DK2155696T3 - Piperazinsalte som d3/d2-antagonister - Google Patents
Piperazinsalte som d3/d2-antagonister Download PDFInfo
- Publication number
- DK2155696T3 DK2155696T3 DK08750834.7T DK08750834T DK2155696T3 DK 2155696 T3 DK2155696 T3 DK 2155696T3 DK 08750834 T DK08750834 T DK 08750834T DK 2155696 T3 DK2155696 T3 DK 2155696T3
- Authority
- DK
- Denmark
- Prior art keywords
- dichlorophenyl
- ethyl
- dimethylcarbamoyl
- disorders
- cyclohexylamine
- Prior art date
Links
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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Otolaryngology (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Dermatology (AREA)
Claims (14)
1. Trans-4-{2-[4-(2(3-dichlorphenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl- cyciohexylamin-monohydrochlorid og/eller hydrater og/elier solvater deraf.
2. Fremgangsmåde til fremstilling af forbindelserne ifølge krav 1, hvilken fremgangsmåde er kendetegnet ved, at frans-4-{2-[4-(2,3-dichlorphenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyciohexyiamin-base suspenderes eller opløses i et passende opløsningsmiddel eller en blanding af opløsningsmidler, derefter HCI eller et salt deraf fremstillet med en base, som er en svagere base end fra/?s-4-{2-[4-(2,3-dichlorphenyl)-piperazin-1-yl]-ethy!}-N,N-dimethylcarbamoyi-cyclohexylaminen, eller en opløsning deraf tilsættes, og reaktionsbiandingen valgfrit koncentreres og/eller afkøles, derefter isoleres det opnåede produkt ved filtrering.
3. Fremgangsmåde iføige krav 2, hvor der anvendes et salt af HCI fremstillet med en base, som er svagere end fra/?s-4-{2-[4-(2,3-dichiorphenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamin-basen.
4. Farmaceutisk sammensætning, der omfatter forbindelsen ifølge krav 1 og én eller flere farmaceutisk acceptable bestanddele.
5. Forbindelse ifølge krav 1 til anvendelse ved behandling og/elier forebyggelse af lidelser, som kræver modulering afen dopaminreceptor.
6. Forbindelse til anvendelse ifølge krav 5, hvor dopaminreceptoren er dopamin Ds- og/eller dopamin Ds-receptor.
7. Forbindelse fil anvendelse ifølge krav 5, hvor lidelsen, som kræver modulering af dopaminreceptor, er valgt blandt skizofreni, skizoaffektive lidelser, skizofreniledsagende kognitiv svækkelse, milde til moderate kognitive svigt, demens, demensassocierede psykotiske tilstande, psykotisk depression, mani, paranoide og deliriske lidelser, dyskinetiske lidelser (f.eks. Parkinsons sygdom), neuroleptisk induceret parkinsonisme, depression, angst og stofmisbrug.
8. Forbindelse ifølge krav 1, der er i form af krystallinsk fra/?s-4-{2-[4-(2,3-dich!orphenyl)-piperazin-1-y!]-ethyi}-N,N-dimethyicarbarnoyl-cyclohexylamin-hydroch!orid-anhydrat (form O-
9. Krystallinsk form ifølge krav 8, hvor del infrarøde spektrum omfatter karakteristiske toppe ved 33212931, 2914, 2466, 1652, 1526, 956, 784 og 715 cnr1 ±4 cm \
10. Krystallinsk form ifølge krav 8 med et infrarødt spektrum som vist i figur 1.
11. Krystallinsk form ifølge krav 8, hvor Raman-spektret omfatter karakteristiske toppe ved 3070, 2986, 2969, 2933, 2914, 2864, 2850, 1578, 1458, 1052 og 475 cnr1 ± 4 cnr1.
12. Krystallinsk form ifølge krav 8 med et Raman-spektrum som vist i figur 2.
13. Krystallinsk form ifølge krav 8, hvor pulver-røntgendiffraktionsmønstret omfatter toppe ved 6,6, 7,3, 13,2, 14,2, 14,6, 16,9,21,1,22,4, 24,8, 26,5 og 26,6° ± 0,2 grader 2Θ.
14. Krystallinsk form ifølge krav 8 med et pulver-røntgendiffraktionsmønster som vist i figur 3.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU0700339A HU230748B1 (hu) | 2007-05-11 | 2007-05-11 | Új piperazin só és előállítási eljárása |
| PCT/HU2008/000044 WO2008139235A2 (en) | 2007-05-11 | 2008-05-13 | Novel piperazine salts as d3/d2 antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2155696T3 true DK2155696T3 (da) | 2017-07-10 |
Family
ID=89987512
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK08750834.7T DK2155696T3 (da) | 2007-05-11 | 2008-05-13 | Piperazinsalte som d3/d2-antagonister |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US7943621B2 (da) |
| EP (1) | EP2155696B1 (da) |
| JP (1) | JP2010526861A (da) |
| KR (2) | KR101668973B1 (da) |
| CN (1) | CN101679315B (da) |
| AP (1) | AP2009005012A0 (da) |
| AU (1) | AU2008249772B2 (da) |
| BR (1) | BRPI0811199A2 (da) |
| CA (1) | CA2684404C (da) |
| CO (1) | CO6241112A2 (da) |
| CY (1) | CY1119076T1 (da) |
| DK (1) | DK2155696T3 (da) |
| EA (1) | EA017270B1 (da) |
| EC (1) | ECSP099772A (da) |
| ES (1) | ES2628025T3 (da) |
| GE (1) | GEP20125522B (da) |
| HR (1) | HRP20170918T1 (da) |
| HU (2) | HU230748B1 (da) |
| IL (1) | IL201533A0 (da) |
| LT (1) | LT2155696T (da) |
| MA (1) | MA31434B1 (da) |
| MX (1) | MX2009012182A (da) |
| MY (1) | MY148078A (da) |
| NI (1) | NI200900203A (da) |
| NZ (1) | NZ580642A (da) |
| PL (1) | PL2155696T3 (da) |
| PT (1) | PT2155696T (da) |
| RS (1) | RS56036B1 (da) |
| SI (1) | SI2155696T1 (da) |
| TN (1) | TN2009000458A1 (da) |
| TW (1) | TWI424846B (da) |
| UA (1) | UA102225C2 (da) |
| WO (1) | WO2008139235A2 (da) |
| ZA (1) | ZA200907511B (da) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE033357T2 (en) * | 2007-05-11 | 2017-11-28 | Richter Gedeon Nyrt | Crystalline form of carbamoylcyclohexane derivatives |
| 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 |
| MY157192A (en) * | 2007-08-03 | 2016-05-13 | Richter Gedeon Nyrt | Pharmaceutical compositions containing dopamine receptor ligands and methods of treatment using dopamine receptor ligands |
| US7875610B2 (en) * | 2007-12-03 | 2011-01-25 | Richter Gedeon Nyrt. | Pyrimidinyl-piperazines useful as D3/D2 receptor ligands |
| KR20130115393A (ko) * | 2008-02-21 | 2013-10-21 | 미쓰비시 타나베 파마 코퍼레이션 | 경구 투여용 고형 제제 |
| AP2975A (en) | 2008-07-16 | 2014-09-30 | 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 |
| WO2014031162A1 (en) * | 2012-08-20 | 2014-02-27 | Forest Laboratories Holdings Limited | 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 |
| US20230414504A1 (en) * | 2020-08-26 | 2023-12-28 | Shanghai Bocimed Pharmaceutical Co., Ltd. | Cariprazine pharmaceutical composition, preparation method and application thereof |
| MX2024005256A (es) * | 2021-10-28 | 2024-09-06 | Abbvie Inc | Tratamiento del trastorno depresivo mayor. |
| TWI852364B (zh) | 2022-02-22 | 2024-08-11 | 大陸商上海雲晟研新生物科技有限公司 | 卡利拉嗪藥用鹽及其晶型、藥物組合物、製備方法和用途 |
| 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 PL PL08750834T patent/PL2155696T3/pl unknown
- 2008-05-13 LT LTEP08750834.7T patent/LT2155696T/lt unknown
- 2008-05-13 SI SI200831816T patent/SI2155696T1/sl unknown
- 2008-05-13 AP AP2009005012A patent/AP2009005012A0/xx unknown
- 2008-05-13 MX MX2009012182A patent/MX2009012182A/es active IP Right Grant
- 2008-05-13 ES ES08750834.7T patent/ES2628025T3/es active Active
- 2008-05-13 BR BRPI0811199-5A2A patent/BRPI0811199A2/pt active IP Right Grant
- 2008-05-13 NZ NZ580642A patent/NZ580642A/en unknown
- 2008-05-13 JP JP2010507992A patent/JP2010526861A/ja not_active Withdrawn
- 2008-05-13 CN CN2008800156277A patent/CN101679315B/zh active Active
- 2008-05-13 RS RS20170549A patent/RS56036B1/sr unknown
- 2008-05-13 GE GEAP200811599A patent/GEP20125522B/en unknown
- 2008-05-13 KR KR1020157019598A patent/KR101668973B1/ko active Active
- 2008-05-13 UA UAA200912891A patent/UA102225C2/ru unknown
- 2008-05-13 CA CA2684404A patent/CA2684404C/en not_active Expired - Fee Related
- 2008-05-13 PT PT87508347T patent/PT2155696T/pt unknown
- 2008-05-13 KR KR1020097022188A patent/KR20100018493A/ko not_active Ceased
- 2008-05-13 AU AU2008249772A patent/AU2008249772B2/en active Active
- 2008-05-13 HR HRP20170918TT patent/HRP20170918T1/hr unknown
- 2008-05-13 MY MYPI20094708A patent/MY148078A/en unknown
- 2008-05-13 DK DK08750834.7T patent/DK2155696T3/da active
- 2008-05-13 WO PCT/HU2008/000044 patent/WO2008139235A2/en not_active Ceased
- 2008-05-13 EP EP08750834.7A patent/EP2155696B1/en active Active
- 2008-05-13 HU HUE08750834A patent/HUE034796T2/en unknown
- 2008-05-13 EA EA200971046A patent/EA017270B1/ru unknown
- 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
-
2017
- 2017-05-12 CY CY20171100512T patent/CY1119076T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DK2155696T3 (da) | Piperazinsalte som d3/d2-antagonister | |
| US7705003B2 (en) | Cyclohexylamides as dopamine D3, D2 and 5-HT1A Antagonists | |
| EP1663996B1 (en) | (thio)carbamoyl-cyclohexane derivatives as d3/d2 receptor antagonists | |
| AU2008251520B2 (en) | Novel solvate and crystalline forms of carbamoyl-cyclohexane derivatives | |
| US8802672B2 (en) | Pyrimidinyl-piperazines useful as D3/D2 receptor ligands | |
| TWI445534B (zh) | 可作為ｄ3／ｄ2受體配體之嘧啶基哌嗪類化合物 | |
| EP1608635B1 (en) | Phenyl sulfone derivatives and their use in the treatment of cns disorders | |
| US20140323471A1 (en) | Polymorphic forms of ivabradine hydrochloride | |
| HK1140473B (zh) | 作为d3/d2拮抗剂的哌嗪盐 | |
| HK1114085A (en) | Cyclohexylamides as dopamine d3, d2 and 5ht1a antagonists | |
| HK1093494B (en) | (thio) carbamoyl-cyclohexane derivatives as d3/d2 receptor antagonists | |
| HUP0103099A2 (hu) | N-Szubsztituált aza-bicikloheptán-származékok, előállításuk és alkalmazásuk |