CO6241112A2 - Sales novedosas de piperazina como antagonistas d3/d2 - Google Patents
Sales novedosas de piperazina como antagonistas d3/d2Info
- Publication number
- CO6241112A2 CO6241112A2 CO09139912A CO09139912A CO6241112A2 CO 6241112 A2 CO6241112 A2 CO 6241112A2 CO 09139912 A CO09139912 A CO 09139912A CO 09139912 A CO09139912 A CO 09139912A CO 6241112 A2 CO6241112 A2 CO 6241112A2
- Authority
- CO
- Colombia
- Prior art keywords
- dimethylcarbamoyl
- cyclohexylamine
- piperazin
- dichlorophenyl
- trans
- Prior art date
Links
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical class C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 2
- 239000005557 antagonist Substances 0.000 title 1
- GIAOVZPOOUDJDR-UHFFFAOYSA-N 4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]-1-(dimethylamino)cyclohexane-1-carboxamide Chemical compound C1CC(N(C)C)(C(N)=O)CCC1CCN1CCN(C=2C(=C(Cl)C=CC=2)Cl)CC1 GIAOVZPOOUDJDR-UHFFFAOYSA-N 0.000 abstract 6
- 150000004677 hydrates Chemical class 0.000 abstract 6
- 239000012453 solvate Substances 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000002904 solvent Substances 0.000 abstract 2
- -1 2,3-dichlorophenyl Chemical group 0.000 abstract 1
- PZWXYRDNQYUIIU-UHFFFAOYSA-N 3-cyclohexyl-1,1-dimethylurea Chemical compound CN(C)C(=O)NC1CCCCC1 PZWXYRDNQYUIIU-UHFFFAOYSA-N 0.000 abstract 1
- 102000015554 Dopamine receptor Human genes 0.000 abstract 1
- 108050004812 Dopamine receptor Proteins 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000001914 filtration Methods 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 239000011541 reaction mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Otolaryngology (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Addiction (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Dermatology (AREA)
Abstract
1.- Monoclorhidrato de trans 4- {2-[4-(2,3-diclorofenil)-piperazin-1-il]-etil}-N,N-dimetilcarbamoil-ciclohexilamina y/o hidratos y/o solvatos del mismo. 2.- Monoclorhidrato de trans 4- {2-[4-(2,3-diclorofenil)-piperazin-1-il]-etil}-N,N-dimetilcarbamoil-ciclohexilamina y/o hidratos y/o solvatos del mismo. 3.- Monobromhidrato de trans 4-{2-[4-(2,3-diclorofenil)-piperazin-1-il]-etil}-N,N-dimetilcarbamoil-ciclohexilamina y/o hidratos y/o solvatos del mismo. 4.- Maleato de trans 4-{2-[4-(2,3-diclorofenil)-piperazin-1-iI]-etil}-N,N-dimetilcarbamoil-ciclohexilamina y/o hidratos y/o solvatos del mismo. 5.- Metanosulfonato de trans 4-{2-[4-(2,3-diclorofenil)-piperazin-1-il]-etil}-N,N-dimetilcarbamoil-ciclohexilamina y/o hidratos y/o solvatos del mismo. 6.- Procedimiento para la preparación de los compuestos de las reivindicaciones 1-5, caracterizado porque la base trans 4-{2-[4-(2,3-diclorofenil)-piperazin-1-il]-etil}-N,N-dimetilcarbamoil-ciclohexilamina se disuelve o suspende en un disolvente o mezcla de disolventes adecuados y, a continuación, se adiciona un ácido, o una sal del mismo preparada con una base más débil que la trans 4-{2-[4-(2,3-diclorofenil)-piperazin-1-il]-etil}-N,N-dimetilcarbamoil-ciclohexilamina, o una disolución de la misma, y, opcionalmente, la mezcla de reacción se concentra y/o enfría y, a continuación, el producto obtenido se aísla mediante filtración. 7.- Una composición farmacéutica que comprende un compuesto según una cualquiera de las reivindicaciones 1-5 y uno o más ingredientes farmacéuticamente aceptables. 8.- Uso de un compuesto según una cualquiera de las reivindicaciones 1-5 y/o hidratos y/o solvatos del mismo para la fabricación de un medicamento para el tratamiento y/o prevención de trastornos que requieren la modulación de un receptor de dopamina.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU0700339A HU230748B1 (hu) | 2007-05-11 | 2007-05-11 | Új piperazin só és előállítási eljárása |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6241112A2 true CO6241112A2 (es) | 2011-01-20 |
Family
ID=89987512
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO09139912A CO6241112A2 (es) | 2007-05-11 | 2009-12-07 | Sales novedosas de piperazina como antagonistas d3/d2 |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US7943621B2 (es) |
| EP (1) | EP2155696B1 (es) |
| JP (1) | JP2010526861A (es) |
| KR (2) | KR20100018493A (es) |
| CN (1) | CN101679315B (es) |
| AP (1) | AP2009005012A0 (es) |
| AU (1) | AU2008249772B2 (es) |
| BR (1) | BRPI0811199A2 (es) |
| CA (1) | CA2684404C (es) |
| CO (1) | CO6241112A2 (es) |
| CY (1) | CY1119076T1 (es) |
| DK (1) | DK2155696T3 (es) |
| EA (1) | EA017270B1 (es) |
| EC (1) | ECSP099772A (es) |
| ES (1) | ES2628025T3 (es) |
| GE (1) | GEP20125522B (es) |
| HK (1) | HK1140473A1 (es) |
| HR (1) | HRP20170918T1 (es) |
| HU (2) | HU230748B1 (es) |
| IL (1) | IL201533A0 (es) |
| LT (1) | LT2155696T (es) |
| MA (1) | MA31434B1 (es) |
| MX (1) | MX2009012182A (es) |
| MY (1) | MY148078A (es) |
| NI (1) | NI200900203A (es) |
| NZ (1) | NZ580642A (es) |
| PL (1) | PL2155696T3 (es) |
| PT (1) | PT2155696T (es) |
| RS (1) | RS56036B1 (es) |
| SI (1) | SI2155696T1 (es) |
| TN (1) | TN2009000458A1 (es) |
| TW (1) | TWI424846B (es) |
| UA (1) | UA102225C2 (es) |
| WO (1) | WO2008139235A2 (es) |
| ZA (1) | ZA200907511B (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA017732B1 (ru) * | 2007-05-11 | 2013-02-28 | Рихтер Гедеон Нирт. | Сольватная и кристаллическая формы гидрохлорида транс-1{4-[2-[4-(2,3-дихлорфенил)пиперазин-1-ил]этил]циклогексил}-3,3-диметилмочевины, способы их получения и их применение в фармацевтических композициях и способах лечения состояний, для которых необходима модуляция дофаминовых рецепторов |
| HUP0700353A2 (en) | 2007-05-18 | 2008-12-29 | Richter Gedeon Nyrt | Metabolites of (thio)carbamoyl-cyclohexane derivatives |
| HUP0700369A2 (en) | 2007-05-24 | 2009-04-28 | Richter Gedeon Nyrt | Use of (thio)-carbamoyl-cyclohexane derivatives in the manufacture of a medicament for the treatment in the manufacture of a medicament for the treatment of schizophrenia |
| EA018064B1 (ru) * | 2007-08-03 | 2013-05-30 | Рихтер Гедеон Нирт. | Способ лечения депрессии |
| US7875610B2 (en) * | 2007-12-03 | 2011-01-25 | Richter Gedeon Nyrt. | Pyrimidinyl-piperazines useful as D3/D2 receptor ligands |
| EA023972B1 (ru) * | 2008-02-21 | 2016-08-31 | Рихтер Гедеон Нирт. | Стабильный твёрдый препарат карипразина для перорального введения и способ его получения |
| MY156288A (en) | 2008-07-16 | 2016-01-29 | Richter Gedeon Nyrt | Pharmaceutical formulations containing dopamine receptor ligands. |
| HU230067B1 (hu) | 2008-12-17 | 2015-06-29 | Richter Gedeon Nyrt | Új piperazin só és eljárás előállítására |
| HUP0800766A2 (en) | 2008-12-18 | 2010-11-29 | Richter Gedeon Vegyeszet | Process for the preparation of piperazine derivatives |
| HUP0800765A2 (en) | 2008-12-18 | 2010-11-29 | Richter Gedeon Nyrt | A new process for the preparation of piperazine derivatives and their hydrochloric salts |
| US8912197B2 (en) | 2012-08-20 | 2014-12-16 | Forest Laboratories Holdings Ltd. | Crystalline form of carbamoyl-cyclohexane derivatives |
| HU231227B1 (hu) | 2012-11-29 | 2022-03-28 | Richter Gedeon Nyrt. | Transz-4-{2-[4-(2,3-diklórfenil)-piperazin-1-il]-etil}N,N-dimetilkarbamoil-ciklohexilamin skizofrénia negatív tüneteinek kezelésére |
| CN105218484B (zh) * | 2015-09-14 | 2018-02-23 | 安徽省逸欣铭医药科技有限公司 | 酒石酸卡利拉嗪及其制备方法和医药用途 |
| CN106543105B (zh) * | 2015-09-22 | 2019-10-11 | 江苏恩华药业股份有限公司 | 一种盐酸卡利拉嗪晶型ⅳ及其制备方法 |
| US11274087B2 (en) | 2016-07-08 | 2022-03-15 | Richter Gedeon Nyrt. | Industrial process for the preparation of cariprazine |
| WO2018229794A1 (en) | 2017-06-13 | 2018-12-20 | Cipla Limited | Amorphous form of cariprazine |
| WO2019016828A1 (en) * | 2017-07-15 | 2019-01-24 | Msn Laboratories Private Limited, R&D Center | NOVEL PROCESSES FOR THE PREPARATION OF TRANS-N- {4- [2- [4- (2,3-DICHLOROPHENYL) PIPERAZIN-1-YL] ETHYL] CYCLOHEXYL} -N ', N'-DIMETHYLUMED HYDROCHLORIDE AND POLYMORPHS THIS ONE |
| WO2020056929A1 (zh) * | 2018-09-21 | 2020-03-26 | 上海诚妙医药科技有限公司 | 卡利拉嗪盐酸盐的新晶型及其制备方法及其用途 |
| HU231500B1 (hu) | 2019-04-10 | 2024-04-28 | Richter Gedeon Nyrt | Karbamoil-ciklohexán származékok autizmus spektrum betegség kezelésére |
| US11547707B2 (en) | 2019-04-10 | 2023-01-10 | Richter Gedeon Nyrt. | Carbamoyl cyclohexane derivatives for treating autism spectrum disorder |
| JP2023540056A (ja) | 2020-08-26 | 2023-09-21 | 上海雲晟研新生物科技有限公司 | カリプラジン薬用塩及びその結晶形、製造方法及び応用 |
| WO2023077094A1 (en) * | 2021-10-28 | 2023-05-04 | Abbvie Inc. | Treatment of major depressive disorder |
| WO2024072930A1 (en) * | 2022-09-30 | 2024-04-04 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Dopamine d3/d2 receptor partial agonists for the treatment of neuropsychiatric disorders |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU227543B1 (en) * | 2001-09-28 | 2011-08-29 | Richter Gedeon Nyrt | N-[4-(2-piperazin- and 2-piperidin-1-yl-ethyl)-cyclohexyl]-sulfon- and sulfamides, process for their preparation, their use and pharmaceutical compositions containing them |
| HU227534B1 (en) * | 2003-08-04 | 2011-08-29 | Richter Gedeon Nyrt | (thio)carbamoyl-cyclohexane derivatives, process for producing them and pharmaceutical compositions containing them |
| HUP0500170A3 (en) * | 2005-02-03 | 2007-11-28 | Richter Gedeon Nyrt | Piperazine derivatives, process for producing them and pharmaceutical compositions containing them |
-
2007
- 2007-05-11 HU HU0700339A patent/HU230748B1/hu not_active IP Right Cessation
-
2008
- 2008-05-09 US US12/118,437 patent/US7943621B2/en active Active
- 2008-05-13 BR BRPI0811199-5A2A patent/BRPI0811199A2/pt not_active Application Discontinuation
- 2008-05-13 KR KR1020097022188A patent/KR20100018493A/ko active Application Filing
- 2008-05-13 KR KR1020157019598A patent/KR101668973B1/ko active IP Right Grant
- 2008-05-13 CN CN2008800156277A patent/CN101679315B/zh active Active
- 2008-05-13 NZ NZ580642A patent/NZ580642A/en unknown
- 2008-05-13 GE GEAP200811599A patent/GEP20125522B/en unknown
- 2008-05-13 DK DK08750834.7T patent/DK2155696T3/en active
- 2008-05-13 PL PL08750834T patent/PL2155696T3/pl unknown
- 2008-05-13 JP JP2010507992A patent/JP2010526861A/ja not_active Withdrawn
- 2008-05-13 EP EP08750834.7A patent/EP2155696B1/en active Active
- 2008-05-13 AP AP2009005012A patent/AP2009005012A0/xx unknown
- 2008-05-13 EA EA200971046A patent/EA017270B1/ru unknown
- 2008-05-13 ES ES08750834.7T patent/ES2628025T3/es active Active
- 2008-05-13 MY MYPI20094708A patent/MY148078A/en unknown
- 2008-05-13 SI SI200831816T patent/SI2155696T1/sl unknown
- 2008-05-13 HU HUE08750834A patent/HUE034796T2/en unknown
- 2008-05-13 RS RS20170549A patent/RS56036B1/sr unknown
- 2008-05-13 CA CA2684404A patent/CA2684404C/en not_active Expired - Fee Related
- 2008-05-13 LT LTEP08750834.7T patent/LT2155696T/lt unknown
- 2008-05-13 AU AU2008249772A patent/AU2008249772B2/en active Active
- 2008-05-13 PT PT87508347T patent/PT2155696T/pt unknown
- 2008-05-13 WO PCT/HU2008/000044 patent/WO2008139235A2/en active Application Filing
- 2008-05-13 UA UAA200912891A patent/UA102225C2/ru unknown
- 2008-05-13 MX MX2009012182A patent/MX2009012182A/es active IP Right Grant
- 2008-07-08 TW TW097125707A patent/TWI424846B/zh active
-
2009
- 2009-10-15 IL IL201533A patent/IL201533A0/en active IP Right Grant
- 2009-10-26 ZA ZA200907511A patent/ZA200907511B/xx unknown
- 2009-10-30 TN TNP2009000458A patent/TN2009000458A1/fr unknown
- 2009-11-09 NI NI200900203A patent/NI200900203A/es unknown
- 2009-11-30 EC EC2009009772A patent/ECSP099772A/es unknown
- 2009-12-07 CO CO09139912A patent/CO6241112A2/es not_active Application Discontinuation
- 2009-12-07 MA MA32405A patent/MA31434B1/fr unknown
-
2010
- 2010-07-08 HK HK10106638.3A patent/HK1140473A1/xx unknown
-
2017
- 2017-05-12 CY CY20171100512T patent/CY1119076T1/el unknown
- 2017-06-16 HR HRP20170918TT patent/HRP20170918T1/hr unknown
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