BR9911079A - Acentuador de acetilcolina, composto, processo tanto para inibir a acetilcolina esterase de enzima quanto para antagonizar o receptor de serotonina 5ht3, e, composição farmacêutica. - Google Patents
Acentuador de acetilcolina, composto, processo tanto para inibir a acetilcolina esterase de enzima quanto para antagonizar o receptor de serotonina 5ht3, e, composição farmacêutica.Info
- Publication number
- BR9911079A BR9911079A BR9911079-2A BR9911079A BR9911079A BR 9911079 A BR9911079 A BR 9911079A BR 9911079 A BR9911079 A BR 9911079A BR 9911079 A BR9911079 A BR 9911079A
- Authority
- BR
- Brazil
- Prior art keywords
- acetylcholine
- compound
- antagonize
- inhibit
- pharmaceutical composition
- Prior art date
Links
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 title abstract 4
- 229960004373 acetylcholine Drugs 0.000 title abstract 4
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 108090000371 Esterases Proteins 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 108091005477 5-HT3 receptors Proteins 0.000 title 1
- 102000035037 5-HT3 receptors Human genes 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- 102000004190 Enzymes Human genes 0.000 title 1
- 239000003623 enhancer Substances 0.000 title 1
- 102000012440 Acetylcholinesterase Human genes 0.000 abstract 2
- 108010022752 Acetylcholinesterase Proteins 0.000 abstract 2
- 229940022698 acetylcholinesterase Drugs 0.000 abstract 2
- 230000009977 dual effect Effects 0.000 abstract 2
- 229940113081 5 Hydroxytryptamine 3 receptor antagonist Drugs 0.000 abstract 1
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 abstract 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 abstract 1
- 229940126062 Compound A Drugs 0.000 abstract 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 abstract 1
- 229940027991 antiseptic and disinfectant quinoline derivative Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000002943 quinolinyl group Chemical class N1=C(C=CC2=CC=CC=C12)* 0.000 abstract 1
- 239000003369 serotonin 5-HT3 receptor antagonist Substances 0.000 abstract 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
"ACENTUADOR DE ACETILCOLINA, COMPOSTO, PROCESSO TANTO PARA INIBIR A ACETILCOLINA ESTERASE DE ENZIMA QUANTO PARA ANTAGONIZAR O RECEPTOR DE SEROTONINA 5HT3, E, COMPOSIçãO FARMACêUTICA" São aqui divulgados derivados de quinolina tendo duas propriedades mecanísticas duais, referidas neste documento de patente como "acentuadores de acetilcolina ", isto é, compostos que evidenciam a atividade de inibição da acetilcolinesterase (AChE), e a atividade de antagonista do receptor 5-HT3. Um composto particularmente preferido é hemifumarato 2-[2-(1-benzilpiperizin-4-il)etil]-2,3-diidro-9-metóxi-1H-pirrolo[3,4-b]qui nolin-1-ona, aqui referido como composto A ("Cm.A").
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8873798P | 1998-06-10 | 1998-06-10 | |
| US9166698P | 1998-07-02 | 1998-07-02 | |
| US10941398P | 1998-11-20 | 1998-11-20 | |
| US11508999P | 1999-01-07 | 1999-01-07 | |
| US13688799P | 1999-06-01 | 1999-06-01 | |
| PCT/US1999/012886 WO1999064421A1 (en) | 1998-06-10 | 1999-06-09 | Acetylcholine enhancers |
| US09/328,643 US6218402B1 (en) | 1998-06-10 | 1999-06-09 | Acetylcholine enhancers |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9911079A true BR9911079A (pt) | 2001-02-20 |
Family
ID=27557353
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9911079-2A BR9911079A (pt) | 1998-06-10 | 1999-06-09 | Acentuador de acetilcolina, composto, processo tanto para inibir a acetilcolina esterase de enzima quanto para antagonizar o receptor de serotonina 5ht3, e, composição farmacêutica. |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US6218402B1 (pt) |
| EP (1) | EP1086102A1 (pt) |
| JP (1) | JP2004508272A (pt) |
| KR (1) | KR20010072598A (pt) |
| CN (1) | CN1138775C (pt) |
| AU (1) | AU751590B2 (pt) |
| BR (1) | BR9911079A (pt) |
| CA (1) | CA2331794A1 (pt) |
| IL (1) | IL139254A0 (pt) |
| MX (1) | MXPA00012248A (pt) |
| NO (1) | NO20006249L (pt) |
| WO (1) | WO1999064421A1 (pt) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3929250B2 (ja) * | 2001-03-08 | 2007-06-13 | 株式会社ルネサステクノロジ | 半導体装置 |
| AU2003301439A1 (en) * | 2002-10-16 | 2004-05-04 | Gilead Sciences, Inc. | Pre-organized tricyclic integrase inhibitor compounds |
| US20070276024A1 (en) * | 2003-10-09 | 2007-11-29 | Inverseon , Inc. | Methods for Treating Diseases and Conditions with Inverse Agonists and for Screening for Agents Acting as Inverse Agonists |
| EP1684764A2 (en) * | 2003-10-09 | 2006-08-02 | Inverseon, Inc. | Methods for treating diseases and conditions with inverse agonists and for screening for agents acting as inverse agonists |
| JP2005154320A (ja) * | 2003-11-25 | 2005-06-16 | Ss Pharmaceut Co Ltd | 眼疾患治療薬 |
| DE602005010413D1 (de) * | 2004-04-14 | 2008-11-27 | Zhenhong R Cai | Phosphonatanaloga von hiv-integrasehemmerverbindungen |
| US7528175B2 (en) * | 2004-10-08 | 2009-05-05 | Inverseon, Inc. | Method of treating airway diseases with beta-adrenergic inverse agonists |
| CN103992312A (zh) * | 2013-02-18 | 2014-08-20 | 江苏欧威医药有限公司 | 1,2,4-噻二唑-3,5-二酮衍生物及其药物组合物和应用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5240934A (en) | 1990-10-19 | 1993-08-31 | Ss Pharmaceutical Co., Ltd. | Quinoline derivatives |
| US5190951A (en) | 1990-10-19 | 1993-03-02 | Ss Pharmaceutical Co., Ltd. | Quinoline derivatives |
| CA2135253A1 (en) | 1994-11-07 | 1996-05-08 | Michael Dennis | Compound screening based on a window of chemical-messenger-independent activity |
-
1999
- 1999-06-09 US US09/328,643 patent/US6218402B1/en not_active Expired - Fee Related
- 1999-06-09 BR BR9911079-2A patent/BR9911079A/pt not_active IP Right Cessation
- 1999-06-09 JP JP2000553430A patent/JP2004508272A/ja not_active Withdrawn
- 1999-06-09 IL IL13925499A patent/IL139254A0/xx unknown
- 1999-06-09 AU AU49553/99A patent/AU751590B2/en not_active Ceased
- 1999-06-09 CA CA002331794A patent/CA2331794A1/en not_active Abandoned
- 1999-06-09 EP EP99933508A patent/EP1086102A1/en not_active Withdrawn
- 1999-06-09 MX MXPA00012248A patent/MXPA00012248A/es unknown
- 1999-06-09 KR KR1020007013991A patent/KR20010072598A/ko not_active Withdrawn
- 1999-06-09 WO PCT/US1999/012886 patent/WO1999064421A1/en not_active Ceased
- 1999-06-09 CN CNB998071102A patent/CN1138775C/zh not_active Expired - Fee Related
-
2000
- 2000-12-08 NO NO20006249A patent/NO20006249L/no not_active Application Discontinuation
-
2001
- 2001-04-17 US US09/836,069 patent/US6586596B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA00012248A (es) | 2003-04-25 |
| US6218402B1 (en) | 2001-04-17 |
| WO1999064421B1 (en) | 2000-02-24 |
| CA2331794A1 (en) | 1999-12-16 |
| WO1999064421A1 (en) | 1999-12-16 |
| NO20006249D0 (no) | 2000-12-08 |
| AU4955399A (en) | 1999-12-30 |
| JP2004508272A (ja) | 2004-03-18 |
| US6586596B2 (en) | 2003-07-01 |
| KR20010072598A (ko) | 2001-07-31 |
| US20010039284A1 (en) | 2001-11-08 |
| IL139254A0 (en) | 2001-11-25 |
| WO1999064421A8 (en) | 2000-04-06 |
| CN1138775C (zh) | 2004-02-18 |
| AU751590B2 (en) | 2002-08-22 |
| CN1304411A (zh) | 2001-07-18 |
| NO20006249L (no) | 2000-12-08 |
| EP1086102A1 (en) | 2001-03-28 |
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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 A 5,6,7 E 8A 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 1911 DE 21/08/2007. |