BRPI0612317B8 - benzimidazóis 2-substituídos, seu processo de preparação e composição farmacêutica - Google Patents
benzimidazóis 2-substituídos, seu processo de preparação e composição farmacêuticaInfo
- Publication number
- BRPI0612317B8 BRPI0612317B8 BRPI0612317A BRPI0612317A BRPI0612317B8 BR PI0612317 B8 BRPI0612317 B8 BR PI0612317B8 BR PI0612317 A BRPI0612317 A BR PI0612317A BR PI0612317 A BRPI0612317 A BR PI0612317A BR PI0612317 B8 BRPI0612317 B8 BR PI0612317B8
- Authority
- BR
- Brazil
- Prior art keywords
- 6alkyl
- het
- heterocycle
- thiomorpholinyl
- substituted
- Prior art date
Links
- -1 2-substituted benzimidazoles Chemical class 0.000 title abstract 8
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 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
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000005987 1-oxo-thiomorpholinyl group Chemical group 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
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 2
- 125000005988 1,1-dioxo-thiomorpholinyl group Chemical group 0.000 abstract 1
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 abstract 1
- HEAHLTGDUHXTTO-UHFFFAOYSA-N 1,3-thiazolidine 1,1-dioxide Chemical compound O=S1(=O)CCNC1 HEAHLTGDUHXTTO-UHFFFAOYSA-N 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 abstract 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000001786 isothiazolyl group Chemical group 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 abstract 1
- 125000000160 oxazolidinyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000004590 pyridopyridyl group Chemical group N1=C(C=CC2=C1C=CC=N2)* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 230000010076 replication Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- PGAZQSBUJDVGIX-UHFFFAOYSA-N thiazepane Chemical compound C1CCNSCC1 PGAZQSBUJDVGIX-UHFFFAOYSA-N 0.000 abstract 1
- NFRGCMIFZVPLSJ-UHFFFAOYSA-N thiazepane 1,1-dioxide Chemical compound O=S1(=O)CCCCCN1 NFRGCMIFZVPLSJ-UHFFFAOYSA-N 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 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
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
benzimidazóis 2-substituídos a presente invenção refere-se a inibidores de replicação de (rsv) de fórmula (i), (i) aos sais de adição e formas estereoquimicamente isoméricas desses inibidores, em que q é hidrgênio, c1-6alquila opcionalmente substituídas por um heterociclo ou q é c1-6alquila substituída tanto por -or4 quanto por um heterociclo; em que esse heterociclo é oxazolidina, tiazolidina, 1-oxo-tiomorfolinila, 1,1-dioxotiazolidina, morfolinia, tiomorfolinila, 1-oxo-tiomorfolinila, 1,1-dioxotiomorfolinila, hexaidroxazepina, hexaidro-tiazepina, 1-oxo-hexaidrotiazepina, 1,1-dioxo-hexaidrotiazepina, pirrolidina, piperidina, homopiperidina, piperazina, heterociclo este que poderá ser substituído por 1-2 substituintes; cada alq é c1-6alcanodiila; r1 e ar2 ou piperidinila, piperazinila, morfonila, tiomorfolinila, piridila, pirazinila, piridazinila, pirimidinila, furanila, tetraidrofuranila, tienila, pirrolila, tiazolila, oxazolila, imidazolila, isotiazolila, pirazolila, isoxazolila, oxadiazolila, quinilinila, quinoxalinila, benzofuranila, benzotienila, benzimidazolila, benzoxazolila, benzoxazolila, benztiazolila, piridopiridila, naftiridinila, 1h-imidazo[4,5-b]piridinila, 3h-imidazo[4,5-b]piridinila, imidazo[1,2-a]piridinila ou 2,3-diidro-1,4-dioxino[2,3-b]piridila; r3 é hidróxic1-6alquila, c1-6alcóxic1-6alquila, cianoc1-6alquila, aminocarbonil-c1-6aquila, mono- ou di(c1-6alquil)aminocarbonil-c1-6aquila, carboxil-c1-6alquila, c1-6alcoxicarbonil-c1-6alquila; r2 é hidrogênio ou c1-6alquila; r3 e r4 são hidrogênio, c1-6alquila, ar2, ar2c1-6alquila, c1-6alquilcarbonila, ar2carbonila, ar2c1-6alquilcarbonila, c1-6alquilsulfonila, aminossulfonila, ar1sulfonila, ar1c1-6alquilsulfonila, c1-6alquilóxic1-6alquila, aminoc1-6alquila, mono- ou di(c1-6alquil)aminoc1-6alquila, hidróxic1-6alquila, aminocarbonilc1-6alquila, c1-6alquiloxicarbonilc1-6aquila, hidroxicarbonilc1-6aquila, aminossulfonilc1-6alquila, het, het-c1-6alquila, het-carbonila, het-sulfonila, het-c1-6alquilsulfonila e het-c1-6alquilcarbonila; het é um heterociclo opcionalmente substituído; composições farmacêuticas que contêm compostos (i) e processos para preparação de compostos (i).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05076440.6 | 2005-06-20 | ||
| EP05076440 | 2005-06-20 | ||
| PCT/EP2006/063367 WO2006136563A1 (en) | 2005-06-20 | 2006-06-20 | 2-substituted benzimidazoles |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0612317A2 BRPI0612317A2 (pt) | 2010-11-03 |
| BRPI0612317B1 BRPI0612317B1 (pt) | 2019-12-03 |
| BRPI0612317B8 true BRPI0612317B8 (pt) | 2021-05-25 |
Family
ID=35285274
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0612317A BRPI0612317B8 (pt) | 2005-06-20 | 2006-06-20 | benzimidazóis 2-substituídos, seu processo de preparação e composição farmacêutica |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US7884215B2 (pt) |
| EP (1) | EP1896450B1 (pt) |
| JP (1) | JP5070207B2 (pt) |
| CN (1) | CN101203507B (pt) |
| AU (1) | AU2006260971B2 (pt) |
| BR (1) | BRPI0612317B8 (pt) |
| CA (1) | CA2612265C (pt) |
| ES (1) | ES2392863T3 (pt) |
| MX (1) | MX2007016313A (pt) |
| PL (1) | PL1896450T3 (pt) |
| RU (1) | RU2441866C2 (pt) |
| WO (1) | WO2006136563A1 (pt) |
| ZA (1) | ZA200711092B (pt) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8211928B2 (en) * | 2009-05-29 | 2012-07-03 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| CN116082247B (zh) * | 2023-01-19 | 2025-08-01 | 浙江工业大学 | 一种苯并咪唑类衍生物及其应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1418175A1 (en) | 1999-06-28 | 2004-05-12 | Janssen Pharmaceutica N.V. | Respiratory syncytial virus replication inhibitors |
| MXPA02000120A (es) * | 1999-06-28 | 2002-07-02 | Janssen Pharmaceutica Nv | Inhibidores de la replicacion del virus sincitial respiratorio. |
| JP2003503403A (ja) * | 1999-06-28 | 2003-01-28 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 呼吸合胞体ウイルス複製阻害剤 |
| US6489338B2 (en) | 2000-06-13 | 2002-12-03 | Bristol-Myers Squibb Company | Imidazopyridine and imidazopyrimidine antiviral agents |
| US7030150B2 (en) * | 2001-05-11 | 2006-04-18 | Trimeris, Inc. | Benzimidazole compounds and antiviral uses thereof |
| US20040166137A1 (en) * | 2002-11-08 | 2004-08-26 | Lackey John William | Hetero-substituted benzimidazole compounds and antiviral uses thereof |
| CA2521907A1 (en) * | 2003-04-10 | 2004-10-21 | Pfizer Inc. | Bicyclic compounds as nr2b receptor antagonists |
-
2006
- 2006-06-20 PL PL06777372T patent/PL1896450T3/pl unknown
- 2006-06-20 ES ES06777372T patent/ES2392863T3/es not_active Expired - Lifetime
- 2006-06-20 AU AU2006260971A patent/AU2006260971B2/en not_active Ceased
- 2006-06-20 CN CN2006800220166A patent/CN101203507B/zh not_active Expired - Fee Related
- 2006-06-20 CA CA2612265A patent/CA2612265C/en not_active Expired - Lifetime
- 2006-06-20 WO PCT/EP2006/063367 patent/WO2006136563A1/en not_active Ceased
- 2006-06-20 RU RU2008102117/04A patent/RU2441866C2/ru active
- 2006-06-20 EP EP06777372A patent/EP1896450B1/en not_active Expired - Lifetime
- 2006-06-20 BR BRPI0612317A patent/BRPI0612317B8/pt not_active IP Right Cessation
- 2006-06-20 MX MX2007016313A patent/MX2007016313A/es active IP Right Grant
- 2006-06-20 JP JP2008517489A patent/JP5070207B2/ja not_active Expired - Fee Related
- 2006-06-20 US US11/993,136 patent/US7884215B2/en active Active
-
2007
- 2007-12-19 ZA ZA200711092A patent/ZA200711092B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006260971A1 (en) | 2006-12-28 |
| EP1896450B1 (en) | 2012-08-15 |
| CA2612265C (en) | 2014-08-19 |
| US7884215B2 (en) | 2011-02-08 |
| CN101203507B (zh) | 2012-05-23 |
| ES2392863T3 (es) | 2012-12-14 |
| MX2007016313A (es) | 2008-03-07 |
| ZA200711092B (en) | 2009-03-25 |
| BRPI0612317B1 (pt) | 2019-12-03 |
| JP5070207B2 (ja) | 2012-11-07 |
| JP2008546740A (ja) | 2008-12-25 |
| BRPI0612317A2 (pt) | 2010-11-03 |
| US20100092426A1 (en) | 2010-04-15 |
| RU2441866C2 (ru) | 2012-02-10 |
| WO2006136563A1 (en) | 2006-12-28 |
| CN101203507A (zh) | 2008-06-18 |
| RU2008102117A (ru) | 2009-07-27 |
| AU2006260971B2 (en) | 2011-09-15 |
| EP1896450A1 (en) | 2008-03-12 |
| CA2612265A1 (en) | 2006-12-28 |
| PL1896450T3 (pl) | 2013-01-31 |
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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 03/12/2019, OBSERVADAS AS CONDICOES LEGAIS. (CO) 10 (DEZ) ANOS CONTADOS A PARTIR DE 03/12/2019, 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 20/06/2006 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 |
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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 2780 DE 16-04-2024 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. |