CR8264A - Derivados de malonamida bloqueadores de la actividad gamma-secretase - Google Patents
Derivados de malonamida bloqueadores de la actividad gamma-secretaseInfo
- Publication number
- CR8264A CR8264A CR8264A CR8264A CR8264A CR 8264 A CR8264 A CR 8264A CR 8264 A CR8264 A CR 8264A CR 8264 A CR8264 A CR 8264A CR 8264 A CR8264 A CR 8264A
- Authority
- CR
- Costa Rica
- Prior art keywords
- lower alkyl
- blockers
- gamma
- halogen
- secretase activity
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
-
- 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
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
- A61K31/558—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
-
- 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
- C07D223/18—Dibenzazepines; Hydrogenated dibenzazepines
- C07D223/20—Dibenz [b, e] azepines; Hydrogenated dibenz [b, e] azepines
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
- C07D313/02—Seven-membered rings
- C07D313/06—Seven-membered rings condensed with carbocyclic rings or ring systems
- C07D313/10—Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
- C07D313/14—[b,f]-condensed
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Pyrane Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
La invencion se refire a derivados de malonamida de la formula I en la que R1 es uno de los grupos siguientes a), b), c), d) R2 es alquilo inferior, alquinilo inferior, -(CH2) n- O -alquilo inferior, -(CH2) n-S-alquilo inferior, -(CH2) n -CN, -(CR'R") n -CF3, -(CR'R") n -CHF2, -(CR'R") n-CH2F,-(CH2)n-C (O) O-alquilo inferior, (CH2) n- halogeno, o es - (CH2) n- cicloalquilo, opcionalmente sustituido por uno o varios sustituyentes elegidos entre el grupo formado por fenilo, halogeno y CF3; R',R" con independencia de n y con independencia entre si son hidrogeno, alquilo inferior, alcoxi inferior, halogeno o hidroxi; R3, R4 con independencia entre si son hidrogeno, alquilo inferior, alcoxi inferior, fenilo o halogeno; R5 es hidrogeno, alquilo inferior, -(CH2) n -CF3 o - (CH2) n- cicloalquilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03019683 | 2003-09-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR8264A true CR8264A (es) | 2008-09-22 |
Family
ID=34224068
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR8264A CR8264A (es) | 2003-09-09 | 2006-03-01 | Derivados de malonamida bloqueadores de la actividad gamma-secretase |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US7160875B2 (es) |
| EP (1) | EP1711470B1 (es) |
| JP (2) | JP4571639B2 (es) |
| KR (3) | KR100838852B1 (es) |
| CN (1) | CN100593539C (es) |
| AR (1) | AR045609A1 (es) |
| AT (1) | ATE428698T1 (es) |
| AU (1) | AU2004270361B2 (es) |
| BR (1) | BRPI0413533A (es) |
| CA (1) | CA2537440C (es) |
| CO (1) | CO5660268A2 (es) |
| CR (1) | CR8264A (es) |
| CY (1) | CY1109225T1 (es) |
| DE (1) | DE602004020680D1 (es) |
| DK (1) | DK1711470T3 (es) |
| EA (1) | EA009940B1 (es) |
| EC (1) | ECSP066414A (es) |
| ES (1) | ES2322652T3 (es) |
| HK (1) | HK1099014A1 (es) |
| HR (1) | HRP20090266T1 (es) |
| IL (1) | IL173905A (es) |
| MA (1) | MA28034A1 (es) |
| MX (1) | MXPA06002562A (es) |
| MY (1) | MY141308A (es) |
| NO (1) | NO20061047L (es) |
| NZ (1) | NZ545538A (es) |
| PL (1) | PL1711470T3 (es) |
| PT (1) | PT1711470E (es) |
| RS (1) | RS20060146A (es) |
| SI (1) | SI1711470T1 (es) |
| TN (1) | TNSN06077A1 (es) |
| TW (1) | TW200519092A (es) |
| UA (1) | UA83501C2 (es) |
| WO (1) | WO2005023772A1 (es) |
| ZA (1) | ZA200601989B (es) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05008172A (es) * | 2003-02-04 | 2005-10-05 | Hoffmann La Roche | Derivados de malonamida como inhibidores gamma-secretasa. |
| NZ545538A (en) * | 2003-09-09 | 2008-12-24 | Hoffmann La Roche | Malonamide derivatives blocking the activity of gama-secretase |
| DK1673347T3 (en) * | 2003-10-06 | 2015-10-12 | Hoffmann La Roche | SUBSTITUTED DIBENZO-AZEPINE AND BENZO-DIAZEPINE DERIVATIVES USED AS GAMMA SECRETASE INHIBITORS |
| US7211573B2 (en) | 2004-12-08 | 2007-05-01 | Hoffmann-La Roche Inc. | Malonamide derivatives |
| EP2018368B1 (en) * | 2006-03-27 | 2012-12-05 | F. Hoffmann-La Roche AG | Malonamide derivatives as gamma secretase inhibitors |
| JP5001372B2 (ja) | 2006-09-20 | 2012-08-15 | エフ．ホフマン−ラ ロシュ アーゲー | ４−オキソ−２，３，４，５−テトラヒドロ−ベンゾ［ｂ］［１，４］ジアゼピン誘導体 |
| 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 |
| JP5148636B2 (ja) * | 2007-03-15 | 2013-02-20 | エフ．ホフマン−ラ ロシュ アーゲー | オレキシンアンタゴニストとしてのマロンアミド |
| US7579464B2 (en) * | 2007-05-25 | 2009-08-25 | Hoffmann-La Roche Inc. | Process for preparation of enantiomerically pure compounds |
| US8741889B2 (en) | 2008-01-11 | 2014-06-03 | Hoffmann-La Roche Inc | Method of treating non-small cell lung cancer and colon cancer with gamma-secretase inhibitor |
| US20090181944A1 (en) * | 2008-01-11 | 2009-07-16 | John Frederick Boylan | Method for cancer therapy |
| US8309299B2 (en) * | 2010-05-19 | 2012-11-13 | Hoffmann-La Roche Inc. | Combination therapy and method for assessing resistance to treatment |
| WO2012040444A2 (en) * | 2010-09-24 | 2012-03-29 | Bristol-Myers Squibb Company | Treatment of patients with incipient alzheimer's disease |
| KR101330184B1 (ko) | 2010-10-15 | 2013-11-15 | 성균관대학교산학협력단 | 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물 |
| WO2012050370A2 (ko) * | 2010-10-15 | 2012-04-19 | 성균관대학교산학협력단 | 감마-세크레타제 저해제를 유효성분으로 함유하는 류마티스성 관절염의 예방 또는 치료용 조성물 |
| US20120114638A1 (en) | 2010-11-08 | 2012-05-10 | John Boylan | Combination therapy |
| US20120184529A1 (en) | 2011-01-14 | 2012-07-19 | Demario Mark D | Combination therapy |
| US20120225860A1 (en) | 2011-03-02 | 2012-09-06 | John Frederick Boylan | Method for administration of a gamma secretase inhibitor |
| TWI530489B (zh) | 2011-03-22 | 2016-04-21 | 必治妥美雅史谷比公司 | 雙（氟烷基）－１，４－苯二氮呯酮化合物 |
| AR087107A1 (es) | 2011-07-27 | 2014-02-12 | Lilly Co Eli | Compuesto inhibidor de la señalizacion de la trayectoria notch |
| TWI614238B (zh) | 2012-09-21 | 2018-02-11 | 必治妥美雅史谷比公司 | 雙（氟烷基）－１，４－苯并二氮呯酮化合物及其前藥 |
| EP2897946B1 (en) | 2012-09-21 | 2016-11-16 | Bristol-Myers Squibb Company | N-substituted bis(fluoroalkkyl)-1,4-benzodiazepinone compounds as notch inhibitors |
| EP2897960B1 (en) | 2012-09-21 | 2016-08-03 | Bristol-Myers Squibb Company | Tricyclic heterocyclic compounds as notch inhibitors |
| WO2014047397A1 (en) | 2012-09-21 | 2014-03-27 | Bristol-Myers Squibb Company | Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds as notch|inhibitors |
| WO2014047370A1 (en) | 2012-09-21 | 2014-03-27 | Bristol-Myers Squibb Company | Fluoroalkyl dibenzodiazepinone compounds |
| US9133139B2 (en) | 2012-09-21 | 2015-09-15 | Bristol-Myers Squibb Company | Fluoroalkyl-1,4-benzodiazepinone compounds |
| JP2015534554A (ja) | 2012-09-21 | 2015-12-03 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アルキル，フルオロアルキル−１，４−ベンゾジアゼピノン化合物 |
| JP2015531792A (ja) | 2012-09-21 | 2015-11-05 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | １，４−ベンゾジアゼピノン化合物のプロドラッグ |
| US9187434B2 (en) | 2012-09-21 | 2015-11-17 | Bristol-Myers Squibb Company | Substituted 1,5-benzodiazepinones compounds |
| CN105101968A (zh) | 2013-04-04 | 2015-11-25 | 百时美施贵宝公司 | 治疗增殖性疾病的组合疗法 |
| EP2932966A1 (en) | 2014-04-16 | 2015-10-21 | Novartis AG | Gamma secretase inhibitors for treating respiratory diseases |
| 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 |
| RU2757276C2 (ru) * | 2016-12-16 | 2021-10-12 | Пайплайн Терапьютикс, Инк. | Способы лечения кохлеарной синаптопатии |
| EP3615068A1 (en) | 2017-04-28 | 2020-03-04 | Novartis AG | Bcma-targeting agent, and combination therapy with a gamma secretase inhibitor |
| EP3615055A1 (en) | 2017-04-28 | 2020-03-04 | Novartis AG | Cells expressing a bcma-targeting chimeric antigen receptor, and combination therapy with a gamma secretase inhibitor |
| US11161825B2 (en) * | 2017-08-15 | 2021-11-02 | Bayer Aktiengesellschaft | 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7-carboxamides |
| EP3802611A2 (en) | 2018-06-01 | 2021-04-14 | Novartis AG | Binding molecules against bcma and uses thereof |
| CA3144324A1 (en) | 2019-06-24 | 2020-12-30 | Novartis Ag | Dosing regimen and combination therapies for multispecific antibodies targeting b-cell maturation antigen |
| WO2023031200A1 (en) * | 2021-08-31 | 2023-03-09 | Basf Se | Herbicidal malonamides containing a condensed ring system |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2404273A1 (en) * | 2000-04-11 | 2001-10-18 | Bristol-Myers Squibb Pharma Company | Substituted lactams as inhibitors of a.beta. protein production |
| GB0012671D0 (en) * | 2000-05-24 | 2000-07-19 | Merck Sharp & Dohme | Therapeutic agents |
| MXPA05008172A (es) * | 2003-02-04 | 2005-10-05 | Hoffmann La Roche | Derivados de malonamida como inhibidores gamma-secretasa. |
| NZ545538A (en) * | 2003-09-09 | 2008-12-24 | Hoffmann La Roche | Malonamide derivatives blocking the activity of gama-secretase |
-
2004
- 2004-08-31 NZ NZ545538A patent/NZ545538A/en not_active IP Right Cessation
- 2004-08-31 RS YUP-2006/0146A patent/RS20060146A/sr unknown
- 2004-08-31 EP EP04764665A patent/EP1711470B1/en active Active
- 2004-08-31 SI SI200431116T patent/SI1711470T1/sl unknown
- 2004-08-31 BR BRPI0413533-4A patent/BRPI0413533A/pt not_active Application Discontinuation
- 2004-08-31 JP JP2006525701A patent/JP4571639B2/ja active Active
- 2004-08-31 ES ES04764665T patent/ES2322652T3/es active Active
- 2004-08-31 PT PT04764665T patent/PT1711470E/pt unknown
- 2004-08-31 DK DK04764665T patent/DK1711470T3/da active
- 2004-08-31 DE DE602004020680T patent/DE602004020680D1/de active Active
- 2004-08-31 UA UAA200602854A patent/UA83501C2/uk unknown
- 2004-08-31 WO PCT/EP2004/009700 patent/WO2005023772A1/en active Application Filing
- 2004-08-31 CN CN200480032641A patent/CN100593539C/zh active Active
- 2004-08-31 MX MXPA06002562A patent/MXPA06002562A/es active IP Right Grant
- 2004-08-31 KR KR1020077017457A patent/KR100838852B1/ko active IP Right Grant
- 2004-08-31 KR KR1020077017458A patent/KR20070087233A/ko not_active Application Discontinuation
- 2004-08-31 AT AT04764665T patent/ATE428698T1/de active
- 2004-08-31 KR KR1020067004763A patent/KR100834177B1/ko active IP Right Grant
- 2004-08-31 CA CA2537440A patent/CA2537440C/en not_active Expired - Fee Related
- 2004-08-31 EA EA200600503A patent/EA009940B1/ru not_active IP Right Cessation
- 2004-08-31 AU AU2004270361A patent/AU2004270361B2/en not_active Ceased
- 2004-08-31 PL PL04764665T patent/PL1711470T3/pl unknown
- 2004-09-02 US US10/933,177 patent/US7160875B2/en active Active
- 2004-09-06 MY MYPI20043603A patent/MY141308A/en unknown
- 2004-09-06 TW TW093126876A patent/TW200519092A/zh unknown
- 2004-09-08 AR ARP040103214A patent/AR045609A1/es not_active Application Discontinuation
-
2006
- 2006-02-23 IL IL173905A patent/IL173905A/en active IP Right Grant
- 2006-02-23 CO CO06018272A patent/CO5660268A2/es not_active Application Discontinuation
- 2006-03-01 CR CR8264A patent/CR8264A/es not_active Application Discontinuation
- 2006-03-03 NO NO20061047A patent/NO20061047L/no not_active Application Discontinuation
- 2006-03-07 TN TNP2006000077A patent/TNSN06077A1/fr unknown
- 2006-03-07 EC EC2006006414A patent/ECSP066414A/es unknown
- 2006-03-08 ZA ZA200601989A patent/ZA200601989B/en unknown
- 2006-03-10 MA MA28867A patent/MA28034A1/fr unknown
-
2007
- 2007-05-21 HK HK07105326.7A patent/HK1099014A1/xx not_active IP Right Cessation
-
2009
- 2009-05-12 HR HR20090266T patent/HRP20090266T1/xx unknown
- 2009-07-10 CY CY20091100729T patent/CY1109225T1/el unknown
-
2010
- 2010-06-18 JP JP2010138970A patent/JP2010229153A/ja active Pending
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