PT97100A - Processo para a preparacao de derivados de indol - Google Patents
Processo para a preparacao de derivados de indol Download PDFInfo
- Publication number
- PT97100A PT97100A PT97100A PT9710091A PT97100A PT 97100 A PT97100 A PT 97100A PT 97100 A PT97100 A PT 97100A PT 9710091 A PT9710091 A PT 9710091A PT 97100 A PT97100 A PT 97100A
- Authority
- PT
- Portugal
- Prior art keywords
- compound
- carbon atoms
- formula
- quinuclidinyl
- ind
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 4
- 229940054051 antipsychotic indole derivative Drugs 0.000 title claims 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical class C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title 1
- -1 3-indolyl group Chemical group 0.000 claims abstract 8
- 150000003839 salts Chemical class 0.000 claims abstract 6
- CJTOFAIRBFMRTI-UHFFFAOYSA-N 3-(1-azabicyclo[2.2.2]octan-3-yl)-1h-indole Chemical class C1=CC=C2C(C3C4CCN(C3)CC4)=CNC2=C1 CJTOFAIRBFMRTI-UHFFFAOYSA-N 0.000 claims abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims abstract 2
- 229910052731 fluorine Inorganic materials 0.000 claims abstract 2
- 239000011737 fluorine Substances 0.000 claims abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 7
- 239000007788 liquid Substances 0.000 claims 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 2
- ZKMZPXWMMSBLNO-UHFFFAOYSA-N 1-azabicyclo[2.2.2]octan-3-one Chemical compound C1CC2C(=O)CN1CC2 ZKMZPXWMMSBLNO-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000005278 alkyl sulfonyloxy group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000005333 aroyloxy group Chemical group 0.000 claims 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 1
- 125000005279 aryl sulfonyloxy group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 230000037396 body weight Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 150000002475 indoles Chemical class 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000006239 protecting group Chemical class 0.000 claims 1
- 229940076279 serotonin Drugs 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/28—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Neurosurgery (AREA)
- Public Health (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Addiction (AREA)
- Anesthesiology (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (1)
- J REIVINDICAÇÕES ia. - Processo para a preparação de derivados de indol, nomeadamente, de derivados de 3-(3-indolil)-quinuclidina de fórmula geral I Ind (I) na qual Ind significa um grupo 3-indolilo insubstituído ou um grupo 3-indolilo monossubstituídó, dissubstituído, trissubstituído ou tetrassubstituído por alquilo com 1 a 4 átomos de carbono, trifluormetilo, alco-xi com 1 a 4 átomos de carbono, alquiltio com 1 a 4 átomos de carbono, fldor, cloro, hidroxi, hidroxi-metilo, ariloxi com 6 a 10 átomos de carbono, aral--quiloxi com 7 a 11 átomos de carbono, aciloxi com 1 a 5 átomos de carbono, aroiloxi com 6 a 10 átomos de earbono, alquilsulfoniloxi com 1 a 4 átomos de carbono, arilsulfoniloxi com 6 a 10 átomos de earbono, earboxi, alcoxicarbonilo com 1 a 4 átomos de carbono e/ou metilenodioxi; e Et significa 3-quinuelidinilo ou 2,3-desidro-3-quinu- clidinilo, e dos seus sais, caracterizado pelo facto de se fazer reagir um composto de fórmula geral II (II) Ind-H na qual o símbolo Ind possui as significações acima referidas, com 3-quinuclidinona ou com um seu sal de maneira a obter-seum composto de 2,3-desidro-3-quinuclidinilo (fórmula geral I em que R = 2,3-desidro-3-quinuclidinilo) e, quando assim se pretende, se reduzir este composto de maneira a obtei>-se um composto de 3-quinuc1idinilo (fórmula I, em que R = 3-quinu-clidinilo) e/οα se transformar um composto que aliás corresponde à fórmula I mas que, em vez de um ou maia átomos de hidrogénio, contém um grupo de protecção eliminável, num composto de fórmula geral I mediante eliminação deste grupo de protee-ção e/ou, num composto de fórmula geral I, se transformar um radical Ind num outro radical Ind e/οα se transformar uma base de fórmula geral I num seu sal por tratamento com um ácido.2â. - Processo para a preparação de composições farmacêuticas, caracterizado pelo facto de se misturar pelo menos um composto de fórmula geral I e/ou um dos seus sais fisiologicamente aceitáveis com pelo menos uma substância veicular e/ou auxiliar sólida, líquida ou semilíquida e se conferir à mistura uma forma apropriada para a via de administração pretendida.3a. - Processo para o tratamento terapêutico de doenças provocadas em seres humanos por um excesso de serotonina em circulação, caracterizado pelo facto de se administrar a esses pacientes uma dose diária de, pelo menos, um composto de fórmula geral I ou de um seu sal farmacologicamente aceitável, de acordo com a reivindicação 1, de preferência, compreendida entre cerca de 0,003 e 20 mg/kg de peso corporal. m. Lisboa, 0 Agente Oficial da Propriedade IndustrialAmérico da Silva Carvalho Agonie Oficial de Propriedade Iftdurtriai R. Castilho, 201-3. £.-1000 LISBOA Telefc. 65 1339-654613
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4009565A DE4009565A1 (de) | 1990-03-24 | 1990-03-24 | Indolderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PT97100A true PT97100A (pt) | 1991-11-29 |
Family
ID=6403022
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PT97100A PT97100A (pt) | 1990-03-24 | 1991-03-21 | Processo para a preparacao de derivados de indol |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US5227386A (pt) |
| EP (1) | EP0450345B1 (pt) |
| JP (1) | JPH04235184A (pt) |
| KR (1) | KR910016747A (pt) |
| AT (1) | ATE123031T1 (pt) |
| AU (1) | AU631303B2 (pt) |
| CA (1) | CA2038908A1 (pt) |
| DE (2) | DE4009565A1 (pt) |
| DK (1) | DK0450345T3 (pt) |
| ES (1) | ES2072467T3 (pt) |
| HU (1) | HU207069B (pt) |
| IE (1) | IE70661B1 (pt) |
| PT (1) | PT97100A (pt) |
| TW (1) | TW217411B (pt) |
| ZA (1) | ZA912198B (pt) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9201038D0 (en) * | 1992-01-16 | 1992-03-11 | Glaxo Group Ltd | Chemical compounds |
| SE9201478D0 (sv) * | 1992-05-11 | 1992-05-11 | Kabi Pharmacia Ab | Heteroaromatic quinuclidinenes, their use and preparation |
| GB9314174D0 (en) * | 1993-07-08 | 1993-08-18 | American Home Prod | 5-ht3-antagonists |
| CA2420235A1 (en) * | 2000-08-21 | 2002-02-28 | Georgetown University | 2-3-disubstituted quinuclidines as modulators of monoamine transporters and therapeutic and diagnostic methods based thereon |
| DE10045112A1 (de) * | 2000-09-11 | 2002-03-21 | Merck Patent Gmbh | Verwendung von Indolderivaten zur Behandlung von Erkrankungen des zentralen Nervensystems |
| DE60132710T2 (de) * | 2000-12-01 | 2008-06-12 | Neurosearch A/S | 3-substituierte chinuclidine und ihre verwendung als nikotinische agonisten |
| DE10121215A1 (de) * | 2001-04-30 | 2002-10-31 | Merck Patent Gmbh | Dihydro-imidazo[4,5-e]indol- und 7H-Pyrrolo[3,2-f]chinoxalin Derivate als nikotinische Acetylcholinrezeptor Liganden und/oder serotonerge Liganden |
| CN1656093A (zh) * | 2002-05-30 | 2005-08-17 | 神经研究公司 | 3－取代的奎宁环及其用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4605652A (en) * | 1985-02-04 | 1986-08-12 | A. H. Robins Company, Inc. | Method of enhancing memory or correcting memory deficiency with arylamido (and arylthioamido)-azabicycloalkanes |
| IE62231B1 (en) * | 1987-12-24 | 1995-01-11 | Wyeth John & Brother Ltd | Heterocyclic compounds |
| DE3810552A1 (de) * | 1988-03-29 | 1989-10-19 | Sandoz Ag | Ester und amide von indol-, benzo(b)thiopen-, benzo(b)furancarbonsaeuren oder 4-amino-2-methoxy-benzolsaeuren mit n-heterocyclischen oder n-heterobicyclischen alkoholen oder aminen, verfahren zu deren herstellung sie enthaltende pharmazeutische zusammensetzungen sowie applikator zur verabreichung derselben |
| AU5650890A (en) * | 1989-05-24 | 1990-12-18 | Nippon Shinyaku Co. Ltd. | Indole derivatives and medicine |
-
1990
- 1990-03-24 DE DE4009565A patent/DE4009565A1/de not_active Withdrawn
-
1991
- 1991-03-09 DE DE59105550T patent/DE59105550D1/de not_active Expired - Fee Related
- 1991-03-09 ES ES91103628T patent/ES2072467T3/es not_active Expired - Lifetime
- 1991-03-09 AT AT91103628T patent/ATE123031T1/de not_active IP Right Cessation
- 1991-03-09 EP EP91103628A patent/EP0450345B1/de not_active Expired - Lifetime
- 1991-03-09 DK DK91103628.3T patent/DK0450345T3/da active
- 1991-03-19 AU AU73609/91A patent/AU631303B2/en not_active Ceased
- 1991-03-21 TW TW080102231A patent/TW217411B/zh active
- 1991-03-21 PT PT97100A patent/PT97100A/pt not_active Application Discontinuation
- 1991-03-22 CA CA002038908A patent/CA2038908A1/en not_active Abandoned
- 1991-03-22 ZA ZA912198A patent/ZA912198B/xx unknown
- 1991-03-22 KR KR1019910004550A patent/KR910016747A/ko not_active Ceased
- 1991-03-22 IE IE96391A patent/IE70661B1/en not_active IP Right Cessation
- 1991-03-22 HU HU91972A patent/HU207069B/hu not_active IP Right Cessation
- 1991-03-22 JP JP3130776A patent/JPH04235184A/ja active Pending
- 1991-03-22 US US07/673,544 patent/US5227386A/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| IE910963A1 (en) | 1991-09-25 |
| HU910972D0 (en) | 1991-10-28 |
| IE70661B1 (en) | 1996-12-11 |
| AU7360991A (en) | 1991-10-03 |
| EP0450345B1 (de) | 1995-05-24 |
| DE4009565A1 (de) | 1991-09-26 |
| CA2038908A1 (en) | 1991-09-25 |
| TW217411B (pt) | 1993-12-11 |
| DE59105550D1 (de) | 1995-06-29 |
| US5227386A (en) | 1993-07-13 |
| DK0450345T3 (da) | 1995-08-07 |
| ES2072467T3 (es) | 1995-07-16 |
| AU631303B2 (en) | 1992-11-19 |
| JPH04235184A (ja) | 1992-08-24 |
| KR910016747A (ko) | 1991-11-05 |
| ATE123031T1 (de) | 1995-06-15 |
| HUT57761A (en) | 1991-12-30 |
| HU207069B (en) | 1993-03-01 |
| EP0450345A1 (de) | 1991-10-09 |
| ZA912198B (en) | 1992-01-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| BB1A | Laying open of patent application |
Effective date: 19910724 |
|
| FC3A | Refusal |
Effective date: 19981207 |