JP5503007B2 - 新規なベンゾイミダゾール誘導体及びｆｘｒアゴニストとしてのそれらの使用 - Google Patents
新規なベンゾイミダゾール誘導体及びｆｘｒアゴニストとしてのそれらの使用 Download PDFInfo
- Publication number
- JP5503007B2 JP5503007B2 JP2012531341A JP2012531341A JP5503007B2 JP 5503007 B2 JP5503007 B2 JP 5503007B2 JP 2012531341 A JP2012531341 A JP 2012531341A JP 2012531341 A JP2012531341 A JP 2012531341A JP 5503007 B2 JP5503007 B2 JP 5503007B2
- Authority
- JP
- Japan
- Prior art keywords
- difluoro
- phenyl
- chloro
- benzimidazole
- cyclohexylmethyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
Links
- WHSLKQFYWQFABL-UHFFFAOYSA-N CC1CCC(C[n]2c(-c3c(CCc(cc4)ccc4-c4nnn[nH]4)cccc3)nc3c2cccc3)CC1 Chemical compound CC1CCC(C[n]2c(-c3c(CCc(cc4)ccc4-c4nnn[nH]4)cccc3)nc3c2cccc3)CC1 WHSLKQFYWQFABL-UHFFFAOYSA-N 0.000 description 1
- NGHROFHNHLSHRE-UHFFFAOYSA-N FC(c1c(COc(cc(cc2)Cl)c2-c2nc(cc(c(F)c3)F)c3[n]2CC2CCCCC2)ccc(-c2nnn[nH]2)c1)(F)F Chemical compound FC(c1c(COc(cc(cc2)Cl)c2-c2nc(cc(c(F)c3)F)c3[n]2CC2CCCCC2)ccc(-c2nnn[nH]2)c1)(F)F NGHROFHNHLSHRE-UHFFFAOYSA-N 0.000 description 1
- QMWBAIRXBNCFDS-UHFFFAOYSA-N FC1(CCC(C[n]2c(-c3c(CCc(cc4)ccc4-c4nnn[nH]4)cccc3)nc3c2cccc3)CC1)F Chemical compound FC1(CCC(C[n]2c(-c3c(CCc(cc4)ccc4-c4nnn[nH]4)cccc3)nc3c2cccc3)CC1)F QMWBAIRXBNCFDS-UHFFFAOYSA-N 0.000 description 1
- GCFATYIQOQLUGR-UHFFFAOYSA-N Fc(c(F)c1)cc2c1nc(-c(c(C#Cc(cc1)ccc1-c1nnn[nH]1)c1)ccc1Cl)[n]2CC1CCCCC1 Chemical compound Fc(c(F)c1)cc2c1nc(-c(c(C#Cc(cc1)ccc1-c1nnn[nH]1)c1)ccc1Cl)[n]2CC1CCCCC1 GCFATYIQOQLUGR-UHFFFAOYSA-N 0.000 description 1
- NLJNNBKCZPVDPF-UHFFFAOYSA-N Fc(c(F)c1)cc2c1nc(-c(cccn1)c1OCc(cccc1)c1Cl)[n]2CC1CCCCC1 Chemical compound Fc(c(F)c1)cc2c1nc(-c(cccn1)c1OCc(cccc1)c1Cl)[n]2CC1CCCCC1 NLJNNBKCZPVDPF-UHFFFAOYSA-N 0.000 description 1
- AENMJOPOXFMHTM-UHFFFAOYSA-N Fc1c(COc(cc(cc2)Cl)c2-c2nc(cccc3)c3[n]2CC2CCCCC2)ccc(-c2nnn[nH]2)c1 Chemical compound Fc1c(COc(cc(cc2)Cl)c2-c2nc(cccc3)c3[n]2CC2CCCCC2)ccc(-c2nnn[nH]2)c1 AENMJOPOXFMHTM-UHFFFAOYSA-N 0.000 description 1
- YNXQWMXDEWWXKK-UHFFFAOYSA-N O=C(c(cc1)cc(F)c1-c1nnn[nH]1)Nc(cc(cc1)Cl)c1-c1nc(cc(c(F)c2)F)c2[n]1CC1CCCCC1 Chemical compound O=C(c(cc1)cc(F)c1-c1nnn[nH]1)Nc(cc(cc1)Cl)c1-c1nc(cc(c(F)c2)F)c2[n]1CC1CCCCC1 YNXQWMXDEWWXKK-UHFFFAOYSA-N 0.000 description 1
- QZYJYBRAXQJGNA-UHFFFAOYSA-N OC(COc1ccc(C[n]2c(-c(ccc(Cl)c3)c3OCC3CCCC3)nc(cc3F)c2cc3F)cc1)=O Chemical compound OC(COc1ccc(C[n]2c(-c(ccc(Cl)c3)c3OCC3CCCC3)nc(cc3F)c2cc3F)cc1)=O QZYJYBRAXQJGNA-UHFFFAOYSA-N 0.000 description 1
- OSSIKCNHACZNRE-UHFFFAOYSA-N OC(c1ccc(CCOc(cc(cc2)Cl)c2-c2nc(cc(c(F)c3)F)c3[n]2CC2CCCCC2)cc1)=O Chemical compound OC(c1ccc(CCOc(cc(cc2)Cl)c2-c2nc(cc(c(F)c3)F)c3[n]2CC2CCCCC2)cc1)=O OSSIKCNHACZNRE-UHFFFAOYSA-N 0.000 description 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
- C07D401/04—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 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09171700 | 2009-09-29 | ||
| EP09171700.9 | 2009-09-29 | ||
| PCT/EP2010/064217 WO2011039130A1 (en) | 2009-09-29 | 2010-09-27 | New benzimidazole derivatives and their use as fxr agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013505977A JP2013505977A (ja) | 2013-02-21 |
| JP5503007B2 true JP5503007B2 (ja) | 2014-05-28 |
Family
ID=43033176
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012531341A Expired - Fee Related JP5503007B2 (ja) | 2009-09-29 | 2010-09-27 | 新規なベンゾイミダゾール誘導体及びｆｘｒアゴニストとしてのそれらの使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8309581B2 (enExample) |
| EP (1) | EP2483247A1 (enExample) |
| JP (1) | JP5503007B2 (enExample) |
| KR (1) | KR101477872B1 (enExample) |
| CN (1) | CN102574812B (enExample) |
| AU (1) | AU2010303146A1 (enExample) |
| BR (1) | BR112012006986A2 (enExample) |
| CA (1) | CA2772815A1 (enExample) |
| IL (1) | IL218037A0 (enExample) |
| IN (1) | IN2012DN01234A (enExample) |
| MX (1) | MX2012002479A (enExample) |
| WO (1) | WO2011039130A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3043865T (pt) | 2013-09-11 | 2021-01-14 | Univ Claude Bernard Lyon | Métodos e composições farmacêuticas para o tratamento da infeção por vírus da hepatite b |
| CN108072684B (zh) * | 2016-11-11 | 2020-06-16 | 中国科学院广州生物医药与健康研究院 | 法尼醇x受体的新配体及其筛选方法和应用 |
| NZ756329A (en) | 2017-02-21 | 2025-09-26 | Genfit | Combination of a ppar agonist with a fxr agonist |
| US20210085662A1 (en) | 2017-03-30 | 2021-03-25 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2888847B1 (fr) * | 2005-07-22 | 2007-08-31 | Sanofi Aventis Sa | Derives de n-(heteriaryl)-1-heteorarylalkyl-1h-indole-2- carboxamides, leur preparation et application en therapeutique |
| KR101237623B1 (ko) * | 2006-06-29 | 2013-02-26 | 에프. 호프만-라 로슈 아게 | 벤즈이미다졸 유도체, 이의 제조방법, ｆｘｒ 작용물질로서이의 용도, 및 이를 함유하는 약학 제제 |
| DE102007008420A1 (de) | 2007-02-21 | 2008-08-28 | Merck Patent Gmbh | Benzimidazolderivate |
| BRPI0815696A2 (pt) * | 2007-08-27 | 2016-06-21 | Hoffmann La Roche | composto derivados de benzimidazol, processo para a sua manufatura, composições farmacêuticas que os compreendem, metódo para o tratamento terapêutico e/ou profilático de enfermidades que são moduladas por agonistas de fxr e uso destes compostos. |
| BRPI0818813A2 (pt) * | 2007-11-15 | 2015-04-22 | Hoffmann La Roche | Compostos derivados de metil-benzimidazol, processo para a manufatura desses compostos, composições farmacêuticas que os compreendem, método para o tratamento terapêutico e/ ou profilático de enfermidades que são afetadas por moduladores de fxr e uso de tais compostos |
| MX2011002516A (es) * | 2008-09-11 | 2011-04-07 | Hoffmann La Roche | Nuevos derivados de bencimidazol. |
| ES2444791T3 (es) * | 2008-10-15 | 2014-02-26 | F. Hoffmann-La Roche Ag | Nuevos derivados de benzimidazol |
-
2010
- 2010-09-20 US US12/885,588 patent/US8309581B2/en not_active Expired - Fee Related
- 2010-09-27 CN CN201080043283.8A patent/CN102574812B/zh not_active Expired - Fee Related
- 2010-09-27 BR BR112012006986A patent/BR112012006986A2/pt not_active Application Discontinuation
- 2010-09-27 KR KR1020127010681A patent/KR101477872B1/ko not_active Expired - Fee Related
- 2010-09-27 AU AU2010303146A patent/AU2010303146A1/en not_active Abandoned
- 2010-09-27 MX MX2012002479A patent/MX2012002479A/es active IP Right Grant
- 2010-09-27 EP EP10757215A patent/EP2483247A1/en not_active Withdrawn
- 2010-09-27 IN IN1234DEN2012 patent/IN2012DN01234A/en unknown
- 2010-09-27 JP JP2012531341A patent/JP5503007B2/ja not_active Expired - Fee Related
- 2010-09-27 WO PCT/EP2010/064217 patent/WO2011039130A1/en not_active Ceased
- 2010-09-27 CA CA2772815A patent/CA2772815A1/en not_active Abandoned
-
2012
- 2012-02-09 IL IL218037A patent/IL218037A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR112012006986A2 (pt) | 2016-04-12 |
| WO2011039130A1 (en) | 2011-04-07 |
| AU2010303146A1 (en) | 2012-04-19 |
| KR20120063536A (ko) | 2012-06-15 |
| CA2772815A1 (en) | 2011-04-07 |
| MX2012002479A (es) | 2012-03-26 |
| EP2483247A1 (en) | 2012-08-08 |
| IL218037A0 (en) | 2012-04-30 |
| IN2012DN01234A (enExample) | 2015-05-15 |
| CN102574812B (zh) | 2016-03-30 |
| US8309581B2 (en) | 2012-11-13 |
| HK1171746A1 (zh) | 2013-04-05 |
| JP2013505977A (ja) | 2013-02-21 |
| US20110077273A1 (en) | 2011-03-31 |
| KR101477872B1 (ko) | 2014-12-30 |
| CN102574812A (zh) | 2012-07-11 |
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