PE20191784A1 - Compuestos inhibidores de vmat2, composiciones y metodos relativos a los mismos - Google Patents
Compuestos inhibidores de vmat2, composiciones y metodos relativos a los mismosInfo
- Publication number
- PE20191784A1 PE20191784A1 PE2019002077A PE2019002077A PE20191784A1 PE 20191784 A1 PE20191784 A1 PE 20191784A1 PE 2019002077 A PE2019002077 A PE 2019002077A PE 2019002077 A PE2019002077 A PE 2019002077A PE 20191784 A1 PE20191784 A1 PE 20191784A1
- Authority
- PE
- Peru
- Prior art keywords
- compositions
- methods relating
- inhibiting compounds
- lower alkyl
- vmat2
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 230000002401 inhibitory effect Effects 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 102000009659 Vesicular Monoamine Transport Proteins Human genes 0.000 abstract 2
- 108010020033 Vesicular Monoamine Transport Proteins Proteins 0.000 abstract 2
- 150000004677 hydrates Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 1
- 230000000926 neurological effect Effects 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Referido a un compuesto de formula I, en donde R1 y R2 son independientemente alquilo inferior, cicloalquilo inferior, entre otros; R3 es alquilo inferior; y R4 es alquilo inferior o cicloalquilalquilo inferior; sales, solvatos e hidratos farmaceuticamente aceptables de los mismos. Un compuesto preferido es 3-(2,2-dimetilpropil)-9,10-dimetoxi-2-metil-1H,2H,3H,4H,6H,7H,11bH-piperazino[2,1-a]isoquinolina y sus sales, solvatos e hidratos farmaceuticamente aceptables de la misma. Estos compuestos son inhibidores del transportador vesicular de monoaminas 2 (VMAT2) y se usa en el tratamiento de enfermedades y trastornos neurologicos y psiquiatricos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762487413P | 2017-04-19 | 2017-04-19 | |
| US201862652837P | 2018-04-04 | 2018-04-04 | |
| PCT/US2018/028031 WO2018195121A1 (en) | 2017-04-19 | 2018-04-17 | Vmat2 inhibitor compounds and compositions thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20191784A1 true PE20191784A1 (es) | 2019-12-24 |
Family
ID=62111264
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019002077A PE20191784A1 (es) | 2017-04-19 | 2018-04-17 | Compuestos inhibidores de vmat2, composiciones y metodos relativos a los mismos |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US11040970B2 (es) |
| EP (1) | EP3612532B1 (es) |
| JP (1) | JP7170662B2 (es) |
| KR (1) | KR20190140968A (es) |
| CN (1) | CN110770236B (es) |
| AU (1) | AU2018254429A1 (es) |
| BR (1) | BR112019021853A2 (es) |
| CA (1) | CA3060251A1 (es) |
| CL (1) | CL2019002919A1 (es) |
| CO (1) | CO2019011604A2 (es) |
| ES (1) | ES2971230T3 (es) |
| JO (1) | JOP20190239A1 (es) |
| MA (1) | MA50145A (es) |
| MX (1) | MX2019012336A (es) |
| PE (1) | PE20191784A1 (es) |
| TW (1) | TW201841913A (es) |
| WO (1) | WO2018195121A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190108149A (ko) | 2017-01-27 | 2019-09-23 | 뉴로크린 바이오사이언시즈 인코퍼레이티드 | 특정 vmat2 억제제의 투여 방법 |
| BR112020005373A2 (pt) | 2017-09-21 | 2020-09-24 | Neurocrine Biosciences Inc. | formulação de valbenazina em alta dosagem e composições, métodos e kits relacionados com valbenazina |
| CA3077149A1 (en) | 2017-10-10 | 2019-04-18 | Neurocrine Biosciences, Inc. | Methods for the administration of (s)-2-amino-3-methyl-butyric acid (2r,3r,11br)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2yl ester and salts thereof |
| BR112020024018A2 (pt) * | 2018-06-14 | 2021-02-23 | Neurocrine Biosciences Inc. | compostos inibidores de vmat2, composições e métodos relacionados a eles |
| WO2020037022A1 (en) | 2018-08-15 | 2020-02-20 | Neurocrine Biosciences, Inc. | Methods for the administration of certain vmat2 inhibitors |
| WO2020086765A1 (en) * | 2018-10-24 | 2020-04-30 | Neurocrine Biosciences, Inc. | Processes for preparing a vmat2 inhibitor |
| IL291471B2 (en) | 2019-09-30 | 2025-04-01 | Incyte Corp | Pyrimido[3,2–D]pyrimidine compounds as immunomodulators |
| JP2023500395A (ja) | 2019-11-11 | 2023-01-05 | インサイト・コーポレイション | Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩及び結晶形態 |
| FI4168409T3 (fi) | 2021-03-22 | 2025-06-25 | Neurocrine Biosciences Inc | VMAT2:n ESTÄJIÄ JA KÄYTTÖMENETELMIÄ |
| WO2022232380A1 (en) | 2021-04-29 | 2022-11-03 | Neurocrine Biosciences, Inc. | Processes for preparing a vmat2 inhibitor |
| US20250064990A1 (en) | 2021-08-20 | 2025-02-27 | Neurocrine Biosciences, Inc. | Methods of screening for vmat2 inhibitors |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5798119A (en) | 1995-06-13 | 1998-08-25 | S. C. Johnson & Son, Inc. | Osmotic-delivery devices having vapor-permeable coatings |
| GB0106177D0 (en) | 2001-03-13 | 2001-05-02 | Hoffmann La Roche | Piperazine derivatives |
| RU2339636C2 (ru) | 2003-06-20 | 2008-11-27 | Ф.Хоффманн-Ля Рош Аг | Гексагидропиридоизохинолины в качестве ингибиторов дипептидилпептидазы iv (dpp-iv) |
| US20060035883A1 (en) | 2004-08-13 | 2006-02-16 | Tedford Clark E | Novel serotonin receptor ligands and their uses thereof |
| EA018378B1 (ru) * | 2006-11-08 | 2013-07-30 | Ньюрокрайн Байосайенсиз, Инк. | ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 3-ИЗОБУТИЛ-9,10-ДИМЕТОКСИ-1,3,4,6,7,11b-ГЕКСАГИДРО-2Н-ПИРИДО[2,1-a]ИЗОХИНОЛИН-2-ОЛА И СВЯЗАННЫЕ С НИМИ СПОСОБЫ |
| FR2912145B1 (fr) | 2007-02-02 | 2009-03-06 | Servier Lab | Nouveaux derives tricycliques,leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US9012471B2 (en) | 2008-04-11 | 2015-04-21 | The Trustees Of Columbia University In The City Of New York | Glucose metabolism modulating compounds |
| CA2972242A1 (en) | 2008-09-18 | 2010-04-22 | Auspex Pharmaceuticals, Inc. | Benzoquinoline inhibitors of vesicular monoamine transporter 2 |
| WO2011075699A2 (en) | 2009-12-18 | 2011-06-23 | Sunovion Pharmaceuticals Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| CN102285984B (zh) | 2010-11-25 | 2012-10-10 | 江苏威凯尔医药科技有限公司 | (2R,3R,11bR)-二氢丁苯那嗪及相关化合物的制备方法 |
| EP2835372B1 (en) | 2012-09-19 | 2016-05-04 | Fujian Institute Of Research On The Structure Of Matter, Chinese Academy Of Sciences | Thiophene [2, 3-d]pyrimidine derivative, and preparation method and use thereof |
| NZ723107A (en) | 2014-02-07 | 2022-11-25 | Neurocrine Biosciences Inc | Pharmaceutical compositions comprising an antipsychotic drug and a vmat2 inhibitor and uses thereof |
| ES2960717T3 (es) | 2015-02-06 | 2024-03-06 | Neurocrine Biosciences Inc | [9,10-Dimetoxi-3-(2-metilpropil)-1H,2H,3H,4H,6H,7H,11BH-pirido-[2,1-A]isoquinolin-2-il]metanol y compuestos, composiciones y métodos relacionados con el mismo |
| WO2018119266A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Benzooxazole derivatives as immunomodulators |
| CN116115764A (zh) | 2016-12-22 | 2023-05-16 | 因赛特公司 | 四氢咪唑并[4,5-c]吡啶衍生物作为pd-l1内在化诱导剂 |
-
2017
- 2017-06-16 JO JOP/2019/0239A patent/JOP20190239A1/ar unknown
-
2018
- 2018-04-17 ES ES18722357T patent/ES2971230T3/es active Active
- 2018-04-17 US US16/606,191 patent/US11040970B2/en active Active
- 2018-04-17 WO PCT/US2018/028031 patent/WO2018195121A1/en not_active Ceased
- 2018-04-17 KR KR1020197033620A patent/KR20190140968A/ko not_active Withdrawn
- 2018-04-17 CN CN201880040884.XA patent/CN110770236B/zh active Active
- 2018-04-17 MX MX2019012336A patent/MX2019012336A/es unknown
- 2018-04-17 EP EP18722357.3A patent/EP3612532B1/en active Active
- 2018-04-17 MA MA050145A patent/MA50145A/fr unknown
- 2018-04-17 PE PE2019002077A patent/PE20191784A1/es unknown
- 2018-04-17 JP JP2019556587A patent/JP7170662B2/ja active Active
- 2018-04-17 BR BR112019021853-0A patent/BR112019021853A2/pt not_active Application Discontinuation
- 2018-04-17 AU AU2018254429A patent/AU2018254429A1/en not_active Abandoned
- 2018-04-17 TW TW107112964A patent/TW201841913A/zh unknown
- 2018-04-17 CA CA3060251A patent/CA3060251A1/en active Pending
-
2019
- 2019-10-14 CL CL2019002919A patent/CL2019002919A1/es unknown
- 2019-10-18 CO CO2019011604A patent/CO2019011604A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN110770236A (zh) | 2020-02-07 |
| EP3612532A1 (en) | 2020-02-26 |
| US11040970B2 (en) | 2021-06-22 |
| KR20190140968A (ko) | 2019-12-20 |
| WO2018195121A1 (en) | 2018-10-25 |
| EP3612532C0 (en) | 2023-12-13 |
| ES2971230T3 (es) | 2024-06-04 |
| EP3612532B1 (en) | 2023-12-13 |
| TW201841913A (zh) | 2018-12-01 |
| AU2018254429A1 (en) | 2019-11-07 |
| JP7170662B2 (ja) | 2022-11-14 |
| BR112019021853A2 (pt) | 2020-05-26 |
| CL2019002919A1 (es) | 2020-01-17 |
| MA50145A (fr) | 2020-07-29 |
| CO2019011604A2 (es) | 2019-10-31 |
| US20200131173A1 (en) | 2020-04-30 |
| CN110770236B (zh) | 2023-03-24 |
| JP2020517607A (ja) | 2020-06-18 |
| MX2019012336A (es) | 2020-07-14 |
| JOP20190239A1 (ar) | 2019-10-09 |
| CA3060251A1 (en) | 2018-10-25 |
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