BR112012001817B8 - furazanobenzimidazóis, seu uso, processo de produção e composição farmacêutica - Google Patents
furazanobenzimidazóis, seu uso, processo de produção e composição farmacêuticaInfo
- Publication number
- BR112012001817B8 BR112012001817B8 BR112012001817A BR112012001817A BR112012001817B8 BR 112012001817 B8 BR112012001817 B8 BR 112012001817B8 BR 112012001817 A BR112012001817 A BR 112012001817A BR 112012001817 A BR112012001817 A BR 112012001817A BR 112012001817 B8 BR112012001817 B8 BR 112012001817B8
- Authority
- BR
- Brazil
- Prior art keywords
- alkoxy
- lower alkyl
- amino
- alkyl
- hydroxy
- Prior art date
Links
Classifications
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- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4245—Oxadiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
furazanobenzimidazóis como profármacos para tratar doenças neoplásicas ou autoimunes. a presente invenção refere-se a um composto de fórmula (ii) em que representa um resíduo benzeno divalente que é não substituído ou substituído por um ou dois substituintes adicionais independentemente selecionados de alquila inferior, halo-alquila inferior, hidróxi-alquila inferior, alcóxi inferior-alquila inferior, alcilóxi-alquila inferior, fenila, hidróxi, alcóxi inferior, hidróxi-alcóxi inferior, alcóxi inferior-alcóxi inferior, fenil-alcóxi inferior, alquilacarbonilóxi inferior, amino, mono(alquil inferior) amino, di(alquil inferior)amino, mono(alquenil inferior)amino, di(alquenil inferior)amino, alcoxicarbonilamino inferior, alquilcarbonilamino inferior, amino substituído em que os dois substituintes no nitrogênio juntos com o nitrogênio forma heterociclila, alquilcarbonila inferior, carbóxi, alcoxicarbonila inferior 15, ciano, halogênio, e nitro; ou em que dois substituintes adjacentes podem ser metilenodióxi; ou um resíduo piridina divalente (z = n) que é não substituído ou substituído adicionalmente por alquila inferior, alcóxi inferior, alcóxi inferior-alcóxi inferior, amino, opcionalmente substituído por um ou dois substituintes selecionados de alquila inferior, alquenila inferiror e alquilcarbonila, halo-alquila inferior 20, alcóxi inferior-alquila inferior, ou halogênio; r1 represente hidrogênio, alquilcarbonila inferior, hidróxi-alquila inferior ou ciano-alquila inferior; e r2 representa um grupo selecionado de: (b), (c) e (d) ou sais farmaceuticamente aceitáveis dos mesmos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09166469.8 | 2009-07-27 | ||
| EP09166469 | 2009-07-27 | ||
| PCT/EP2010/060803 WO2011012577A1 (en) | 2009-07-27 | 2010-07-26 | Furazanobenzimidazoles as prodrugs to treat neoplastic or autoimmune diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BR112012001817A2 BR112012001817A2 (pt) | 2016-03-15 |
| BR112012001817B1 BR112012001817B1 (pt) | 2020-09-29 |
| BR112012001817B8 true BR112012001817B8 (pt) | 2021-05-25 |
Family
ID=41226617
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112012001817A BR112012001817B8 (pt) | 2009-07-27 | 2010-07-26 | furazanobenzimidazóis, seu uso, processo de produção e composição farmacêutica |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8802858B2 (pt) |
| EP (1) | EP2459553B1 (pt) |
| JP (1) | JP5576485B2 (pt) |
| KR (1) | KR101758400B1 (pt) |
| CN (1) | CN102471329B (pt) |
| AU (1) | AU2010277688B2 (pt) |
| BR (1) | BR112012001817B8 (pt) |
| CA (1) | CA2767875C (pt) |
| CY (1) | CY1115809T1 (pt) |
| DK (1) | DK2459553T3 (pt) |
| EA (1) | EA021380B1 (pt) |
| ES (1) | ES2524119T3 (pt) |
| HK (1) | HK1166316A1 (pt) |
| HR (1) | HRP20141120T1 (pt) |
| IL (1) | IL217195A (pt) |
| MX (1) | MX336240B (pt) |
| NZ (1) | NZ597376A (pt) |
| PL (1) | PL2459553T3 (pt) |
| PT (1) | PT2459553E (pt) |
| RS (1) | RS53679B1 (pt) |
| SI (1) | SI2459553T1 (pt) |
| TW (1) | TWI457337B (pt) |
| UA (1) | UA106763C2 (pt) |
| WO (1) | WO2011012577A1 (pt) |
| ZA (1) | ZA201200228B (pt) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE032643T2 (en) | 2011-01-21 | 2017-10-30 | Basilea Pharmaceutica Ag | Use of BUBR1 as a biomarker for response to furazanobenzimidazoles |
| PT2666015T (pt) * | 2011-01-21 | 2017-03-22 | Basilea Pharmaceutica Ag | Utilização de estatmina como um biomarcador da resposta farmacológica a furazanobenzimidazolos |
| DK2666014T3 (en) | 2011-01-21 | 2017-01-09 | Basilea Pharmaceutica Ag | USE OF GLU-tubulin as a biomarker of PHARMACEUTICAL RESPONSE TO FURAZANOBENZIMIDAZOLER |
| PL2678679T3 (pl) | 2011-02-24 | 2017-07-31 | Basilea Pharmaceutica Ag | Zastosowanie acetylowanej tubuliny jako biomarkera odpowiedzi lekowej na furazanobenzoimidazole |
| CN103502467B (zh) * | 2011-03-29 | 2016-08-17 | 巴斯利尔药物股份公司 | 磷酸化-Akt作为药物响应的生物标志物的用途 |
| US9558575B2 (en) | 2012-02-28 | 2017-01-31 | Blackberry Limited | Methods and devices for selecting objects in images |
| ITRM20130248A1 (it) * | 2013-04-24 | 2014-10-25 | Medivis S R L | Formulazioni di riboflavina per il cross-linking transepiteliale. |
| WO2015173341A1 (en) * | 2014-05-13 | 2015-11-19 | Basilea Pharmaceutica Ag | Dosage principle for anti-cancer furazanylbenzimidazoles |
| WO2017068182A1 (en) | 2015-10-22 | 2017-04-27 | Basilea Pharmaceutica Ag | Use of eb1 as a biomarker of drug response |
| CA3059301A1 (en) * | 2017-04-20 | 2018-10-25 | Pi Industries Ltd. | Novel phenylamine compounds |
| CN116947836A (zh) * | 2017-04-26 | 2023-10-27 | 巴斯利尔药物国际股份公司 | 制备呋咱并苯并咪唑及其晶型的方法 |
| WO2018210868A1 (en) | 2017-05-16 | 2018-11-22 | Basilea Pharmaceutica International AG | Novel dosage principle for drugs useful for treating neoplastic diseases |
| EP3713565A1 (en) | 2017-11-20 | 2020-09-30 | Basilea Pharmaceutica International AG | Pharmaceutical combinations for use in the treatment of neoplastic diseases |
| WO2020058405A1 (en) | 2018-09-20 | 2020-03-26 | Basilea Pharmaceutica International AG | Pharmaceutical combinations for use in the treatment of neoplastic diseases |
| WO2021048135A1 (en) | 2019-09-09 | 2021-03-18 | Basilea Pharmaceutica International AG | Pharmaceutical combinations comprising a furazanobenzimidazoles and a cd40 agonist for use in the treatment of neoplastic diseases |
| CN111454254B (zh) * | 2020-04-26 | 2023-06-02 | 云白药征武科技(上海)有限公司 | 一种具有含氟取代基的苯并咪唑衍生物的制备及其应用 |
| CN111423429A (zh) * | 2020-05-19 | 2020-07-17 | 江西科技师范大学 | 苯并咪唑联呋咱类系列化合物及其合成方法 |
| WO2022053549A1 (en) | 2020-09-10 | 2022-03-17 | Basilea Pharmaceutica International AG | Use of c-myc as a biomarker of drug response |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6897208B2 (en) * | 2001-10-26 | 2005-05-24 | Aventis Pharmaceuticals Inc. | Benzimidazoles |
| PL372198A1 (en) * | 2002-02-06 | 2005-07-11 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| DK1636215T3 (da) * | 2003-05-23 | 2008-06-02 | Basilea Pharmaceutica Ag | Furazanobenzimidazoler |
| ES2346323T3 (es) * | 2004-02-11 | 2010-10-14 | Basilea Pharmaceutica Ag | Bencimidazoles sustituidos y su uso para inducir apoptosis. |
-
2010
- 2010-07-26 PL PL10740196T patent/PL2459553T3/pl unknown
- 2010-07-26 ES ES10740196.0T patent/ES2524119T3/es active Active
- 2010-07-26 PT PT107401960T patent/PT2459553E/pt unknown
- 2010-07-26 MX MX2012000611A patent/MX336240B/es unknown
- 2010-07-26 BR BR112012001817A patent/BR112012001817B8/pt active IP Right Grant
- 2010-07-26 US US13/384,467 patent/US8802858B2/en active Active
- 2010-07-26 NZ NZ597376A patent/NZ597376A/en unknown
- 2010-07-26 EP EP10740196.0A patent/EP2459553B1/en active Active
- 2010-07-26 CN CN201080033104.2A patent/CN102471329B/zh active Active
- 2010-07-26 SI SI201030829T patent/SI2459553T1/sl unknown
- 2010-07-26 AU AU2010277688A patent/AU2010277688B2/en active Active
- 2010-07-26 UA UAA201201704A patent/UA106763C2/uk unknown
- 2010-07-26 JP JP2012522131A patent/JP5576485B2/ja active Active
- 2010-07-26 KR KR1020127005138A patent/KR101758400B1/ko active IP Right Grant
- 2010-07-26 WO PCT/EP2010/060803 patent/WO2011012577A1/en active Application Filing
- 2010-07-26 RS RS20140669A patent/RS53679B1/en unknown
- 2010-07-26 CA CA2767875A patent/CA2767875C/en active Active
- 2010-07-26 DK DK10740196.0T patent/DK2459553T3/da active
- 2010-07-26 EA EA201200189A patent/EA021380B1/ru unknown
- 2010-07-27 TW TW099124742A patent/TWI457337B/zh active
-
2011
- 2011-12-25 IL IL217195A patent/IL217195A/en active IP Right Grant
-
2012
- 2012-01-11 ZA ZA2012/00228A patent/ZA201200228B/en unknown
- 2012-07-17 HK HK12106968.1A patent/HK1166316A1/xx unknown
-
2014
- 2014-11-19 HR HRP20141120AT patent/HRP20141120T1/hr unknown
- 2014-12-03 CY CY20141101010T patent/CY1115809T1/el unknown
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Legal Events
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| 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] |
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| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 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 29/09/2020, 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 26/07/2010 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF |