BR112012001817B8 - furazanobenzimidazóis, seu uso, processo de produção e composição farmacêutica - Google Patents

furazanobenzimidazóis, seu uso, processo de produção e composição farmacêutica

Info

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
Application number
BR112012001817A
Other languages
English (en)
Other versions
BR112012001817A2 (pt
BR112012001817B1 (pt
Inventor
Bachmann Felix
Pohlmann Jens
Original Assignee
Basilea Pharmaceutica Ag
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
Application filed by Basilea Pharmaceutica Ag filed Critical Basilea Pharmaceutica Ag
Publication of BR112012001817A2 publication Critical patent/BR112012001817A2/pt
Publication of BR112012001817B1 publication Critical patent/BR112012001817B1/pt
Publication of BR112012001817B8 publication Critical patent/BR112012001817B8/pt

Links

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
    • C07D413/04—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

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.
BR112012001817A 2009-07-27 2010-07-26 furazanobenzimidazóis, seu uso, processo de produção e composição farmacêutica BR112012001817B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09166469 2009-07-27
EP09166469.8 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2666014B1 (en) 2011-01-21 2016-10-05 Basilea Pharmaceutica AG Use of glu-tubulin as a biomarker of drug 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
DK2666016T3 (en) 2011-01-21 2017-04-10 Basilea Pharmaceutica Ag USE OF BUBR1 AS A BIOMARKETER FOR PHARMACEUTICAL RESPONSE TO FURAZANOBENZIMIDAZOLES
CN103392130B (zh) * 2011-02-24 2015-11-25 巴斯利尔药物股份公司 乙酰化微管蛋白作为对呋咱并苯并咪唑类的药物反应的生物标志物的用途
PL2691533T3 (pl) * 2011-03-29 2017-09-29 Basilea Pharmaceutica Ag Zastosowanie fosfo-Akt jako biomarkera odpowiedzi na leki
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
US20180306790A1 (en) * 2015-10-22 2018-10-25 Basilea Pharmaceutica International AG Use of eb1 as a biomarker of drug response
EP3612514B1 (en) * 2017-04-20 2022-03-30 PI Industries Ltd Novel phenylamine compounds
KR20240038149A (ko) * 2017-04-26 2024-03-22 바실리어 파마슈티카 인터내셔널 리미티드 푸라자노벤즈이미다졸 및 이의 결정 형태의 제조 공정
EP3624790A1 (en) 2017-05-16 2020-03-25 Basilea Pharmaceutica International AG Novel dosage principle for drugs useful for treating neoplastic diseases
WO2019097073A1 (en) 2017-11-20 2019-05-23 Basilea Pharmaceutica International AG Pharmaceutical combinations for use in the treatment of neoplastic diseases
EP3853224A1 (en) 2018-09-20 2021-07-28 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6897208B2 (en) * 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
KR20040084896A (ko) * 2002-02-06 2004-10-06 버텍스 파마슈티칼스 인코포레이티드 Ｇｓｋ-3의 억제제로서 유용한 헤테로아릴 화합물
JP4829791B2 (ja) * 2003-05-23 2011-12-07 バジリア ファルマスーチカ アーゲー フラザノベンゾイミダゾール
WO2005077939A1 (en) * 2004-02-11 2005-08-25 Basilea Pharmaceutica Ag Substituted benzimidazoles and their use for inducing apoptosis

Also Published As

Publication number Publication date
JP2013500304A (ja) 2013-01-07
KR101758400B1 (ko) 2017-07-14
CN102471329A (zh) 2012-05-23
SI2459553T1 (sl) 2015-01-30
KR20120055571A (ko) 2012-05-31
US20120264792A1 (en) 2012-10-18
NZ597376A (en) 2014-01-31
JP5576485B2 (ja) 2014-08-20
UA106763C2 (uk) 2014-10-10
TWI457337B (zh) 2014-10-21
CY1115809T1 (el) 2017-01-25
PL2459553T3 (pl) 2015-03-31
PT2459553E (pt) 2014-11-24
MX336240B (es) 2016-01-13
ES2524119T3 (es) 2014-12-04
CA2767875A1 (en) 2011-02-03
IL217195A (en) 2014-03-31
RS53679B1 (en) 2015-04-30
AU2010277688A1 (en) 2012-02-09
CA2767875C (en) 2016-03-15
CN102471329B (zh) 2014-11-05
BR112012001817A2 (pt) 2016-03-15
MX2012000611A (es) 2012-01-27
EP2459553A1 (en) 2012-06-06
ZA201200228B (en) 2012-09-26
AU2010277688B2 (en) 2013-12-05
EA201200189A1 (ru) 2012-08-30
BR112012001817B1 (pt) 2020-09-29
US8802858B2 (en) 2014-08-12
HK1166316A1 (en) 2012-10-26
EA021380B1 (ru) 2015-06-30
DK2459553T3 (da) 2014-11-03
EP2459553B1 (en) 2014-10-01
TW201107318A (en) 2011-03-01
HRP20141120T1 (hr) 2015-01-30
WO2011012577A1 (en) 2011-02-03
IL217195A0 (en) 2012-02-29

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Legal Events

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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]

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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.

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