RU2009112397A - Бициклические азотсодержащие гетероциклические соединения для применения в качестве ингибиторов стеароил соа десатуразы - Google Patents
Бициклические азотсодержащие гетероциклические соединения для применения в качестве ингибиторов стеароил соа десатуразы Download PDFInfo
- Publication number
- RU2009112397A RU2009112397A RU2009112397/04A RU2009112397A RU2009112397A RU 2009112397 A RU2009112397 A RU 2009112397A RU 2009112397/04 A RU2009112397/04 A RU 2009112397/04A RU 2009112397 A RU2009112397 A RU 2009112397A RU 2009112397 A RU2009112397 A RU 2009112397A
- Authority
- RU
- Russia
- Prior art keywords
- methyl
- amino
- oxo
- hydropyridino
- pyrazin
- Prior art date
Links
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 35
- 125000000217 alkyl group Chemical group 0.000 claims abstract 22
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 21
- 125000003118 aryl group Chemical group 0.000 claims abstract 16
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 14
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 12
- 239000001257 hydrogen Substances 0.000 claims abstract 12
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 8
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 6
- 229910052736 halogen Inorganic materials 0.000 claims abstract 6
- 150000002367 halogens Chemical group 0.000 claims abstract 6
- 125000002950 monocyclic group Chemical group 0.000 claims abstract 4
- 125000001424 substituent group Chemical group 0.000 claims abstract 4
- 125000002947 alkylene group Chemical group 0.000 claims abstract 3
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 3
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims abstract 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims abstract 2
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 101
- -1 CF 3 Chemical group 0.000 claims 90
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 66
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 64
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 63
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 52
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 36
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 24
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 10
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 7
- 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- DNSISZSEWVHGLH-UHFFFAOYSA-N butanamide Chemical compound CCCC(N)=O DNSISZSEWVHGLH-UHFFFAOYSA-N 0.000 claims 5
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 5
- 125000003373 pyrazinyl group Chemical group 0.000 claims 5
- BHHMPZQRVWVAAR-UHFFFAOYSA-N 7-bromo-8-methylpyrido[2,3-b]pyrazine Chemical compound C1=CN=C2C(C)=C(Br)C=NC2=N1 BHHMPZQRVWVAAR-UHFFFAOYSA-N 0.000 claims 4
- LAQJGAKLLZAETL-UHFFFAOYSA-N 2h-pyrazin-3-one Chemical compound O=C1CN=CC=N1 LAQJGAKLLZAETL-UHFFFAOYSA-N 0.000 claims 3
- 125000004860 4-ethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])C([H])([H])[H] 0.000 claims 3
- KXKVLQRXCPHEJC-UHFFFAOYSA-N acetic acid trimethyl ester Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- AGRIQBHIKABLPJ-UHFFFAOYSA-N 1-Pyrrolidinecarboxaldehyde Chemical compound O=CN1CCCC1 AGRIQBHIKABLPJ-UHFFFAOYSA-N 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- OBNCKNCVKJNDBV-UHFFFAOYSA-N ethyl butyrate Chemical compound CCCC(=O)OCC OBNCKNCVKJNDBV-UHFFFAOYSA-N 0.000 claims 2
- FKRCODPIKNYEAC-UHFFFAOYSA-N ethyl propionate Chemical compound CCOC(=O)CC FKRCODPIKNYEAC-UHFFFAOYSA-N 0.000 claims 2
- QPJVMBTYPHYUOC-UHFFFAOYSA-N methyl benzoate Chemical compound COC(=O)C1=CC=CC=C1 QPJVMBTYPHYUOC-UHFFFAOYSA-N 0.000 claims 2
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000006479 2-pyridyl methyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 1
- 125000006275 3-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C([H])C(*)=C1[H] 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 1
- 125000006201 3-phenylpropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 239000005711 Benzoic acid Substances 0.000 claims 1
- 229940123980 Desaturase inhibitor Drugs 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Substances 0.000 claims 1
- 108010087894 Fatty acid desaturases Proteins 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 1
- 102000016553 Stearoyl-CoA Desaturase Human genes 0.000 claims 1
- 235000010233 benzoic acid Nutrition 0.000 claims 1
- 125000000440 benzylamino group Chemical group [H]N(*)C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 1
- 229940095102 methyl benzoate Drugs 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 claims 1
- RSIPQHOWTCNEBI-UHFFFAOYSA-N n-hydroxypropanamide Chemical compound CCC(=O)NO RSIPQHOWTCNEBI-UHFFFAOYSA-N 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- LBSPXSWCJDGBOR-UHFFFAOYSA-N propanoic acid;pyrazine Chemical compound CCC(O)=O.C1=CN=CC=N1 LBSPXSWCJDGBOR-UHFFFAOYSA-N 0.000 claims 1
- 235000019260 propionic acid Nutrition 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- NIPZZXUFJPQHNH-UHFFFAOYSA-N pyrazine-2-carboxylic acid Chemical compound OC(=O)C1=CN=CC=N1 NIPZZXUFJPQHNH-UHFFFAOYSA-N 0.000 claims 1
- 239000010802 sludge Substances 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- LFKDJXLFVYVEFG-UHFFFAOYSA-N tert-butyl carbamate Chemical compound CC(C)(C)OC(N)=O LFKDJXLFVYVEFG-UHFFFAOYSA-N 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- 101100240528 Caenorhabditis elegans nhr-23 gene Proteins 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical group O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- 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
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- 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
- A61P17/06—Antipsoriatics
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
- C07D241/40—Benzopyrazines
- C07D241/44—Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Ophthalmology & Optometry (AREA)
- Gastroenterology & Hepatology (AREA)
- Vascular Medicine (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US84964806P | 2006-10-05 | 2006-10-05 | |
| US60/849,648 | 2006-10-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2009112397A true RU2009112397A (ru) | 2010-10-10 |
Family
ID=39106151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2009112397/04A RU2009112397A (ru) | 2006-10-05 | 2007-10-05 | Бициклические азотсодержащие гетероциклические соединения для применения в качестве ингибиторов стеароил соа десатуразы |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US7732453B2 (enExample) |
| EP (1) | EP2066665A2 (enExample) |
| JP (1) | JP2010505881A (enExample) |
| KR (1) | KR20090057416A (enExample) |
| CN (1) | CN101522676A (enExample) |
| AU (1) | AU2007303056A1 (enExample) |
| BR (1) | BRPI0717502A2 (enExample) |
| CA (1) | CA2665476A1 (enExample) |
| IL (1) | IL197828A0 (enExample) |
| MX (1) | MX2009003658A (enExample) |
| RU (1) | RU2009112397A (enExample) |
| WO (1) | WO2008043087A2 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101522676A (zh) * | 2006-10-05 | 2009-09-02 | Cv医药有限公司 | 用作硬脂酰-CoA脱氢酶抑制剂的双环含氮杂环化合物 |
| US7893066B2 (en) * | 2006-10-05 | 2011-02-22 | Gilead Palo Alto, Inc. | Pyridol[2,3-B]pyrazinones for use as stearoyl CoA desaturase inhibitors |
| JP2010523653A (ja) * | 2007-04-09 | 2010-07-15 | ギリアード・パロ・アルト・インコーポレイテッド | ステアロイルＣｏＡデサチュラーゼのインヒビターとして使用するためのプテリジノン誘導体 |
| US20080255161A1 (en) * | 2007-04-11 | 2008-10-16 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| US20090105283A1 (en) * | 2007-04-11 | 2009-04-23 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| KR101589628B1 (ko) * | 2008-03-05 | 2016-01-28 | 메르크 파텐트 게엠베하 | 인슐린 분비 자극제들로서의 피리도피라지논 유도체들, 이들을 얻기 위한 방법들 및 당뇨병 치료를 위한 이들의 용도 |
| JP2011516498A (ja) * | 2008-04-04 | 2011-05-26 | ギリアード サイエンシーズ， インコーポレイテッド | ステアロイル−ＣｏＡデサチュラーゼの阻害剤として使用するためのトリアゾロピリジノン誘導体 |
| CA2719362A1 (en) * | 2008-04-04 | 2009-10-08 | Gilead Sciences, Inc. | Pyrrolotriazinone derivatives for use as stearoyl coa desaturase inhibitors |
| EP2276748A1 (en) * | 2008-04-10 | 2011-01-26 | Gilead Sciences, Inc. | Bicyclic nitrogen containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors |
| US20100267752A1 (en) * | 2008-10-15 | 2010-10-21 | Gilead Palo Alto, Inc. | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| MX2014004426A (es) | 2011-10-15 | 2014-07-09 | Genentech Inc | Metodos de uso de antagonistas de scd1. |
| RU2606230C1 (ru) * | 2015-10-20 | 2017-01-10 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" | (Z)-Этил 2-(4-(4-хлорфенил)-2,4-диоксо-3-(3-оксо-3,4-дигидрохиноксалин-2(1Н)-илиден)бутанамидо)-4-метил-5-фенилтиофен-3-карбоксилат, обладающий противодиабетической активностью, и способ его получения |
| US11278591B2 (en) | 2016-03-22 | 2022-03-22 | Balchem Corporation | Compositions comprising choline |
| JP2019533022A (ja) | 2016-10-24 | 2019-11-14 | ユマニティ セラピューティクス，インコーポレーテッド | 化合物及びその使用 |
| CA3049010A1 (en) | 2017-01-06 | 2018-07-12 | Yumanity Therapeutics, Inc. | Methods for the treatment of neurological disorders |
| CA3083000A1 (en) | 2017-10-24 | 2019-05-02 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| CA3094527A1 (en) | 2018-03-23 | 2019-09-26 | Yumanity Therapeutics, Inc. | Compounds and uses thereof |
| US12098146B2 (en) | 2019-01-24 | 2024-09-24 | Janssen Pharmaceutica Nv | Compounds and uses thereof |
| EA202192047A1 (ru) | 2019-11-13 | 2021-12-08 | Юманити Терапьютикс, Инк. | Соединения и их применение |
| US11512097B2 (en) | 2019-11-25 | 2022-11-29 | Amgen Inc. | Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use |
| JP2023549540A (ja) | 2020-11-18 | 2023-11-27 | デシフェラ・ファーマシューティカルズ，エルエルシー | Ｇｃｎ２およびｐｅｒｋキナーゼ阻害剤およびその使用方法 |
| PE20250609A1 (es) | 2021-12-03 | 2025-02-26 | Deciphera Pharmaceuticals Llc | Inhibidores de gcn2 y perk quinasa y metodos de uso de los mismos |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| US5364620A (en) | 1983-12-22 | 1994-11-15 | Elan Corporation, Plc | Controlled absorption diltiazem formulation for once daily administration |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| CA2020073A1 (en) | 1989-07-03 | 1991-01-04 | Eric E. Allen | Substituted quinazolinones as angiotensin ii antagonists |
| AU1917999A (en) * | 1998-03-31 | 1999-10-18 | Warner-Lambert Company | Quinoxalinones as serine protease inhibitors such as factor xa and thrombin |
| PT1094816E (pt) | 1998-07-06 | 2009-03-10 | Bristol Myers Squibb Co | Sulfonamidas bifenílicas duplamente antagonistas receptores de angiotensina e endotelina |
| KR20020027649A (ko) | 1999-09-15 | 2002-04-13 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | 카이나제 억제제로서의 프테리딘온 |
| WO2002076954A1 (en) * | 2001-03-23 | 2002-10-03 | Smithkline Beecham Corporation | Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases |
| AU2002249275A1 (en) | 2002-03-08 | 2003-09-22 | Warner-Lambert Company Llc | Oxo azabicyclic compounds |
| US7196090B2 (en) * | 2002-07-25 | 2007-03-27 | Warner-Lambert Company | Kinase inhibitors |
| US20040142950A1 (en) * | 2003-01-17 | 2004-07-22 | Bunker Amy Mae | Amide and ester matrix metalloproteinase inhibitors |
| US7456180B2 (en) * | 2003-07-30 | 2008-11-25 | Xenon Pharmaceuticals Inc. | Piperazine derivatives and their use as therapeutic agents |
| WO2006066361A1 (en) * | 2004-12-24 | 2006-06-29 | The University Of Queensland | Method of treatment or prophylaxis |
| US7893066B2 (en) * | 2006-10-05 | 2011-02-22 | Gilead Palo Alto, Inc. | Pyridol[2,3-B]pyrazinones for use as stearoyl CoA desaturase inhibitors |
| CN101522676A (zh) * | 2006-10-05 | 2009-09-02 | Cv医药有限公司 | 用作硬脂酰-CoA脱氢酶抑制剂的双环含氮杂环化合物 |
| JP2010523653A (ja) | 2007-04-09 | 2010-07-15 | ギリアード・パロ・アルト・インコーポレイテッド | ステアロイルＣｏＡデサチュラーゼのインヒビターとして使用するためのプテリジノン誘導体 |
| US20080255161A1 (en) * | 2007-04-11 | 2008-10-16 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| US20090105283A1 (en) * | 2007-04-11 | 2009-04-23 | Dmitry Koltun | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS |
| CA2719362A1 (en) * | 2008-04-04 | 2009-10-08 | Gilead Sciences, Inc. | Pyrrolotriazinone derivatives for use as stearoyl coa desaturase inhibitors |
| JP2011516498A (ja) * | 2008-04-04 | 2011-05-26 | ギリアード サイエンシーズ， インコーポレイテッド | ステアロイル−ＣｏＡデサチュラーゼの阻害剤として使用するためのトリアゾロピリジノン誘導体 |
-
2007
- 2007-10-05 CN CNA2007800367748A patent/CN101522676A/zh active Pending
- 2007-10-05 AU AU2007303056A patent/AU2007303056A1/en not_active Abandoned
- 2007-10-05 BR BRPI0717502-7A patent/BRPI0717502A2/pt not_active IP Right Cessation
- 2007-10-05 MX MX2009003658A patent/MX2009003658A/es not_active Application Discontinuation
- 2007-10-05 WO PCT/US2007/080627 patent/WO2008043087A2/en not_active Ceased
- 2007-10-05 EP EP07853820A patent/EP2066665A2/en not_active Ceased
- 2007-10-05 RU RU2009112397/04A patent/RU2009112397A/ru not_active Application Discontinuation
- 2007-10-05 US US11/868,386 patent/US7732453B2/en not_active Expired - Fee Related
- 2007-10-05 JP JP2009531633A patent/JP2010505881A/ja active Pending
- 2007-10-05 KR KR1020097006958A patent/KR20090057416A/ko not_active Withdrawn
- 2007-10-05 CA CA002665476A patent/CA2665476A1/en not_active Abandoned
-
2009
- 2009-03-26 IL IL197828A patent/IL197828A0/en unknown
-
2010
- 2010-04-26 US US12/767,515 patent/US8148376B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN101522676A (zh) | 2009-09-02 |
| IL197828A0 (en) | 2009-12-24 |
| EP2066665A2 (en) | 2009-06-10 |
| JP2010505881A (ja) | 2010-02-25 |
| MX2009003658A (es) | 2009-04-22 |
| US7732453B2 (en) | 2010-06-08 |
| AU2007303056A1 (en) | 2008-04-10 |
| KR20090057416A (ko) | 2009-06-05 |
| WO2008043087A3 (en) | 2008-05-22 |
| US8148376B2 (en) | 2012-04-03 |
| CA2665476A1 (en) | 2008-04-10 |
| BRPI0717502A2 (pt) | 2015-06-16 |
| US20100204238A1 (en) | 2010-08-12 |
| WO2008043087A2 (en) | 2008-04-10 |
| US20080139570A1 (en) | 2008-06-12 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2665476A1 (en) | Bicyclic nitrogen-containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors | |
| JP2010505881A5 (enExample) | ||
| RU2373209C2 (ru) | Пирролотриазиновые соединения как ингибиторы киназ | |
| RU2007148217A (ru) | Получение производных n-фенил-2-пиримидинамина | |
| CA2410662A1 (en) | Novel peptides as ns3-serine protease inhibitors of hepatitis c virus | |
| JP2010516635A5 (enExample) | ||
| RU2015105561A (ru) | Замещенные гетероазепиноны | |
| RU2006147267A (ru) | Конденсированное гетероциклическое соединение | |
| JP2009521467A5 (enExample) | ||
| JP2004508365A5 (enExample) | ||
| JP2005508336A5 (enExample) | ||
| HRP20120656T1 (hr) | Derivati indazolil amida za liječenje poremećaja posredovanih glukokortikoidnim receptorom | |
| RU2009149307A (ru) | Новое амидное производное для ингибирования роста раковых клеток | |
| RU2007101073A (ru) | Пятичленные гетероциклы, применимые в качестве ингибиторов сериновой протеазы | |
| RU2000128036A (ru) | Амидиновые соединения | |
| SI3106463T1 (en) | Compounds of substituted pyrazolo (1,5-) pyrimidine as inhibitors of TRK kinase | |
| CA2461812A1 (en) | 3-(arylamino)methylene-1,3-dihydro-2h-indol-2-ones as kinase inhibitors | |
| CN1980892A (zh) | Dpp－iv抑制剂 | |
| RU2008112683A (ru) | Ингибиторы fap | |
| MXPA04009497A (es) | Piridinoilpiperidinas como antagonistas de 5-ht1f. | |
| RU2009118491A (ru) | Замещенные соединения тетрагидропироллопиразина и их применение в лекарственных средствах (имеющих свою торговую марку gra 3 363) | |
| JP2010523653A5 (enExample) | ||
| HUP0402344A2 (hu) | Helyettesített 2-amino-cikloalkán-karboxamidok, felhasználásuk cisztein-proteáz-inhibitorként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények | |
| RU2004138789A (ru) | Производные n-(3-оксо-2,3-дигидро-1h-изоиндол1-1- ил)ацетил)гуанидина в качестве ингибиторов nhe-1 для лечения инфаркта и стенокардии | |
| RU2004117543A (ru) | Амиды антраниловой кислоты и их применение в качестве ингибиторов тирозинкиназного рецептора фактора роста сосудистого эндотелия (vegf) |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20120118 |