RU2012116124A - О-БЕНЗИЛ НИКОТИНАМИДНЫЕ АНАЛОГИ КАК ПОЗИТИВНЫЕ АЛЛОСТЕРИЧЕСКИЕ МОДУЛЯТОРЫ mGluR5 - Google Patents
О-БЕНЗИЛ НИКОТИНАМИДНЫЕ АНАЛОГИ КАК ПОЗИТИВНЫЕ АЛЛОСТЕРИЧЕСКИЕ МОДУЛЯТОРЫ mGluR5 Download PDFInfo
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- RU2012116124A RU2012116124A RU2012116124/13A RU2012116124A RU2012116124A RU 2012116124 A RU2012116124 A RU 2012116124A RU 2012116124/13 A RU2012116124/13 A RU 2012116124/13A RU 2012116124 A RU2012116124 A RU 2012116124A RU 2012116124 A RU2012116124 A RU 2012116124A
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- Prior art keywords
- substituted
- heterocycloalkyl
- cycloalkyl
- alkyl
- aryl
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- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 title claims abstract 5
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 title claims abstract 5
- 150000001875 compounds Chemical class 0.000 claims abstract 27
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims abstract 24
- 125000003118 aryl group Chemical group 0.000 claims abstract 21
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 20
- 125000000392 cycloalkenyl group Chemical group 0.000 claims abstract 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 19
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims abstract 18
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 17
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims abstract 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 16
- 150000004820 halides Chemical class 0.000 claims abstract 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 16
- 229940124530 sulfonamide Drugs 0.000 claims abstract 16
- 150000003456 sulfonamides Chemical class 0.000 claims abstract 16
- 150000003573 thiols Chemical class 0.000 claims abstract 16
- 125000000217 alkyl group Chemical group 0.000 claims abstract 15
- 125000000229 (C1-C4)alkoxy 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 7
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims abstract 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims abstract 7
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims abstract 7
- 229910052799 carbon Inorganic materials 0.000 claims abstract 7
- 150000003857 carboxamides Chemical class 0.000 claims abstract 7
- 229930195712 glutamate Natural products 0.000 claims abstract 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims abstract 5
- 125000004122 cyclic group Chemical group 0.000 claims abstract 5
- 230000004044 response Effects 0.000 claims abstract 5
- 125000001424 substituent group Chemical group 0.000 claims abstract 5
- 150000001204 N-oxides Chemical class 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 238000006243 chemical reaction Methods 0.000 claims abstract 3
- 101001032838 Rattus norvegicus Metabotropic glutamate receptor 5 Proteins 0.000 claims abstract 2
- 210000003292 kidney cell Anatomy 0.000 claims abstract 2
- 150000002431 hydrogen Chemical class 0.000 claims 6
- -1 i-pentyl Chemical group 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 208000028017 Psychotic disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 230000004064 dysfunction Effects 0.000 claims 2
- 208000024714 major depressive disease Diseases 0.000 claims 2
- 230000000926 neurological effect Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000020016 psychiatric disease Diseases 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 208000017194 Affective disease Diseases 0.000 claims 1
- 208000000044 Amnesia Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010048962 Brain oedema Diseases 0.000 claims 1
- 206010008748 Chorea Diseases 0.000 claims 1
- 206010012218 Delirium Diseases 0.000 claims 1
- 208000024254 Delusional disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 208000014094 Dystonic disease Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
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- 208000002193 Pain Diseases 0.000 claims 1
- 206010033664 Panic attack Diseases 0.000 claims 1
- 208000020186 Schizophreniform disease Diseases 0.000 claims 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims 1
- 230000007000 age related cognitive decline Effects 0.000 claims 1
- 230000003281 allosteric effect Effects 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000005872 benzooxazolyl group Chemical group 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 1
- 208000006752 brain edema Diseases 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 208000012601 choreatic disease Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- DYMRYCZRMAHYKE-UHFFFAOYSA-N n-diazonitramide Chemical compound [O-][N+](=O)N=[N+]=[N-] DYMRYCZRMAHYKE-UHFFFAOYSA-N 0.000 claims 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 238000010534 nucleophilic substitution reaction Methods 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 208000019906 panic disease Diseases 0.000 claims 1
- 208000002851 paranoid schizophrenia Diseases 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 208000022610 schizoaffective disease Diseases 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 229910000104 sodium hydride Inorganic materials 0.000 claims 1
- 239000012312 sodium hydride Substances 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/84—Nitriles
- C07D213/85—Nitriles in position 3
-
- 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
- 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
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
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- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Biomedical Technology (AREA)
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- Psychiatry (AREA)
- Addiction (AREA)
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- Diabetes (AREA)
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- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Orthopedic Medicine & Surgery (AREA)
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- Emergency Medicine (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24441709P | 2009-09-21 | 2009-09-21 | |
| US61/244,417 | 2009-09-21 | ||
| PCT/US2010/049697 WO2011035324A1 (en) | 2009-09-21 | 2010-09-21 | O-benzyl nicotinamide analogs as mglur5 positive allosteric modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2012116124A true RU2012116124A (ru) | 2013-10-27 |
Family
ID=43759065
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012116124/13A RU2012116124A (ru) | 2009-09-21 | 2010-09-21 | О-БЕНЗИЛ НИКОТИНАМИДНЫЕ АНАЛОГИ КАК ПОЗИТИВНЫЕ АЛЛОСТЕРИЧЕСКИЕ МОДУЛЯТОРЫ mGluR5 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20110183980A1 (OSRAM) |
| EP (1) | EP2482657A4 (OSRAM) |
| JP (1) | JP2013505297A (OSRAM) |
| CN (1) | CN102638979A (OSRAM) |
| AU (1) | AU2010295288A1 (OSRAM) |
| BR (1) | BR112012006330A2 (OSRAM) |
| CA (1) | CA2774981A1 (OSRAM) |
| IL (1) | IL218772A0 (OSRAM) |
| IN (1) | IN2012DN03322A (OSRAM) |
| MX (1) | MX2012003394A (OSRAM) |
| RU (1) | RU2012116124A (OSRAM) |
| WO (1) | WO2011035324A1 (OSRAM) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2542100C1 (ru) * | 2013-12-24 | 2015-02-20 | Федеральное государственное бюджетное учреждение науки Институт химии растворов им. Г.А. Крестова Российской Академии Наук (ИХС РАН) | Сокристаллическая форма теофиллина с дифлунисалом или диклофенаком |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8772301B2 (en) | 2009-12-18 | 2014-07-08 | Sunovion Pharmaceuticals, Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| CN103037693A (zh) * | 2010-05-24 | 2013-04-10 | 范德比尔特大学 | 作为mglur5正向变构调节剂的取代的6-甲基烟酰胺 |
| TWI713497B (zh) | 2015-02-26 | 2020-12-21 | 南韓商愛思開生物製藥股份有限公司 | 咪唑并嘧啶及咪唑并三衍生物及包含該衍生物之醫藥組成物 |
| CA3145305A1 (en) | 2019-07-11 | 2021-01-14 | ESCAPE Bio, Inc. | Indazoles and azaindazoles as lrrk2 inhibitors |
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| AR208397A1 (es) * | 1973-02-20 | 1976-12-27 | Ciba Geigy Ag | Procedimiento para la elaboracion de compuestos de 1-piridiloxi-2-hidroxi-3-amino-propano1-piraziniloxi-2-hidroxi-3-amino-propano y 1-pirimidiniloxi-2-hidroxi-3-amino-propan |
| JP2689093B2 (ja) * | 1986-01-30 | 1997-12-10 | 石原産業株式会社 | 置換ピリジンスルホンアミド系化合物、それらを含有する除草剤並びにそれらの化合物の製造方法 |
| JP2000212076A (ja) * | 1998-11-20 | 2000-08-02 | Takeda Chem Ind Ltd | βアミロイド蛋白産生・分泌阻害剤 |
| US6586475B1 (en) * | 1998-11-20 | 2003-07-01 | Takeda Chemical Industries, Ltd. | β-amyloid protein production/secretion inhibitors |
| US20030031715A1 (en) * | 2000-10-11 | 2003-02-13 | Kinam Park | Pharmaceutical applications of hydrotropic agents, polymers thereof, and hydrogels thereof |
| JP2002322163A (ja) * | 2001-04-20 | 2002-11-08 | Sumitomo Pharmaceut Co Ltd | ピペラジン誘導体 |
| US6667327B2 (en) * | 2002-02-04 | 2003-12-23 | Hoffmann-La Roche Inc. | Pyridine amido derivatives |
| US20040072802A1 (en) * | 2002-10-09 | 2004-04-15 | Jingwu Duan | Beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-alpha |
| JPWO2004078719A1 (ja) * | 2003-03-06 | 2006-06-08 | 小野薬品工業株式会社 | インドール誘導体化合物およびその化合物を有効成分とする薬剤 |
| GB0418267D0 (en) * | 2004-08-16 | 2004-09-15 | Glaxo Group Ltd | Novel compounds |
| CN101155781B (zh) * | 2005-04-06 | 2012-11-07 | 霍夫曼-拉罗奇有限公司 | 作为cb1逆激动剂的吡啶-3-甲酰胺衍生物 |
| WO2007008963A1 (en) * | 2005-07-13 | 2007-01-18 | Jenrin Discovery | Mao-b inhibitors useful for treating obesity |
| AR058554A1 (es) * | 2005-12-20 | 2008-02-13 | Novartis Ag | Compuestos heterociclicos nitrogenados de 6 miembros sustituidos, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades mediadas por mglur5. |
| CN101321731A (zh) * | 2005-12-20 | 2008-12-10 | 诺瓦提斯公司 | 作为代谢型谷氨酸受体调节剂的烟酸衍生物 |
| CA2665804A1 (en) * | 2006-08-23 | 2008-02-28 | Astellas Pharma Inc. | Urea compound or salt thereof |
| WO2008031550A2 (en) * | 2006-09-11 | 2008-03-20 | Novartis Ag | Nicotinic acid derivatives as modulators of metabotropic glutanate receptors |
| WO2008038841A1 (en) * | 2006-09-30 | 2008-04-03 | Japan Tobacco Inc. | Thiadiazolone derivative and use thereof |
| TW200821305A (en) * | 2006-10-05 | 2008-05-16 | Astrazeneca Ab | MGluR5 modulators |
| US8853392B2 (en) * | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| CA2706328C (en) * | 2007-11-20 | 2016-04-19 | Janssen Pharmaceutica N.V. | Cycloalkyloxy- and heterocycloalkyloxypyridine compounds as modulators of the histamine h3 receptor |
| JP5301557B2 (ja) * | 2007-12-04 | 2013-09-25 | エフ．ホフマン−ラ ロシュ アーゲー | イソオキサゾロ−ピリジン誘導体 |
| US7897621B2 (en) * | 2008-03-31 | 2011-03-01 | Hoffmann-La Roche Inc. | 2-trifluoromethylnicotinamide derivatives as HDL-cholesterol raising agents |
| EP3725775A1 (en) * | 2009-02-17 | 2020-10-21 | Syntrix Biosystems, Inc. | Pyridine- and pyrimidinecarboxamides as cxcr2 modulators |
| US8222246B2 (en) * | 2009-04-02 | 2012-07-17 | Hoffmann-La Roche Inc. | Substituted isoxazoles |
| CA2757412C (en) * | 2009-05-07 | 2016-04-05 | F. Hoffmann-La Roche Ag | Isoxazole-pyridine derivatives as gaba modulators |
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- 2010-09-21 RU RU2012116124/13A patent/RU2012116124A/ru not_active Application Discontinuation
- 2010-09-21 US US12/886,950 patent/US20110183980A1/en not_active Abandoned
- 2010-09-21 EP EP10818037.3A patent/EP2482657A4/en not_active Withdrawn
- 2010-09-21 AU AU2010295288A patent/AU2010295288A1/en not_active Abandoned
- 2010-09-21 WO PCT/US2010/049697 patent/WO2011035324A1/en not_active Ceased
- 2010-09-21 JP JP2012530978A patent/JP2013505297A/ja active Pending
- 2010-09-21 CN CN2010800523979A patent/CN102638979A/zh active Pending
- 2010-09-21 BR BR112012006330A patent/BR112012006330A2/pt not_active IP Right Cessation
- 2010-09-21 CA CA2774981A patent/CA2774981A1/en not_active Abandoned
- 2010-09-21 MX MX2012003394A patent/MX2012003394A/es not_active Application Discontinuation
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2012
- 2012-03-21 IL IL218772A patent/IL218772A0/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2542100C1 (ru) * | 2013-12-24 | 2015-02-20 | Федеральное государственное бюджетное учреждение науки Институт химии растворов им. Г.А. Крестова Российской Академии Наук (ИХС РАН) | Сокристаллическая форма теофиллина с дифлунисалом или диклофенаком |
Also Published As
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| MX2012003394A (es) | 2012-08-15 |
| CA2774981A1 (en) | 2011-03-24 |
| WO2011035324A1 (en) | 2011-03-24 |
| AU2010295288A1 (en) | 2012-05-03 |
| US20110183980A1 (en) | 2011-07-28 |
| BR112012006330A2 (pt) | 2017-07-04 |
| EP2482657A1 (en) | 2012-08-08 |
| IL218772A0 (en) | 2012-06-28 |
| CN102638979A (zh) | 2012-08-15 |
| JP2013505297A (ja) | 2013-02-14 |
| IN2012DN03322A (OSRAM) | 2015-10-23 |
| EP2482657A4 (en) | 2013-05-15 |
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