JPWO2020012422A5 - - Google Patents
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- JPWO2020012422A5 JPWO2020012422A5 JP2021500532A JP2021500532A JPWO2020012422A5 JP WO2020012422 A5 JPWO2020012422 A5 JP WO2020012422A5 JP 2021500532 A JP2021500532 A JP 2021500532A JP 2021500532 A JP2021500532 A JP 2021500532A JP WO2020012422 A5 JPWO2020012422 A5 JP WO2020012422A5
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- Prior art keywords
- disorders
- disorder
- methyl
- formula
- alkyl
- Prior art date
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 65
- 208000035475 disorder Diseases 0.000 claims 58
- 125000000217 alkyl group Chemical group 0.000 claims 26
- 229910052799 carbon Inorganic materials 0.000 claims 24
- 208000028017 Psychotic disease Diseases 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 16
- 206010012289 Dementia Diseases 0.000 claims 12
- 125000001475 halogen functional group Chemical group 0.000 claims 12
- 208000010877 cognitive disease Diseases 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 208000019116 sleep disease Diseases 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 229920002401 polyacrylamide Polymers 0.000 claims 9
- 208000019901 Anxiety disease Diseases 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 201000000980 schizophrenia Diseases 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 208000012202 Pervasive developmental disease Diseases 0.000 claims 6
- 239000004480 active ingredient Substances 0.000 claims 6
- 208000029560 autism spectrum disease Diseases 0.000 claims 6
- 230000003542 behavioural effect Effects 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
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- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims 4
- 230000001066 destructive effect Effects 0.000 claims 4
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- 229940079593 drug Drugs 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
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- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 3
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 3
- 102100036837 Metabotropic glutamate receptor 2 Human genes 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 239000000556 agonist Substances 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 102000047725 alpha7 Nicotinic Acetylcholine Receptor Human genes 0.000 claims 3
- 108700006085 alpha7 Nicotinic Acetylcholine Receptor Proteins 0.000 claims 3
- 239000002439 beta secretase inhibitor Substances 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims 3
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 3
- 239000003395 histamine H3 receptor antagonist Substances 0.000 claims 3
- 150000004677 hydrates Chemical class 0.000 claims 3
- 229960004502 levodopa Drugs 0.000 claims 3
- 108010038421 metabotropic glutamate receptor 2 Proteins 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 239000011593 sulfur Substances 0.000 claims 3
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 2
- -1 1-methyl-1H-indole-5-yl Chemical group 0.000 claims 2
- 206010065040 AIDS dementia complex Diseases 0.000 claims 2
- 208000029197 Amphetamine-Related disease Diseases 0.000 claims 2
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- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010065390 Inflammatory pain Diseases 0.000 claims 2
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims 2
- 208000030663 Libido disease Diseases 0.000 claims 2
- 206010026749 Mania Diseases 0.000 claims 2
- 208000003863 Marijuana Abuse Diseases 0.000 claims 2
- 229940099433 NMDA receptor antagonist Drugs 0.000 claims 2
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- 206010033799 Paralysis Diseases 0.000 claims 2
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- 206010039966 Senile dementia Diseases 0.000 claims 2
- 206010040981 Sleep attacks Diseases 0.000 claims 2
- 208000027520 Somatoform disease Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 208000011962 Substance-induced mood disease Diseases 0.000 claims 2
- 231100000395 Substance-induced mood disorder Toxicity 0.000 claims 2
- 208000011963 Substance-induced psychotic disease Diseases 0.000 claims 2
- 231100000393 Substance-induced psychotic disorder Toxicity 0.000 claims 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims 2
- 208000031674 Traumatic Acute Stress disease Diseases 0.000 claims 2
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- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 201000004810 Vascular dementia Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 208000028505 alcohol-related disease Diseases 0.000 claims 2
- 230000007815 allergy Effects 0.000 claims 2
- 230000001430 anti-depressive effect Effects 0.000 claims 2
- 230000000561 anti-psychotic effect Effects 0.000 claims 2
- 239000000935 antidepressant agent Substances 0.000 claims 2
- 229940005513 antidepressants Drugs 0.000 claims 2
- 230000036528 appetite Effects 0.000 claims 2
- 235000019789 appetite Nutrition 0.000 claims 2
- 206010003119 arrhythmia Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 2
- 229960001948 caffeine Drugs 0.000 claims 2
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims 2
- 208000013677 cerebrovascular dementia Diseases 0.000 claims 2
- 208000026106 cerebrovascular disease Diseases 0.000 claims 2
- 230000006999 cognitive decline Effects 0.000 claims 2
- 230000001149 cognitive effect Effects 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
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- 208000010118 dystonia Diseases 0.000 claims 2
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- 208000029364 generalized anxiety disease Diseases 0.000 claims 2
- 208000019622 heart disease Diseases 0.000 claims 2
- 230000000147 hypnotic effect Effects 0.000 claims 2
- 208000000509 infertility Diseases 0.000 claims 2
- 230000036512 infertility Effects 0.000 claims 2
- 231100000535 infertility Toxicity 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000000968 intestinal effect Effects 0.000 claims 2
- 201000010901 lateral sclerosis Diseases 0.000 claims 2
- 210000003141 lower extremity Anatomy 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 208000005264 motor neuron disease Diseases 0.000 claims 2
- 210000003205 muscle Anatomy 0.000 claims 2
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 claims 2
- 230000001537 neural effect Effects 0.000 claims 2
- 208000004296 neuralgia Diseases 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 230000001272 neurogenic effect Effects 0.000 claims 2
- 208000021722 neuropathic pain Diseases 0.000 claims 2
- 229960002715 nicotine Drugs 0.000 claims 2
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 208000024309 orgasm disease Diseases 0.000 claims 2
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- 239000000932 sedative agent Substances 0.000 claims 2
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- 230000009885 systemic effect Effects 0.000 claims 2
- 230000009529 traumatic brain injury Effects 0.000 claims 2
- JJQQOTDMHDOYTF-UHFFFAOYSA-N (1,2-dimethylpyrrolo[2,3-b]pyridin-5-yl)methanamine Chemical compound CN1C(=CC=2C1=NC=C(C=2)CN)C JJQQOTDMHDOYTF-UHFFFAOYSA-N 0.000 claims 1
- BESDAEWBKZKOOE-UHFFFAOYSA-N (3-bromo-1-methylpyrrolo[2,3-b]pyridin-5-yl)methanamine Chemical compound BrC1=CN(C2=NC=C(C=C21)CN)C BESDAEWBKZKOOE-UHFFFAOYSA-N 0.000 claims 1
- UNOXCWIALZCQIP-UHFFFAOYSA-N (3-chloro-1-methylpyrrolo[2,3-b]pyridin-5-yl)methanamine Chemical compound Cn1cc(Cl)c2cc(CN)cnc12 UNOXCWIALZCQIP-UHFFFAOYSA-N 0.000 claims 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 1
- SWISCHSCULZVBC-UHFFFAOYSA-N 6-chloro-N-[(1-methylindol-5-yl)methyl]-4-oxospiro[3H-chromene-2,3'-azetidine]-1'-carboxamide Chemical compound ClC=1C=CC2=C(C(CC3(O2)CN(C3)C(=O)NCC=2C=C3C=CN(C3=CC=2)C)=O)C=1 SWISCHSCULZVBC-UHFFFAOYSA-N 0.000 claims 1
- FYMWXTXPAIVRIU-UHFFFAOYSA-N CC=1NC2=CC=C(C=C2C1)CNC(=O)N1CC2(OC3=C(C(C2)=O)C=C(C=C3)C(F)(F)F)C1 Chemical compound CC=1NC2=CC=C(C=C2C1)CNC(=O)N1CC2(OC3=C(C(C2)=O)C=C(C=C3)C(F)(F)F)C1 FYMWXTXPAIVRIU-UHFFFAOYSA-N 0.000 claims 1
- XDXRTNDNZZFDPW-UHFFFAOYSA-N CC=1NC2=CC=C(C=C2C1)CNC(=O)N1CC2(OC3=C(C(C2)=O)C=CC(=C3)C(F)(F)F)C1 Chemical compound CC=1NC2=CC=C(C=C2C1)CNC(=O)N1CC2(OC3=C(C(C2)=O)C=CC(=C3)C(F)(F)F)C1 XDXRTNDNZZFDPW-UHFFFAOYSA-N 0.000 claims 1
- UYEQFCNSGDUMDF-UHFFFAOYSA-N CN1C2=CC=C(CN(C3)CC3(C=CC3=C4)OC3=CC=C4F)C=C2C=C1 Chemical compound CN1C2=CC=C(CN(C3)CC3(C=CC3=C4)OC3=CC=C4F)C=C2C=C1 UYEQFCNSGDUMDF-UHFFFAOYSA-N 0.000 claims 1
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- YAENGOXVNACGGL-UHFFFAOYSA-N FC1=CC2=C(C(CC3(O2)CN(C3)C(=O)NCC=3C=C2C=C(NC2=CC3)C(F)(F)F)=O)C=C1 Chemical compound FC1=CC2=C(C(CC3(O2)CN(C3)C(=O)NCC=3C=C2C=C(NC2=CC3)C(F)(F)F)=O)C=C1 YAENGOXVNACGGL-UHFFFAOYSA-N 0.000 claims 1
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- LXOXUGXUUINWLS-UHFFFAOYSA-N FC1=CC2=C(C(CC3(O2)CN(C3)C(=O)NCC=3C=C2C=CN(C2=CC3)C)=O)C=C1 Chemical compound FC1=CC2=C(C(CC3(O2)CN(C3)C(=O)NCC=3C=C2C=CN(C2=CC3)C)=O)C=C1 LXOXUGXUUINWLS-UHFFFAOYSA-N 0.000 claims 1
- CUKVZAWHRNNHFS-UHFFFAOYSA-N FC=1C=C(C2=C(C(CC3(O2)CN(C3)C(=O)NCC=3C=C2C=C(NC2=CC3)C)=O)C1)F Chemical compound FC=1C=C(C2=C(C(CC3(O2)CN(C3)C(=O)NCC=3C=C2C=C(NC2=CC3)C)=O)C1)F CUKVZAWHRNNHFS-UHFFFAOYSA-N 0.000 claims 1
- COBVBBSZLRJQHS-UHFFFAOYSA-N FC=1C=CC2=C(C(CC3(O2)CN(C3)C(=O)NCC=3C=C2C=C(NC2=CC3)C)=O)C1 Chemical compound FC=1C=CC2=C(C(CC3(O2)CN(C3)C(=O)NCC=3C=C2C=C(NC2=CC3)C)=O)C1 COBVBBSZLRJQHS-UHFFFAOYSA-N 0.000 claims 1
- HJQGJYHJSNIXEE-UHFFFAOYSA-N FC=1C=CC2=C(CCC3(O2)CN(C3)C(=O)NCC=3C=C2C=CN(C2=CC3)C)C1 Chemical compound FC=1C=CC2=C(CCC3(O2)CN(C3)C(=O)NCC=3C=C2C=CN(C2=CC3)C)C1 HJQGJYHJSNIXEE-UHFFFAOYSA-N 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- 229940127523 NMDA Receptor Antagonists Drugs 0.000 claims 1
- 239000000164 antipsychotic agent Substances 0.000 claims 1
- 229940005529 antipsychotics Drugs 0.000 claims 1
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 1
- 150000004678 hydrides Chemical class 0.000 claims 1
- IXCSERBJSXMMFS-UHFFFAOYSA-N hydrogen chloride Substances Cl.Cl IXCSERBJSXMMFS-UHFFFAOYSA-N 0.000 claims 1
- 229910000041 hydrogen chloride Inorganic materials 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 229940044551 receptor antagonist Drugs 0.000 claims 1
- 239000002464 receptor antagonist Substances 0.000 claims 1
- 230000004044 response Effects 0.000 claims 1
- RXJKFRMDXUJTEX-UHFFFAOYSA-N triethylphosphine Chemical compound CCP(CC)CC RXJKFRMDXUJTEX-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HUP1800248A HU231333B1 (hu) | 2018-07-13 | 2018-07-13 | Spirokromán származékok |
| HUP1800248 | 2018-07-13 | ||
| PCT/IB2019/055948 WO2020012422A1 (en) | 2018-07-13 | 2019-07-12 | Spirochromane derivatives |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021531260A JP2021531260A (ja) | 2021-11-18 |
| JP2021531260A5 JP2021531260A5 (https=) | 2022-07-20 |
| JPWO2020012422A5 true JPWO2020012422A5 (https=) | 2022-07-20 |
| JP7487167B2 JP7487167B2 (ja) | 2024-05-20 |
Family
ID=89992725
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021500532A Active JP7487167B2 (ja) | 2018-07-13 | 2019-07-12 | スピロクロマン誘導体 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US20210330650A1 (https=) |
| EP (1) | EP3820869B1 (https=) |
| JP (1) | JP7487167B2 (https=) |
| KR (1) | KR20210033002A (https=) |
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| AU (1) | AU2019300514B2 (https=) |
| BR (1) | BR112020026996A2 (https=) |
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| ES (1) | ES2964617T3 (https=) |
| GE (2) | GEAP202315557A (https=) |
| HU (2) | HU231333B1 (https=) |
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| PE (1) | PE20211809A1 (https=) |
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Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU231414B1 (hu) | 2018-07-13 | 2023-08-28 | Richter Gedeon Nyrt. | Tiadiazin származékok |
| TWI901650B (zh) | 2020-03-26 | 2025-10-21 | 匈牙利商羅特格登公司 | 啶及吡啶并〔3,4-c〕嗒衍生物 |
| CN115403579A (zh) * | 2021-05-27 | 2022-11-29 | 上海拓界生物医药科技有限公司 | 一种新的螺环衍生物及其用途 |
| HU231691B1 (hu) | 2021-09-29 | 2025-10-28 | Richter Gedeon Nyrt | GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok |
| WO2025175249A1 (en) | 2024-02-14 | 2025-08-21 | Olema Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
Family Cites Families (19)
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| WO2006016548A1 (ja) | 2004-08-09 | 2006-02-16 | Eisai R & D Management Co., Ltd. | ヘテロ環化合物を含有する新規な抗マラリア剤 |
| NZ566036A (en) | 2005-09-13 | 2010-06-25 | Janssen Pharmaceutica Nv | 2-Aniline-4-aryl substituted thiazole derivatives that modulate the alpha7 nicotinic receptor |
| CN101490056A (zh) * | 2006-05-17 | 2009-07-22 | 阿斯利康(瑞典)有限公司 | 烟碱乙酰胆碱受体的配体101 |
| TW200813067A (en) * | 2006-05-17 | 2008-03-16 | Astrazeneca Ab | Nicotinic acetylcholine receptor ligands |
| US20100298314A1 (en) | 2006-12-20 | 2010-11-25 | Schering Corporation | Novel jnk inhibitors |
| MX2010003156A (es) | 2007-10-04 | 2010-04-01 | Hoffmann La Roche | Derivados de aril amida substituida con tetrazol y usos de los mismos. |
| MX2010003155A (es) | 2007-10-04 | 2010-04-01 | Hoffmann La Roche | Derivados de ciclopropil aril amida y uso de los mismos. |
| KR20100124272A (ko) | 2008-02-07 | 2010-11-26 | 아보트 러보러터리즈 | 양성 알로스테릭 조절제로서의 아미드 유도체 및 이의 사용방법 |
| AR070936A1 (es) | 2008-03-19 | 2010-05-12 | Janssen Pharmaceutica Nv | 1,2,4 -triazoles trisustituidos |
| EP2110377A1 (en) * | 2008-04-15 | 2009-10-21 | DAC S.r.l. | Spirocyclic derivatives as histone deacetylase inhibitors |
| WO2009127678A1 (en) * | 2008-04-17 | 2009-10-22 | Glaxo Group Limited | Indoles as modulators of nicotinic acetylcholin receptor subtype alpha-71 |
| JP5486591B2 (ja) | 2008-05-09 | 2014-05-07 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | アセチルコリン受容体モジュレーターとしての三置換ピラゾール |
| CA2725940A1 (en) | 2008-05-30 | 2009-12-23 | Merck Sharp & Dohme Corp. | Novel substituted azabenzoxazoles |
| EP3795573B1 (en) | 2009-12-31 | 2022-07-06 | Hutchison Medipharma Limited | Certain triazolopyrazines, compositions thereof and methods of use therefor |
| WO2012042915A1 (en) | 2010-10-01 | 2012-04-05 | Raqualia Pharma Inc. | Sulfamoyl benzoic acid heterobicyclic derivatives as trpm8 antagonists |
| US9617210B2 (en) * | 2013-03-13 | 2017-04-11 | Lupin Limited | Pyrrole derivatives as alpha 7 NACHR modulators |
| AR107928A1 (es) | 2016-03-22 | 2018-06-28 | Merck Sharp & Dohme | Moduladores alostéricos de receptores de acetilcolina nicotínicos |
| US10870630B2 (en) | 2016-11-01 | 2020-12-22 | Merck Sharp & Dohme Corp. | Substituted bicyclic heteroaryl allosteric modulators of nicotinic acetylcholine receptors |
| WO2018112204A1 (en) * | 2016-12-14 | 2018-06-21 | Cephalon, Inc. | Spiropiperidine derivatives |
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2018
- 2018-07-13 HU HUP1800248A patent/HU231333B1/hu unknown
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2019
- 2019-06-27 TW TW108122548A patent/TWI821321B/zh active
- 2019-07-12 CA CA3104258A patent/CA3104258A1/en active Pending
- 2019-07-12 US US17/259,972 patent/US20210330650A1/en not_active Abandoned
- 2019-07-12 CU CU2020000108A patent/CU24680B1/es unknown
- 2019-07-12 AU AU2019300514A patent/AU2019300514B2/en not_active Ceased
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- 2019-07-12 PE PE2021000053A patent/PE20211809A1/es unknown
- 2019-07-12 KR KR1020217004264A patent/KR20210033002A/ko not_active Abandoned
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- 2019-07-12 EP EP19744868.1A patent/EP3820869B1/en active Active
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- 2019-07-12 CN CN201980046665.7A patent/CN112823157B/zh active Active
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2020
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2021
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