JP2010529135A5 - - Google Patents
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- JP2010529135A5 JP2010529135A5 JP2010511277A JP2010511277A JP2010529135A5 JP 2010529135 A5 JP2010529135 A5 JP 2010529135A5 JP 2010511277 A JP2010511277 A JP 2010511277A JP 2010511277 A JP2010511277 A JP 2010511277A JP 2010529135 A5 JP2010529135 A5 JP 2010529135A5
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- Prior art keywords
- optionally substituted
- carbon atoms
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- amino
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- Prior art date
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 201
- 239000001257 hydrogen Substances 0.000 claims description 201
- 125000004432 carbon atom Chemical group C* 0.000 claims description 177
- 150000002431 hydrogen Chemical group 0.000 claims description 149
- 229910052736 halogen Inorganic materials 0.000 claims description 125
- 150000002367 halogens Chemical group 0.000 claims description 125
- 150000001875 compounds Chemical class 0.000 claims description 120
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 104
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 104
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 104
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 94
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims description 94
- 125000001072 heteroaryl group Chemical group 0.000 claims description 93
- 125000003107 substituted aryl group Chemical group 0.000 claims description 90
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 89
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 65
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 62
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 62
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 62
- 125000004001 thioalkyl group Chemical group 0.000 claims description 62
- 229910052757 nitrogen Inorganic materials 0.000 claims description 61
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 58
- 125000001424 substituent group Chemical group 0.000 claims description 57
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 56
- 125000003342 alkenyl group Chemical group 0.000 claims description 54
- 125000000304 alkynyl group Chemical group 0.000 claims description 54
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 54
- QAWTYRYXDYHQNU-UHFFFAOYSA-N diazathiane Chemical class NSN QAWTYRYXDYHQNU-UHFFFAOYSA-N 0.000 claims description 53
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 52
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 49
- 125000005415 substituted alkoxy group Chemical group 0.000 claims description 48
- 125000000217 alkyl group Chemical group 0.000 claims description 44
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 41
- 125000000623 heterocyclic group Chemical group 0.000 claims description 40
- 150000003973 alkyl amines Chemical class 0.000 claims description 37
- 229930195712 glutamate Natural products 0.000 claims description 30
- 230000004044 response Effects 0.000 claims description 30
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims description 26
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 26
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 26
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 25
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 23
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 21
- 241000124008 Mammalia Species 0.000 claims description 21
- 238000010276 construction Methods 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
- 150000001204 N-oxides Chemical class 0.000 claims description 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 16
- -1 bicyclic compound Chemical class 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 150000003857 carboxamides Chemical class 0.000 claims description 13
- 125000005518 carboxamido group Chemical group 0.000 claims description 13
- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 claims description 12
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 claims description 12
- 101001032838 Rattus norvegicus Metabotropic glutamate receptor 5 Proteins 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 12
- 210000003292 kidney cell Anatomy 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000004076 pyridyl group Chemical group 0.000 claims description 12
- 201000000980 schizophrenia Diseases 0.000 claims description 12
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 claims description 11
- 125000006730 (C2-C5) alkynyl group Chemical group 0.000 claims description 11
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 11
- 125000002837 carbocyclic group Chemical group 0.000 claims description 11
- 235000013922 glutamic acid Nutrition 0.000 claims description 11
- 239000004220 glutamic acid Substances 0.000 claims description 11
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims description 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 8
- 208000027534 Emotional disease Diseases 0.000 claims description 8
- 208000028017 Psychotic disease Diseases 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 8
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims description 6
- PXXJHWLDUBFPOL-UHFFFAOYSA-N benzamidine Chemical group NC(=N)C1=CC=CC=C1 PXXJHWLDUBFPOL-UHFFFAOYSA-N 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 229910052710 silicon Inorganic materials 0.000 claims description 6
- 239000010703 silicon Substances 0.000 claims description 6
- 208000012902 Nervous system disease Diseases 0.000 claims description 5
- 125000004429 atom Chemical group 0.000 claims description 5
- 230000004064 dysfunction Effects 0.000 claims description 5
- PXZQEOJJUGGUIB-UHFFFAOYSA-N isoindolin-1-one Chemical class C1=CC=C2C(=O)NCC2=C1 PXZQEOJJUGGUIB-UHFFFAOYSA-N 0.000 claims description 5
- 230000000926 neurological effect Effects 0.000 claims description 5
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical class C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 claims description 5
- 208000020016 psychiatric disease Diseases 0.000 claims description 5
- YWPMKTWUFVOFPL-UHFFFAOYSA-N 3,4-dihydro-2h-isoquinolin-1-one Chemical class C1=CC=C2C(=O)NCCC2=C1 YWPMKTWUFVOFPL-UHFFFAOYSA-N 0.000 claims description 4
- QGNQEODJYRGEJX-UHFFFAOYSA-N 4h-isoquinoline-1,3-dione Chemical class C1=CC=C2C(=O)NC(=O)CC2=C1 QGNQEODJYRGEJX-UHFFFAOYSA-N 0.000 claims description 4
- 208000017194 Affective disease Diseases 0.000 claims description 4
- 206010001497 Agitation Diseases 0.000 claims description 4
- 208000000044 Amnesia Diseases 0.000 claims description 4
- 208000031091 Amnestic disease Diseases 0.000 claims description 4
- 208000019901 Anxiety disease Diseases 0.000 claims description 4
- 206010048962 Brain oedema Diseases 0.000 claims description 4
- 206010008748 Chorea Diseases 0.000 claims description 4
- 206010012289 Dementia Diseases 0.000 claims description 4
- 208000014094 Dystonic disease Diseases 0.000 claims description 4
- 208000030814 Eating disease Diseases 0.000 claims description 4
- 208000019454 Feeding and Eating disease Diseases 0.000 claims description 4
- 208000019695 Migraine disease Diseases 0.000 claims description 4
- 208000019022 Mood disease Diseases 0.000 claims description 4
- 208000016285 Movement disease Diseases 0.000 claims description 4
- 208000025966 Neurological disease Diseases 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 4
- 208000002193 Pain Diseases 0.000 claims description 4
- 206010033664 Panic attack Diseases 0.000 claims description 4
- 208000027099 Paranoid disease Diseases 0.000 claims description 4
- 230000032683 aging Effects 0.000 claims description 4
- 230000006986 amnesia Effects 0.000 claims description 4
- 230000036506 anxiety Effects 0.000 claims description 4
- 208000006752 brain edema Diseases 0.000 claims description 4
- 208000012601 choreatic disease Diseases 0.000 claims description 4
- 230000006999 cognitive decline Effects 0.000 claims description 4
- 208000010877 cognitive disease Diseases 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- 235000014632 disordered eating Nutrition 0.000 claims description 4
- 208000010118 dystonia Diseases 0.000 claims description 4
- 206010015037 epilepsy Diseases 0.000 claims description 4
- 208000024714 major depressive disease Diseases 0.000 claims description 4
- 206010027599 migraine Diseases 0.000 claims description 4
- 201000003631 narcolepsy Diseases 0.000 claims description 4
- 235000020824 obesity Nutrition 0.000 claims description 4
- 208000019906 panic disease Diseases 0.000 claims description 4
- 230000000698 schizophrenic effect Effects 0.000 claims description 4
- 208000019116 sleep disease Diseases 0.000 claims description 4
- 208000020685 sleep-wake disease Diseases 0.000 claims description 4
- 208000011117 substance-related disease Diseases 0.000 claims description 4
- 125000006617 triphenylamine group Chemical group 0.000 claims description 3
- 150000003573 thiols Chemical group 0.000 claims 34
- 125000003118 aryl group Chemical group 0.000 claims 4
- NKSZCPBUWGZONP-UHFFFAOYSA-N 3,4-dihydroisoquinoline Chemical compound C1=CC=C2C=NCCC2=C1 NKSZCPBUWGZONP-UHFFFAOYSA-N 0.000 claims 1
- 125000002993 cycloalkylene group Chemical group 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 description 70
- 238000000034 method Methods 0.000 description 34
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 24
- MOIPGXQKZSZOQX-UHFFFAOYSA-N carbonyl bromide Chemical compound BrC(Br)=O MOIPGXQKZSZOQX-UHFFFAOYSA-N 0.000 description 12
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 8
- 0 CCCC*(*)*(C(C(C(C)=N)=C(*)**=C(C)C)=O)N Chemical compound CCCC*(*)*(C(C(C(C)=N)=C(*)**=C(C)C)=O)N 0.000 description 6
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 description 4
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- ODHXBMXNKOYIBV-UHFFFAOYSA-N triphenylamine Chemical compound C1=CC=CC=C1N(C=1C=CC=CC=1)C1=CC=CC=C1 ODHXBMXNKOYIBV-UHFFFAOYSA-N 0.000 description 3
- MCFDHXXQFUDVES-UHFFFAOYSA-N Cc1n[o]c([IH]C)n1 Chemical compound Cc1n[o]c([IH]C)n1 MCFDHXXQFUDVES-UHFFFAOYSA-N 0.000 description 2
- 230000019771 cognition Effects 0.000 description 2
- 230000037410 cognitive enhancement Effects 0.000 description 2
- 230000002708 enhancing effect Effects 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 229940126062 Compound A Drugs 0.000 description 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94168607P | 2007-06-03 | 2007-06-03 | |
| US60/941,686 | 2007-06-03 | ||
| US98504107P | 2007-11-02 | 2007-11-02 | |
| US60/985,041 | 2007-11-02 | ||
| PCT/US2008/065647 WO2008151184A1 (en) | 2007-06-03 | 2008-06-03 | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529135A JP2010529135A (ja) | 2010-08-26 |
| JP2010529135A5 true JP2010529135A5 (enExample) | 2012-07-12 |
| JP5622568B2 JP5622568B2 (ja) | 2014-11-12 |
Family
ID=41480433
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010511277A Expired - Fee Related JP5622568B2 (ja) | 2007-06-03 | 2008-06-03 | ベンズアミドｍＧｌｕＲ５の正のアロステリック調節因子ならびにその作製および使用方法 |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP2162136A4 (enExample) |
| JP (1) | JP5622568B2 (enExample) |
| KR (1) | KR20100033981A (enExample) |
| CN (1) | CN101795689B (enExample) |
| AU (1) | AU2008259776A1 (enExample) |
| BR (1) | BRPI0812363A2 (enExample) |
| CA (1) | CA2689282A1 (enExample) |
| EA (1) | EA200971143A1 (enExample) |
| IL (1) | IL202508A0 (enExample) |
| MX (1) | MX2009013169A (enExample) |
| NZ (1) | NZ581817A (enExample) |
| SG (1) | SG185285A1 (enExample) |
| WO (1) | WO2008151184A1 (enExample) |
Families Citing this family (77)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG177221A1 (en) | 2006-12-15 | 2012-01-30 | Abbott Lab | Novel oxadiazole compounds |
| US8853392B2 (en) | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| US8034806B2 (en) | 2007-11-02 | 2011-10-11 | Vanderbilt University | Bicyclic mGluR5 positive allosteric modulators and methods of making and using same |
| GB0811643D0 (en) | 2008-06-25 | 2008-07-30 | Cancer Rec Tech Ltd | New therapeutic agents |
| TW201028421A (en) * | 2009-01-15 | 2010-08-01 | Abbott Lab | Novel benzenesulfonamides as calcium channel blockers |
| US8389536B2 (en) | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
| US8586581B2 (en) | 2009-12-17 | 2013-11-19 | Hoffmann-La Roche Inc | Ethynyl compounds useful for treatment of CNS disorders |
| CA2784830C (en) | 2009-12-18 | 2018-03-27 | Sunovion Pharmaceuticals Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| BR112012014235A2 (pt) | 2009-12-18 | 2016-06-14 | Janssen Pharmaceutica Nv | tiazóis bicíclicos como moduladores alostéricos de receptores mglur5 |
| AU2010332811B2 (en) | 2009-12-18 | 2014-07-24 | Janssen Pharmaceutica Nv | Bicyclic thiazoles as allosteric modulators of mGluR5 receptors |
| RS54180B1 (sr) | 2009-12-23 | 2015-12-31 | Takeda Pharmaceutical Company Limited | Fuzionisani heteroaromatski pirolidinoni kao syk inhibitori |
| US8420661B2 (en) | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| AU2011258389A1 (en) * | 2010-05-24 | 2012-12-06 | Vanderbilt University | Substituted-6-methylnicotinamides as mGluR5 positive allosteric modulators |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| US8772300B2 (en) | 2011-04-19 | 2014-07-08 | Hoffmann-La Roche Inc. | Phenyl or pyridinyl-ethynyl derivatives |
| KR101554803B1 (ko) | 2011-04-26 | 2015-09-21 | 에프. 호프만-라 로슈 아게 | Mglur5의 양성 알로스테릭 조절체로서 에틴일 유도체 |
| MY165141A (en) | 2011-04-26 | 2018-02-28 | Hoffmann La Roche | Pyrazolidin-3-one derivatives |
| JP6026525B2 (ja) | 2011-06-22 | 2016-11-16 | 武田薬品工業株式会社 | 置換６−アザ−イソインドリン−１−オン誘導体 |
| US20130123254A1 (en) | 2011-09-30 | 2013-05-16 | Barbara Biemans | Pharmaceutically acceptable mglur5 positive allosteric modulators and their methods of identification |
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| UA110995C2 (uk) | 2011-10-07 | 2016-03-10 | Ф. Хоффманн-Ля Рош Аг | Етинільні похідні як модулятори метаботропного глутаматного рецептора |
| JP5977837B2 (ja) * | 2011-12-21 | 2016-08-24 | ノヴィラ・セラピューティクス・インコーポレイテッド | Ｂ型肝炎抗ウイルス剤 |
| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
| WO2014012851A1 (en) | 2012-07-17 | 2014-01-23 | F. Hoffmann-La Roche Ag | Arylethynyl derivatives |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| SI2900659T1 (sl) | 2012-09-27 | 2016-12-30 | F.Hoffmann-La Roche Ag | Ariletinilni derivati |
| AU2013333988B2 (en) * | 2012-10-18 | 2017-03-09 | F. Hoffmann-La Roche Ag | Ethynyl derivatives as modulators of mGluR5 receptor activity |
| UA114934C2 (uk) * | 2012-10-18 | 2017-08-28 | Ф. Хоффманн-Ля Рош Аг | Похідне етинілу як модулятор активності метаботропного глутаматного рецептора підтипу 5 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| HUE036571T2 (hu) | 2013-04-19 | 2018-07-30 | Incyte Holdings Corp | Biciklusos heterociklusok mint FGFR inhibitorok |
| MA38885B1 (fr) * | 2013-09-25 | 2018-11-30 | Hoffmann La Roche | Dérivés d'éthynyle modulateurs allosteriques positifs (pam) du recepteur metabotropique du glutamate 4 (mglu4) |
| TWI649310B (zh) * | 2014-01-10 | 2019-02-01 | 赫孚孟拉羅股份公司 | 乙炔基衍生物 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| MX388991B (es) | 2015-02-20 | 2025-03-20 | Incyte Corp | Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr) |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| 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 |
| CN106146391A (zh) * | 2015-04-15 | 2016-11-23 | 中国科学院上海药物研究所 | 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途 |
| MA42508B1 (fr) | 2015-06-03 | 2020-05-29 | Hoffmann La Roche | Dérivés d'éthynyle |
| RS62639B1 (sr) | 2015-07-06 | 2021-12-31 | Alkermes Inc | Hetero-halo inhibitori histonskih deacetilaza |
| EP3319968A1 (en) | 2015-07-06 | 2018-05-16 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| CA2984711C (en) | 2015-07-15 | 2023-08-29 | F. Hoffmann-La Roche Ag | Ethynyl derivatives as metabotropic glutamate receptor modulators |
| GB201517217D0 (en) | 2015-09-29 | 2015-11-11 | Astex Therapeutics Ltd And Cancer Res Technology Ltd | Pharmaceutical compounds |
| GB201517216D0 (en) | 2015-09-29 | 2015-11-11 | Cancer Res Technology Ltd And Astex Therapeutics Ltd | Pharmaceutical compounds |
| CA3030788A1 (en) | 2016-07-18 | 2018-01-25 | F. Hoffmann-La Roche Ag | Ethynyl derivatives |
| AU2018207402B2 (en) | 2017-01-11 | 2023-09-28 | Alkermes, Inc. | Bicyclic inhibitors of histone deacetylase |
| GB201704965D0 (en) | 2017-03-28 | 2017-05-10 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| GB201704966D0 (en) | 2017-03-28 | 2017-05-10 | Astex Therapeutics Ltd | Pharmaceutical compounds |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| EA039417B1 (ru) | 2017-08-07 | 2022-01-25 | Родин Терапеутикс, Инк. | Бициклические ингибиторы гистондеацетилазы |
| EP3788047B1 (en) | 2018-05-04 | 2024-09-04 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
| BR112020022373A2 (pt) | 2018-05-04 | 2021-02-02 | Incyte Corporation | sais de um inibidor de fgfr |
| DE102019200805A1 (de) * | 2019-01-23 | 2020-07-23 | Henkel Ag & Co. Kgaa | Neue fluoreszierende Materialien auf Basis von Phthalimiden |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| KR20220100879A (ko) | 2019-10-14 | 2022-07-18 | 인사이트 코포레이션 | Fgfr 저해제로서의 이환식 헤테로사이클 |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| KR20220131900A (ko) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Fgfr 억제제의 유도체 |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021257857A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Naphthyridinone compounds as jak2 v617f inhibitors |
| WO2021257863A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Pyrrolotriazine compounds as jak2 v617f inhibitors |
| US11767323B2 (en) | 2020-07-02 | 2023-09-26 | Incyte Corporation | Tricyclic pyridone compounds as JAK2 V617F inhibitors |
| TW202216713A (zh) | 2020-07-02 | 2022-05-01 | 美商英塞特公司 | 作為ｊａｋ２ ｖ６１７ｆ抑制劑之三環脲化合物 |
| CA3185726A1 (en) * | 2020-07-29 | 2022-02-03 | Dae Kyu Choi | Dual regulator for mglur5 and 5-ht2a receptors and use thereof |
| CN116209663A (zh) | 2020-08-17 | 2023-06-02 | 安力高医药股份有限公司 | 用于靶向pd-l1的方法和组合物 |
| WO2022046989A1 (en) | 2020-08-27 | 2022-03-03 | Incyte Corporation | Tricyclic urea compounds as jak2 v617f inhibitors |
| US11919908B2 (en) | 2020-12-21 | 2024-03-05 | Incyte Corporation | Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors |
| EP4298099A1 (en) | 2021-02-25 | 2024-01-03 | Incyte Corporation | Spirocyclic lactams as jak2 v617f inhibitors |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313611A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
| CN116514790A (zh) * | 2022-01-24 | 2023-08-01 | 华东师范大学 | 一类靶向于stat3的三联芳香杂环哌嗪类小分子有机化合物及其应用 |
| AU2023213484A1 (en) * | 2022-01-27 | 2024-07-25 | Vivozon,Inc. | Pharmaceutical composition for preventing or treating mental disorder |
| PE20251706A1 (es) | 2022-03-17 | 2025-07-02 | Incyte Corp | Compuestos de urea triciclica como inhibidores de v617f de jak2 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| GB9823871D0 (en) * | 1998-10-30 | 1998-12-23 | Pharmacia & Upjohn Spa | 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents |
| MXPA04000695A (es) * | 2001-07-23 | 2005-08-26 | Galileo Pharmaceuticals Inc | Compuestos citoprotectores, formulaciones farmaceuticas y cosmeticas y metodos. |
| WO2004009549A2 (en) * | 2002-07-18 | 2004-01-29 | Actelion Pharmaceuticals Ltd | Piperidines useful for the treatment of central nervous system disorders |
| JP2006521358A (ja) * | 2003-03-26 | 2006-09-21 | メルク エンド カムパニー インコーポレーテッド | 代謝調節型グルタミン酸受容体のベンズアミドモジュレータ |
| MXPA06003951A (es) * | 2003-10-07 | 2006-06-27 | Renovis Inc | Derivados de amida como ligandos del canal de ion y composiciones farmaceuticas y sus metodos de uso. |
| GB0324159D0 (en) * | 2003-10-15 | 2003-11-19 | Glaxo Group Ltd | Novel compounds |
| GB0325956D0 (en) * | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| JPWO2005108399A1 (ja) * | 2004-05-10 | 2008-03-21 | 萬有製薬株式会社 | イミダゾピリジン化合物 |
| GB0503646D0 (en) * | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
| AP2007004119A0 (en) * | 2005-02-28 | 2007-08-31 | Renovis Inc | Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same |
-
2008
- 2008-06-03 NZ NZ581817A patent/NZ581817A/en not_active IP Right Cessation
- 2008-06-03 AU AU2008259776A patent/AU2008259776A1/en not_active Abandoned
- 2008-06-03 CA CA002689282A patent/CA2689282A1/en not_active Abandoned
- 2008-06-03 JP JP2010511277A patent/JP5622568B2/ja not_active Expired - Fee Related
- 2008-06-03 BR BRPI0812363-2A2A patent/BRPI0812363A2/pt not_active IP Right Cessation
- 2008-06-03 KR KR1020097027281A patent/KR20100033981A/ko not_active Withdrawn
- 2008-06-03 CN CN200880100770.6A patent/CN101795689B/zh not_active Expired - Fee Related
- 2008-06-03 EA EA200971143A patent/EA200971143A1/ru unknown
- 2008-06-03 MX MX2009013169A patent/MX2009013169A/es not_active Application Discontinuation
- 2008-06-03 EP EP08770045A patent/EP2162136A4/en not_active Withdrawn
- 2008-06-03 WO PCT/US2008/065647 patent/WO2008151184A1/en not_active Ceased
- 2008-06-03 SG SG2012074621A patent/SG185285A1/en unknown
-
2009
- 2009-12-03 IL IL202508A patent/IL202508A0/en unknown
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