AR038967A1 - Derivados de 2,3 - diaril - pirazolidinas como inhibidores de enzimas que degradan la neurotensina - Google Patents
Derivados de 2,3 - diaril - pirazolidinas como inhibidores de enzimas que degradan la neurotensinaInfo
- Publication number
- AR038967A1 AR038967A1 ARP030100880A ARP030100880A AR038967A1 AR 038967 A1 AR038967 A1 AR 038967A1 AR P030100880 A ARP030100880 A AR P030100880A AR P030100880 A ARP030100880 A AR P030100880A AR 038967 A1 AR038967 A1 AR 038967A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halogen
- alkoxy
- hydroxy
- neurotensin
- Prior art date
Links
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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P25/22—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/04—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se refiere a un grupo de novedosos derivados de 2,3-diaril-pirazolidinas, procedimiento, composición farmacéutica y usos. Los compuestos tienen actividad inhibitoria de las enzimas que degradan el neuropéptido neurotensina y pueden ser utilizados para el tratamiento de afecciones y enfermedades causadas por perturbaciones de la transmisión mediada por neurotensina, como psicosis, Parkinson, depresión y ansiedad. Reivindicación 1: Derivados de 2,3-diaril-pirazolidina, caracterizados porque son de la fórmula (1) en donde: S1 es H, halógeno, hidroxi o alcoxi C1-3, S2 es H, o halógeno, S3 es H, halógeno, hidroxi o alcoxi C1-3; S4 es H, halógeno o alquilo C1-6 opcionalmente sustituido con hidroxi, alcoxi C1-3, amino, mono o dialquilamino que tiene 1-3 átomos de C en el(los) grupo(s) alquilo, SH o S-alquilo C1-3; X representa N o C; Y representa N u O cuando X es N, o Y es N cuando X es C; R3 y R4 son H o alquilo C1-3 independientemente uno de otro, R5 es H, o alquilo C1-6 el cual puede estar sustituido con halógeno, CN, CF3, hidroxi, alcoxi C1-3, sulfonilalquil C1-3, amino, mono- o dialquilamino que tiene 1-3 átomos de C en el(los) grupos alquilo cuando X es C o N, o R5 representa alcoxi C1-6, SH o S-alquilo C1-3, cuando X es C. R´5 es H o alquilo C1-3, R6 es H o alquilo C1-3, R7 es H o alquilo C1-3, R5 y R6 juntos o R´5 y R6 juntos pueden formar un grupo cíclico de 3-7 miembros el cual puede estar sustituido con un alquilo inferior, halógeno, CN, o CF3 y R5 + R´5 juntos pueden formar un anillo de 3-7 miembros, y Z1, Z2 y Z3 representan C, o Z1 es nitrógeno y Z2 y Z3 son C, o Z1 y Z3 son C y Z2 es nitrógeno, o Z1 y Z2 son C y Z3 es N, A es un sistema (poli) cicloalquilo que consiste de anillos de 4-10 miembros el cual puede estar sustituido con halógeno, CF3, alquilo o alcoxi C1-3, CN, OH SH, y sales farmacológicamente aceptables de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02076482 | 2002-03-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR038967A1 true AR038967A1 (es) | 2005-02-02 |
Family
ID=27838122
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030100880A AR038967A1 (es) | 2002-03-18 | 2003-03-13 | Derivados de 2,3 - diaril - pirazolidinas como inhibidores de enzimas que degradan la neurotensina |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US7186741B2 (es) |
| EP (1) | EP1487802B1 (es) |
| JP (1) | JP4484525B2 (es) |
| KR (1) | KR20040106290A (es) |
| CN (1) | CN100509788C (es) |
| AR (1) | AR038967A1 (es) |
| AT (1) | ATE493390T1 (es) |
| AU (1) | AU2003219165B2 (es) |
| BR (1) | BR0306149A (es) |
| CA (1) | CA2462694C (es) |
| DE (1) | DE60335525D1 (es) |
| DK (1) | DK1487802T3 (es) |
| ES (1) | ES2358894T3 (es) |
| HK (1) | HK1070646A1 (es) |
| HR (1) | HRP20040275A2 (es) |
| IL (1) | IL160944A0 (es) |
| MX (1) | MXPA04004743A (es) |
| NO (1) | NO20044405L (es) |
| PL (1) | PL371440A1 (es) |
| PT (1) | PT1487802E (es) |
| RU (1) | RU2304578C2 (es) |
| SI (1) | SI1487802T1 (es) |
| UA (1) | UA77775C2 (es) |
| WO (1) | WO2003078400A1 (es) |
| ZA (1) | ZA200404741B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1801098A1 (en) | 2005-12-16 | 2007-06-27 | Merck Sante | 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors |
| CN102241678B (zh) | 2011-04-26 | 2014-10-29 | 辽宁利锋科技开发有限公司 | 含有脂环结构化合物的抗肿瘤作用与应用 |
| CN106459004B (zh) | 2014-06-06 | 2020-09-15 | 研究三角协会 | 爱帕琳肽受体(apj)激动剂及其用途 |
| AU2016366310C1 (en) | 2015-12-09 | 2021-09-09 | Research Triangle Institute | Improved apelin receptor (APJ) agonists and uses thereof |
| CN117180430A (zh) * | 2023-08-23 | 2023-12-08 | 四川大学华西医院 | Nln神经溶素在制备作为治疗肺癌药物的新用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3712365A1 (de) * | 1987-04-11 | 1988-10-27 | Hoechst Ag | Neue 2-acylpyrrolidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel sowie deren verwendung |
| PH27357A (en) * | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
| FR2665898B1 (fr) * | 1990-08-20 | 1994-03-11 | Sanofi | Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2711140B1 (fr) * | 1993-10-12 | 1996-01-05 | Sanofi Sa | 1-Naphtylpyrazole-3-carboxamides substitués actifs sur la neurotensine, leur préparation, les compositions pharmaceutiques en contenant. |
-
2003
- 2003-03-13 AR ARP030100880A patent/AR038967A1/es unknown
- 2003-03-17 JP JP2003576406A patent/JP4484525B2/ja not_active Expired - Fee Related
- 2003-03-17 MX MXPA04004743A patent/MXPA04004743A/es active IP Right Grant
- 2003-03-17 UA UA20041008453A patent/UA77775C2/uk unknown
- 2003-03-17 DE DE60335525T patent/DE60335525D1/de not_active Expired - Lifetime
- 2003-03-17 WO PCT/EP2003/050064 patent/WO2003078400A1/en active Application Filing
- 2003-03-17 IL IL16094403A patent/IL160944A0/xx unknown
- 2003-03-17 ES ES03714961T patent/ES2358894T3/es not_active Expired - Lifetime
- 2003-03-17 US US10/490,549 patent/US7186741B2/en not_active Expired - Fee Related
- 2003-03-17 PT PT03714961T patent/PT1487802E/pt unknown
- 2003-03-17 RU RU2004114262/04A patent/RU2304578C2/ru not_active IP Right Cessation
- 2003-03-17 BR BR0306149-3A patent/BR0306149A/pt not_active IP Right Cessation
- 2003-03-17 CA CA2462694A patent/CA2462694C/en not_active Expired - Fee Related
- 2003-03-17 SI SI200331966T patent/SI1487802T1/sl unknown
- 2003-03-17 AU AU2003219165A patent/AU2003219165B2/en not_active Ceased
- 2003-03-17 EP EP03714961A patent/EP1487802B1/en not_active Expired - Lifetime
- 2003-03-17 KR KR10-2004-7014581A patent/KR20040106290A/ko not_active Application Discontinuation
- 2003-03-17 CN CNB038015668A patent/CN100509788C/zh not_active Expired - Fee Related
- 2003-03-17 DK DK03714961.4T patent/DK1487802T3/da active
- 2003-03-17 PL PL03371440A patent/PL371440A1/xx not_active Application Discontinuation
- 2003-03-17 AT AT03714961T patent/ATE493390T1/de active
-
2004
- 2004-03-19 HR HR20040275A patent/HRP20040275A2/hr not_active Application Discontinuation
- 2004-06-15 ZA ZA200404741A patent/ZA200404741B/en unknown
- 2004-10-15 NO NO20044405A patent/NO20044405L/no not_active Application Discontinuation
-
2005
- 2005-04-14 HK HK05103186.3A patent/HK1070646A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| RU2304578C2 (ru) | 2007-08-20 |
| AU2003219165B2 (en) | 2008-03-13 |
| ZA200404741B (en) | 2005-08-29 |
| JP4484525B2 (ja) | 2010-06-16 |
| JP2005527528A (ja) | 2005-09-15 |
| CA2462694C (en) | 2010-08-10 |
| CN100509788C (zh) | 2009-07-08 |
| HK1070646A1 (en) | 2005-06-24 |
| IL160944A0 (en) | 2004-08-31 |
| AU2003219165A1 (en) | 2003-09-29 |
| PL371440A1 (en) | 2005-06-13 |
| CN1592742A (zh) | 2005-03-09 |
| HRP20040275A2 (en) | 2004-08-31 |
| DK1487802T3 (da) | 2011-04-04 |
| US7186741B2 (en) | 2007-03-06 |
| EP1487802A1 (en) | 2004-12-22 |
| EP1487802B1 (en) | 2010-12-29 |
| KR20040106290A (ko) | 2004-12-17 |
| BR0306149A (pt) | 2004-10-19 |
| US20040242493A1 (en) | 2004-12-02 |
| DE60335525D1 (de) | 2011-02-10 |
| ES2358894T3 (es) | 2011-05-16 |
| CA2462694A1 (en) | 2003-09-25 |
| RU2004114262A (ru) | 2005-09-20 |
| MXPA04004743A (es) | 2004-08-02 |
| NO20044405L (no) | 2004-10-15 |
| SI1487802T1 (sl) | 2011-04-29 |
| ATE493390T1 (de) | 2011-01-15 |
| UA77775C2 (en) | 2007-01-15 |
| PT1487802E (pt) | 2011-03-11 |
| WO2003078400A1 (en) | 2003-09-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |