BRPI0518465A2 - composto, mÉtodo para a preparaÇço de composto, composiÇço farmacÊutica, mÉtodo de preparar uma composiÇço, e, uso de um composto - Google Patents
composto, mÉtodo para a preparaÇço de composto, composiÇço farmacÊutica, mÉtodo de preparar uma composiÇço, e, uso de um compostoInfo
- Publication number
- BRPI0518465A2 BRPI0518465A2 BRPI0518465-7A BRPI0518465A BRPI0518465A2 BR PI0518465 A2 BRPI0518465 A2 BR PI0518465A2 BR PI0518465 A BRPI0518465 A BR PI0518465A BR PI0518465 A2 BRPI0518465 A2 BR PI0518465A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- alkyl
- hydrogen
- preparing
- tetrahydropyridin
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 8
- 238000000034 method Methods 0.000 title abstract 5
- 239000000203 mixture Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- XUDGCZURHPXFLU-UHFFFAOYSA-N 2-(1,2,3,4-tetrahydropyridin-4-yl)-1h-indole Chemical class C1=CNCCC1C1=CC2=CC=CC=C2N1 XUDGCZURHPXFLU-UHFFFAOYSA-N 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 abstract 2
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102000004980 Dopamine D2 Receptors Human genes 0.000 abstract 1
- 108090001111 Dopamine D2 Receptors Proteins 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000009286 beneficial effect Effects 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000009977 dual effect Effects 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 229940076279 serotonin Drugs 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
- 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
- A61P25/22—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
COMPOSTO, MÉTODO PARA A PREPARAÇçO DE COMPOSTO, COMPOSIÇçO FARMACÊUTICA, MÉTODO DE PREPARAR UMA COMPOSIÇçO, E, USO DE UM COMPOSTO. A presente invenção diz respeito a um grupo de novos tetraidropiridin-4-il indóis com um modo duplo de ação: inibição da reabsorção de serotonina e afinidade para receptores de dopamina-D2, a métodos para a preparação destes compostos e a novos intermediários úteis para a síntese dos ditos tetraidropiridin-4-il indóis. A invenção também diz respeito ao uso de um composto divulgado neste para a fabricação de uma droga que dá um efeito benéfico. A invenção diz respeito a novos tetraidropiridin-4-il indóis da fórmula (1) e tautômeros, estereoisômeros, pró-drogas, N-óxidos, sais, hidratos e solvatos farmaceuticamente aceitáveis do mesmo, em que: - R~ 1~ é hidrogênio, halogênio, alquila (C~ 1-3~) ou alcóxi (C~ 1-3~), CN ou CF~ 3~, - R~ 2~ é hidrogênio ou alquila (C~ 1-3~), R~ 3~ é hidrogênio ou alquila (C~ 1-3~ ), - Z é hidrogênio ou alquila (C~ 1-3~), alcóxi (C~ 1-3~) ou alquiltio (C~ 1-3~), - A é hidrogênio ou alquila (C~ 1-3~) ou - A e Z juntos formam um anel de 5 ou 6 membros saturado ou (parcialmente) insaturado que pode ser substituído com halogênio, alquila (C~ 1-3~) ou fenila, em que o anel Z representas carbono, enxofre ou nitrogênio.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04106351 | 2004-12-07 | ||
| PCT/EP2005/056501 WO2006061373A2 (en) | 2004-12-07 | 2005-12-06 | Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-d2 receptors and serotonin reuptake sites |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0518465A2 true BRPI0518465A2 (pt) | 2008-11-18 |
Family
ID=34930005
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0518465-7A BRPI0518465A2 (pt) | 2004-12-07 | 2005-12-06 | composto, mÉtodo para a preparaÇço de composto, composiÇço farmacÊutica, mÉtodo de preparar uma composiÇço, e, uso de um composto |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1828168A2 (pt) |
| JP (1) | JP2008523027A (pt) |
| KR (1) | KR20070091009A (pt) |
| CN (1) | CN101072770A (pt) |
| AR (1) | AR052146A1 (pt) |
| AU (1) | AU2005313387A1 (pt) |
| BR (1) | BRPI0518465A2 (pt) |
| CA (1) | CA2587936A1 (pt) |
| MX (1) | MX2007006757A (pt) |
| RU (1) | RU2007125692A (pt) |
| SA (1) | SA05260388B1 (pt) |
| TW (1) | TW200626575A (pt) |
| WO (1) | WO2006061373A2 (pt) |
| ZA (1) | ZA200704155B (pt) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009116071A2 (en) * | 2008-02-05 | 2009-09-24 | Watson Pharma Private Limited | An improved process for preparation of paliperidone |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8900382D0 (en) * | 1989-01-09 | 1989-03-08 | Janssen Pharmaceutica Nv | 2-aminopyrimidinone derivatives |
| CA2373855A1 (en) * | 1999-05-12 | 2000-11-23 | Solvay Pharmaceuticals B.V. | Method of treating psychotic disorders |
| AU2003257407A1 (en) * | 2002-08-29 | 2004-03-19 | H. Lundbeck A/S | S-(+)-3-{1-(2-(2,3-dihydro-1h-indol-3-yl)ethyl)-3,6-dihydro-2h-pyridin-4-yl}-6-chloro-1h-indole and acid addition salts thereof |
-
2005
- 2005-12-06 CN CNA2005800419599A patent/CN101072770A/zh active Pending
- 2005-12-06 SA SA5260388A patent/SA05260388B1/ar unknown
- 2005-12-06 MX MX2007006757A patent/MX2007006757A/es active IP Right Grant
- 2005-12-06 WO PCT/EP2005/056501 patent/WO2006061373A2/en not_active Ceased
- 2005-12-06 KR KR1020077015615A patent/KR20070091009A/ko not_active Withdrawn
- 2005-12-06 AU AU2005313387A patent/AU2005313387A1/en not_active Abandoned
- 2005-12-06 BR BRPI0518465-7A patent/BRPI0518465A2/pt not_active IP Right Cessation
- 2005-12-06 JP JP2007544893A patent/JP2008523027A/ja not_active Withdrawn
- 2005-12-06 TW TW094142934A patent/TW200626575A/zh unknown
- 2005-12-06 EP EP05817509A patent/EP1828168A2/en not_active Withdrawn
- 2005-12-06 CA CA002587936A patent/CA2587936A1/en not_active Abandoned
- 2005-12-06 AR ARP050105089A patent/AR052146A1/es not_active Application Discontinuation
- 2005-12-06 RU RU2007125692/04A patent/RU2007125692A/ru not_active Application Discontinuation
-
2007
- 2007-05-22 ZA ZA200704155A patent/ZA200704155B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200704155B (en) | 2008-08-27 |
| SA05260388B1 (ar) | 2009-06-09 |
| AU2005313387A1 (en) | 2006-06-15 |
| WO2006061373A2 (en) | 2006-06-15 |
| TW200626575A (en) | 2006-08-01 |
| EP1828168A2 (en) | 2007-09-05 |
| AR052146A1 (es) | 2007-03-07 |
| MX2007006757A (es) | 2007-11-09 |
| CA2587936A1 (en) | 2006-06-15 |
| RU2007125692A (ru) | 2009-01-20 |
| JP2008523027A (ja) | 2008-07-03 |
| CN101072770A (zh) | 2007-11-14 |
| KR20070091009A (ko) | 2007-09-06 |
| WO2006061373A3 (en) | 2006-09-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 5A E 6A ANUIDADES. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2160 DE 29/05/2012. |