JP6912039B2 - 置換ベンゾイミダゾール、それらの調製及び医薬品としてのそれらの使用 - Google Patents
置換ベンゾイミダゾール、それらの調製及び医薬品としてのそれらの使用 Download PDFInfo
- Publication number
- JP6912039B2 JP6912039B2 JP2018506999A JP2018506999A JP6912039B2 JP 6912039 B2 JP6912039 B2 JP 6912039B2 JP 2018506999 A JP2018506999 A JP 2018506999A JP 2018506999 A JP2018506999 A JP 2018506999A JP 6912039 B2 JP6912039 B2 JP 6912039B2
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- alkyl
- mmol
- compound
- substituted
- 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.)
- Active
Links
- 0 *c([n](*)c1c2*)nc1c(*)c(*)c2C(C(*)=C1*)=C(*)N(*)C1=O Chemical compound *c([n](*)c1c2*)nc1c(*)c(*)c2C(C(*)=C1*)=C(*)N(*)C1=O 0.000 description 4
- VHJMPHDWNNQOKM-UHFFFAOYSA-N CC1=CC(c(cc2)cc(NCCOC(F)(F)F)c2N)=CN(C)C1=O Chemical compound CC1=CC(c(cc2)cc(NCCOC(F)(F)F)c2N)=CN(C)C1=O VHJMPHDWNNQOKM-UHFFFAOYSA-N 0.000 description 2
- LZNWLEPJPMWRAU-UHFFFAOYSA-N CC1=CC(c(cc2)cc(NCCOCC(F)(F)F)c2[N+]([O-])=O)=CN(C)C1=O Chemical compound CC1=CC(c(cc2)cc(NCCOCC(F)(F)F)c2[N+]([O-])=O)=CN(C)C1=O LZNWLEPJPMWRAU-UHFFFAOYSA-N 0.000 description 2
- MKZMIAGKYGHZTF-KRWDZBQOSA-N CCO[C@@H](C)CNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1NC(C(CC1)CCC1(F)F)=O Chemical compound CCO[C@@H](C)CNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1NC(C(CC1)CCC1(F)F)=O MKZMIAGKYGHZTF-KRWDZBQOSA-N 0.000 description 2
- PXZKFECAINECTN-UHFFFAOYSA-N CC(C)(CC(c(cc1)cc(NCCOC(F)(F)F)c1N)=CN1C)C1=O Chemical compound CC(C)(CC(c(cc1)cc(NCCOC(F)(F)F)c1N)=CN1C)C1=O PXZKFECAINECTN-UHFFFAOYSA-N 0.000 description 1
- XSEWRPXQLCGDQL-NTEUORMPSA-N CC(C)OC/C(/C)=N/c(cc(cc1)Br)c1[N+]([O-])=O Chemical compound CC(C)OC/C(/C)=N/c(cc(cc1)Br)c1[N+]([O-])=O XSEWRPXQLCGDQL-NTEUORMPSA-N 0.000 description 1
- RETZKOVMQQKTET-UHFFFAOYSA-N CC(C)OCCNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1N Chemical compound CC(C)OCCNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1N RETZKOVMQQKTET-UHFFFAOYSA-N 0.000 description 1
- XCYVXDCJCCRFQM-UHFFFAOYSA-N CC(C)OCCNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1[N+]([O-])=O Chemical compound CC(C)OCCNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1[N+]([O-])=O XCYVXDCJCCRFQM-UHFFFAOYSA-N 0.000 description 1
- PHCNFIFMPMPDQX-CQSZACIVSA-N CC(C)OC[C@@H](C)Nc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1[N+]([O-])=O Chemical compound CC(C)OC[C@@H](C)Nc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1[N+]([O-])=O PHCNFIFMPMPDQX-CQSZACIVSA-N 0.000 description 1
- CHZCPIPXCVHABA-UHFFFAOYSA-N CC1=CC(c(cc2)cc(NCCC(F)(F)F)c2[N+]([O-])=O)=CN(C)C1=O Chemical compound CC1=CC(c(cc2)cc(NCCC(F)(F)F)c2[N+]([O-])=O)=CN(C)C1=O CHZCPIPXCVHABA-UHFFFAOYSA-N 0.000 description 1
- VAYRDQOBRYXFLR-UHFFFAOYSA-N CC1=CC(c(cc2)cc(NCCOC(F)(F)F)c2NC(C2CCOCC2)=O)=CN(C)C1=O Chemical compound CC1=CC(c(cc2)cc(NCCOC(F)(F)F)c2NC(C2CCOCC2)=O)=CN(C)C1=O VAYRDQOBRYXFLR-UHFFFAOYSA-N 0.000 description 1
- WMNNABKFYKETDN-GOSISDBHSA-N CC1=CC(c(cc2)cc(NCCOC(F)(F)F)c2NC([C@@H]2OCCC2)=O)=CN(C)C1=O Chemical compound CC1=CC(c(cc2)cc(NCCOC(F)(F)F)c2NC([C@@H]2OCCC2)=O)=CN(C)C1=O WMNNABKFYKETDN-GOSISDBHSA-N 0.000 description 1
- WXAKFDPGXRUIKH-UHFFFAOYSA-N CC1=CC(c(cc2)cc(NCCOCC(F)(F)F)c2N)=CN(C)C1=O Chemical compound CC1=CC(c(cc2)cc(NCCOCC(F)(F)F)c2N)=CN(C)C1=O WXAKFDPGXRUIKH-UHFFFAOYSA-N 0.000 description 1
- ZEWABZLDZQPDSD-UHFFFAOYSA-N CC1=CC(c(cc2)cc3c2nc(C2CC2)[n]3CCOC)=CN(C)C1=O Chemical compound CC1=CC(c(cc2)cc3c2nc(C2CC2)[n]3CCOC)=CN(C)C1=O ZEWABZLDZQPDSD-UHFFFAOYSA-N 0.000 description 1
- MGUONTZTOXWFRF-UHFFFAOYSA-N CC1=CC(c(cc2)cc3c2nc(C2CCCCC2)[n]3CCOC)=CN(C)C1=O Chemical compound CC1=CC(c(cc2)cc3c2nc(C2CCCCC2)[n]3CCOC)=CN(C)C1=O MGUONTZTOXWFRF-UHFFFAOYSA-N 0.000 description 1
- MYXRAGJJJUOGSZ-UHFFFAOYSA-N CC1=CC(c(cc2NCCOC)ccc2N)=CN(C)C1=O Chemical compound CC1=CC(c(cc2NCCOC)ccc2N)=CN(C)C1=O MYXRAGJJJUOGSZ-UHFFFAOYSA-N 0.000 description 1
- IOPDSZLMUOSZHZ-UHFFFAOYSA-N CCOCCNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1N Chemical compound CCOCCNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1N IOPDSZLMUOSZHZ-UHFFFAOYSA-N 0.000 description 1
- ZFRDNEQQDDWQHJ-KRWDZBQOSA-N CCO[C@@H](C)C[n]1c(cc(cc2)C(C=C3C)=CN(C)C3=O)c2nc1C(CC1)CCC1(F)F Chemical compound CCO[C@@H](C)C[n]1c(cc(cc2)C(C=C3C)=CN(C)C3=O)c2nc1C(CC1)CCC1(F)F ZFRDNEQQDDWQHJ-KRWDZBQOSA-N 0.000 description 1
- KUBZLZAZMNELCG-MRVPVSSYSA-N CCO[C@H](C)CNc(cc(cc1)Br)c1N Chemical compound CCO[C@H](C)CNc(cc(cc1)Br)c1N KUBZLZAZMNELCG-MRVPVSSYSA-N 0.000 description 1
- QMWWEMLJYVJWOS-MRVPVSSYSA-N CCO[C@H](C)CNc(cc(cc1)Br)c1[N+]([O-])=O Chemical compound CCO[C@H](C)CNc(cc(cc1)Br)c1[N+]([O-])=O QMWWEMLJYVJWOS-MRVPVSSYSA-N 0.000 description 1
- BBUARUBIXANZIS-CYBMUJFWSA-N CCO[C@H](C)CNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1N Chemical compound CCO[C@H](C)CNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1N BBUARUBIXANZIS-CYBMUJFWSA-N 0.000 description 1
- OSBPHVXQBVVYMK-OAHLLOKOSA-N CCO[C@H](C)CNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1NC(C(C1)CC1(F)F)=O Chemical compound CCO[C@H](C)CNc(cc(cc1)C(C=C2C)=CN(C)C2=O)c1NC(C(C1)CC1(F)F)=O OSBPHVXQBVVYMK-OAHLLOKOSA-N 0.000 description 1
- WIZDANJNJRRRQZ-INIZCTEOSA-N C[C@@H](COC)[n]1c(cc(cc2)C(C=C3C)=CN(C)C3=O)c2nc1C(CC1)CCC1(F)F Chemical compound C[C@@H](COC)[n]1c(cc(cc2)C(C=C3C)=CN(C)C3=O)c2nc1C(CC1)CCC1(F)F WIZDANJNJRRRQZ-INIZCTEOSA-N 0.000 description 1
- RGFKQNCZZJVQFC-UHFFFAOYSA-N Cc([n](CCOC(F)(F)F)c1c2)nc1ccc2C(C=C1C)=CN(C)C1=O Chemical compound Cc([n](CCOC(F)(F)F)c1c2)nc1ccc2C(C=C1C)=CN(C)C1=O RGFKQNCZZJVQFC-UHFFFAOYSA-N 0.000 description 1
- ILYVDFJXCZLQOG-UHFFFAOYSA-N Cc1nc(ccc(Br)c2)c2[n]1CCOC(F)(F)F Chemical compound Cc1nc(ccc(Br)c2)c2[n]1CCOC(F)(F)F ILYVDFJXCZLQOG-UHFFFAOYSA-N 0.000 description 1
- VOJANFHOLSIPBC-UHFFFAOYSA-N FC(CC1)(CCC1c([nH]c1c2)nc1ccc2Br)F Chemical compound FC(CC1)(CCC1c([nH]c1c2)nc1ccc2Br)F VOJANFHOLSIPBC-UHFFFAOYSA-N 0.000 description 1
- GXZZKJRWIAZFFL-UHFFFAOYSA-N [O-][N+](c(ccc(Br)c1)c1NCCOCC(F)(F)F)=O Chemical compound [O-][N+](c(ccc(Br)c1)c1NCCOCC(F)(F)F)=O GXZZKJRWIAZFFL-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
- C07D401/10—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 linked by a carbon chain containing aromatic rings
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- 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
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Transplantation (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562204178P | 2015-08-12 | 2015-08-12 | |
| US62/204,178 | 2015-08-12 | ||
| US201662358101P | 2016-07-04 | 2016-07-04 | |
| US62/358,101 | 2016-07-04 | ||
| PCT/CA2016/050952 WO2017024412A1 (en) | 2015-08-12 | 2016-08-12 | Substituted benzimidazoles, their preparation and their use as pharmaceuticals |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018522925A JP2018522925A (ja) | 2018-08-16 |
| JP2018522925A5 JP2018522925A5 (enExample) | 2019-09-26 |
| JP6912039B2 true JP6912039B2 (ja) | 2021-07-28 |
Family
ID=57982882
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018506999A Active JP6912039B2 (ja) | 2015-08-12 | 2016-08-12 | 置換ベンゾイミダゾール、それらの調製及び医薬品としてのそれらの使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (4) | US10703740B2 (enExample) |
| EP (1) | EP3334719B1 (enExample) |
| JP (1) | JP6912039B2 (enExample) |
| KR (1) | KR102784592B1 (enExample) |
| CN (2) | CN108137539B (enExample) |
| AU (2) | AU2016305515A1 (enExample) |
| CA (1) | CA2994478C (enExample) |
| ES (1) | ES2904258T3 (enExample) |
| IL (1) | IL257340B2 (enExample) |
| MX (1) | MX382832B (enExample) |
| WO (1) | WO2017024412A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6912039B2 (ja) * | 2015-08-12 | 2021-07-28 | ネオメド インスティテュートNeomed Institute | 置換ベンゾイミダゾール、それらの調製及び医薬品としてのそれらの使用 |
| GB201617627D0 (en) | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201617630D0 (en) | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| JP7165501B2 (ja) * | 2017-03-15 | 2022-11-04 | 住友ファーマ株式会社 | 新規ベンズイミダゾール化合物からなる医薬 |
| WO2018207882A1 (ja) * | 2017-05-12 | 2018-11-15 | 武田薬品工業株式会社 | 複素環化合物 |
| GB201806320D0 (en) | 2018-04-18 | 2018-05-30 | Cellcentric Ltd | Process |
| WO2020093162A1 (en) * | 2018-11-07 | 2020-05-14 | Neomed Institute | Treatment of bet inhibitor-resistant cancers and other diseases responsive to dual bet and cbp/ep300 inhibition therapy |
| JP2022053557A (ja) * | 2019-02-08 | 2022-04-06 | マルホ株式会社 | ピリドン誘導体 |
| CN112174945B (zh) * | 2019-07-02 | 2022-06-07 | 四川大学 | 具有抗癌作用的吲唑类化合物及其制备方法和用途 |
| CN115232074A (zh) * | 2022-08-22 | 2022-10-25 | 湖南复瑞生物医药技术有限责任公司 | 一种1-烷基取代-2-甲基-5-溴苯并咪唑的合成方法 |
| WO2024249796A2 (en) * | 2023-06-02 | 2024-12-05 | Epigenetix, Inc. | Extended and delayed release compositions of substituted benzimidazoles |
Family Cites Families (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4550166A (en) | 1984-05-21 | 1985-10-29 | American Cyanamid Company | (Pyridinyl)-1,2,4-triazolo[4,3-a]pyridines |
| US4785005A (en) | 1986-06-25 | 1988-11-15 | Rorer Pharmaceutical Corporation | 6-(6-alkylpyridone)-carbostyril compounds and their cardiotonic uses |
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| DE4237656A1 (de) * | 1992-06-13 | 1993-12-16 | Merck Patent Gmbh | Benzimidazolderivate |
| US6465484B1 (en) | 1997-09-26 | 2002-10-15 | Merck & Co., Inc. | Angiogenesis inhibitors |
| US6162804A (en) | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| EP1109555A4 (en) | 1998-08-31 | 2001-11-21 | Merck & Co Inc | Novel angiogenesis inhibitors |
| MY139563A (en) | 2002-09-04 | 2009-10-30 | Bristol Myers Squibb Co | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
| CA2550064A1 (en) | 2003-12-18 | 2005-07-07 | Pfizer Products Inc. | Methods of treating acute inflammation in animals with p38 map kinase inhibitors |
| DK1737459T3 (da) | 2004-03-19 | 2009-10-26 | Warner Lambert Co | Imidazopyridin og imidazopyrimidinderivater som antibakterielle midler |
| PE20121506A1 (es) | 2006-07-14 | 2012-11-26 | Amgen Inc | Compuestos triazolopiridinas como inhibidores de c-met |
| AU2007337886C1 (en) | 2006-12-22 | 2014-10-16 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as FGFR inhibitors |
| US8314087B2 (en) * | 2007-02-16 | 2012-11-20 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and methods of use |
| US8119658B2 (en) | 2007-10-01 | 2012-02-21 | Bristol-Myers Squibb Company | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| BRPI0817434A2 (pt) | 2007-10-17 | 2015-06-16 | Novartis Ag | Composto orgânicos |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| WO2011060235A1 (en) | 2009-11-16 | 2011-05-19 | Schering Corporation | Imidazole derivatives and methods of use thereof |
| UA112425C2 (uk) | 2010-12-13 | 2016-09-12 | Еррей Біофарма Інк. | ЗАМІЩЕНІ N-(1H-ІНДАЗОЛ-4-ІЛ)ІМІДАЗО[1,2-a]ПІРИДИН-3-КАРБОКСАМІДНІ СПОЛУКИ ЯК ІНГІБІТОРИ РЕЦЕПТОРНОЇ ТИРОЗИНКІНАЗИ ІІІ ТИПУ |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| RU2014111823A (ru) | 2011-08-29 | 2015-10-10 | Инфинити Фармасьютикалз, Инк. | Гетероциклические соединения и их применения |
| US8987250B2 (en) * | 2012-04-20 | 2015-03-24 | Gilead Sciences, Inc. | Therapeutic compounds |
| WO2013186229A1 (en) | 2012-06-11 | 2013-12-19 | Ucb Pharma S.A. | Tnf -alpha modulating benzimidazoles |
| WO2013185284A1 (en) | 2012-06-12 | 2013-12-19 | Abbott Laboratories | Pyridinone and pyridazinone derivatives |
| CA2886187C (en) | 2012-09-28 | 2020-04-14 | Vanderbilt University | Fused heterocyclic compounds as selective bmp inhibitors |
| US20140094456A1 (en) | 2012-10-02 | 2014-04-03 | Intermune, Inc. | Anti-fibrotic pyridinones |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| US20160193206A1 (en) | 2012-12-20 | 2016-07-07 | Bayer Pharma Aktiengesellschaft | Bet-protein-inhibiting dihydropyridopyrazinones |
| AU2013365926B9 (en) | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2014128655A1 (en) | 2013-02-25 | 2014-08-28 | Aurigene Discovery Technologies Limited | Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors |
| BR112015022417A2 (pt) | 2013-03-14 | 2017-07-18 | Convergene Llc | métodos e composições para inibição de proteínas contendo bromodomínio |
| WO2014152029A2 (en) | 2013-03-15 | 2014-09-25 | Epigenetix, Inc. | Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors |
| WO2014145051A1 (en) | 2013-03-15 | 2014-09-18 | Jiazhong Zhang | Heterocyclic compounds and uses thereof |
| US8975417B2 (en) | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| CN105492439B (zh) | 2013-06-21 | 2019-11-22 | 齐尼思表观遗传学有限公司 | 作为溴结构域抑制剂的取代的双环化合物 |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| EP3019493B1 (de) | 2013-07-09 | 2017-06-14 | Bayer Pharma Aktiengesellschaft | Modifizierte bet-proteininhibitorische dihydrochinoxalinone und dihydropyridopyrazinone |
| US20150051208A1 (en) * | 2013-08-14 | 2015-02-19 | Boehringer Ingelheim International Gmbh | Pyridinones |
| WO2015049629A1 (en) | 2013-10-01 | 2015-04-09 | Piramal Enterprises Limited | Imidazoquinoline compounds as bromodomain inhibitors |
| CA3148196A1 (en) | 2013-10-18 | 2015-04-23 | Celgene Quanticel Research, Inc. | Bromodomain inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015089075A1 (en) | 2013-12-09 | 2015-06-18 | Abbvie Inc. | Dihydropyridinone and dihydropyridazinone derivatives useful as bromodomain inhibitors |
| GB201321729D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| JP6480944B2 (ja) | 2014-01-09 | 2019-03-13 | オリオン コーポレーション | ブロモドメイン阻害剤としての二環式複素環誘導体 |
| RU2692485C2 (ru) | 2014-04-02 | 2019-06-25 | Интермьюн, Инк. | Противофиброзные пиридиноны |
| UA119870C2 (uk) | 2014-04-23 | 2019-08-27 | Інсайт Корпорейшн | 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET |
| US20190092761A1 (en) | 2014-11-13 | 2019-03-28 | Convergene Llc | Methods and Compositions for Inhibition of Bromodomain and Extratermial Proteins |
| EP3227281A4 (en) | 2014-12-01 | 2018-05-30 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| CA2966450A1 (en) | 2014-12-17 | 2016-06-23 | Olesya KHARENKO | Inhibitors of bromodomains |
| WO2016097870A1 (en) | 2014-12-17 | 2016-06-23 | Zenith Epigenetics Corp. | Substituted bicyclic compounds as bromodomain inhibitors |
| GB201503720D0 (en) | 2015-03-05 | 2015-04-22 | Glaxosmithkline Ip No 2 Ltd | Chemical compound |
| GB201504689D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| GB201506660D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| JP6912039B2 (ja) * | 2015-08-12 | 2021-07-28 | ネオメド インスティテュートNeomed Institute | 置換ベンゾイミダゾール、それらの調製及び医薬品としてのそれらの使用 |
-
2016
- 2016-08-12 JP JP2018506999A patent/JP6912039B2/ja active Active
- 2016-08-12 CN CN201680059249.7A patent/CN108137539B/zh active Active
- 2016-08-12 MX MX2018001756A patent/MX382832B/es unknown
- 2016-08-12 CA CA2994478A patent/CA2994478C/en active Active
- 2016-08-12 CN CN202111621671.6A patent/CN114605387A/zh active Pending
- 2016-08-12 AU AU2016305515A patent/AU2016305515A1/en not_active Abandoned
- 2016-08-12 KR KR1020187006581A patent/KR102784592B1/ko active Active
- 2016-08-12 US US15/751,801 patent/US10703740B2/en active Active
- 2016-08-12 ES ES16834372T patent/ES2904258T3/es active Active
- 2016-08-12 IL IL257340A patent/IL257340B2/en unknown
- 2016-08-12 EP EP16834372.1A patent/EP3334719B1/en active Active
- 2016-08-12 WO PCT/CA2016/050952 patent/WO2017024412A1/en not_active Ceased
-
2020
- 2020-05-22 US US16/881,803 patent/US11365186B2/en active Active
-
2021
- 2021-01-12 AU AU2021200147A patent/AU2021200147B2/en active Active
-
2022
- 2022-05-13 US US17/743,792 patent/US11981657B2/en active Active
-
2024
- 2024-04-08 US US18/629,321 patent/US20240425481A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| IL257340A (en) | 2018-03-29 |
| AU2021200147A1 (en) | 2021-03-18 |
| CN108137539A (zh) | 2018-06-08 |
| IL257340B2 (en) | 2023-10-01 |
| US20230120413A1 (en) | 2023-04-20 |
| KR102784592B1 (ko) | 2025-03-19 |
| US10703740B2 (en) | 2020-07-07 |
| US20180237417A1 (en) | 2018-08-23 |
| MX2018001756A (es) | 2018-09-06 |
| US20240425481A1 (en) | 2024-12-26 |
| ES2904258T3 (es) | 2022-04-04 |
| AU2021200147B2 (en) | 2022-09-08 |
| BR112018002547A2 (pt) | 2018-09-18 |
| CN108137539B (zh) | 2022-01-11 |
| CA2994478A1 (en) | 2017-02-16 |
| IL257340B1 (en) | 2023-06-01 |
| HK1256752A1 (en) | 2019-10-04 |
| EP3334719B1 (en) | 2021-09-15 |
| CN114605387A (zh) | 2022-06-10 |
| KR20180039669A (ko) | 2018-04-18 |
| JP2018522925A (ja) | 2018-08-16 |
| US11981657B2 (en) | 2024-05-14 |
| MX382832B (es) | 2025-03-13 |
| AU2016305515A1 (en) | 2018-03-08 |
| EP3334719A1 (en) | 2018-06-20 |
| WO2017024412A1 (en) | 2017-02-16 |
| US20210107893A1 (en) | 2021-04-15 |
| EP3334719A4 (en) | 2019-02-06 |
| US11365186B2 (en) | 2022-06-21 |
| CA2994478C (en) | 2023-10-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6912039B2 (ja) | 置換ベンゾイミダゾール、それらの調製及び医薬品としてのそれらの使用 | |
| JP6154004B2 (ja) | ブロモドメイン阻害剤のベンゾ[c]イソオキサゾロアゼピン及びその使用 | |
| JP2016519660A (ja) | ブロモドメイン阻害剤としてのオキサゾロ[5,4−c]キノリン−2−オン化合物 | |
| JP2017511801A (ja) | BETブロモドメイン阻害剤としての9H−ピリミド[4,5−b]インドールおよび関連類似体 | |
| WO2018205938A1 (zh) | Parp抑制剂、其药物组合物、制备方法和应用 | |
| US20200299262A1 (en) | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals | |
| US10836742B2 (en) | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals | |
| BR112018002547B1 (pt) | Benzimidazóis substituídos, seus usos, e composição farmacêutica | |
| HK1256752B (en) | Substituted benzimidazoles, their preparation and their use as pharmaceuticals |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20190813 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20190813 |
|
| RD04 | Notification of resignation of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7424 Effective date: 20190919 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20200630 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20200714 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20201007 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20210113 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20210608 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20210624 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6912039 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| S111 | Request for change of ownership or part of ownership |
Free format text: JAPANESE INTERMEDIATE CODE: R313113 |
|
| R350 | Written notification of registration of transfer |
Free format text: JAPANESE INTERMEDIATE CODE: R350 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |