AR045859A1 - Derivados de dibenzoazepina y de benzodiazepinas sustitudos, procesos de preparacion y usos - Google Patents
Derivados de dibenzoazepina y de benzodiazepinas sustitudos, procesos de preparacion y usosInfo
- Publication number
- AR045859A1 AR045859A1 ARP040103592A ARP040103592A AR045859A1 AR 045859 A1 AR045859 A1 AR 045859A1 AR P040103592 A ARP040103592 A AR P040103592A AR P040103592 A ARP040103592 A AR P040103592A AR 045859 A1 AR045859 A1 AR 045859A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- hydrogen
- cycloalkyl
- chf2
- benzodiazepinas
- Prior art date
Links
- 150000007655 dibenzoazepines Chemical class 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 4
- 150000002431 hydrogen Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- -1 -CH2CF Chemical group 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P25/28—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
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D223/16—Benzazepines; Hydrogenated benzazepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/12—1,5-Benzodiazepines; Hydrogenated 1,5-benzodiazepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/24—Oxygen atoms
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Reivindicación 1: Compuestos de fórmula general (1), en donde: R es -(CHR')q-arilo o -(CHR')q-heteroarilo, que están sin sustituir o mono, di- o tri-sustituidos por alquilo inferior, alcoxilo inferior, CF3 o halógeno, o es alquilo inferior, -(CH2)n- O-alquilo inferior, -(CH2)n-S-alquilo inferior, -(CH2)q-cicloalquilo, -(CH2)n-(CH2F), (CH2)n-CF3, (CH2)n-CHF2-CF3, (CH2)n-CHF2-CHF2, (CH2)n-CR'R''-CF3, y en donde R' y R'' forman junto con el átomo de carbono un anillo cicloalquilo; R2 es hidrógeno o alquilo inferior; R3 es hidrógeno, alquilo inferior, -CH2CF, CF3, o es arilo, opcionalmente mono, di o tri-sustituidos por halógeno, o es -(CH2)nNR5R6, en donde R5 y R6 son independientemente el uno del otro hidrógeno o alquilo inferior; R4 es uno de los grupos de fórmulas (2), en donde: R7 es hidrógeno, alquilo inferior, o -(CH2)n-cicloalquilo; R8, R9 son, independientemente, hidrógeno, alquilo inferior, -(CH2)n-cicloalquilo o -C(O)-fenilo; y a sales de adición ácida farmacéuticamente aceptables, enantiómeros ópticamente puros, racematos o mezclas diastereoméricas de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03022650 | 2003-10-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045859A1 true AR045859A1 (es) | 2005-11-16 |
Family
ID=34384575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103592A AR045859A1 (es) | 2003-10-06 | 2004-10-04 | Derivados de dibenzoazepina y de benzodiazepinas sustitudos, procesos de preparacion y usos |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US7166587B2 (es) |
| EP (1) | EP1673347B1 (es) |
| JP (1) | JP4503607B2 (es) |
| KR (2) | KR100884872B1 (es) |
| CN (1) | CN1894217B (es) |
| AR (1) | AR045859A1 (es) |
| AU (1) | AU2004283803B2 (es) |
| BR (1) | BRPI0415070B8 (es) |
| CA (1) | CA2541470C (es) |
| CO (1) | CO5690560A2 (es) |
| CY (1) | CY1116865T1 (es) |
| DK (1) | DK1673347T3 (es) |
| ES (1) | ES2548720T3 (es) |
| HR (1) | HRP20151197T1 (es) |
| HU (1) | HUE025548T2 (es) |
| IL (1) | IL174513A (es) |
| MX (1) | MXPA06003870A (es) |
| MY (1) | MY143797A (es) |
| NO (1) | NO20061469L (es) |
| NZ (1) | NZ546036A (es) |
| PL (1) | PL1673347T3 (es) |
| PT (1) | PT1673347E (es) |
| RU (1) | RU2356895C2 (es) |
| SI (1) | SI1673347T1 (es) |
| TW (1) | TWI293627B (es) |
| WO (1) | WO2005040126A1 (es) |
| ZA (1) | ZA200602802B (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| US7211573B2 (en) | 2004-12-08 | 2007-05-01 | Hoffmann-La Roche Inc. | Malonamide derivatives |
| WO2007029587A1 (ja) * | 2005-09-05 | 2007-03-15 | Dainippon Sumitomo Pharma Co., Ltd. | βセクレターゼ阻害剤 |
| MX2008012136A (es) * | 2006-03-27 | 2008-10-03 | Hoffmann La Roche | Derivados de malonamida como inhibidores de gama secretasa. |
| WO2008034735A2 (en) | 2006-09-20 | 2008-03-27 | F. Hoffmann-La Roche Ag | 4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]diazepine derivatives |
| JP5379692B2 (ja) | 2006-11-09 | 2013-12-25 | プロビオドルグ エージー | 潰瘍、癌及び他の疾患の治療のためのグルタミニルシクラーゼの阻害薬としての３−ヒドロキシ−１，５−ジヒドロ−ピロール−２−オン誘導体 |
| EP2091948B1 (en) | 2006-11-30 | 2012-04-18 | Probiodrug AG | Novel inhibitors of glutaminyl cyclase |
| KR101150574B1 (ko) | 2007-02-02 | 2012-05-30 | 에프. 호프만-라 로슈 아게 | 6-옥소-6,7-다이하이드로-5ｈ-다이벤조［ｂ,ｄ］아제핀-7-일 유도체 |
| EP2117540A1 (en) | 2007-03-01 | 2009-11-18 | Probiodrug AG | New use of glutaminyl cyclase inhibitors |
| FR2913886B1 (fr) | 2007-03-22 | 2012-03-02 | Guerbet Sa | Utilisation de nanoparticules metalliques dans le diagnostique de la maladie d'alzheimer |
| WO2008128985A1 (en) | 2007-04-18 | 2008-10-30 | Probiodrug Ag | Thiourea derivatives as glutaminyl cyclase inhibitors |
| US7579464B2 (en) * | 2007-05-25 | 2009-08-25 | Hoffmann-La Roche Inc. | Process for preparation of enantiomerically pure compounds |
| WO2011029920A1 (en) | 2009-09-11 | 2011-03-17 | Probiodrug Ag | Heterocylcic derivatives as inhibitors of glutaminyl cyclase |
| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| ES2481823T3 (es) | 2010-03-10 | 2014-07-31 | Probiodrug Ag | Inhibidores heterocíclicos de glutaminil ciclasa (QC, EC 2.3.2.5) |
| EP2560953B1 (en) | 2010-04-21 | 2016-01-06 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
| WO2011140213A1 (en) * | 2010-05-05 | 2011-11-10 | Amicus Therapeutics, Inc. | Method of treating alzheimer's disease using pharmacological chaperones to increase presenilin function and gamma-secretase activity |
| ES2570167T3 (es) | 2011-03-16 | 2016-05-17 | Probiodrug Ag | Derivados de benzimidazol como inhibidores de glutaminil ciclasa |
| JO3148B1 (ar) | 2011-07-27 | 2017-09-20 | Lilly Co Eli | مركب مثبط لإشارات مسار notch |
| WO2017075264A1 (en) * | 2015-10-30 | 2017-05-04 | Inception 3, Inc. | Dibenzo azepine compounds and their use in the treatment of otic diseases and disorders |
| KR20190098998A (ko) | 2016-12-16 | 2019-08-23 | 파이프라인 테라퓨틱스, 아이엔씨. | 달팽이관 시냅스질환의 치료 방법 |
| EP3461819B1 (en) | 2017-09-29 | 2020-05-27 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
| BR112020023204A2 (pt) * | 2018-05-15 | 2021-02-23 | Bristol-Myers Squibb Company | composições que compreendem compostos de bisfluoroalquil-1,4-benzodiazepinona e métodos de uso dos mesmos |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9314981D0 (en) * | 1993-07-20 | 1993-09-01 | Glaxo Spa | Chemical compounds |
| CA2347671A1 (en) * | 1998-12-24 | 2000-07-06 | Dupont Pharmaceuticals Company | Succinoylamino benzodiazepines as inhibitors of a.beta. protein production |
| JP2004500419A (ja) * | 2000-04-11 | 2004-01-08 | デュポン ファーマシューティカルズ カンパニー | Ａβタンパク質産生阻害剤としての置換ラクタム |
| HK1049333A1 (zh) * | 2000-06-01 | 2003-05-09 | Bristol-Myers Squibb Pharma Company | 以环状琥珀酸酯代替内酰胺，作为制造Aβ蛋白质的抑制剂 |
| MXPA05008172A (es) * | 2003-02-04 | 2005-10-05 | Hoffmann La Roche | Derivados de malonamida como inhibidores gamma-secretasa. |
| BRPI0413533A (pt) * | 2003-09-09 | 2006-10-10 | Hoffmann La Roche | derivados de malonamida que bloqueiam a atividade de gama-secretase |
-
2004
- 2004-09-27 WO PCT/EP2004/010821 patent/WO2005040126A1/en not_active Ceased
- 2004-09-27 MX MXPA06003870A patent/MXPA06003870A/es active IP Right Grant
- 2004-09-27 CN CN2004800333748A patent/CN1894217B/zh not_active Expired - Lifetime
- 2004-09-27 NZ NZ546036A patent/NZ546036A/en unknown
- 2004-09-27 PT PT47870282T patent/PT1673347E/pt unknown
- 2004-09-27 SI SI200432267T patent/SI1673347T1/sl unknown
- 2004-09-27 KR KR1020087003016A patent/KR100884872B1/ko not_active Expired - Lifetime
- 2004-09-27 KR KR1020067006540A patent/KR100867035B1/ko not_active Expired - Lifetime
- 2004-09-27 HR HRP20151197TT patent/HRP20151197T1/hr unknown
- 2004-09-27 AU AU2004283803A patent/AU2004283803B2/en not_active Expired
- 2004-09-27 JP JP2006530028A patent/JP4503607B2/ja not_active Expired - Lifetime
- 2004-09-27 EP EP04787028.2A patent/EP1673347B1/en not_active Expired - Lifetime
- 2004-09-27 US US10/951,229 patent/US7166587B2/en not_active Expired - Lifetime
- 2004-09-27 PL PL04787028T patent/PL1673347T3/pl unknown
- 2004-09-27 RU RU2006115165/04A patent/RU2356895C2/ru not_active IP Right Cessation
- 2004-09-27 CA CA2541470A patent/CA2541470C/en not_active Expired - Lifetime
- 2004-09-27 ES ES04787028.2T patent/ES2548720T3/es not_active Expired - Lifetime
- 2004-09-27 DK DK04787028.2T patent/DK1673347T3/en active
- 2004-09-27 BR BRPI0415070A patent/BRPI0415070B8/pt not_active IP Right Cessation
- 2004-09-27 HU HUE04787028A patent/HUE025548T2/en unknown
- 2004-10-04 AR ARP040103592A patent/AR045859A1/es unknown
- 2004-10-04 TW TW093130014A patent/TWI293627B/zh active
- 2004-10-05 MY MYPI20044077A patent/MY143797A/en unknown
-
2006
- 2006-03-23 IL IL174513A patent/IL174513A/en active IP Right Grant
- 2006-03-31 NO NO20061469A patent/NO20061469L/no not_active Application Discontinuation
- 2006-04-05 ZA ZA200602802A patent/ZA200602802B/en unknown
- 2006-04-07 CO CO06034536A patent/CO5690560A2/es not_active Application Discontinuation
-
2015
- 2015-10-29 CY CY20151100963T patent/CY1116865T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |