции 2-(трет-бутиламино)-4-((1r,3r,4r)-3-гидрокси-4-метилциклогексиламино)пиримидин-5-карбоксамида
JP6903577B2 (ja) 2014-12-16 2021-07-14 シグナル ファーマシューティカルズ，エルエルシー 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法
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
US10252981B2 (en) 2015-07-24 2019-04-09 Celgene Corporation Methods of synthesis of (1R,2R,5R)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3459731A (en) * 1966-12-16 1969-08-05 Corn Products Co Cyclodextrin polyethers and their production
CZ154398A3 (cs) 1995-11-23 1998-08-12 Janssen Pharmaceutica N.V. Pevné směsi cyklodextrinů připravené vytlačováním taveniny
NO311614B1 (no) 1996-10-01 2001-12-17 Janssen Pharmaceutica Nv Substituerte diamino-1,3,5-triazinderivater
ATE232521T1 (de) 1998-03-27 2003-02-15 Janssen Pharmaceutica Nv Hiv hemmende pyrimidin derivate
EP0945447A1 (en) 1998-03-27 1999-09-29 Janssen Pharmaceutica N.V. Trisubstituted 1,3,5-triazine derivatives for treatment of HIV infections
BRPI9915552B8 (pt) * 1998-11-10 2021-05-25 Janssen Pharmaceutica Nv pirimidinas inibidoras da reprodução do hiv
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
EP1282606B1 (en) 2000-05-08 2015-04-22 Janssen Pharmaceutica NV Hiv replication inhibiting pyrimidines and triazines
US20030105090A1 (en) * 2000-12-21 2003-06-05 David Bebbington 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
MXPA05005146A (es) 2002-11-15 2005-07-22 Tibotec Pharm Ltd Indolpiridinio sustituido como compuestos antiinfecciosos.
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
US7531548B2 (en) * 2004-09-30 2009-05-12 Tibotec Pharmaceuticals Ltd HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines
AU2005288864B2 (en) 2004-09-30 2012-08-23 Janssen Sciences Ireland Uc HIV inhibiting 5-heterocyclyl pyrimidines
CN101027288B (zh) 2004-09-30 2013-04-17 泰博特克药品有限公司 抑制hiv的5-取代嘧啶
EP2004632B1 (en) 2006-03-30 2014-03-12 Janssen R&D Ireland Hiv inhibiting 5-amido substituted pyrimidines
BRPI0720858B8 (pt) 2006-12-29 2021-05-25 Janssen R & D Ireland pirimidinas 6-substituídas inibidoras de hiv e composição farmacêutica que as compreende
AU2007341228B2 (en) * 2006-12-29 2013-04-18 Janssen Sciences Ireland Uc HIV inhibiting 5,6-substituted pyrimidines

Also Published As

Publication number Publication date
AU2005288866B2 (en) 2012-07-26
CN101027288A (zh) 2007-08-29
TW200626561A (en) 2006-08-01
JP5046943B2 (ja) 2012-10-10
WO2006035069A1 (en) 2006-04-06
IL181056A (en) 2014-02-27
ATE542802T1 (de) 2012-02-15
JP2008514681A (ja) 2008-05-08
ZA200702656B (en) 2008-08-27
CA2575472C (en) 2013-07-30
ES2380631T3 (es) 2012-05-17
CA2575472A1 (en) 2006-04-06
BRPI0516748B1 (pt) 2019-11-19
IL181056A0 (en) 2007-07-04
US20080262007A1 (en) 2008-10-23
AR051315A1 (es) 2007-01-03
AU2005288866A1 (en) 2006-04-06
KR20070057837A (ko) 2007-06-07
BRPI0516748B8 (pt) 2021-05-25
EP1797047B1 (en) 2012-01-25
EP1797047A1 (en) 2007-06-20
RU2007116172A (ru) 2008-11-10
US8946248B2 (en) 2015-02-03
RU2410379C2 (ru) 2011-01-27
MX2007003796A (es) 2007-04-25
CN101027288B (zh) 2013-04-17

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Legal Events

Date Code Title Description
B25D Requested change of name of applicant approved

Owner name: TIBOTEC PHARMACEUTICALS (IE)

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)

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

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

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

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 17A ANUIDADE.

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.