JP2020528431A5 - - Google Patents
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- JP2020528431A5 JP2020528431A5 JP2020503842A JP2020503842A JP2020528431A5 JP 2020528431 A5 JP2020528431 A5 JP 2020528431A5 JP 2020503842 A JP2020503842 A JP 2020503842A JP 2020503842 A JP2020503842 A JP 2020503842A JP 2020528431 A5 JP2020528431 A5 JP 2020528431A5
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- Prior art keywords
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- 125000000217 alkyl group Chemical group 0.000 claims description 39
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 29
- 208000035475 disorder Diseases 0.000 claims description 27
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims description 17
- 150000001875 compounds Chemical class 0.000 claims description 14
- 208000030459 obsessive-compulsive personality disease Diseases 0.000 claims description 14
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims description 12
- 208000002193 Pain Diseases 0.000 claims description 12
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims description 12
- 150000003839 salts Chemical group 0.000 claims description 10
- 208000015114 central nervous system disease Diseases 0.000 claims description 9
- 238000011282 treatment Methods 0.000 claims description 9
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims description 6
- -1 NH 2 Inorganic materials 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims description 6
- 229940127240 opiate Drugs 0.000 claims description 6
- 208000019901 Anxiety disease Diseases 0.000 claims description 5
- 208000019454 Feeding and Eating disease Diseases 0.000 claims description 5
- 208000018460 Feeding disease Diseases 0.000 claims description 5
- 208000030990 Impulse-control disease Diseases 0.000 claims description 5
- 206010034158 Pathological gambling Diseases 0.000 claims description 5
- 206010034912 Phobia Diseases 0.000 claims description 5
- 208000028017 Psychotic disease Diseases 0.000 claims description 5
- 206010041250 Social phobia Diseases 0.000 claims description 5
- 230000000694 effects Effects 0.000 claims description 5
- 230000003370 grooming effect Effects 0.000 claims description 5
- 230000002969 morbid Effects 0.000 claims description 5
- 208000019906 panic disease Diseases 0.000 claims description 5
- 208000019899 phobic disease Diseases 0.000 claims description 5
- 208000026331 Disruptive, Impulse Control, and Conduct disease Diseases 0.000 claims description 4
- 229940121991 Serotonin and norepinephrine reuptake inhibitor Drugs 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000011159 matrix material Substances 0.000 claims description 4
- 230000000877 morphologic effect Effects 0.000 claims description 4
- 229920000642 polymer Polymers 0.000 claims description 4
- 239000003775 serotonin noradrenalin reuptake inhibitor Substances 0.000 claims description 4
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 3
- 208000007848 Alcoholism Diseases 0.000 claims description 3
- 208000029197 Amphetamine-Related disease Diseases 0.000 claims description 3
- 208000000094 Chronic Pain Diseases 0.000 claims description 3
- 208000022497 Cocaine-Related disease Diseases 0.000 claims description 3
- 208000001640 Fibromyalgia Diseases 0.000 claims description 3
- 206010019233 Headaches Diseases 0.000 claims description 3
- 208000012488 Opiate Overdose Diseases 0.000 claims description 3
- 208000026251 Opioid-Related disease Diseases 0.000 claims description 3
- 208000027520 Somatoform disease Diseases 0.000 claims description 3
- 239000000556 agonist Substances 0.000 claims description 3
- 201000007930 alcohol dependence Diseases 0.000 claims description 3
- 125000003342 alkenyl group Chemical group 0.000 claims description 3
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 125000000304 alkynyl group Chemical group 0.000 claims description 3
- 125000003118 aryl group Chemical group 0.000 claims description 3
- 201000006145 cocaine dependence Diseases 0.000 claims description 3
- 206010013663 drug dependence Diseases 0.000 claims description 3
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 3
- 206010016256 fatigue Diseases 0.000 claims description 3
- 231100000869 headache Toxicity 0.000 claims description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 3
- 201000001119 neuropathy Diseases 0.000 claims description 3
- 230000007823 neuropathy Effects 0.000 claims description 3
- 201000005040 opiate dependence Diseases 0.000 claims description 3
- 208000027753 pain disease Diseases 0.000 claims description 3
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 3
- 229920006395 saturated elastomer Polymers 0.000 claims description 3
- GJJFMKBJSRMPLA-HIFRSBDPSA-N (1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenyl-1-cyclopropanecarboxamide Chemical compound C=1C=CC=CC=1[C@@]1(C(=O)N(CC)CC)C[C@@H]1CN GJJFMKBJSRMPLA-HIFRSBDPSA-N 0.000 claims description 2
- ZEUITGRIYCTCEM-KRWDZBQOSA-N (S)-duloxetine Chemical compound C1([C@@H](OC=2C3=CC=CC=C3C=CC=2)CCNC)=CC=CS1 ZEUITGRIYCTCEM-KRWDZBQOSA-N 0.000 claims description 2
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 claims description 2
- GDLIGKIOYRNHDA-UHFFFAOYSA-N Clomipramine Chemical compound C1CC2=CC=C(Cl)C=C2N(CCCN(C)C)C2=CC=CC=C21 GDLIGKIOYRNHDA-UHFFFAOYSA-N 0.000 claims description 2
- 208000012902 Nervous system disease Diseases 0.000 claims description 2
- 102000048266 Nociceptin Human genes 0.000 claims description 2
- 108090000622 Nociceptin Proteins 0.000 claims description 2
- 239000005557 antagonist Substances 0.000 claims description 2
- 239000000164 antipsychotic agent Substances 0.000 claims description 2
- 229960002430 atomoxetine Drugs 0.000 claims description 2
- VHGCDTVCOLNTBX-QGZVFWFLSA-N atomoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=CC=C1C VHGCDTVCOLNTBX-QGZVFWFLSA-N 0.000 claims description 2
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 claims description 2
- 229960001736 buprenorphine Drugs 0.000 claims description 2
- 229960004606 clomipramine Drugs 0.000 claims description 2
- 229920001577 copolymer Polymers 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 229960002866 duloxetine Drugs 0.000 claims description 2
- 229960001797 methadone Drugs 0.000 claims description 2
- 239000004005 microsphere Substances 0.000 claims description 2
- 229960000600 milnacipran Drugs 0.000 claims description 2
- UZHSEJADLWPNLE-GRGSLBFTSA-N naloxone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(O)C2=C5[C@@]13CCN4CC=C UZHSEJADLWPNLE-GRGSLBFTSA-N 0.000 claims description 2
- 229960004127 naloxone Drugs 0.000 claims description 2
- DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 claims description 2
- 229960003086 naltrexone Drugs 0.000 claims description 2
- PULGYDLMFSFVBL-SMFNREODSA-N nociceptin Chemical compound C([C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(O)=O)[C@@H](C)O)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 PULGYDLMFSFVBL-SMFNREODSA-N 0.000 claims description 2
- 229960005017 olanzapine Drugs 0.000 claims description 2
- KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims description 2
- 239000004031 partial agonist Substances 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 238000011321 prophylaxis Methods 0.000 claims description 2
- 229960004431 quetiapine Drugs 0.000 claims description 2
- URKOMYMAXPYINW-UHFFFAOYSA-N quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 claims description 2
- 229960001534 risperidone Drugs 0.000 claims description 2
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims description 2
- UNAANXDKBXWMLN-UHFFFAOYSA-N sibutramine Chemical compound C=1C=C(Cl)C=CC=1C1(C(N(C)C)CC(C)C)CCC1 UNAANXDKBXWMLN-UHFFFAOYSA-N 0.000 claims description 2
- 229960004425 sibutramine Drugs 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 20
- 229940079593 drug Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 description 21
- 0 Fc1ccc(*CCCN2C[C@]3c(cccc4*C(C5)=I)c4N5[C@@]3CC2)cc1 Chemical compound Fc1ccc(*CCCN2C[C@]3c(cccc4*C(C5)=I)c4N5[C@@]3CC2)cc1 0.000 description 2
- 241000700159 Rattus Species 0.000 description 2
- 230000007812 deficiency Effects 0.000 description 2
- 230000004199 lung function Effects 0.000 description 2
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 description 2
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- AHOUBRCZNHFOSL-YOEHRIQHSA-N (+)-Casbol Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-YOEHRIQHSA-N 0.000 description 1
- WSEQXVZVJXJVFP-HXUWFJFHSA-N (R)-citalopram Chemical compound C1([C@@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 WSEQXVZVJXJVFP-HXUWFJFHSA-N 0.000 description 1
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 description 1
- 206010061619 Deformity Diseases 0.000 description 1
- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 description 1
- 229940005529 antipsychotics Drugs 0.000 description 1
- 229960001653 citalopram Drugs 0.000 description 1
- 229960002464 fluoxetine Drugs 0.000 description 1
- 229960004038 fluvoxamine Drugs 0.000 description 1
- CJOFXWAVKWHTFT-XSFVSMFZSA-N fluvoxamine Chemical compound COCCCC\C(=N/OCCN)C1=CC=C(C(F)(F)F)C=C1 CJOFXWAVKWHTFT-XSFVSMFZSA-N 0.000 description 1
- 208000013403 hyperactivity Diseases 0.000 description 1
- 229940125425 inverse agonist Drugs 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 229960002296 paroxetine Drugs 0.000 description 1
- 230000036387 respiratory rate Effects 0.000 description 1
- 229960002073 sertraline Drugs 0.000 description 1
- VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000009423 ventilation Methods 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762537287P | 2017-07-26 | 2017-07-26 | |
| US62/537,287 | 2017-07-26 | ||
| US201862639244P | 2018-03-06 | 2018-03-06 | |
| US62/639,244 | 2018-03-06 | ||
| US201862682546P | 2018-06-08 | 2018-06-08 | |
| US62/682,546 | 2018-06-08 | ||
| PCT/US2018/043100 WO2019023062A1 (en) | 2017-07-26 | 2018-07-20 | ORGANIC COMPOUNDS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020528431A JP2020528431A (ja) | 2020-09-24 |
| JP2020528431A5 true JP2020528431A5 (https=) | 2021-08-26 |
| JP7223742B2 JP7223742B2 (ja) | 2023-02-16 |
Family
ID=65040269
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020503842A Active JP7223742B2 (ja) | 2017-07-26 | 2018-07-20 | 有機化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US11376249B2 (https=) |
| EP (1) | EP3658145A4 (https=) |
| JP (1) | JP7223742B2 (https=) |
| KR (1) | KR102899502B1 (https=) |
| CN (1) | CN111093665A (https=) |
| AU (2) | AU2018307479B2 (https=) |
| BR (1) | BR112020001666A2 (https=) |
| CA (1) | CA3071119A1 (https=) |
| IL (1) | IL272249B2 (https=) |
| MX (1) | MX2020000968A (https=) |
| WO (1) | WO2019023062A1 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20140146192A (ko) | 2012-04-14 | 2014-12-24 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| PL3838274T3 (pl) * | 2016-01-26 | 2024-04-02 | Intra-Cellular Therapies, Inc. | Pochodna pirydo[3',4':4,5]pirolo[1,2,3-DE]chinoksaliny do zastosowania w leczeniu zaburzeń OUN |
| DK3407889T3 (da) | 2016-03-25 | 2021-08-09 | Intra Cellular Therapies Inc | Organiske forbindelser og deres anvendelse til behandling og forebyggelse af lidelser i centralnervesystemet |
| EP3525763B1 (en) | 2016-10-12 | 2025-03-05 | Intra-Cellular Therapies, Inc. | Amorphous solid dispersions |
| RU2767410C2 (ru) | 2017-03-24 | 2022-03-17 | Интра-Селлулар Терапиз, Инк. | Новые композиции и способы |
| EP3658144B1 (en) | 2017-07-26 | 2022-01-26 | Intra-Cellular Therapies, Inc. | Pyridopyrroloquinoxaline compounds, their compositions and uses in therapy |
| US11440911B2 (en) | 2017-09-26 | 2022-09-13 | Intra-Cellular Therapies, Inc. | Salts and crystals |
| WO2019178484A1 (en) | 2018-03-16 | 2019-09-19 | Intra-Cellular Therapies, Inc. | Novel methods |
| CN112040940A (zh) | 2018-03-23 | 2020-12-04 | 细胞内治疗公司 | 有机化合物 |
| EP3801527B1 (en) | 2018-06-08 | 2025-02-19 | Intra-Cellular Therapies, Inc. | Fused gamma-carbolines for acute treatment of anxiety or depression |
| WO2020047408A1 (en) | 2018-08-31 | 2020-03-05 | Intra-Cellular Therapies, Inc. | Novel methods |
| BR112021003655A2 (pt) * | 2018-08-31 | 2021-05-18 | Intra-Cellular Therapies, Inc. | métodos novos |
| WO2020131899A1 (en) | 2018-12-17 | 2020-06-25 | Intra-Cellular Therapies, Inc. | Organic compound |
| IL315005B2 (en) | 2018-12-17 | 2026-04-01 | Intra Cellular Therapies Inc | Synthesis of condensed gamma-carbolines and converted heterocycles |
| JP7520013B2 (ja) | 2018-12-17 | 2024-07-22 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 置換複素環縮合γ－カルボリンの合成 |
| JP7649743B2 (ja) | 2018-12-21 | 2025-03-21 | 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 |
| US12195463B2 (en) | 2018-12-21 | 2025-01-14 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN118105390A (zh) * | 2019-01-23 | 2024-05-31 | 细胞内治疗公司 | 治疗成瘾的方法 |
| CA3134674A1 (en) * | 2019-04-04 | 2020-10-08 | Intra-Cellular Therapies, Inc. | Methods of treating neuropathic pain |
| WO2021007245A1 (en) | 2019-07-07 | 2021-01-14 | Intra-Cellular Therapies, Inc. | Novel methods |
| US12478623B2 (en) | 2019-09-25 | 2025-11-25 | Intra-Cellular Therapies, Inc. | Methods of treating central nervous system disorders comprising administering lumateperone and a nitric oxide donor |
| EP4072554A4 (en) | 2019-12-11 | 2023-12-20 | Intra-Cellular Therapies, Inc. | ORGANIC CONNECTION |
| WO2022132182A1 (en) * | 2020-12-18 | 2022-06-23 | Hung, Shu-Mei | Feed pipe height adjustment mechanism for livestock feeding systems |
| MX2024004725A (es) * | 2021-10-19 | 2024-05-10 | Intra Cellular Therapies Inc | Metodos novedosos. |
| US12414948B2 (en) | 2022-05-18 | 2025-09-16 | Intra-Cellular Therapies, Inc. | Methods |
| WO2024145659A1 (en) * | 2022-12-30 | 2024-07-04 | Intra-Cellular Therapies, Inc. | Heterocycle fused gamma-carbolines acting on the serotonine 5-ht2a receptor |
| WO2025257090A1 (en) | 2024-06-10 | 2025-12-18 | Interquim, S.A. | Process for the preparation of synthesis intermediates of lumateperone and lumateperone analogues |
| WO2026011138A1 (en) * | 2024-07-03 | 2026-01-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
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-
2018
- 2018-07-20 WO PCT/US2018/043100 patent/WO2019023062A1/en not_active Ceased
- 2018-07-20 EP EP18838429.1A patent/EP3658145A4/en active Pending
- 2018-07-20 MX MX2020000968A patent/MX2020000968A/es unknown
- 2018-07-20 CN CN201880057546.7A patent/CN111093665A/zh active Pending
- 2018-07-20 CA CA3071119A patent/CA3071119A1/en active Pending
- 2018-07-20 KR KR1020207005454A patent/KR102899502B1/ko active Active
- 2018-07-20 IL IL272249A patent/IL272249B2/en unknown
- 2018-07-20 BR BR112020001666-7A patent/BR112020001666A2/pt not_active Application Discontinuation
- 2018-07-20 AU AU2018307479A patent/AU2018307479B2/en active Active
- 2018-07-20 JP JP2020503842A patent/JP7223742B2/ja active Active
- 2018-07-20 US US16/634,055 patent/US11376249B2/en active Active
-
2022
- 2022-06-03 US US17/832,282 patent/US20220296591A1/en active Pending
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2024
- 2024-09-17 AU AU2024219805A patent/AU2024219805A1/en active Pending
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