CY1116865T1 - Παραγωγα υποκατεστημενης διβενζο-αζεπινης και βενζο-διαζεπινης χρησιμα ως αναστολεις της γαμμα-σεκρετασης - Google Patents
Παραγωγα υποκατεστημενης διβενζο-αζεπινης και βενζο-διαζεπινης χρησιμα ως αναστολεις της γαμμα-σεκρετασηςInfo
- Publication number
- CY1116865T1 CY1116865T1 CY20151100963T CY151100963T CY1116865T1 CY 1116865 T1 CY1116865 T1 CY 1116865T1 CY 20151100963 T CY20151100963 T CY 20151100963T CY 151100963 T CY151100963 T CY 151100963T CY 1116865 T1 CY1116865 T1 CY 1116865T1
- Authority
- CY
- Cyprus
- Prior art keywords
- lower alkyl
- hydrogen
- cycloalkyl
- substituted
- divenzo
- Prior art date
Links
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
Η παρούσα εφεύρεση σχετίζεται με ενώσεις του γενικού τύπου (I), όπου η R1 είναι -(CHR')q –αρύλιο ή -(CHR')q-ετεροαρύλιο, τα οποία είναι μη υποκατεστημένα ή μονο-, δι- ή τρι-υποκατεστημένα με κατώτερο αλκύλιο, κατώτερο άλκοξυ, CF3 ή αλογόνο, ή είναι κατώτερο αλκύλιο, κατώτερο αλκενύλιο, -(CH2)n-Si(CH3)3, -(CΗ2)n-O-κατώτερο αλκύλιο, -(CH2)n-S-κατώτερο αλκύλιο, -(CΗ2)q-κυκλοαλκύλιο, -(CH2)n-[CH(OH)]m-(CF2)p-CHqF(3-q), ή είναι -(CH2)n-CR2-CF3, όπου οι δύο ρίζες R μαζί με το άτομο άνθρακα σχηματίζουν δακτύλιο κυκλοαλκυλίου· η R' είναι υδρογόνο ή κατώτερο αλκύλιο· n είναι 1, 2 ή 3· m είναι 0 ή 1· p είναι 0,1, 2, 3,4, 5 ή 6· q είναι 0, 1, 2 ή 3· η R2 είναι υδρογόνο ή κατώτερο αλκύλιο· η R3 είναι υδρογόνο, κατώτερο αλκύλιο, -CH2CF2CF3, CH2CF3, (CH2)2CF3, CF3, CHF2, CH2F, ή είναι αρύλιο, προαιρετικά μονο-, δι- ή τρι-υποκατεστημένο με αλογόνο, ή είναι (CH2)nNR5R6, όπου οι R5 και R6 είναι ανεξαρτήτως μεταξύ των υδρογόνο ή κατώτερο αλκύλιο· η R4 είναι μία από τις ακόλουθες ομάδες όπου η R7 είναι υδρογόνο, κατώτερο αλκύλιο, -(CH2)n-CF3 ή -(CΗ2)n-κυκλοαλκύλιο· η R8 είναι υδρογόνο, κατώτερο αλκύλιο, -C(O)-φαινύλιο, -C(O)-κατώτερο αλκύλιο, -C(O)O-(CΗ2)n-κυκλοαλκύλιο, -C(O)O-(CΗ2)n-κατώτερο αλκύλιο, -C(O)ΝΗ-(CΗ2)n-κατώτερο αλκύλιο ή -C(O)ΝΗ-(CH2)n-κυκλο-αλκύλιο· η R9 είναι υδρογόνο, κατώτερο αλκύλιο, -(CH2)n-κυκλοαλκύλιο ή -(CH2)n-CF3· και με φαρμακευτικώς κατάλληλα άλατα προσθήκης οξέος, οπτικώς καθαρά εναντιομερή, ρακεμικά μίγματα ή διαστερεομερικά μίγματα αυτών για τη θεραπευτική αγωγή της νόσου του Alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03022650 | 2003-10-06 | ||
| EP04787028.2A EP1673347B1 (en) | 2003-10-06 | 2004-09-27 | Substituted dibenzo-azepine and benzo-diazepine derivatives useful as gamma-secretase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1116865T1 true CY1116865T1 (el) | 2017-04-05 |
Family
ID=34384575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20151100963T CY1116865T1 (el) | 2003-10-06 | 2015-10-29 | Παραγωγα υποκατεστημενης διβενζο-αζεπινης και βενζο-διαζεπινης χρησιμα ως αναστολεις της γαμμα-σεκρετασης |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US7166587B2 (el) |
| EP (1) | EP1673347B1 (el) |
| JP (1) | JP4503607B2 (el) |
| KR (2) | KR100884872B1 (el) |
| CN (1) | CN1894217B (el) |
| AR (1) | AR045859A1 (el) |
| AU (1) | AU2004283803B2 (el) |
| BR (1) | BRPI0415070B8 (el) |
| CA (1) | CA2541470C (el) |
| CO (1) | CO5690560A2 (el) |
| CY (1) | CY1116865T1 (el) |
| DK (1) | DK1673347T3 (el) |
| ES (1) | ES2548720T3 (el) |
| HR (1) | HRP20151197T1 (el) |
| HU (1) | HUE025548T2 (el) |
| IL (1) | IL174513A (el) |
| MX (1) | MXPA06003870A (el) |
| MY (1) | MY143797A (el) |
| NO (1) | NO20061469L (el) |
| NZ (1) | NZ546036A (el) |
| PL (1) | PL1673347T3 (el) |
| PT (1) | PT1673347E (el) |
| RU (1) | RU2356895C2 (el) |
| SI (1) | SI1673347T1 (el) |
| TW (1) | TWI293627B (el) |
| WO (1) | WO2005040126A1 (el) |
| ZA (1) | ZA200602802B (el) |
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 |
| JP5030781B2 (ja) * | 2005-09-05 | 2012-09-19 | 良明 木曽 | βセクレターゼ阻害剤 |
| CN101410378B (zh) * | 2006-03-27 | 2012-12-05 | 霍夫曼-拉罗奇有限公司 | 作为γ分泌酶抑制剂的丙二酰胺衍生物 |
| KR101096476B1 (ko) | 2006-09-20 | 2011-12-20 | 에프. 호프만-라 로슈 아게 | 4-옥소-2,3,4,5-테트라히드로-벤조[ｂ][1,4]디아제핀 유도체 |
| EP2089383B1 (en) | 2006-11-09 | 2015-09-16 | Probiodrug AG | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| JP5523107B2 (ja) | 2006-11-30 | 2014-06-18 | プロビオドルグ エージー | グルタミニルシクラーゼの新規阻害剤 |
| CN101622232A (zh) | 2007-02-02 | 2010-01-06 | 弗·哈夫曼-拉罗切有限公司 | 6-氧代-6,7-二氢-5h-二苯并[b,d]氮杂䓬-7-基衍生物 |
| KR20090115951A (ko) | 2007-03-01 | 2009-11-10 | 프로비오드룩 아게 | 글루타미닐 사이클라제 저해제의 신규 용도 |
| FR2913886B1 (fr) | 2007-03-22 | 2012-03-02 | Guerbet Sa | Utilisation de nanoparticules metalliques dans le diagnostique de la maladie d'alzheimer |
| US9656991B2 (en) | 2007-04-18 | 2017-05-23 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| US7579464B2 (en) * | 2007-05-25 | 2009-08-25 | Hoffmann-La Roche Inc. | Process for preparation of enantiomerically pure compounds |
| CN102695546B (zh) | 2009-09-11 | 2014-09-10 | 前体生物药物股份公司 | 作为谷氨酰胺酰环化酶抑制剂的杂环衍生物 |
| ES2586231T3 (es) | 2010-03-03 | 2016-10-13 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
| DK2545047T3 (da) | 2010-03-10 | 2014-07-28 | Probiodrug Ag | Heterocycliske inhibitorer af glutaminylcyclase (QC, EC 2.3.2.5) |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| US20130102538A1 (en) * | 2010-05-05 | 2013-04-25 | Amicus Therapeutics, Inc. | Method of treating alzheimer's disease using pharmacological chaperones to increase presenilin function and gamma-secretase activity |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| JO3148B1 (ar) | 2011-07-27 | 2017-09-20 | Lilly Co Eli | مركب مثبط لإشارات مسار notch |
| NZ741553A (en) | 2015-10-30 | 2019-08-30 | Inception 3 Inc | Dibenzo azepine compounds and their use in the treatment of otic diseases and disorders |
| JP6904612B2 (ja) | 2016-12-16 | 2021-07-21 | パイプライン セラピューティクス， インコーポレイテッド | 蝸牛シナプス障害を処置する方法 |
| PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
| CN112236147A (zh) * | 2018-05-15 | 2021-01-15 | 百时美施贵宝公司 | 包含双氟烷基-1,4-苯并二氮杂*酮化合物的组合物和其使用方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU778005B2 (en) * | 1998-12-24 | 2004-11-11 | Bristol-Myers Squibb Pharma Company | Succinoylamino benzodiazepines as inhibitors of Abeta protein production |
| CA2404273A1 (en) * | 2000-04-11 | 2001-10-18 | Bristol-Myers Squibb Pharma Company | Substituted lactams as inhibitors of a.beta. protein production |
| CN1386118A (zh) * | 2000-06-01 | 2002-12-18 | 布里斯托尔-迈尔斯斯奎布药品公司 | 作为Aβ蛋白产生抑制剂的被环状琥珀酸酯取代的内酰胺类化合物 |
| BRPI0407262A (pt) * | 2003-02-04 | 2006-01-31 | Hoffmann La Roche | Derivados de malonamida como inibidores gama-secretase |
| KR20070087233A (ko) * | 2003-09-09 | 2007-08-27 | 에프. 호프만-라 로슈 아게 | 감마-세크리테이즈의 활성을 차단하는 말론아미드 유도체 |
-
2004
- 2004-09-27 WO PCT/EP2004/010821 patent/WO2005040126A1/en active Application Filing
- 2004-09-27 MX MXPA06003870A patent/MXPA06003870A/es active IP Right Grant
- 2004-09-27 RU RU2006115165/04A patent/RU2356895C2/ru not_active IP Right Cessation
- 2004-09-27 KR KR1020087003016A patent/KR100884872B1/ko active IP Right Grant
- 2004-09-27 HU HUE04787028A patent/HUE025548T2/en unknown
- 2004-09-27 AU AU2004283803A patent/AU2004283803B2/en active Active
- 2004-09-27 JP JP2006530028A patent/JP4503607B2/ja active Active
- 2004-09-27 PT PT47870282T patent/PT1673347E/pt unknown
- 2004-09-27 KR KR1020067006540A patent/KR100867035B1/ko active IP Right Grant
- 2004-09-27 NZ NZ546036A patent/NZ546036A/en unknown
- 2004-09-27 CN CN2004800333748A patent/CN1894217B/zh active Active
- 2004-09-27 SI SI200432267T patent/SI1673347T1/sl unknown
- 2004-09-27 EP EP04787028.2A patent/EP1673347B1/en active Active
- 2004-09-27 CA CA2541470A patent/CA2541470C/en active Active
- 2004-09-27 PL PL04787028T patent/PL1673347T3/pl unknown
- 2004-09-27 US US10/951,229 patent/US7166587B2/en active Active
- 2004-09-27 BR BRPI0415070A patent/BRPI0415070B8/pt active IP Right Grant
- 2004-09-27 ES ES04787028.2T patent/ES2548720T3/es active Active
- 2004-09-27 DK DK04787028.2T patent/DK1673347T3/en active
- 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
- 2015-11-09 HR HRP20151197TT patent/HRP20151197T1/hr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CY1116865T1 (el) | Παραγωγα υποκατεστημενης διβενζο-αζεπινης και βενζο-διαζεπινης χρησιμα ως αναστολεις της γαμμα-σεκρετασης | |
| CY1109225T1 (el) | ΠΑΡΑΓΩΓΑ ΜΗΛΟΝΑΜΙΔΙΟΥ ΤΑ ΟΠΟΙΑ ΠΑΡΕΜΠΟΔΙΖΟΥΝ ΤΗ ΔΡΑΣΗ ΤΗΣ γ-ΣΕΚΡΕΤΑΣΗΣ | |
| RU2500680C2 (ru) | Новые замещенные пиридин-2-оны и пиридазин-3-оны | |
| RU2010116253A (ru) | Производные n-гидроксилсульфонамида как новые физиологически применимые доноры нитроксила | |
| PE20090042A1 (es) | Analogos de ciclopamina | |
| EA200802389A1 (ru) | Азиридинилэпотилоновые соединения | |
| NO20085160L (no) | Nye glucokinaseaktivatorer og deres anvendelse | |
| PE20090630A1 (es) | Derivados de indol 2-carboxi sustituidos y metodos para su utilizacion | |
| RU2007147340A (ru) | Новые производные 2-азетидинона в качестве ингибиторов всасывания холестерина для лечения гиперлипидемических состояний | |
| CY1110960T1 (el) | ΠΑΡΑΓΩΓΑ ΤΗΣ 4-(2-ΑΜΙΝΟ-1-ΥΔΡΟΞΥΑΙΘΥΛ)ΦΑΙΝΟΛΗΣ ΩΣ ΑΓΩΝΙΣΤΕΣ ΤΟΥ β2 ΑΔΡΕΝΕΡΓΙΚΟΥ ΥΠΟΔΟΧΕΑ | |
| HUP0301671A2 (hu) | 4-Fenil-piridin-származékok, mint neurokinin-1-receptor antagonisták, eljárás az előállításukra és alkalmazásuk | |
| TW200635585A (en) | Monocyclic substituted methanones | |
| AR084976A1 (es) | Compuestos de bifenileno sustituidos y metodos de uso de los mismos para el tratamiento de enfermedades virales | |
| AR058347A1 (es) | Entidades quimias composiciones y metodos | |
| AR060623A1 (es) | Compuestos derivados de 2-azetidinona y un metodo de preparacion | |
| RU2007147344A (ru) | Новые производные 2-азетидинона для лечения гиперлипидемических заболеваний | |
| RU2014145819A (ru) | Бициклическое соединение | |
| JP2010527915A5 (el) | ||
| AR077819A1 (es) | Compuestos heterociclicos antagonistas de esfingosina -1-fosfato (sip) | |
| AR042002A1 (es) | Benzoxazinonas sustituidas, proceso de obtencion y usos para tratamiento de enfermedades del sistema nervioso central. | |
| PE20030705A1 (es) | Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades androgeno-dependientes | |
| HUP0303801A2 (hu) | Heterociklusos alkoxi-, alkil-tio- és alkil-amino-benzazol-származékok, mint 5-hidroxi-triptamin-6 ligandumok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények | |
| JP2009518397A5 (el) | ||
| AR041376A1 (es) | Piperazinas sustituidas por heterociclos para el tratamiento de la esquizofrenia | |
| DK1583752T3 (da) | Cykliseringsfremgangsmåde til substituerede benzothiazolderivater |