BRPI0507076A - quinolinas substituìdas e seu uso como inibidores micobacterianos - Google Patents
quinolinas substituìdas e seu uso como inibidores micobacterianosInfo
- Publication number
- BRPI0507076A BRPI0507076A BRPI0507076-7A BRPI0507076A BRPI0507076A BR PI0507076 A BRPI0507076 A BR PI0507076A BR PI0507076 A BRPI0507076 A BR PI0507076A BR PI0507076 A BRPI0507076 A BR PI0507076A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- hydrogen
- het
- alkyloxy
- hydroxy
- Prior art date
Links
- 150000003248 quinolines Chemical class 0.000 title abstract 3
- 229940111121 antirheumatic drug quinolines Drugs 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 150000002431 hydrogen Chemical class 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- -1 cyano, hydroxy Chemical group 0.000 abstract 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 2
- 125000006350 alkyl thio alkyl group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 208000027531 mycobacterial infectious disease Diseases 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 241000589343 Methylobacter luteus Species 0.000 abstract 1
- 241000186367 Mycobacterium avium Species 0.000 abstract 1
- 241000187492 Mycobacterium marinum Species 0.000 abstract 1
- 241000187480 Mycobacterium smegmatis Species 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 229940027991 antiseptic and disinfectant quinoline derivative Drugs 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 230000001717 pathogenic effect Effects 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
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000008827 tuberculosis Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- 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
- A61P31/10—Antimycotics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
QUINOLINAS SUBSTITUìDAS E SEU USO COMO INIBIDORES MICOBACTERIANOS. A presente invenção refere-se a novos derivados de quinolina substituida de acordo com a fórmula geral (la) ou com a fómula geral (lb) bem como a sais, amina quaternárias, formas estereoquimicamente isoméricas, formas tautoméricas e formas de N-óxido desses derivados, onde R¬ 1¬ é hidrogênio, halo, haloalquila, ciano, hidróxi, Ar, Het, alquila, alquilóxi, alquilito, alquiloxialquila, alquiltioalquila, Ar-alquila ou di(Ar)alquila; p é 1, 2, 3 ou 4; R¬ 2¬ é hidrogênio, hidróxi, tio, alquilólxi, alquiloxialquilóxi, alquiltio, mono ou di(alquil)amino ou um radical de fórmula ; R¬ 3¬ é alquila, Ar, Ar-alquila, Het ou Het-alquila; R¬ 4¬ é hidrogênio, alquila ou benzila; R¬ 5¬ é hidrogênio, halo, haloalquila, hidróxi, Ar, alquila, alquilóxi, alquiltio, alquiloxialquila, alquiltioalquila, Ar-alquila ou di(Ar)alquila; ou dois radicais vicinais R¬ 5¬ poderão ser tornados juntos para formar juntamente com o anel fenila ao qual se ligam uma naftila; r é 1,2,3,4 ou 5; R¬ 6¬ é hidrogênio, alquila, Ar ou Het; R¬ 7¬ é hidrogênio ou alquila; R¬ 8¬ é oxo; ou R¬ 7¬ e R¬ 8¬ tomados juntos formam o radical -CH<154>CH-N<154>; Z é CH~ 2~ ou C(<154>O). Os compostos reivindicados são úteis para o tratamento de doenças micobacterianas, particularmente aquelas doenças causadas por micobactérias patogênicas tais como M. tuberculosis, M.bovis, M. avium, M. smegmatis e M. marinum. Também são reivindicados uma composição farmacêutica que contém um composto da presente invenção, o uso dos compostos ou composições reivindicados para a produção de um medicamento para o tratamento de doenças micobacterianas e um processo para preparar os compostos reivindicados.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US53876804P | 2004-01-23 | 2004-01-23 | |
| US60/538,768 | 2004-01-23 | ||
| PCT/EP2005/050267 WO2005070924A1 (en) | 2004-01-23 | 2005-01-21 | Substituted quinolines and their use as mycobacterial inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0507076A true BRPI0507076A (pt) | 2007-06-19 |
| BRPI0507076B1 BRPI0507076B1 (pt) | 2019-06-25 |
| BRPI0507076B8 BRPI0507076B8 (pt) | 2021-05-25 |
Family
ID=34807224
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0507076A BRPI0507076B8 (pt) | 2004-01-23 | 2005-01-21 | quinolinas substituídas, seu processo de preparação, composição farmacêutica que as compreende e seu uso como inibidores micobacterianos |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7338949B2 (pt) |
| EP (1) | EP1711492B1 (pt) |
| JP (1) | JP4773975B2 (pt) |
| KR (1) | KR101150172B1 (pt) |
| CN (1) | CN1910177B (pt) |
| AP (1) | AP2188A (pt) |
| AT (1) | ATE392423T1 (pt) |
| AU (1) | AU2005206330B2 (pt) |
| BR (1) | BRPI0507076B8 (pt) |
| CA (1) | CA2553266C (pt) |
| DE (1) | DE602005006101T2 (pt) |
| EA (1) | EA011359B1 (pt) |
| ES (1) | ES2306082T3 (pt) |
| IL (1) | IL177013A0 (pt) |
| NO (1) | NO337705B1 (pt) |
| NZ (1) | NZ547277A (pt) |
| UA (1) | UA85570C2 (pt) |
| WO (1) | WO2005070924A1 (pt) |
| ZA (1) | ZA200606070B (pt) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA011572B9 (ru) * | 2004-01-29 | 2018-01-31 | Янссен Фармацевтика Н.В. | Производные хинолина для применения в качестве микобактериальных ингибиторов |
| CA2528849C (en) * | 2005-06-08 | 2014-01-14 | Janssen Pharmaceutica N.V. | Quinoline derivatives as antibacterial agents |
| JO2837B1 (en) * | 2005-08-03 | 2014-09-15 | جانسن فارمسيتكا ان في | Quinoline derivatives acting as antibacterial agents |
| JO2855B1 (en) | 2005-08-03 | 2015-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinoline derivatives acting as antibacterial agents |
| WO2007022946A1 (de) | 2005-08-21 | 2007-03-01 | Abbott Gmbh & Co. Kg | Heterocyclische verbindungen und ihre verwendung als bindungspartner für 5-ht5-rezeptoren |
| JO2685B1 (en) | 2006-12-06 | 2013-03-03 | جانسين فارماسوتيكا ان في | Quinoline antibacterial derivatives |
| JO3271B1 (ar) | 2006-12-06 | 2018-09-16 | Janssen Pharmaceutica Nv | مشتقات الكوينولين المضادة للجراثيم |
| JO2684B1 (en) * | 2006-12-06 | 2013-03-03 | جانسين فارماسوتيكا ان في | Quinoline antibacterial derivatives |
| JO2970B1 (en) | 2006-12-06 | 2016-03-15 | جانسين فارماسوتيكا ان. في | Quinoline antibacterial derivatives |
| CA2711912A1 (en) * | 2008-01-14 | 2009-07-23 | Jyoti Chattopadhyaya | Quinoline, naphthalene and conformationally constrained quinoline or naphthalene derivates as anti-mycobacterial agents |
| KR102110355B1 (ko) * | 2012-04-27 | 2020-05-14 | 얀센 파마슈티카 엔.브이. | 항균성 퀴놀린 유도체 |
| CA2869453C (en) * | 2012-04-27 | 2021-03-02 | Janssen Pharmaceutica Nv | Antibacterial quinoline derivatives |
| CA2984202A1 (en) * | 2015-04-29 | 2016-11-03 | The State Of Israel, Ministry Of Agriculture & Rural Development, Agricultural Research Organization (Aro) (Volcani Center) | Anti-phytopathogenic compositions |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5965572A (en) | 1996-10-28 | 1999-10-12 | The United States Of America As Respresented By The Secretary Of The Army | Methods for treating antibiotic-resistant infections |
| AU740603B2 (en) * | 1997-06-02 | 2001-11-08 | Janssen Pharmaceutica N.V. | (imidazol-5-yl)methyl-2-quinolinone derivatives as inhibitors of smooth muscle cell proliferation |
| US6103905A (en) | 1997-06-19 | 2000-08-15 | Sepracor, Inc. | Quinoline-indole antimicrobial agents, uses and compositions related thereto |
| US6172084B1 (en) * | 1997-06-19 | 2001-01-09 | Sepracor, Inc. | Quinoline-indole antimicrobial agents, uses and compositions related thereto |
| US6838467B2 (en) * | 2000-02-24 | 2005-01-04 | Janssen Pharmaceutica N. V. | Dosing regimen |
| CZ20031145A3 (cs) * | 2000-10-02 | 2003-12-17 | Janssen Pharmaceutica N.V. | Antagonisté metabotropního glutamátového receptoru |
| DK1527050T3 (da) | 2002-07-25 | 2010-07-19 | Janssen Pharmaceutica Nv | Quinolin-derivater og deres anvendelse som mycobakterielle inhibitorer |
-
2005
- 2005-01-21 AP AP2006003693A patent/AP2188A/xx active
- 2005-01-21 WO PCT/EP2005/050267 patent/WO2005070924A1/en not_active Ceased
- 2005-01-21 CN CN2005800026797A patent/CN1910177B/zh not_active Expired - Fee Related
- 2005-01-21 AT AT05701586T patent/ATE392423T1/de active
- 2005-01-21 EP EP05701586A patent/EP1711492B1/en not_active Expired - Lifetime
- 2005-01-21 UA UAA200605780A patent/UA85570C2/uk unknown
- 2005-01-21 ES ES05701586T patent/ES2306082T3/es not_active Expired - Lifetime
- 2005-01-21 CA CA2553266A patent/CA2553266C/en not_active Expired - Fee Related
- 2005-01-21 US US10/596,386 patent/US7338949B2/en not_active Expired - Lifetime
- 2005-01-21 EA EA200601363A patent/EA011359B1/ru not_active IP Right Cessation
- 2005-01-21 BR BRPI0507076A patent/BRPI0507076B8/pt not_active IP Right Cessation
- 2005-01-21 DE DE602005006101T patent/DE602005006101T2/de not_active Expired - Lifetime
- 2005-01-21 JP JP2006550174A patent/JP4773975B2/ja not_active Expired - Fee Related
- 2005-01-21 KR KR1020067013237A patent/KR101150172B1/ko not_active Expired - Fee Related
- 2005-01-21 NZ NZ547277A patent/NZ547277A/xx not_active IP Right Cessation
- 2005-01-21 AU AU2005206330A patent/AU2005206330B2/en not_active Ceased
-
2006
- 2006-07-20 IL IL177013A patent/IL177013A0/en active IP Right Grant
- 2006-07-21 ZA ZA200606070A patent/ZA200606070B/xx unknown
- 2006-08-22 NO NO20063747A patent/NO337705B1/no not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| AP2006003693A0 (en) | 2006-08-31 |
| NO20063747L (no) | 2006-08-22 |
| KR20060127016A (ko) | 2006-12-11 |
| CN1910177A (zh) | 2007-02-07 |
| AU2005206330A1 (en) | 2005-08-04 |
| US7338949B2 (en) | 2008-03-04 |
| CA2553266A1 (en) | 2005-08-04 |
| EP1711492B1 (en) | 2008-04-16 |
| UA85570C2 (uk) | 2009-02-10 |
| KR101150172B1 (ko) | 2012-05-25 |
| EP1711492A1 (en) | 2006-10-18 |
| AP2188A (en) | 2010-12-14 |
| BRPI0507076B1 (pt) | 2019-06-25 |
| JP4773975B2 (ja) | 2011-09-14 |
| WO2005070924A1 (en) | 2005-08-04 |
| DE602005006101D1 (de) | 2008-05-29 |
| DE602005006101T2 (de) | 2009-07-02 |
| CN1910177B (zh) | 2010-05-05 |
| BRPI0507076B8 (pt) | 2021-05-25 |
| ES2306082T3 (es) | 2008-11-01 |
| US20070082895A1 (en) | 2007-04-12 |
| NZ547277A (en) | 2009-08-28 |
| NO337705B1 (no) | 2016-06-06 |
| IL177013A0 (en) | 2006-12-10 |
| EA011359B1 (ru) | 2009-02-27 |
| ATE392423T1 (de) | 2008-05-15 |
| ZA200606070B (en) | 2007-12-27 |
| EA200601363A1 (ru) | 2006-12-29 |
| JP2007518775A (ja) | 2007-07-12 |
| CA2553266C (en) | 2013-03-12 |
| WO2005070924A8 (en) | 2006-05-11 |
| AU2005206330B2 (en) | 2010-09-16 |
| HK1100927A1 (zh) | 2007-10-05 |
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Legal Events
| Date | Code | Title | Description |
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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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| 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 25/06/2019, OBSERVADAS AS CONDICOES LEGAIS. (CO) 10 (DEZ) ANOS CONTADOS A PARTIR DE 25/06/2019, 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 21/01/2005 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 |
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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 2654 DE 16-11-2021 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. |