CN102471329B - 用作治疗肿瘤性或自身免疫性疾病的前药的呋咱并苯并咪唑 - Google Patents
用作治疗肿瘤性或自身免疫性疾病的前药的呋咱并苯并咪唑 Download PDFInfo
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- CN102471329B CN102471329B CN201080033104.2A CN201080033104A CN102471329B CN 102471329 B CN102471329 B CN 102471329B CN 201080033104 A CN201080033104 A CN 201080033104A CN 102471329 B CN102471329 B CN 102471329B
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- 0 CC(*)(/C=C1)/C=*/C=C/C1(C)C(C[n]1c(-c2n[o]nc2N*)nc2c1cccc2)=O Chemical compound CC(*)(/C=C1)/C=*/C=C/C1(C)C(C[n]1c(-c2n[o]nc2N*)nc2c1cccc2)=O 0.000 description 3
- SQXFMHVFWFRLCE-UHFFFAOYSA-N N#CCCNc1n[o]nc1-c1nc2ccccc2[nH]1 Chemical compound N#CCCNc1n[o]nc1-c1nc2ccccc2[nH]1 SQXFMHVFWFRLCE-UHFFFAOYSA-N 0.000 description 2
- QEPDSNAEMKSMGN-UHFFFAOYSA-N Nc1n[o]nc1-c1nc2ccccc2[nH]1 Chemical compound Nc1n[o]nc1-c1nc2ccccc2[nH]1 QEPDSNAEMKSMGN-UHFFFAOYSA-N 0.000 description 2
- GPRYKVSEZCQIHD-UHFFFAOYSA-N CC(c(cc1)ccc1N)=O Chemical compound CC(c(cc1)ccc1N)=O GPRYKVSEZCQIHD-UHFFFAOYSA-N 0.000 description 1
- NOHXJNWKJRULHU-UHFFFAOYSA-N CC(c(cc1)ccc1NC(OCc1ccccc1)=O)=O Chemical compound CC(c(cc1)ccc1NC(OCc1ccccc1)=O)=O NOHXJNWKJRULHU-UHFFFAOYSA-N 0.000 description 1
- OWVDGXUZPPZKEU-YCBFMBTMSA-N CC(c(cc1)ccc1NC([C@H](CCCCNC(OCc1ccccc1)=O)NC(OCc1ccccc1)=O)=O)=[U] Chemical compound CC(c(cc1)ccc1NC([C@H](CCCCNC(OCc1ccccc1)=O)NC(OCc1ccccc1)=O)=O)=[U] OWVDGXUZPPZKEU-YCBFMBTMSA-N 0.000 description 1
- NNBPHEDYWIUSID-NSHDSACASA-N C[C@@H](C(Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2N)nc2c1cccc2)=O)=O)N Chemical compound C[C@@H](C(Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2N)nc2c1cccc2)=O)=O)N NNBPHEDYWIUSID-NSHDSACASA-N 0.000 description 1
- JRYVAPPAMZHVKT-ZDUSSCGKSA-N C[C@@H](C(Nc(cc1)ncc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O)=O)N Chemical compound C[C@@H](C(Nc(cc1)ncc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O)=O)N JRYVAPPAMZHVKT-ZDUSSCGKSA-N 0.000 description 1
- BWOVACANEIVHST-UHFFFAOYSA-N N#CCc1nc2ccccc2[nH]1 Chemical compound N#CCc1nc2ccccc2[nH]1 BWOVACANEIVHST-UHFFFAOYSA-N 0.000 description 1
- WHIQJYVDSGYHOS-UHFFFAOYSA-N N/C(/c1nc2ccccc2[nH]1)=N\O Chemical compound N/C(/c1nc2ccccc2[nH]1)=N\O WHIQJYVDSGYHOS-UHFFFAOYSA-N 0.000 description 1
- OUJIEDIEHHTXRP-UHFFFAOYSA-N N=C(Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O)OCc1ccccc1 Chemical compound N=C(Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O)OCc1ccccc1 OUJIEDIEHHTXRP-UHFFFAOYSA-N 0.000 description 1
- UAWZWNFVRHZXEP-UHFFFAOYSA-N NCC(Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2N)nc2c1cccc2)=O)=O Chemical compound NCC(Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2N)nc2c1cccc2)=O)=O UAWZWNFVRHZXEP-UHFFFAOYSA-N 0.000 description 1
- CTYUHRVKZFYIBA-UHFFFAOYSA-N NCC(Nc(cc1)ncc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O)=O Chemical compound NCC(Nc(cc1)ncc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O)=O CTYUHRVKZFYIBA-UHFFFAOYSA-N 0.000 description 1
- BGUQVHDJTWRUEV-INIZCTEOSA-N NCCCC[C@@H](C(Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2N)nc2c1cccc2)=O)=O)N Chemical compound NCCCC[C@@H](C(Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2N)nc2c1cccc2)=O)=O)N BGUQVHDJTWRUEV-INIZCTEOSA-N 0.000 description 1
- DCFSUGWNRNJJJR-KRWDZBQOSA-N NCCCC[C@@H](C(Nc(cc1)ncc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O)=O)N Chemical compound NCCCC[C@@H](C(Nc(cc1)ncc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O)=O)N DCFSUGWNRNJJJR-KRWDZBQOSA-N 0.000 description 1
- LSFOZQQVTWFMNS-UHFFFAOYSA-N Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O Chemical compound Nc(cc1)ccc1C(C[n]1c(-c2n[o]nc2NCCC#N)nc2c1cccc2)=O LSFOZQQVTWFMNS-UHFFFAOYSA-N 0.000 description 1
- LCEHPUQALGIADG-UHFFFAOYSA-N O=C(CBr)c(cc1)ccc1NC(C(CCCCNC(OCc1ccccc1)=O)NC(OCc1ccccc1)=O)=O Chemical compound O=C(CBr)c(cc1)ccc1NC(C(CCCCNC(OCc1ccccc1)=O)NC(OCc1ccccc1)=O)=O LCEHPUQALGIADG-UHFFFAOYSA-N 0.000 description 1
- SGOOUOYLZRYRQG-UHFFFAOYSA-N O=C(CBr)c(cc1)ccc1NC(OCc1ccccc1)=O Chemical compound O=C(CBr)c(cc1)ccc1NC(OCc1ccccc1)=O SGOOUOYLZRYRQG-UHFFFAOYSA-N 0.000 description 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
- C07D413/04—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)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
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 (2)
| Publication Number | Publication Date |
|---|---|
| CN102471329A CN102471329A (zh) | 2012-05-23 |
| CN102471329B true CN102471329B (zh) | 2014-11-05 |
Family
ID=41226617
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080033104.2A Active CN102471329B (zh) | 2009-07-27 | 2010-07-26 | 用作治疗肿瘤性或自身免疫性疾病的前药的呋咱并苯并咪唑 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8802858B2 (enExample) |
| EP (1) | EP2459553B1 (enExample) |
| JP (1) | JP5576485B2 (enExample) |
| KR (1) | KR101758400B1 (enExample) |
| CN (1) | CN102471329B (enExample) |
| AU (1) | AU2010277688B2 (enExample) |
| BR (1) | BR112012001817B8 (enExample) |
| CA (1) | CA2767875C (enExample) |
| CY (1) | CY1115809T1 (enExample) |
| DK (1) | DK2459553T3 (enExample) |
| EA (1) | EA021380B1 (enExample) |
| ES (1) | ES2524119T3 (enExample) |
| HR (1) | HRP20141120T1 (enExample) |
| IL (1) | IL217195A (enExample) |
| MX (1) | MX336240B (enExample) |
| NZ (1) | NZ597376A (enExample) |
| PL (1) | PL2459553T3 (enExample) |
| PT (1) | PT2459553E (enExample) |
| RS (1) | RS53679B1 (enExample) |
| SI (1) | SI2459553T1 (enExample) |
| TW (1) | TWI457337B (enExample) |
| UA (1) | UA106763C2 (enExample) |
| WO (1) | WO2011012577A1 (enExample) |
| ZA (1) | ZA201200228B (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2666014T (pt) | 2011-01-21 | 2016-12-22 | Basilea Pharmaceutica Ag | Utilização de glu-tubulina como um biomarcador da resposta farmacológica a furazanobenzimidazolos |
| PT2666015T (pt) * | 2011-01-21 | 2017-03-22 | Basilea Pharmaceutica Ag | Utilização de estatmina como um biomarcador da resposta farmacológica a furazanobenzimidazolos |
| PL2666016T3 (pl) | 2011-01-21 | 2017-07-31 | Basilea Pharmaceutica Ag | Zastosowanie BUBR1 jako biomarkera odpowiedzi lekowej |
| 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 |
| WO2012130887A1 (en) | 2011-03-29 | 2012-10-04 | Basilea Pharmaceutica Ag | Use of phospho-akt as a biomarker of drug response |
| 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 |
| EP3365680A1 (en) | 2015-10-22 | 2018-08-29 | Basilea Pharmaceutica International AG | Use of eb1 as a biomarker of drug response |
| MX2019012468A (es) * | 2017-04-20 | 2019-12-11 | Pi Industries Ltd | Nuevos compuestos de fenilamina. |
| MX388196B (es) * | 2017-04-26 | 2025-03-19 | Basilea Pharm Int Ag | Procesos para la preparacion de furazanobencimidazoles y formas cristalinas de estos. |
| US11633383B2 (en) * | 2017-05-16 | 2023-04-25 | Basilea Pharmaceutica International AG | 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 |
| US20220370418A1 (en) | 2019-09-09 | 2022-11-24 | 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003066629A2 (en) * | 2002-02-06 | 2003-08-14 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| US20040048868A1 (en) * | 2001-10-26 | 2004-03-11 | Edwards Michael L. | Benzimidazoles |
| CN1812986A (zh) * | 2003-05-23 | 2006-08-02 | 巴斯利尔药物股份公司 | 呋咱并苯并咪唑类化合物 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE473973T1 (de) * | 2004-02-11 | 2010-07-15 | Basilea Pharmaceutica Ag | Substituierte benzimidazole und deren verwendung zur induktion von apoptose |
-
2010
- 2010-07-26 PL PL10740196T patent/PL2459553T3/pl unknown
- 2010-07-26 SI SI201030829T patent/SI2459553T1/sl unknown
- 2010-07-26 AU AU2010277688A patent/AU2010277688B2/en active Active
- 2010-07-26 ES ES10740196.0T patent/ES2524119T3/es active Active
- 2010-07-26 US US13/384,467 patent/US8802858B2/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 EA EA201200189A patent/EA021380B1/ru unknown
- 2010-07-26 CN CN201080033104.2A patent/CN102471329B/zh active Active
- 2010-07-26 CA CA2767875A patent/CA2767875C/en active Active
- 2010-07-26 DK DK10740196.0T patent/DK2459553T3/da active
- 2010-07-26 RS RS20140669A patent/RS53679B1/sr unknown
- 2010-07-26 EP EP10740196.0A patent/EP2459553B1/en active Active
- 2010-07-26 NZ NZ597376A patent/NZ597376A/en not_active IP Right Cessation
- 2010-07-26 WO PCT/EP2010/060803 patent/WO2011012577A1/en not_active Ceased
- 2010-07-26 HR HRP20141120AT patent/HRP20141120T1/hr unknown
- 2010-07-26 BR BR112012001817A patent/BR112012001817B8/pt active IP Right Grant
- 2010-07-26 KR KR1020127005138A patent/KR101758400B1/ko active Active
- 2010-07-26 PT PT107401960T patent/PT2459553E/pt unknown
- 2010-07-26 MX MX2012000611A patent/MX336240B/es 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
-
2014
- 2014-12-03 CY CY20141101010T patent/CY1115809T1/el unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040048868A1 (en) * | 2001-10-26 | 2004-03-11 | Edwards Michael L. | Benzimidazoles |
| WO2003066629A2 (en) * | 2002-02-06 | 2003-08-14 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| CN1812986A (zh) * | 2003-05-23 | 2006-08-02 | 巴斯利尔药物股份公司 | 呋咱并苯并咪唑类化合物 |
Non-Patent Citations (1)
| Title |
|---|
| "Synthesis and biological activity of strongly fluorescent tricyclic analogues of Acyclovir and Ganciclovir";Tomasz Goslinski，et al;《Journal of Medicinal Chemistry》;20021008;第45卷(第23期);第5052-5057页 * |
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