JP6997718B2 - 新規共結晶 - Google Patents
新規共結晶 Download PDFInfo
- Publication number
- JP6997718B2 JP6997718B2 JP2018550675A JP2018550675A JP6997718B2 JP 6997718 B2 JP6997718 B2 JP 6997718B2 JP 2018550675 A JP2018550675 A JP 2018550675A JP 2018550675 A JP2018550675 A JP 2018550675A JP 6997718 B2 JP6997718 B2 JP 6997718B2
- Authority
- JP
- Japan
- Prior art keywords
- crystal
- iti
- free base
- isonicotinamide
- nicotinamide
- 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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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/16—Peri-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
- C07D213/82—Amides; Imides in position 3
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662314339P | 2016-03-28 | 2016-03-28 | |
| US62/314,339 | 2016-03-28 | ||
| PCT/US2017/024597 WO2017172811A1 (en) | 2016-03-28 | 2017-03-28 | Novel co-crystals |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019513140A JP2019513140A (ja) | 2019-05-23 |
| JP2019513140A5 JP2019513140A5 (enExample) | 2020-04-30 |
| JP6997718B2 true JP6997718B2 (ja) | 2022-01-18 |
Family
ID=59965148
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018550675A Active JP6997718B2 (ja) | 2016-03-28 | 2017-03-28 | 新規共結晶 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US11014925B2 (enExample) |
| EP (1) | EP3436016B1 (enExample) |
| JP (1) | JP6997718B2 (enExample) |
| WO (1) | WO2017172811A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105168219B (zh) * | 2008-05-27 | 2018-11-20 | 细胞内治疗公司 | 用于睡眠障碍和其他疾病的方法和组合物 |
| EP3076967B1 (en) * | 2013-12-03 | 2021-07-28 | Intra-Cellular Therapies, Inc. | Methods for treating residual symptoms of schizophrenia |
| RU2743513C2 (ru) | 2016-01-26 | 2021-02-19 | Интра-Селлулар Терапиз, Инк. | Органические соединения |
| WO2017172784A1 (en) * | 2016-03-28 | 2017-10-05 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
| EP3497104B1 (en) | 2016-08-09 | 2021-10-06 | Teva Pharmaceuticals International GmbH | Solid state forms of lumateperone ditosylate salt |
| WO2018071233A1 (en) | 2016-10-12 | 2018-04-19 | Intra-Cellular Therapies, Inc. | Amorphous solid dispersions |
| MX387784B (es) | 2017-03-24 | 2025-03-18 | Intra Celular Therapies Inc | Composiciones novedosas y metodos. |
| CN110636845A (zh) | 2017-04-10 | 2019-12-31 | 雷迪博士实验室有限公司 | 卢美哌隆对甲苯磺酸盐的无定形形式和固体分散体 |
| CA3071137A1 (en) | 2017-07-26 | 2019-01-31 | Intra-Cellular Therapies, Inc. | Prodrugs of substituted heterocycle fused gamma-carbolines |
| JP2020535231A (ja) | 2017-09-26 | 2020-12-03 | 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. | 新規な塩および結晶 |
| CN112040940A (zh) | 2018-03-23 | 2020-12-04 | 细胞内治疗公司 | 有机化合物 |
| EP3628007B1 (en) | 2018-06-06 | 2023-05-03 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
| CA3102948A1 (en) | 2018-06-08 | 2019-12-12 | Intra-Cellular Therapies, Inc. | Novel methods |
| EP3843738A4 (en) * | 2018-08-31 | 2022-06-01 | Intra-Cellular Therapies, Inc. | NEW METHODS |
| CA3108558A1 (en) * | 2018-08-31 | 2020-03-05 | Intra-Cellular Therapies, Inc. | Novel methods |
| WO2020112941A2 (en) | 2018-11-27 | 2020-06-04 | Teva Czech Industries S.R.O | Solid state forms of lumateperone salts and processes for preparation of lumateperone and salts thereof |
| EP3898221A4 (en) | 2018-12-17 | 2022-09-14 | Intra-Cellular Therapies, Inc. | ORGANIC COMPOUND |
| MX2021007143A (es) | 2018-12-17 | 2021-08-18 | Intra Cellular Therapies Inc | Sintesis de gamma-carbolinas fusionadas con heterociclo sustituido. |
| JP7377871B2 (ja) | 2018-12-21 | 2023-11-10 | 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 |
| 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 |
| CN114072150A (zh) | 2019-07-07 | 2022-02-18 | 细胞内治疗公司 | 新方法 |
| 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 COMPOUND |
| IL300886A (en) * | 2020-09-04 | 2023-04-01 | Intra Cellular Therapies Inc | New salts, crystals and co-crystals |
| EP4352057A4 (en) * | 2021-06-07 | 2025-04-16 | Intra-Cellular Therapies, Inc. | NEW SALTS AND CRYSTALS |
| US12414948B2 (en) | 2022-05-18 | 2025-09-16 | Intra-Cellular Therapies, Inc. | Methods |
| WO2025240804A1 (en) | 2024-05-16 | 2025-11-20 | Intra-Cellular Therapies, Inc. | Novel compositions, devices and methods |
Citations (7)
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|---|---|---|---|---|
| JP2003502331A (ja) | 1999-06-15 | 2003-01-21 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | 置換複素環縮合ガンマーカルボリン |
| JP2010521464A (ja) | 2007-03-12 | 2010-06-24 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 置換ヘテロ環縮合ガンマ−カルボリンの合成 |
| JP2011513485A (ja) | 2008-03-12 | 2011-04-28 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 置換ヘテロ環縮合ガンマ−カルボリン類固体 |
| JP2011523949A (ja) | 2008-05-27 | 2011-08-25 | イントラ−セルラー・セラピーズ・インコーポレイテッド | 睡眠障害および他の障害のための方法および組成物 |
| JP2013525352A (ja) | 2010-04-22 | 2013-06-20 | 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 |
| WO2014145192A1 (en) | 2013-03-15 | 2014-09-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| WO2015085004A1 (en) | 2013-12-03 | 2015-06-11 | Intra-Cellular Therapies, Inc. | Novel methods |
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| BRPI0706523A2 (pt) | 2006-01-13 | 2011-01-04 | Wyeth Corp | composto de fórmula i; composição farmacêutica; método de tratamento de distúrbios que estão relacionados com ou são afetados pela inibição da recaptação de norepinefrina, o receptor de 5-ht6 ou o receptor de 5-ht2a; método de tratamento de um distúrbio de aprendizado, de um distúrbio cognitivo, de um distúrbio de memória, de um distúrbio de personalidade, de um distúrbio comportamental, de um distúrbio de movimento, de um distúrbio neurodegenerativo, de abstinência de droga, de distúrbio de sono, de um distúrbio alimentar, de uma toxicidade de droga aguda, de um distúrbio cardiovascular, de uma disfunção sexual, de um distúrbio gastrintestinal, de um distúrbio genitourinário, de um distúrbio de dor, de um distúrbio nervoso ou de um distúrbio de sintoma vasomotor; método de tratamento de doença de alzheimer, de um distúrbio de deficiência da atenção, de esquizofrenia, de doença de parkinson, de discinésia tardia, de ataxia, de bradicinésia, de discinésias paroxìsmicas, de sìndrome da perna irrequieta, de tremor, de tremor essencial, de epilepsia, de apoplexia ou de trauma na cabeça; método de tratamento de doença arterial coronariana, de enfarte do miocárdio, de ataque isquêmico transitório, de angina, de fibrilação atrial, de agregação plaquetária, de risco de formação de coágulo sanguìneo, de sìndrome do intestino irritável, de constipação crÈnica, de doença do refluxo gastrintestinal, de dispepsia, de incontinência urinária por estresse ou de incontinência urinária de urgência; método de tratamento de depressão, de distúrbio compulsivo obsessivo, de tendência ao suicìdio, de distúrbio de ansiedade, de distúrbio bipolar, de distúrbio de pánico, de abstinência de nicotina, de abstinência de álcool, de abstinência de cocaìna, de abstinência de heroìna, de abstinência de anfetamina, de abstinência de drogas narcóticas, de insÈnia, de apnéia do sono, de narcolepsia, de distúrbio afetivo sanzonal, de sìndrome da perna irrequieta, de distúrbio de sono de turno de trabalho, de sìndrome da fase do sono retardada, de anorexia nervosa, de bulimia nervosa, de sìndrome do comer noturno, de superalimentação compulsiva, de sìndrome da fadiga crÈnica, de fibromialgia, de neuropatia de dor, de dor antinociceptiva, de sìndrome da dor crÈnica, de neuropatia diabética, de fogacho ou de suor noturno; e uso de um composto |
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Also Published As
| Publication number | Publication date |
|---|---|
| EP3436016B1 (en) | 2022-04-27 |
| US20200017500A9 (en) | 2020-01-16 |
| EP3436016A1 (en) | 2019-02-06 |
| US20190112310A1 (en) | 2019-04-18 |
| US11014925B2 (en) | 2021-05-25 |
| JP2019513140A (ja) | 2019-05-23 |
| WO2017172811A1 (en) | 2017-10-05 |
| EP3436016A4 (en) | 2019-09-18 |
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