JP2016518343A5 - - Google Patents
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- JP2016518343A5 JP2016518343A5 JP2016503395A JP2016503395A JP2016518343A5 JP 2016518343 A5 JP2016518343 A5 JP 2016518343A5 JP 2016503395 A JP2016503395 A JP 2016503395A JP 2016503395 A JP2016503395 A JP 2016503395A JP 2016518343 A5 JP2016518343 A5 JP 2016518343A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- optionally
- methyl
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 227
- -1 tetrahydro-2H-pyran-4-yl Chemical group 0.000 claims 104
- 125000003118 aryl group Chemical group 0.000 claims 93
- 125000001072 heteroaryl group Chemical group 0.000 claims 81
- 125000005843 halogen group Chemical group 0.000 claims 60
- 229910052799 carbon Inorganic materials 0.000 claims 54
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 52
- 229910052739 hydrogen Inorganic materials 0.000 claims 45
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 42
- 125000004076 pyridyl group Chemical group 0.000 claims 35
- 229910052757 nitrogen Inorganic materials 0.000 claims 33
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 32
- 229910052731 fluorine Inorganic materials 0.000 claims 29
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 29
- 125000003545 alkoxy group Chemical group 0.000 claims 27
- 229910052801 chlorine Inorganic materials 0.000 claims 27
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 150000002367 halogens Chemical class 0.000 claims 26
- 125000005842 heteroatom Chemical group 0.000 claims 26
- 239000003814 drug Substances 0.000 claims 24
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 24
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 23
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 21
- 125000000753 cycloalkyl group Chemical group 0.000 claims 20
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 20
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 20
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 19
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 18
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 16
- 229940121836 Phosphodiesterase 1 inhibitor Drugs 0.000 claims 16
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 15
- 208000014674 injury Diseases 0.000 claims 15
- 125000002720 diazolyl group Chemical group 0.000 claims 14
- 125000001425 triazolyl group Chemical group 0.000 claims 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 208000035475 disorder Diseases 0.000 claims 13
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 13
- 125000003386 piperidinyl group Chemical group 0.000 claims 13
- 229910052794 bromium Inorganic materials 0.000 claims 12
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 12
- 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 11
- 125000001153 fluoro group Chemical group F* 0.000 claims 11
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 11
- 150000003839 salts Chemical group 0.000 claims 11
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 11
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 10
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 208000027418 Wounds and injury Diseases 0.000 claims 10
- 230000006378 damage Effects 0.000 claims 10
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 10
- 125000002757 morpholinyl group Chemical group 0.000 claims 10
- 125000003831 tetrazolyl group Chemical group 0.000 claims 10
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 9
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 9
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 9
- 208000015114 central nervous system disease Diseases 0.000 claims 9
- 125000001188 haloalkyl group Chemical group 0.000 claims 9
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 9
- 125000004512 1,2,3-thiadiazol-4-yl group Chemical group S1N=NC(=C1)* 0.000 claims 8
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 8
- 125000002947 alkylene group Chemical group 0.000 claims 8
- 125000000732 arylene group Chemical group 0.000 claims 8
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 8
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 8
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 7
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 7
- 125000005549 heteroarylene group Chemical group 0.000 claims 7
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 7
- 230000003834 intracellular effect Effects 0.000 claims 7
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 7
- 125000005551 pyridylene group Chemical group 0.000 claims 7
- 208000020431 spinal cord injury Diseases 0.000 claims 7
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 6
- 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 6
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 6
- 235000010290 biphenyl Nutrition 0.000 claims 6
- 239000004305 biphenyl Substances 0.000 claims 6
- 208000029028 brain injury Diseases 0.000 claims 6
- 229910052791 calcium Inorganic materials 0.000 claims 6
- 239000011575 calcium Substances 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 6
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims 6
- RGTBLCLLSZPOKR-UHFFFAOYSA-N 5-methyl-1,2,4-oxadiazole Chemical compound CC1=NC=NO1 RGTBLCLLSZPOKR-UHFFFAOYSA-N 0.000 claims 5
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000004419 alkynylene group Chemical group 0.000 claims 5
- IYABWNGZIDDRAK-UHFFFAOYSA-N allene Chemical group C=C=C IYABWNGZIDDRAK-UHFFFAOYSA-N 0.000 claims 5
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 5
- 125000001769 aryl amino group Chemical group 0.000 claims 5
- 125000001309 chloro group Chemical group Cl* 0.000 claims 5
- 125000001207 fluorophenyl group Chemical group 0.000 claims 5
- 125000005241 heteroarylamino group Chemical group 0.000 claims 5
- 125000004464 hydroxyphenyl group Chemical group 0.000 claims 5
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 5
- 125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 claims 5
- 230000008733 trauma Effects 0.000 claims 5
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 4
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 3
- 125000004493 2-methylbut-1-yl group Chemical group CC(C*)CC 0.000 claims 3
- 125000004217 4-methoxybenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])* 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 3
- 125000004171 alkoxy aryl group Chemical group 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 3
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims 3
- 125000004289 pyrazol-3-yl group Chemical group [H]N1N=C(*)C([H])=C1[H] 0.000 claims 3
- 125000006513 pyridinyl methyl group Chemical group 0.000 claims 3
- 125000006621 (C3-C8) cycloalkyl-(C1-C6) alkyl group Chemical group 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 231100000317 environmental toxin Toxicity 0.000 claims 2
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 125000004274 oxetan-2-yl group Chemical group [H]C1([H])OC([H])(*)C1([H])[H] 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000005576 pyrimidinylene group Chemical group 0.000 claims 2
- 239000000523 sample Substances 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- UGUHFDPGDQDVGX-UHFFFAOYSA-N 1,2,3-thiadiazole Chemical compound C1=CSN=N1 UGUHFDPGDQDVGX-UHFFFAOYSA-N 0.000 claims 1
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims 1
- 208000011990 Corticobasal Degeneration Diseases 0.000 claims 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 1
- 208000024412 Friedreich ataxia Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 208000001089 Multiple system atrophy Diseases 0.000 claims 1
- 206010033892 Paraplegia Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 102000029797 Prion Human genes 0.000 claims 1
- 108091000054 Prion Proteins 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 206010057430 Retinal injury Diseases 0.000 claims 1
- 208000032930 Spastic paraplegia Diseases 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000006430 alkyl cyclopropyl group Chemical group 0.000 claims 1
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 1
- 206010002022 amyloidosis Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 239000012472 biological sample Substances 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 230000006931 brain damage Effects 0.000 claims 1
- 231100000874 brain damage Toxicity 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 230000037041 intracellular level Effects 0.000 claims 1
- 125000001288 lysyl group Chemical group 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 208000027232 peripheral nervous system disease Diseases 0.000 claims 1
- 125000004574 piperidin-2-yl group Chemical group N1C(CCCC1)* 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 108700012359 toxins Proteins 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361799603P | 2013-03-15 | 2013-03-15 | |
| US61/799,603 | 2013-03-15 | ||
| PCT/US2014/030412 WO2014145617A2 (en) | 2013-03-15 | 2014-03-17 | Novel uses |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018200930A Division JP2019031544A (ja) | 2013-03-15 | 2018-10-25 | 新規使用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016518343A JP2016518343A (ja) | 2016-06-23 |
| JP2016518343A5 true JP2016518343A5 (https=) | 2017-04-13 |
Family
ID=51538509
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016503395A Withdrawn JP2016518343A (ja) | 2013-03-15 | 2014-03-17 | 新規使用 |
| JP2018200930A Withdrawn JP2019031544A (ja) | 2013-03-15 | 2018-10-25 | 新規使用 |
| JP2020034938A Pending JP2020105186A (ja) | 2013-03-15 | 2020-03-02 | 新規使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018200930A Withdrawn JP2019031544A (ja) | 2013-03-15 | 2018-10-25 | 新規使用 |
| JP2020034938A Pending JP2020105186A (ja) | 2013-03-15 | 2020-03-02 | 新規使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (4) | US9545406B2 (https=) |
| EP (2) | EP2968338B1 (https=) |
| JP (3) | JP2016518343A (https=) |
| ES (2) | ES2717688T3 (https=) |
| WO (1) | WO2014145617A2 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9545406B2 (en) | 2013-03-15 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Method of treating a CNS injury with a PDE1 inhibitor |
| EP3436083A4 (en) | 2016-03-28 | 2019-11-27 | Intra-Cellular Therapies, Inc. | NOVEL COMPOSITIONS AND METHOD |
| WO2018049417A1 (en) | 2016-09-12 | 2018-03-15 | Intra-Cellular Therapies, Inc. | Novel uses |
| JP7401442B2 (ja) * | 2018-01-31 | 2023-12-19 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 新規使用 |
| WO2019178484A1 (en) | 2018-03-16 | 2019-09-19 | Intra-Cellular Therapies, Inc. | Novel methods |
| AU2019275453B2 (en) * | 2018-05-25 | 2023-12-21 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2019237037A1 (en) | 2018-06-08 | 2019-12-12 | Intra-Cellular Therapies, Inc. | Novel methods |
| WO2019241141A1 (en) * | 2018-06-11 | 2019-12-19 | The United States Government As Represented By The Department Of Veterans Affairs | Method for treating myocardial reperfusion injury using an inhibitor of the cyclic nucleotide phosphodiesterase pde1 |
| US12396992B2 (en) | 2019-01-07 | 2025-08-26 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US11628171B2 (en) * | 2019-03-13 | 2023-04-18 | Children's Medical Center Corporation | Method for treating brain or nerve injury |
| EP4025202A4 (en) * | 2019-09-03 | 2023-08-02 | Intra-Cellular Therapies, Inc. | NOVEL CONNECTIONS |
| AU2020343329C1 (en) | 2019-09-03 | 2026-02-12 | Intra-Cellular Therapies, Inc. | Methods of treatment |
| US20230355625A1 (en) * | 2019-11-27 | 2023-11-09 | Intra-Cellular Therapies, Inc. | Methods of treatment |
| US12364695B2 (en) | 2020-06-02 | 2025-07-22 | Intra-Cellular Therapies, Inc. | Methods of treating inflammatory disease |
| EP4469052A4 (en) * | 2022-01-27 | 2026-02-11 | Intra Cellular Therapies Inc | NEW COMPOSITIONS |
| JP2025521115A (ja) | 2022-05-18 | 2025-07-08 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 新規方法 |
| WO2025111568A1 (en) | 2023-11-22 | 2025-05-30 | Intra-Cellular Therapies, Inc. | Lumateperone and analogues, as 5-ht2a or 5-ht2a/d2 receptor modulators, for use in the treatment of psychiatric disorders caused by viral, bacterial, or autoimmune encephalitis, and of psychiatric symptoms thereof |
| WO2025255013A1 (en) * | 2024-06-03 | 2025-12-11 | Intra-Cellular Therapies, Inc. | Organic compounds |
Family Cites Families (82)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6032638B2 (ja) | 1976-09-01 | 1985-07-29 | 武田薬品工業株式会社 | ３−アミノピラゾロ〔３，４−ｄ〕ピリミジン誘導体 |
| EP0077372A1 (de) | 1981-04-22 | 1983-04-27 | Byk Gulden Lomberg Chemische Fabrik GmbH | NEUE PYRAZOLO(3,4-d)PYRIMIDINE, VERFAHREN ZU DEREN HERSTELLUNG UND SIE ENTHALTENDE ARZNEIMITTEL |
| US4469868A (en) | 1982-05-24 | 1984-09-04 | Warner-Lambert Company | Alkylimidazo[1,2-c]pyrazolo[3,4-e]pyrimidines |
| US4603203A (en) | 1983-12-14 | 1986-07-29 | Takeda Chemical Industries, Ltd. | 3-aminopyrazolo[3,4-d]pyrimidine derivatives and production thereof |
| US4666908A (en) | 1985-04-05 | 1987-05-19 | Warner-Lambert Company | 5-Substituted pyrazolo[4,3-d]pyrimidine-7-ones and methods of use |
| KR920004437B1 (ko) | 1989-09-12 | 1992-06-05 | 삼성전자 주식회사 | 금전등록기의 거래선 관리방법 |
| ZA914727B (en) | 1990-06-21 | 1992-03-25 | Schering Corp | Polycyclic guanine derivatives |
| US5202328A (en) | 1991-03-06 | 1993-04-13 | Merck & Co., Inc. | Substituted fused pyrimidinones |
| US5294612A (en) | 1992-03-30 | 1994-03-15 | Sterling Winthrop Inc. | 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof |
| WO1994019351A1 (en) | 1993-02-26 | 1994-09-01 | Schering Corporation | 2-benzyl-polycyclic guanine derivatives and process for preparing them |
| GB9304919D0 (en) | 1993-03-10 | 1993-04-28 | Celltech Ltd | Chemical compounds |
| GB9315017D0 (en) | 1993-07-20 | 1993-09-01 | Glaxo Lab Sa | Chemical compounds |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| US5824683A (en) | 1995-11-28 | 1998-10-20 | Schering Corporation | 2'- 4'-halo- 1,1'-biphenyl!-4-yl!methyl!-5'-methyl-spiro cyclopentane-1,7' (8'H)- 3H! imidazo 2,1-b!purin!-4' (5'H)-ones |
| GB9526245D0 (en) | 1995-12-21 | 1996-02-21 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9622363D0 (en) | 1996-10-28 | 1997-01-08 | Celltech Therapeutics Ltd | Chemical compounds |
| US6057329A (en) | 1996-12-23 | 2000-05-02 | Celltech Therapeutics Limited | Fused polycyclic 2-aminopyrimidine derivatives |
| SE9701398D0 (sv) | 1997-04-15 | 1997-04-15 | Astra Pharma Prod | Novel compounds |
| IT1291372B1 (it) | 1997-05-21 | 1999-01-07 | Schering Plough S P A | Uso di analoghi eterociclici di 1,2,4-triazolo (1,5-c) pirimidine per la preparazione di medicamenti utili per il trattamento delle malattie |
| US6013621A (en) | 1997-10-17 | 2000-01-11 | The Rockfeller University | Method of treating psychosis and/or hyperactivity |
| GB9722520D0 (en) | 1997-10-24 | 1997-12-24 | Pfizer Ltd | Compounds |
| DE69943144D1 (de) | 1998-03-31 | 2011-03-03 | Kyowa Hakko Kirin Co Ltd | Stickstoffenthaltende heterocyclische verbindungen |
| US6133273A (en) | 1998-05-08 | 2000-10-17 | American Home Products Corporation | Pyrazolopyrimidine-2,4-dione sulfonamides |
| US6459908B1 (en) | 1998-12-31 | 2002-10-01 | Qwest Communications International Inc. | Method and system for supporting wireless features in a Generic C wireline architecture |
| GB9907658D0 (en) | 1999-04-06 | 1999-05-26 | Zeneca Ltd | Chemical compounds |
| WO2001000214A1 (en) | 1999-06-30 | 2001-01-04 | Merck & Co., Inc. | Src kinase inhibitor compounds |
| AU5636900A (en) | 1999-06-30 | 2001-01-31 | Merck & Co., Inc. | Src kinase inhibitor compounds |
| DE19931206A1 (de) | 1999-07-07 | 2001-01-11 | Stief Christian | Arzneimittel zur Erhöhung des cAMP-Spiegels und deren Verwendung |
| DE60023926T2 (de) | 1999-09-10 | 2006-07-20 | Merck & Co., Inc. | Tyrosin kinase inhibitoren |
| JP2003510325A (ja) | 1999-09-30 | 2003-03-18 | ニューロジェン・コーポレーション | ある種のアルキレンジアミン−置換ピラゾロ［１，５−ａ］−１，５−ピリミジン及びピラゾロ［１，５−ａ］−１，３，５−トリアジン |
| AP2002002455A0 (en) | 1999-10-11 | 2002-06-30 | Pfizer | 5-(2-substituted-5-heterocyclylsulphonylpyrid-3-yl)-dIhydropyrazolo[4,3-D] pyrimidin-7-ones as phosphodiesterase inhibitors. |
| TWI265925B (en) | 1999-10-11 | 2006-11-11 | Pfizer | Pyrazolo[4,3-d]pyrimidin-7-ones useful in inhibiting type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterases(cGMP PDE5), process and intermediates for their preparation, their uses and composition comprising them |
| IL139073A0 (en) | 1999-10-21 | 2001-11-25 | Pfizer | Treatment of neuropathy |
| MY125533A (en) | 1999-12-06 | 2006-08-30 | Bristol Myers Squibb Co | Heterocyclic dihydropyrimidine compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| JP2004500425A (ja) | 2000-04-19 | 2004-01-08 | リリー アイコス リミテッド ライアビリティ カンパニー | パーキンソン病の処置に対する環状ｇｍｐ特異的ホスホジエステラーゼインヒビターの使用 |
| US6693099B2 (en) | 2000-10-17 | 2004-02-17 | The Procter & Gamble Company | Substituted piperazine compounds optionally containing a quinolyl moiety for treating multidrug resistance |
| EP1372656B1 (en) | 2001-03-16 | 2005-06-22 | Pfizer Limited | Pyrazolo[4,3-d]pyrimidinone compounds as cgmp pde inhibitors |
| WO2002088079A2 (en) | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
| SE0102315D0 (sv) | 2001-06-28 | 2001-06-28 | Astrazeneca Ab | Compounds |
| WO2003020724A1 (en) | 2001-08-28 | 2003-03-13 | Schering Corporation | Polycyclic guanine phosphodiesterase v inhibitors |
| EP1575916B1 (en) | 2001-08-31 | 2013-05-22 | The Rockefeller University | Phosphodiesterase activity and regulation of phosphodiesterase 1-b-mediated signaling in brain |
| CA2465893A1 (en) | 2001-11-09 | 2003-05-22 | Schering Corporation | Polycyclic guanine derivative phosphodiesterase v inhibitors |
| AU2003219770B2 (en) | 2002-02-15 | 2008-10-09 | Merckle Gmbh | Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof |
| IL163575A0 (en) | 2002-02-21 | 2005-12-18 | Univ Rockefeller | Compositions and method for regulation of calcium-dependent signalling in brain |
| GB0230045D0 (en) | 2002-12-23 | 2003-01-29 | Glaxo Group Ltd | Compounds |
| AU2003272728A1 (en) * | 2002-09-27 | 2004-04-19 | Children's Medical Center Corporation | Methods and compositions for treatment of neurological disorder |
| WO2004031375A2 (en) * | 2002-10-01 | 2004-04-15 | Bayer Healthcare Ag | Regulation of human 3’, 5’ cyclic nucleotide phosphodiesterase pde1c |
| US20070155662A1 (en) * | 2003-03-11 | 2007-07-05 | Stefan Golz | Diagnostics and therapeutics for diseases associated with phosphodiesterase 1a (pde1a) |
| EP1613747A1 (en) | 2003-03-31 | 2006-01-11 | Pfizer Products Inc. | Crystal structure of 3 ,5 -cyclic nucleotide phosphodiesterase 1b (pde1b) and uses thereof |
| MXPA05010373A (es) | 2003-04-01 | 2005-12-05 | Applied Research Systems | Inhibidores de fosfodiesterasas en infertilidad. |
| US20050113379A1 (en) | 2003-09-05 | 2005-05-26 | Ping Ge | Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands |
| US20050287665A1 (en) * | 2004-06-23 | 2005-12-29 | Henrich Cheng | Method for inducing neural differentiation |
| AU2005282379B8 (en) * | 2004-09-08 | 2012-04-05 | Spinal Modulation Inc. | Neurostimulation methods and systems |
| US8273750B2 (en) | 2005-06-06 | 2012-09-25 | Takeda Pharmaceutical Company Limited | Organic compounds |
| EP1919287A4 (en) | 2005-08-23 | 2010-04-28 | Intra Cellular Therapies Inc | ORGANIC COMPOUNDS FOR TREATING A REDUCED DOPAMINE RECEPTOR SIGNALING ACTIVITY |
| JP5453086B2 (ja) | 2006-06-06 | 2014-03-26 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 有機化合物 |
| US20070286890A1 (en) | 2006-06-07 | 2007-12-13 | John Garnett Walt | Eyelash applicator and method |
| JP2010509399A (ja) * | 2006-11-13 | 2010-03-25 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 有機化合物 |
| US9006258B2 (en) | 2006-12-05 | 2015-04-14 | Intra-Cellular Therapies, Inc. | Method of treating female sexual dysfunction with a PDE1 inhibitor |
| ES2588238T3 (es) | 2007-12-06 | 2016-10-31 | Intra-Cellular Therapies, Inc. | Derivados de pirazolopirimidin-4,6-diona y su uso como producto farmacéutico |
| AU2008335811B2 (en) * | 2007-12-06 | 2012-05-17 | Intra-Cellular Therapies, Inc. | Organic compounds |
| AU2009322904A1 (en) | 2008-12-06 | 2010-06-10 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2010065147A1 (en) | 2008-12-06 | 2010-06-10 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN102231953A (zh) | 2008-12-06 | 2011-11-02 | 细胞内治疗公司 | 有机化合物 |
| KR20110098732A (ko) | 2008-12-06 | 2011-09-01 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| JP5989993B2 (ja) | 2008-12-06 | 2016-09-07 | イントラ−セルラー・セラピーズ・インコーポレイテッドＩｎｔｒａ−Ｃｅｌｌｕｌａｒ Ｔｈｅｒａｐｉｅｓ， Ｉｎｃ． | 有機化合物 |
| MX2011005936A (es) * | 2008-12-06 | 2011-12-16 | Intra Cellular Therapies Inc | Compuestos organicos. |
| JP2012518685A (ja) * | 2009-02-25 | 2012-08-16 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 眼障害のためのｐｄｅ１阻害剤 |
| US9468637B2 (en) | 2009-05-13 | 2016-10-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| JP2013507360A (ja) | 2009-10-08 | 2013-03-04 | イントラ−セルラー・セラピーズ・インコーポレイテッド | ホスホジエステラーゼ１−標的トレーサーおよび方法 |
| EP2560676B8 (en) | 2010-04-22 | 2016-10-12 | Intra-Cellular Therapies, Inc. | Organic compounds |
| TW201206937A (en) | 2010-05-31 | 2012-02-16 | Intra Cellular Therapies Inc | Organic compounds |
| WO2011153135A1 (en) | 2010-05-31 | 2011-12-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US9434730B2 (en) | 2010-05-31 | 2016-09-06 | Intra-Cellular Therapies, Inc. | PDE1 inhibitor compounds |
| US9763948B2 (en) | 2010-05-31 | 2017-09-19 | Intra-Cellular Therapies, Inc. | PDE1 inhibitory compounds and methods |
| EP2717877B1 (en) | 2011-06-10 | 2017-11-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CA2845039A1 (en) | 2011-08-18 | 2013-02-21 | Shire Ag | Combinations of a 5-ht4 receptor agonist and a pde4 inhibitor for use in therapy |
| AR091507A1 (es) * | 2012-06-21 | 2015-02-11 | Intra Cellular Therapies Inc | SALES DE (6aR,9aS)-5,6a,7,8,9,9a-HEXAHIDRO-5-METIL-3-(FENILAMINO)-2-((4-(6-FLUOROPIRIDIN-2-IL)FENIL)METIL)-CICLOPENT[4,5]IMIDAZO[1,2-a]PIRAZOLO[4,3-e]PIRIMIDIN-4(2H)-ONA |
| CA2906640C (en) | 2013-03-15 | 2021-07-20 | Intra-Cellular Therapies, Inc. | Substituted imidazo-[1,2-a]pyrazolo[4.3-e]pyrimidin-4[5h]-one compounds and pharmaceutical compositions and use therof as pde1 inhibitors |
| US9545406B2 (en) | 2013-03-15 | 2017-01-17 | Intra-Cellular Therapies, Inc. | Method of treating a CNS injury with a PDE1 inhibitor |
| WO2018049417A1 (en) | 2016-09-12 | 2018-03-15 | Intra-Cellular Therapies, Inc. | Novel uses |
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- 2014-03-17 JP JP2016503395A patent/JP2016518343A/ja not_active Withdrawn
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- 2014-03-17 ES ES14763482T patent/ES2717688T3/es active Active
- 2014-03-17 EP EP18205841.2A patent/EP3479825B1/en active Active
- 2014-03-17 ES ES18205841T patent/ES2871327T3/es active Active
- 2014-03-17 WO PCT/US2014/030412 patent/WO2014145617A2/en not_active Ceased
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