JP2018505204A5 - - Google Patents
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- Publication number
- JP2018505204A5 JP2018505204A5 JP2017542400A JP2017542400A JP2018505204A5 JP 2018505204 A5 JP2018505204 A5 JP 2018505204A5 JP 2017542400 A JP2017542400 A JP 2017542400A JP 2017542400 A JP2017542400 A JP 2017542400A JP 2018505204 A5 JP2018505204 A5 JP 2018505204A5
- Authority
- JP
- Japan
- Prior art keywords
- disorder
- pharmaceutically acceptable
- depression
- pharmaceutical composition
- combined
- 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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- 238000000034 method Methods 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- ZCSHNCUQKCANBX-UHFFFAOYSA-N lithium diisopropylamide Chemical compound [Li+].CC(C)[N-]C(C)C ZCSHNCUQKCANBX-UHFFFAOYSA-N 0.000 claims 6
- DYHSDKLCOJIUFX-UHFFFAOYSA-N tert-butoxycarbonyl anhydride Chemical compound CC(C)(C)OC(=O)OC(=O)OC(C)(C)C DYHSDKLCOJIUFX-UHFFFAOYSA-N 0.000 claims 6
- 208000012902 Nervous system disease Diseases 0.000 claims 4
- 208000028552 Treatment-Resistant Depressive disease Diseases 0.000 claims 4
- 208000024714 major depressive disease Diseases 0.000 claims 4
- 208000020016 psychiatric disease Diseases 0.000 claims 4
- LDLCZOVUSADOIV-UHFFFAOYSA-N 2-bromoethanol Chemical compound OCCBr LDLCZOVUSADOIV-UHFFFAOYSA-N 0.000 claims 3
- 206010042458 Suicidal ideation Diseases 0.000 claims 3
- 230000000926 neurological effect Effects 0.000 claims 3
- MSWTVSDFEYSRMQ-UHFFFAOYSA-N tert-butyl n-methyl-n-(2-oxoethyl)carbamate Chemical compound O=CCN(C)C(=O)OC(C)(C)C MSWTVSDFEYSRMQ-UHFFFAOYSA-N 0.000 claims 3
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 3
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 206010010144 Completed suicide Diseases 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 208000025966 Neurological disease Diseases 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 2
- 238000004296 chiral HPLC Methods 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000003981 vehicle Substances 0.000 claims 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 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 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000020401 Depressive disease Diseases 0.000 claims 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 206010041250 Social phobia Diseases 0.000 claims 1
- 206010065604 Suicidal behaviour Diseases 0.000 claims 1
- 206010042464 Suicide attempt Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 229940124330 analgesic enhancer Drugs 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 208000028683 bipolar I disease Diseases 0.000 claims 1
- 208000025307 bipolar depression Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 239000002475 cognitive enhancer Substances 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000003104 endogenous depression Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- OVMFTCUOUXRUJP-LLVKDONJSA-N CNC[C@H]1OCC[n]2nc(cccc3)c3c12 Chemical compound CNC[C@H]1OCC[n]2nc(cccc3)c3c12 OVMFTCUOUXRUJP-LLVKDONJSA-N 0.000 description 3
- PJSHHOSKOCNWNP-UHFFFAOYSA-N CC(C)(C)OC(N(C)CC1OCC[n]2nc(cccc3)c3c12)=O Chemical compound CC(C)(C)OC(N(C)CC1OCC[n]2nc(cccc3)c3c12)=O PJSHHOSKOCNWNP-UHFFFAOYSA-N 0.000 description 2
- OVMFTCUOUXRUJP-NSHDSACASA-N CNC[C@@H]1OCC[n]2nc(cccc3)c3c12 Chemical compound CNC[C@@H]1OCC[n]2nc(cccc3)c3c12 OVMFTCUOUXRUJP-NSHDSACASA-N 0.000 description 2
- WLDDONJNJUQPDI-UHFFFAOYSA-N CC(C)(C)OC(N(C)CC(c1c(cccc2)c2n[n]1CCO)O)=O Chemical compound CC(C)(C)OC(N(C)CC(c1c(cccc2)c2n[n]1CCO)O)=O WLDDONJNJUQPDI-UHFFFAOYSA-N 0.000 description 1
- PJSHHOSKOCNWNP-AWEZNQCLSA-N CC(C)(C)OC(N(C)C[C@@H]1OCC[n]2nc(cccc3)c3c12)=O Chemical compound CC(C)(C)OC(N(C)C[C@@H]1OCC[n]2nc(cccc3)c3c12)=O PJSHHOSKOCNWNP-AWEZNQCLSA-N 0.000 description 1
- PJSHHOSKOCNWNP-CQSZACIVSA-N CC(C)(C)OC(N(C)C[C@H]1OCC[n]2nc(cccc3)c3c12)=O Chemical compound CC(C)(C)OC(N(C)C[C@H]1OCC[n]2nc(cccc3)c3c12)=O PJSHHOSKOCNWNP-CQSZACIVSA-N 0.000 description 1
- OVMFTCUOUXRUJP-UHFFFAOYSA-N CNCC1OCC[n]2nc(cccc3)c3c12 Chemical compound CNCC1OCC[n]2nc(cccc3)c3c12 OVMFTCUOUXRUJP-UHFFFAOYSA-N 0.000 description 1
- YKKZOHDZPPHABF-UHFFFAOYSA-N OCC[n]1nc(cccc2)c2c1 Chemical compound OCC[n]1nc(cccc2)c2c1 YKKZOHDZPPHABF-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2019134260A JP6928629B2 (ja) | 2015-02-11 | 2019-07-22 | Ｃｎｓ疾患を治療するための縮合ジヒドロ−４ｈ−ピラゾロ［５，１−ｃ］［１，４］オキサジニル化合物およびアナログ |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562115043P | 2015-02-11 | 2015-02-11 | |
| US62/115,043 | 2015-02-11 | ||
| PCT/US2016/017527 WO2016130790A1 (en) | 2015-02-11 | 2016-02-11 | Fused dihydro-4h-pyrazolo[5,1-c][1,4]oxazinyl compounds and analogs for treating cns disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019134260A Division JP6928629B2 (ja) | 2015-02-11 | 2019-07-22 | Ｃｎｓ疾患を治療するための縮合ジヒドロ−４ｈ−ピラゾロ［５，１−ｃ］［１，４］オキサジニル化合物およびアナログ |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018505204A JP2018505204A (ja) | 2018-02-22 |
| JP2018505204A5 true JP2018505204A5 (https=) | 2019-03-28 |
| JP6561128B2 JP6561128B2 (ja) | 2019-08-14 |
Family
ID=55456906
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017542400A Expired - Fee Related JP6561128B2 (ja) | 2015-02-11 | 2016-02-11 | Ｃｎｓ疾患を治療するための縮合ジヒドロ−４ｈ−ピラゾロ［５，１−ｃ］［１，４］オキサジニル化合物およびアナログ |
| JP2019134260A Expired - Fee Related JP6928629B2 (ja) | 2015-02-11 | 2019-07-22 | Ｃｎｓ疾患を治療するための縮合ジヒドロ−４ｈ−ピラゾロ［５，１−ｃ］［１，４］オキサジニル化合物およびアナログ |
| JP2021129696A Ceased JP2021183624A (ja) | 2015-02-11 | 2021-08-06 | Ｃｎｓ疾患を治療するための縮合ジヒドロ−４ｈ−ピラゾロ［５，１−ｃ］［１，４］オキサジニル化合物およびアナログ |
| JP2022193341A Ceased JP2023036611A (ja) | 2015-02-11 | 2022-12-02 | Ｃｎｓ疾患を治療するための縮合ジヒドロ－４ｈ－ピラゾロ［５，１－ｃ］［１，４］オキサジニル化合物およびアナログ |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019134260A Expired - Fee Related JP6928629B2 (ja) | 2015-02-11 | 2019-07-22 | Ｃｎｓ疾患を治療するための縮合ジヒドロ−４ｈ−ピラゾロ［５，１−ｃ］［１，４］オキサジニル化合物およびアナログ |
| JP2021129696A Ceased JP2021183624A (ja) | 2015-02-11 | 2021-08-06 | Ｃｎｓ疾患を治療するための縮合ジヒドロ−４ｈ−ピラゾロ［５，１−ｃ］［１，４］オキサジニル化合物およびアナログ |
| JP2022193341A Ceased JP2023036611A (ja) | 2015-02-11 | 2022-12-02 | Ｃｎｓ疾患を治療するための縮合ジヒドロ－４ｈ－ピラゾロ［５，１－ｃ］［１，４］オキサジニル化合物およびアナログ |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US9758529B2 (https=) |
| EP (3) | EP3539967A1 (https=) |
| JP (4) | JP6561128B2 (https=) |
| KR (1) | KR102623321B1 (https=) |
| CN (2) | CN111171047B (https=) |
| AU (4) | AU2016219247B2 (https=) |
| BR (1) | BR112017017349B1 (https=) |
| CA (1) | CA2976092A1 (https=) |
| DK (1) | DK3256476T3 (https=) |
| EA (1) | EA201791802A1 (https=) |
| ES (1) | ES2712627T3 (https=) |
| IL (2) | IL253907B (https=) |
| MX (1) | MX371197B (https=) |
| NZ (1) | NZ734972A (https=) |
| PH (1) | PH12017501423A1 (https=) |
| PL (1) | PL3256476T3 (https=) |
| PT (1) | PT3256476T (https=) |
| SG (1) | SG11201706516WA (https=) |
| UA (1) | UA123262C2 (https=) |
| WO (1) | WO2016130790A1 (https=) |
| ZA (1) | ZA201706074B (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111171047B (zh) * | 2015-02-11 | 2023-06-23 | 赛诺维信制药公司 | 用于治疗cns障碍的稠合二氢-4h-吡唑并[5,1-c][1,4]噁嗪基化合物 |
| CA3032141A1 (en) | 2016-07-29 | 2018-02-01 | Vadim ALEXANDROV | Compounds and compositions and uses thereof |
| UA125519C2 (uk) | 2016-07-29 | 2022-04-13 | Суновіон Фармасьютікалз Інк. | Сполуки і композиції і їх застосування |
| KR101753092B1 (ko) | 2016-12-14 | 2017-07-04 | 성일하이텍(주) | 리튬 함유 폐액으로부터 인산리튬 제조방법 |
| US10850989B2 (en) | 2016-12-20 | 2020-12-01 | Sungeel Hitech Co., Ltd. | Method for preparing solid lithium salt from lithium solution |
| CN121221782A (zh) | 2017-06-30 | 2025-12-30 | 傲拓神经科学公司 | 用于治疗抑郁的nk-1拮抗剂组合物和方法 |
| BR112020001433A2 (pt) | 2017-08-02 | 2020-07-28 | Sunovion Pharmaceuticals Inc. | compostos de isocromano e usos dos mesmos |
| WO2019236808A1 (en) | 2018-06-07 | 2019-12-12 | Sunovion Pharmaceuticals Inc. | Salts of a oxazino[4,3-b]indazole derivative and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof |
| US20210393621A1 (en) | 2018-10-26 | 2021-12-23 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
| MX2021010880A (es) | 2019-03-14 | 2022-01-18 | Sunovion Pharmaceuticals Inc | Sales de un compuesto de isocromanilo y formas cristalinas, procesos de preparacion, usos terapeuticos y composiciones farmaceuticas de las mismas. |
| TW202237622A (zh) * | 2020-12-04 | 2022-10-01 | 美商蘇諾維恩藥業公司 | 雜環化合物的鹽及其晶型、製備方法、治療用途與醫藥組合物 |
| WO2022217233A1 (en) * | 2021-04-08 | 2022-10-13 | Sunovion Pharmaceuticals Inc. | Fused dihydro-4h-pyrazolo[5,1-c][1,4]oxazinyl compounds and analogs for treating cns disorders |
| EP4416133A1 (en) * | 2021-10-11 | 2024-08-21 | Baylor College of Medicine | G-protein-coupled receptor regulators and methods of use thereof |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3995052A (en) * | 1973-07-09 | 1976-11-30 | Ayerst Mckenna And Harrison Ltd. | Indenopyran- and indenothiopyranalkylamines III in the treatment of depression |
| US4041169A (en) * | 1975-03-05 | 1977-08-09 | Ayerst Mckenna And Harrison Ltd. | Pharmaceutical method for using pyrano-and thiopyranoindole derivatives |
| MX2008013053A (es) * | 2006-04-12 | 2008-10-17 | Wyeth Corp | Derivados de dihidri[1,4]oxazino[2,3,4-hi]indazol-sustituidos como ligandos de 5-hidroxitriptamina-6. |
| KR20110132564A (ko) * | 2009-02-11 | 2011-12-08 | 선오비온 파마슈티컬스 인코포레이티드 | 히스타민 ｈ3 역 작용제 및 길항제, 및 이의 사용 방법 |
| CN106883246B (zh) * | 2009-12-04 | 2020-05-29 | 桑诺维恩药品公司 | 多环化合物及其使用方法 |
| CN103313989B (zh) * | 2010-12-16 | 2016-05-04 | 霍夫曼-拉罗奇有限公司 | 三环pi3k抑制剂化合物和使用方法 |
| KR20140082765A (ko) * | 2011-10-05 | 2014-07-02 | 에프. 호프만-라 로슈 아게 | V1a 길항제로서의 사이클로헥실-4H,6H-5-옥사-2,3,10b-트라이아자-벤조[e]아줄렌 |
| WO2013067248A1 (en) * | 2011-11-04 | 2013-05-10 | Vertex Pharmaceuticals Incorporated | Benzoxazines as modulators of ion channels |
| AU2012357169B2 (en) * | 2011-12-22 | 2017-03-30 | Merck Patent Gmbh | Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators |
| CN104797255A (zh) * | 2012-06-20 | 2015-07-22 | 范德比尔特大学 | 作为mglur5受体变构调节剂的取代的双环烷氧基吡唑类似物 |
| JP2014214130A (ja) * | 2013-04-26 | 2014-11-17 | 大正製薬株式会社 | ジヒドロイミダゾオキサゾール誘導体を含有する医薬 |
| CN111171047B (zh) * | 2015-02-11 | 2023-06-23 | 赛诺维信制药公司 | 用于治疗cns障碍的稠合二氢-4h-吡唑并[5,1-c][1,4]噁嗪基化合物 |
| PL3256466T3 (pl) * | 2015-02-11 | 2022-05-23 | Sunovion Pharmaceuticals Inc. | Związki 1-heterocykliloizochromanylu i analogi do leczenia zaburzeń oun |
-
2016
- 2016-02-11 CN CN202010051639.8A patent/CN111171047B/zh not_active Expired - Fee Related
- 2016-02-11 WO PCT/US2016/017527 patent/WO2016130790A1/en not_active Ceased
- 2016-02-11 CN CN201680018684.5A patent/CN107567454B/zh not_active Expired - Fee Related
- 2016-02-11 BR BR112017017349-2A patent/BR112017017349B1/pt not_active IP Right Cessation
- 2016-02-11 EP EP18213435.3A patent/EP3539967A1/en not_active Withdrawn
- 2016-02-11 DK DK16708260.1T patent/DK3256476T3/en active
- 2016-02-11 JP JP2017542400A patent/JP6561128B2/ja not_active Expired - Fee Related
- 2016-02-11 EA EA201791802A patent/EA201791802A1/ru unknown
- 2016-02-11 EP EP16708260.1A patent/EP3256476B1/en active Active
- 2016-02-11 MX MX2017010362A patent/MX371197B/es active IP Right Grant
- 2016-02-11 AU AU2016219247A patent/AU2016219247B2/en not_active Expired - Fee Related
- 2016-02-11 EP EP21198192.3A patent/EP4006039B1/en active Active
- 2016-02-11 PT PT16708260T patent/PT3256476T/pt unknown
- 2016-02-11 US US15/041,827 patent/US9758529B2/en not_active Expired - Fee Related
- 2016-02-11 UA UAA201708954A patent/UA123262C2/uk unknown
- 2016-02-11 ES ES16708260T patent/ES2712627T3/es active Active
- 2016-02-11 KR KR1020177025289A patent/KR102623321B1/ko active Active
- 2016-02-11 PL PL16708260T patent/PL3256476T3/pl unknown
- 2016-02-11 SG SG11201706516WA patent/SG11201706516WA/en unknown
- 2016-02-11 CA CA2976092A patent/CA2976092A1/en active Pending
- 2016-02-11 NZ NZ734972A patent/NZ734972A/en not_active IP Right Cessation
-
2017
- 2017-08-02 US US15/666,719 patent/US20180057506A1/en not_active Abandoned
- 2017-08-08 IL IL253907A patent/IL253907B/en active IP Right Grant
- 2017-08-09 PH PH12017501423A patent/PH12017501423A1/en unknown
- 2017-09-06 ZA ZA2017/06074A patent/ZA201706074B/en unknown
-
2019
- 2019-05-06 US US16/403,734 patent/US20200024286A1/en not_active Abandoned
- 2019-07-22 JP JP2019134260A patent/JP6928629B2/ja not_active Expired - Fee Related
-
2020
- 2020-09-29 IL IL277658A patent/IL277658B/en unknown
- 2020-11-11 AU AU2020267209A patent/AU2020267209A1/en not_active Abandoned
-
2021
- 2021-02-19 US US17/179,477 patent/US20210300942A1/en not_active Abandoned
- 2021-08-06 JP JP2021129696A patent/JP2021183624A/ja not_active Ceased
-
2022
- 2022-10-28 AU AU2022259828A patent/AU2022259828A1/en not_active Abandoned
- 2022-12-02 JP JP2022193341A patent/JP2023036611A/ja not_active Ceased
-
2024
- 2024-06-24 AU AU2024204310A patent/AU2024204310A1/en not_active Abandoned
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