AU2014248680B2 - Substituted 2-azabicycles and their use as orexin receptor modulators - Google Patents
Substituted 2-azabicycles and their use as orexin receptor modulators Download PDFInfo
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- AU2014248680B2 AU2014248680B2 AU2014248680A AU2014248680A AU2014248680B2 AU 2014248680 B2 AU2014248680 B2 AU 2014248680B2 AU 2014248680 A AU2014248680 A AU 2014248680A AU 2014248680 A AU2014248680 A AU 2014248680A AU 2014248680 B2 AU2014248680 B2 AU 2014248680B2
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- azabicyclo
- pyridin
- methanone
- trifluoromethyl
- heptan
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- XIUVBVUIWHYEMR-UHFFFAOYSA-N O=C(c(cccc1)c1-c1ncccn1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1F Chemical compound O=C(c(cccc1)c1-c1ncccn1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1F XIUVBVUIWHYEMR-UHFFFAOYSA-N 0.000 description 1
- DLRXJKZYHRTQQH-UHFFFAOYSA-N O=C(c(cccc1F)c1-[n]1nccn1)N(CC(CC1)C2)C1C2Nc(cc1)ncc1Cl Chemical compound O=C(c(cccc1F)c1-[n]1nccn1)N(CC(CC1)C2)C1C2Nc(cc1)ncc1Cl DLRXJKZYHRTQQH-UHFFFAOYSA-N 0.000 description 1
- ZFCYESHCPYTKHK-UHFFFAOYSA-N O=C(c(cccc1F)c1-c1ncccn1)N(CC(C1)C2)C1C2Oc1ccc(C(F)(F)F)nn1 Chemical compound O=C(c(cccc1F)c1-c1ncccn1)N(CC(C1)C2)C1C2Oc1ccc(C(F)(F)F)nn1 ZFCYESHCPYTKHK-UHFFFAOYSA-N 0.000 description 1
- HUKWIAXQBOHZIX-UHFFFAOYSA-N O=C(c(cccc1F)c1-c1ncccn1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1 Chemical compound O=C(c(cccc1F)c1-c1ncccn1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1 HUKWIAXQBOHZIX-UHFFFAOYSA-N 0.000 description 1
- VOWAFSMPTGLLTI-UHFFFAOYSA-N O=C(c(cccc1F)c1-c1ncccn1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1F Chemical compound O=C(c(cccc1F)c1-c1ncccn1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1F VOWAFSMPTGLLTI-UHFFFAOYSA-N 0.000 description 1
- IXWIQPARZXLOIR-UHFFFAOYSA-N O=C(c(cccc1F)c1-c1ncccn1)N(CC(CC1)C2)C1C2Nc1ncc(C(F)(F)F)cn1 Chemical compound O=C(c(cccc1F)c1-c1ncccn1)N(CC(CC1)C2)C1C2Nc1ncc(C(F)(F)F)cn1 IXWIQPARZXLOIR-UHFFFAOYSA-N 0.000 description 1
- FYPXPKRVTVNMNW-UHFFFAOYSA-N O=C(c(nccc1)c1-c(nccc1)c1F)N1C(C(C2)Nc3ncc(C(F)(F)F)cc3)C2(C2)C2C1 Chemical compound O=C(c(nccc1)c1-c(nccc1)c1F)N1C(C(C2)Nc3ncc(C(F)(F)F)cc3)C2(C2)C2C1 FYPXPKRVTVNMNW-UHFFFAOYSA-N 0.000 description 1
- VICJEHAIUJBBEL-UHFFFAOYSA-N O=C(c(nccc1)c1-c1ncc[s]1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1 Chemical compound O=C(c(nccc1)c1-c1ncc[s]1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1 VICJEHAIUJBBEL-UHFFFAOYSA-N 0.000 description 1
- HFJOEQVRZKYVLC-UHFFFAOYSA-N O=C(c1c(-c(nc2)ncc2F)nccc1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1 Chemical compound O=C(c1c(-c(nc2)ncc2F)nccc1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1 HFJOEQVRZKYVLC-UHFFFAOYSA-N 0.000 description 1
- XIKRYFBAIPJPHB-UHFFFAOYSA-N O=C(c1c(-c2ccccc2)nccn1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1 Chemical compound O=C(c1c(-c2ccccc2)nccn1)N(CC(C1)C2)C1C2Oc1ncc(C(F)(F)F)cc1 XIKRYFBAIPJPHB-UHFFFAOYSA-N 0.000 description 1
- 0 ON=C1[C@](C2)*CC2C1 Chemical compound ON=C1[C@](C2)*CC2C1 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
-
- 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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D403/14—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 three or more hetero 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
- C07D405/14—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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| CA2856291C (en) | 2011-11-17 | 2020-08-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
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| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
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| US10668066B2 (en) | 2015-08-14 | 2020-06-02 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Crystal form of orexin receptor antagonist compound, and preparation method and application thereof |
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| GB2558975B (en) * | 2017-09-01 | 2019-01-23 | Chronos Therapeutics Ltd | Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists |
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