AU2015360583B2 - Small molecule inhibitors of fibrosis - Google Patents
Small molecule inhibitors of fibrosis Download PDFInfo
- Publication number
- AU2015360583B2 AU2015360583B2 AU2015360583A AU2015360583A AU2015360583B2 AU 2015360583 B2 AU2015360583 B2 AU 2015360583B2 AU 2015360583 A AU2015360583 A AU 2015360583A AU 2015360583 A AU2015360583 A AU 2015360583A AU 2015360583 B2 AU2015360583 B2 AU 2015360583B2
- Authority
- AU
- Australia
- Prior art keywords
- compound
- formula
- alkyl
- alkylene
- cycloalkyl
- 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.)
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Links
- 0 CC(CC*)*(*=C*1c2ccc(*(CC3)CC*3c3ccc(*)cc3)cc2)C1=O Chemical compound CC(CC*)*(*=C*1c2ccc(*(CC3)CC*3c3ccc(*)cc3)cc2)C1=O 0.000 description 15
- FGYADSCZTQOAFK-UHFFFAOYSA-N C[n]1c2ccccc2nc1 Chemical compound C[n]1c2ccccc2nc1 FGYADSCZTQOAFK-UHFFFAOYSA-N 0.000 description 2
- ITQTTZVARXURQS-UHFFFAOYSA-N Cc1cccnc1 Chemical compound Cc1cccnc1 ITQTTZVARXURQS-UHFFFAOYSA-N 0.000 description 2
- FKNQCJSGGFJEIZ-UHFFFAOYSA-N Cc1ccncc1 Chemical compound Cc1ccncc1 FKNQCJSGGFJEIZ-UHFFFAOYSA-N 0.000 description 2
- TWGNOYAGHYUFFR-UHFFFAOYSA-N Cc1cncnc1 Chemical compound Cc1cncnc1 TWGNOYAGHYUFFR-UHFFFAOYSA-N 0.000 description 2
- AIKUBOPKWKZULG-UHFFFAOYSA-N Cc1cnncc1 Chemical compound Cc1cnncc1 AIKUBOPKWKZULG-UHFFFAOYSA-N 0.000 description 2
- IOESHGVPCMWQSU-UHFFFAOYSA-N O=C(C=C1)C=CN1I Chemical compound O=C(C=C1)C=CN1I IOESHGVPCMWQSU-UHFFFAOYSA-N 0.000 description 2
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- UFDHBUVRMLSOSV-NPZVTGPUSA-N CCC(C)N(C1=O)N=CN1c(cc1)ccc1NCCNc(cc1)ccc1OC[C@H]1O[C@@](CC2=C[N-][NH+](CCC(C)N(C3=O)N=CN3c(cc3)ccc3N(CC3)CCN3c(cc3)ccc3OC[C@H]3O[C@@](Cc4cnncc4)(c(cccc4)c4Cl)OC3)C=C2)(c(cc2C)ccc2Cl)OC1 Chemical compound CCC(C)N(C1=O)N=CN1c(cc1)ccc1NCCNc(cc1)ccc1OC[C@H]1O[C@@](CC2=C[N-][NH+](CCC(C)N(C3=O)N=CN3c(cc3)ccc3N(CC3)CCN3c(cc3)ccc3OC[C@H]3O[C@@](Cc4cnncc4)(c(cccc4)c4Cl)OC3)C=C2)(c(cc2C)ccc2Cl)OC1 UFDHBUVRMLSOSV-NPZVTGPUSA-N 0.000 description 1
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- JGRXWZIVIRCZRO-FQXCHJBKSA-N CCC(C)N(C=NN1c(cc2)ccc2N(CC2)CCN2c(cc2)ccc2OC[C@H]2O[C@](Cc3ccccc3)(c3ccccc3)OC2)C1=O Chemical compound CCC(C)N(C=NN1c(cc2)ccc2N(CC2)CCN2c(cc2)ccc2OC[C@H]2O[C@](Cc3ccccc3)(c3ccccc3)OC2)C1=O JGRXWZIVIRCZRO-FQXCHJBKSA-N 0.000 description 1
- YMAPNGUJQWOOOA-HISYPHHESA-N CCC(CC)N(C1=O)N=CN1c(cc1)ccc1N(CC1)CCN1c(ccc(OC[C@H]1O[C@](C[n]2nc(CCC(CC)N(C3=O)N=CN3c(cc3)ccc3N(CC3)CCN3c(ccc(OC[C@H]3O[C@](C[n]4nccn4)(c(ccc(Cl)c4)c4Cl)OC3)c3)c3C#N)cn2)(c(ccc(Cl)c2)c2Cl)OC1)c1)c1F Chemical compound CCC(CC)N(C1=O)N=CN1c(cc1)ccc1N(CC1)CCN1c(ccc(OC[C@H]1O[C@](C[n]2nc(CCC(CC)N(C3=O)N=CN3c(cc3)ccc3N(CC3)CCN3c(ccc(OC[C@H]3O[C@](C[n]4nccn4)(c(ccc(Cl)c4)c4Cl)OC3)c3)c3C#N)cn2)(c(ccc(Cl)c2)c2Cl)OC1)c1)c1F YMAPNGUJQWOOOA-HISYPHHESA-N 0.000 description 1
- HCWHZLPXKGIFOM-KMFSKSIHSA-N CC[C@@H](C)N(C1=O)N=CN1c(cc1)ccc1N(CC1)CCN1c(cc1)ccc1OC[C@@H]1O[C@@](C[n]2nccn2)(c2ccccc2)OC1 Chemical compound CC[C@@H](C)N(C1=O)N=CN1c(cc1)ccc1N(CC1)CCN1c(cc1)ccc1OC[C@@H]1O[C@@](C[n]2nccn2)(c2ccccc2)OC1 HCWHZLPXKGIFOM-KMFSKSIHSA-N 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- TYJMXMFZUFPWIK-UHFFFAOYSA-N CN1N=CC=CC1=O Chemical compound CN1N=CC=CC1=O TYJMXMFZUFPWIK-UHFFFAOYSA-N 0.000 description 1
- FUSFWUFSEJXMRQ-UHFFFAOYSA-N COC(CBr)OC Chemical compound COC(CBr)OC FUSFWUFSEJXMRQ-UHFFFAOYSA-N 0.000 description 1
- CSUGQXMRKOKBFI-UHFFFAOYSA-N C[n]1ncc2ccccc12 Chemical compound C[n]1ncc2ccccc12 CSUGQXMRKOKBFI-UHFFFAOYSA-N 0.000 description 1
- UQFQONCQIQEYPJ-UHFFFAOYSA-N C[n]1nccc1 Chemical compound C[n]1nccc1 UQFQONCQIQEYPJ-UHFFFAOYSA-N 0.000 description 1
- CGFBQTMCOVITFC-UHFFFAOYSA-N I[n]1c(cc(cc2)-c(ccc3n4)cc3n[n]4I)c2nc1 Chemical compound I[n]1c(cc(cc2)-c(ccc3n4)cc3n[n]4I)c2nc1 CGFBQTMCOVITFC-UHFFFAOYSA-N 0.000 description 1
- LIGACIXOYTUXAW-UHFFFAOYSA-N O=C(CBr)c1ccccc1 Chemical compound O=C(CBr)c1ccccc1 LIGACIXOYTUXAW-UHFFFAOYSA-N 0.000 description 1
- USGQFWSEBWJWOJ-UHFFFAOYSA-N O=C(C[n]1nccn1)c1ccccc1 Chemical compound O=C(C[n]1nccn1)c1ccccc1 USGQFWSEBWJWOJ-UHFFFAOYSA-N 0.000 description 1
- GNTOZDWVVUXXRL-BVGRYSDNSA-N O=C(N(CC1CCCC1)N=C1)N1c(cc1)ccc1NCCNc(c(F)c1)ccc1OC[C@H]1O[C@](C[n]2nccn2)(c(ccc(Cl)c2)c2Cl)OC1 Chemical compound O=C(N(CC1CCCC1)N=C1)N1c(cc1)ccc1NCCNc(c(F)c1)ccc1OC[C@H]1O[C@](C[n]2nccn2)(c(ccc(Cl)c2)c2Cl)OC1 GNTOZDWVVUXXRL-BVGRYSDNSA-N 0.000 description 1
- AAILEWXSEQLMNI-UHFFFAOYSA-O O=C1[NH2+]N=CC=C1 Chemical compound O=C1[NH2+]N=CC=C1 AAILEWXSEQLMNI-UHFFFAOYSA-O 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/4192—1,2,3-Triazoles
-
- 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
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- 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
- 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
- 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
- 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
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- 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
-
- 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
-
- 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
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N57/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic phosphorus compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462090267P | 2014-12-10 | 2014-12-10 | |
| US62/090,267 | 2014-12-10 | ||
| US201562117846P | 2015-02-18 | 2015-02-18 | |
| US62/117,846 | 2015-02-18 | ||
| PCT/US2015/064814 WO2016094570A1 (en) | 2014-12-10 | 2015-12-09 | Small molecule inhibitors of fibrosis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2015360583A1 AU2015360583A1 (en) | 2017-06-22 |
| AU2015360583B2 true AU2015360583B2 (en) | 2020-01-23 |
Family
ID=56108132
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2015360583A Active AU2015360583B2 (en) | 2014-12-10 | 2015-12-09 | Small molecule inhibitors of fibrosis |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US10336735B2 (enExample) |
| EP (1) | EP3250036B1 (enExample) |
| JP (1) | JP6706023B2 (enExample) |
| KR (1) | KR102548066B1 (enExample) |
| CN (1) | CN107404878B (enExample) |
| AU (1) | AU2015360583B2 (enExample) |
| CA (1) | CA2968874C (enExample) |
| ES (1) | ES2879963T3 (enExample) |
| WO (1) | WO2016094570A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11028078B2 (en) * | 2011-09-07 | 2021-06-08 | The Johns Hopkins University | Itraconazole analogs and use thereof |
| US11571431B2 (en) | 2013-12-04 | 2023-02-07 | Galmed Research And Development Ltd | Aramchol salts |
| WO2015116947A1 (en) * | 2014-02-01 | 2015-08-06 | University Of Connecticut | Itraconazole analogues and methods of use thereof |
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