JP2011509288A5 - - Google Patents
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- JP2011509288A5 JP2011509288A5 JP2010541889A JP2010541889A JP2011509288A5 JP 2011509288 A5 JP2011509288 A5 JP 2011509288A5 JP 2010541889 A JP2010541889 A JP 2010541889A JP 2010541889 A JP2010541889 A JP 2010541889A JP 2011509288 A5 JP2011509288 A5 JP 2011509288A5
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- JP
- Japan
- Prior art keywords
- compound
- substituted
- pyrido
- unsubstituted
- vinyl
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 183
- 229920002554 vinyl polymer Polymers 0.000 claims description 77
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 74
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzenecarbonitrile Natural products N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims description 48
- -1 3-methoxy-2-propoxyphenyl Chemical group 0.000 claims description 47
- 125000001072 heteroaryl group Chemical group 0.000 claims description 36
- 125000003118 aryl group Chemical group 0.000 claims description 35
- 125000000623 heterocyclic group Chemical group 0.000 claims description 32
- 125000000217 alkyl group Chemical group 0.000 claims description 31
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 27
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 26
- 208000002193 Pain Diseases 0.000 claims description 19
- 229910052736 halogen Inorganic materials 0.000 claims description 18
- 150000002367 halogens Chemical class 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 16
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 16
- 125000001188 haloalkyl group Chemical group 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 15
- 239000001257 hydrogen Substances 0.000 claims description 15
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
- 125000003342 alkenyl group Chemical group 0.000 claims description 12
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 12
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 12
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 10
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 10
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 10
- 150000002431 hydrogen Chemical class 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 125000004001 thioalkyl group Chemical group 0.000 claims description 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- 208000035475 disorder Diseases 0.000 claims description 6
- 208000004296 neuralgia Diseases 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 5
- 102000011040 TRPV Cation Channels Human genes 0.000 claims description 4
- 108010062740 TRPV Cation Channels Proteins 0.000 claims description 4
- 102000003568 TRPV3 Human genes 0.000 claims description 4
- 101150043371 Trpv3 gene Proteins 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 208000021722 neuropathic pain Diseases 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- YAYOVHRLVOHYMW-UHFFFAOYSA-N 1h-pyrimidin-6-one;hydrochloride Chemical compound Cl.O=C1C=CN=CN1 YAYOVHRLVOHYMW-UHFFFAOYSA-N 0.000 claims description 3
- LGTIWXWIILLBLU-WYMLVPIESA-N 2-[(e)-2-(2-cyclopentyloxy-3-methoxyphenyl)ethenyl]-3-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrido[1,2-a]pyrimidin-4-one Chemical compound COC1=CC=CC(\C=C\C2=C(C(=O)N3C=CC=CC3=N2)C=2C=C3OCCOC3=CC=2)=C1OC1CCCC1 LGTIWXWIILLBLU-WYMLVPIESA-N 0.000 claims description 3
- YYSAQADMDKBWCD-ISLYRVAYSA-N 2-[(e)-2-(2-cyclopentyloxy-3-methoxyphenyl)ethenyl]-3-phenylpyrido[1,2-a]pyrimidin-4-one Chemical compound C1CCCC1OC=1C(OC)=CC=CC=1\C=C\C=1N=C2C=CC=CN2C(=O)C=1C1=CC=CC=C1 YYSAQADMDKBWCD-ISLYRVAYSA-N 0.000 claims description 3
- VIKIMOKNEKYFBO-OUKQBFOZSA-N 2-[(e)-2-(2-cyclopentyloxy-3-methoxyphenyl)ethenyl]-3-pyridin-4-ylpyrido[1,2-a]pyrimidin-4-one Chemical compound C1CCCC1OC=1C(OC)=CC=CC=1\C=C\C=1N=C2C=CC=CN2C(=O)C=1C1=CC=NC=C1 VIKIMOKNEKYFBO-OUKQBFOZSA-N 0.000 claims description 3
- MOWBZAVXDWNQEZ-SDNWHVSQSA-N 2-[(e)-2-(4-chlorophenyl)ethenyl]-3-phenylpyrido[1,2-a]pyrimidin-4-one Chemical compound C1=CC(Cl)=CC=C1\C=C\C1=C(C=2C=CC=CC=2)C(=O)N2C=CC=CC2=N1 MOWBZAVXDWNQEZ-SDNWHVSQSA-N 0.000 claims description 3
- YQIFMLKKZUNMIL-FOCLMDBBSA-N 2-[(e)-2-[2-(cyclopropylmethoxy)-3-methoxyphenyl]ethenyl]-3-phenylpyrido[1,2-a]pyrimidin-4-one Chemical compound C1CC1COC=1C(OC)=CC=CC=1\C=C\C=1N=C2C=CC=CN2C(=O)C=1C1=CC=CC=C1 YQIFMLKKZUNMIL-FOCLMDBBSA-N 0.000 claims description 3
- VAKQBHALQXEEAG-UHFFFAOYSA-N 2-phenylpyrido[1,2-a]pyrimidin-4-one Chemical compound N1=C2C=CC=CN2C(=O)C=C1C1=CC=CC=C1 VAKQBHALQXEEAG-UHFFFAOYSA-N 0.000 claims description 3
- ULSLDSMNKAWCJA-WUKNDPDISA-N 4-[2-[(e)-2-(2-cyclopentyloxy-3-methoxyphenyl)ethenyl]-4-oxopyrido[1,2-a]pyrimidin-3-yl]benzonitrile Chemical compound C1CCCC1OC=1C(OC)=CC=CC=1\C=C\C=1N=C2C=CC=CN2C(=O)C=1C1=CC=C(C#N)C=C1 ULSLDSMNKAWCJA-WUKNDPDISA-N 0.000 claims description 3
- RMBXOXFAKCBYLC-WUKNDPDISA-N 4-[2-[(e)-2-(2-cyclopentyloxy-3-methoxyphenyl)ethenyl]-9-methoxy-4-oxopyrido[1,2-a]pyrimidin-3-yl]benzonitrile Chemical compound C1CCCC1OC=1C(OC)=CC=CC=1\C=C\C=1N=C2C(OC)=CC=CN2C(=O)C=1C1=CC=C(C#N)C=C1 RMBXOXFAKCBYLC-WUKNDPDISA-N 0.000 claims description 3
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims description 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 3
- LSBDFXRDZJMBSC-UHFFFAOYSA-N Amide-Phenylacetic acid Natural products NC(=O)CC1=CC=CC=C1 LSBDFXRDZJMBSC-UHFFFAOYSA-N 0.000 claims description 3
- 208000000094 Chronic Pain Diseases 0.000 claims description 3
- 208000004550 Postoperative Pain Diseases 0.000 claims description 3
- 208000005298 acute pain Diseases 0.000 claims description 3
- 125000001887 cyclopentyloxy group Chemical group C1(CCCC1)O* 0.000 claims description 3
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 3
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 3
- 201000004384 Alopecia Diseases 0.000 claims description 2
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 208000006820 Arthralgia Diseases 0.000 claims description 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 2
- 206010058019 Cancer Pain Diseases 0.000 claims description 2
- 208000015943 Coeliac disease Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 206010012289 Dementia Diseases 0.000 claims description 2
- 201000004624 Dermatitis Diseases 0.000 claims description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 2
- 208000012661 Dyskinesia Diseases 0.000 claims description 2
- 208000004232 Enteritis Diseases 0.000 claims description 2
- 206010017886 Gastroduodenal ulcer Diseases 0.000 claims description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 208000019693 Lung disease Diseases 0.000 claims description 2
- 208000027530 Meniere disease Diseases 0.000 claims description 2
- 208000019695 Migraine disease Diseases 0.000 claims description 2
- 208000007101 Muscle Cramp Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 208000001294 Nociceptive Pain Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 206010033645 Pancreatitis Diseases 0.000 claims description 2
- 208000008469 Peptic Ulcer Diseases 0.000 claims description 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims description 2
- 208000017442 Retinal disease Diseases 0.000 claims description 2
- 206010038923 Retinopathy Diseases 0.000 claims description 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims description 2
- 208000005392 Spasm Diseases 0.000 claims description 2
- 208000009205 Tinnitus Diseases 0.000 claims description 2
- 206010060875 Uraemic pruritus Diseases 0.000 claims description 2
- 206010046543 Urinary incontinence Diseases 0.000 claims description 2
- 208000024780 Urticaria Diseases 0.000 claims description 2
- 206010047700 Vomiting Diseases 0.000 claims description 2
- 208000009621 actinic keratosis Diseases 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000000172 allergic effect Effects 0.000 claims description 2
- 201000010105 allergic rhinitis Diseases 0.000 claims description 2
- 231100000360 alopecia Toxicity 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 230000036760 body temperature Effects 0.000 claims description 2
- 230000003925 brain function Effects 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 210000001508 eye Anatomy 0.000 claims description 2
- 239000012458 free base Substances 0.000 claims description 2
- 230000006870 function Effects 0.000 claims description 2
- 231100000029 gastro-duodenal ulcer Toxicity 0.000 claims description 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 230000009610 hypersensitivity Effects 0.000 claims description 2
- 208000009326 ileitis Diseases 0.000 claims description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 2
- 230000007794 irritation Effects 0.000 claims description 2
- 230000000302 ischemic effect Effects 0.000 claims description 2
- 206010027175 memory impairment Diseases 0.000 claims description 2
- 206010027599 migraine Diseases 0.000 claims description 2
- 210000004400 mucous membrane Anatomy 0.000 claims description 2
- 210000004165 myocardium Anatomy 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 201000001119 neuropathy Diseases 0.000 claims description 2
- 230000007823 neuropathy Effects 0.000 claims description 2
- 208000037916 non-allergic rhinitis Diseases 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 230000000414 obstructive effect Effects 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 2
- 230000001823 pruritic effect Effects 0.000 claims description 2
- 208000023504 respiratory system disease Diseases 0.000 claims description 2
- 230000035945 sensitivity Effects 0.000 claims description 2
- 210000003491 skin Anatomy 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 231100000886 tinnitus Toxicity 0.000 claims description 2
- 208000004371 toothache Diseases 0.000 claims description 2
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 2
- 230000008673 vomiting Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 9
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 description 16
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 6
- 239000002585 base Substances 0.000 description 5
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 4
- 230000002140 halogenating effect Effects 0.000 description 3
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 3
- FTNJQNQLEGKTGD-UHFFFAOYSA-N 1,3-benzodioxole Chemical compound C1=CC=C2OCOC2=C1 FTNJQNQLEGKTGD-UHFFFAOYSA-N 0.000 description 2
- CJFXRYQGAWAIFV-FMIVXFBMSA-N 2-[(e)-2-(1,3-benzodioxol-4-yl)ethenyl]-3-[4-(trifluoromethyl)phenyl]pyrido[1,2-a]pyrimidin-4-one Chemical compound C1=CC(C(F)(F)F)=CC=C1C(C(N1C=CC=CC1=N1)=O)=C1\C=C\C1=CC=CC2=C1OCO2 CJFXRYQGAWAIFV-FMIVXFBMSA-N 0.000 description 2
- QKZAKNAEWCBPAX-ZHACJKMWSA-N 2-[(e)-2-thiophen-2-ylethenyl]-3-[4-(trifluoromethyl)phenyl]pyrido[1,2-a]pyrimidin-4-one Chemical compound C1=CC(C(F)(F)F)=CC=C1C(C(N1C=CC=CC1=N1)=O)=C1\C=C\C1=CC=CS1 QKZAKNAEWCBPAX-ZHACJKMWSA-N 0.000 description 2
- ICSNLGPSRYBMBD-UHFFFAOYSA-N 2-aminopyridine Chemical compound NC1=CC=CC=N1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- PCLIMKBDDGJMGD-UHFFFAOYSA-N N-bromosuccinimide Chemical compound BrN1C(=O)CCC1=O PCLIMKBDDGJMGD-UHFFFAOYSA-N 0.000 description 2
- LQZMLBORDGWNPD-UHFFFAOYSA-N N-iodosuccinimide Chemical compound IN1C(=O)CCC1=O LQZMLBORDGWNPD-UHFFFAOYSA-N 0.000 description 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 2
- 125000000304 alkynyl group Chemical group 0.000 description 2
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000005859 coupling reaction Methods 0.000 description 2
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 239000003586 protic polar solvent Substances 0.000 description 2
- 150000003222 pyridines Chemical class 0.000 description 2
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 0 *C(C=CC[C@@]1C=CC(N=C(C=CI=C2)N2C2=*)=C2[Al])=C1OC=* Chemical compound *C(C=CC[C@@]1C=CC(N=C(C=CI=C2)N2C2=*)=C2[Al])=C1OC=* 0.000 description 1
- HPARLNRMYDSBNO-UHFFFAOYSA-N 1,4-benzodioxine Chemical compound C1=CC=C2OC=COC2=C1 HPARLNRMYDSBNO-UHFFFAOYSA-N 0.000 description 1
- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 description 1
- VFMCUTPRJLZEEW-UHFFFAOYSA-N 4h-pyrido[1,2-a]pyrimidine Chemical class C1=CC=CN2CC=CN=C21 VFMCUTPRJLZEEW-UHFFFAOYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 238000009739 binding Methods 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 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 description 1
- 208000027753 pain disease Diseases 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN82MU2008 | 2008-01-11 | ||
| IN82/MUM/2008 | 2008-01-11 | ||
| US2877008P | 2008-02-14 | 2008-02-14 | |
| US61/028,770 | 2008-02-14 | ||
| IN548/MUM/2008 | 2008-03-18 | ||
| IN548MU2008 | 2008-03-18 | ||
| IN798MU2008 | 2008-04-04 | ||
| IN798/MUM/2008 | 2008-04-04 | ||
| US4827608P | 2008-04-28 | 2008-04-28 | |
| US61/048,276 | 2008-04-28 | ||
| PCT/IN2009/000025 WO2009109987A2 (en) | 2008-01-11 | 2009-01-07 | Fused pyrimidine derivatives as trpv3 modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011509288A JP2011509288A (ja) | 2011-03-24 |
| JP2011509288A5 true JP2011509288A5 (https=) | 2012-02-16 |
| JP5419894B2 JP5419894B2 (ja) | 2014-02-19 |
Family
ID=41056428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010541889A Expired - Fee Related JP5419894B2 (ja) | 2008-01-11 | 2009-01-07 | Ｔｒｐｖ３モジュレーターとしての縮合ピリミジン誘導体 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8349846B2 (https=) |
| EP (1) | EP2229388A4 (https=) |
| JP (1) | JP5419894B2 (https=) |
| AU (1) | AU2009220825A1 (https=) |
| CA (1) | CA2724008A1 (https=) |
| EA (1) | EA018133B1 (https=) |
| GE (1) | GEP20125574B (https=) |
| MX (1) | MX2010005769A (https=) |
| NZ (1) | NZ595781A (https=) |
| WO (1) | WO2009109987A2 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8119647B2 (en) * | 2008-04-23 | 2012-02-21 | Glenmark Pharmaceuticals S.A. | Fused pyrimidineone compounds as TRPV3 modulators |
| JP2012514577A (ja) | 2008-12-26 | 2012-06-28 | グレンマーク ファーマシューティカルズ， エセ．アー． | Ｔｒｐｖ３アンタゴニストとしての縮合イミダゾール誘導体 |
| SG11201406818VA (en) * | 2012-04-23 | 2014-11-27 | Genentech Inc | Intermediates and processes for preparing compounds |
| AU2020391161A1 (en) | 2019-11-25 | 2022-06-09 | Amgen Inc. | Heterocyclic compounds as Delta-5 Desaturase inhibitors and methods of use |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3907798A (en) * | 1966-06-15 | 1975-09-23 | Sterling Drug Inc | Preparation of 4H-pyrido{8 1,2-a{9 pyrimidin-4-ones from cyclic alkylidene 2-pyridylaminomethylenemalonates |
| HU168014B (https=) * | 1973-03-30 | 1976-02-28 | ||
| US3960863A (en) * | 1974-06-25 | 1976-06-01 | Sankyo Company Limited | Pyrido[1,2-a]pyrimidinone derivatives |
| US4223031A (en) * | 1978-05-05 | 1980-09-16 | Mead Johnson & Company | Azolopyrimidinones |
| IL59802A (en) * | 1979-05-08 | 1983-07-31 | Erba Farmitalia | Substituted pyrido(1,2-a)pyrimidine carboxylic acid derivatives,their preparation and pharmaceutical compositions containing them |
| AU551718B2 (en) * | 1981-07-15 | 1986-05-08 | Farmitalia Carlo Erba S.P.A. | Substituted thiazolo(3,2-alpha)pyrimidines |
| US4537962A (en) * | 1982-02-04 | 1985-08-27 | Farmitalia Carlo Erba, S.P.A. | Substituted 1,3,4-thiadiazolo[3,2-A]pyrimidines and compositions containing them |
| GB8300728D0 (en) * | 1983-01-12 | 1983-02-16 | Erba Farmitalia | Substituted carboxy-thiazolo / 3 2 - a / pyrimidine derivatives |
| US5204352A (en) * | 1987-09-29 | 1993-04-20 | The United States Of America As Represented By The Secretary Of The Army | Compounds exhibiting anti-parasitic activity and a method for their use |
| US5252572A (en) * | 1988-02-03 | 1993-10-12 | Chinoin Gyogyszer- Es Vegyeszeti Termekek Gyara Rt. | Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same |
| IT1263804B (it) * | 1993-01-22 | 1996-09-03 | Luso Farmaco Inst | Derivati pirimidinonici fusi con eterocicli azotati ad attivita' a ii antagonista |
| CA2161011A1 (en) * | 1994-02-23 | 1995-08-31 | Fumio Suzuki | Xanthine derivatives |
| JPH07242666A (ja) | 1994-03-08 | 1995-09-19 | Fujisawa Pharmaceut Co Ltd | 複素環化合物 |
| US6323208B1 (en) * | 1997-09-05 | 2001-11-27 | Pfizer Inc | Atropisomers of 2,3-disubstituted-(5.6)-heteroaryl fused-pyrimidin-4-ones |
| EP1028964A1 (en) * | 1997-11-11 | 2000-08-23 | Pfizer Products Inc. | Thienopyrimidine and thienopyridine derivatives useful as anticancer agents |
| US6559145B2 (en) | 2000-07-12 | 2003-05-06 | Pharmacia & Upjohn Company | Heterocycle carboxamides as antiviral agents |
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| JP4448170B2 (ja) * | 2004-08-18 | 2010-04-07 | ベッチャー・ローベルト | エノサル歯科インプラント |
| CA2578789A1 (en) * | 2004-09-03 | 2006-03-16 | Celgene Corporation | Substituted heterocyclic compounds and uses thereof |
| US20060128710A1 (en) * | 2004-12-09 | 2006-06-15 | Chih-Hung Lee | Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof |
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| JP2009511465A (ja) * | 2005-10-07 | 2009-03-19 | グレンマーク・ファーマシューティカルズ・エスエー | 置換ベンゾ縮合誘導体およびバニロイド受容体リガンドとしてのその使用 |
| US7893260B2 (en) * | 2005-11-04 | 2011-02-22 | Hydra Biosciences, Inc. | Substituted quinazolin-4-one compounds for antagonizing TRPV3 function |
| GB0525069D0 (en) * | 2005-12-08 | 2006-01-18 | Novartis Ag | Organic compounds |
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| US8980954B2 (en) * | 2006-04-25 | 2015-03-17 | Stc.Unm | Substituted cis- and trans-stilbenes as therapeutic agents |
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-
2009
- 2009-01-07 CA CA2724008A patent/CA2724008A1/en not_active Abandoned
- 2009-01-07 WO PCT/IN2009/000025 patent/WO2009109987A2/en not_active Ceased
- 2009-01-07 NZ NZ595781A patent/NZ595781A/xx not_active IP Right Cessation
- 2009-01-07 AU AU2009220825A patent/AU2009220825A1/en not_active Abandoned
- 2009-01-07 MX MX2010005769A patent/MX2010005769A/es active IP Right Grant
- 2009-01-07 JP JP2010541889A patent/JP5419894B2/ja not_active Expired - Fee Related
- 2009-01-07 EA EA201000674A patent/EA018133B1/ru not_active IP Right Cessation
- 2009-01-07 US US12/811,975 patent/US8349846B2/en not_active Expired - Fee Related
- 2009-01-07 GE GEAP200911911A patent/GEP20125574B/en unknown
- 2009-01-07 EP EP09717522A patent/EP2229388A4/en not_active Withdrawn
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