AR035927A1 - Compuesto de lactama (n)-((s)-2-hidroxi-3-metilbutiril)-1-(l-alaninil)-(s)-1-amino-3-metil-4,5,6,7-tetrahidro-2h-3-benzazepin-2-ona , composicion farmaceutica que lo comprende, procedimiento para la inhibicion de la liberacion de peptido b-amiloide y/o su sintesis que lo emplea y su uso para la fabr - Google Patents
Compuesto de lactama (n)-((s)-2-hidroxi-3-metilbutiril)-1-(l-alaninil)-(s)-1-amino-3-metil-4,5,6,7-tetrahidro-2h-3-benzazepin-2-ona , composicion farmaceutica que lo comprende, procedimiento para la inhibicion de la liberacion de peptido b-amiloide y/o su sintesis que lo emplea y su uso para la fabrInfo
- Publication number
- AR035927A1 AR035927A1 ARP010105312A ARP010105312A AR035927A1 AR 035927 A1 AR035927 A1 AR 035927A1 AR P010105312 A ARP010105312 A AR P010105312A AR P010105312 A ARP010105312 A AR P010105312A AR 035927 A1 AR035927 A1 AR 035927A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- inhibition
- synthesis
- amyloid peptide
- benzazepin
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 230000005764 inhibitory process Effects 0.000 title abstract 4
- 230000015572 biosynthetic process Effects 0.000 title abstract 3
- 238000003786 synthesis reaction Methods 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 abstract 2
- 206010061818 Disease progression Diseases 0.000 abstract 1
- 125000003412 L-alanyl group Chemical group [H]N([H])[C@@](C([H])([H])[H])(C(=O)[*])[H] 0.000 abstract 1
- -1 Lactam compound Chemical class 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 230000005750 disease progression Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Public Health (AREA)
- Genetics & Genomics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24955200P | 2000-11-17 | 2000-11-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR035927A1 true AR035927A1 (es) | 2004-07-28 |
Family
ID=22943982
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010105312A AR035927A1 (es) | 2000-11-17 | 2001-11-14 | Compuesto de lactama (n)-((s)-2-hidroxi-3-metilbutiril)-1-(l-alaninil)-(s)-1-amino-3-metil-4,5,6,7-tetrahidro-2h-3-benzazepin-2-ona , composicion farmaceutica que lo comprende, procedimiento para la inhibicion de la liberacion de peptido b-amiloide y/o su sintesis que lo emplea y su uso para la fabr |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US20050261495A1 (https=) |
| EP (1) | EP1341531B1 (https=) |
| JP (1) | JP4116437B2 (https=) |
| KR (1) | KR100819679B1 (https=) |
| CN (1) | CN1486184A (https=) |
| AR (1) | AR035927A1 (https=) |
| AU (2) | AU4319202A (https=) |
| BR (1) | BR0115427A (https=) |
| CA (1) | CA2427227C (https=) |
| CY (1) | CY1106366T1 (https=) |
| CZ (1) | CZ20031351A3 (https=) |
| DE (1) | DE60126132T2 (https=) |
| DK (1) | DK1341531T3 (https=) |
| DZ (1) | DZ3453A1 (https=) |
| EA (1) | EA005954B1 (https=) |
| EC (1) | ECSP034600A (https=) |
| ES (1) | ES2278804T3 (https=) |
| HR (1) | HRP20030383B1 (https=) |
| HU (1) | HU228117B1 (https=) |
| IL (2) | IL155960A0 (https=) |
| MX (1) | MXPA03004292A (https=) |
| MY (1) | MY134559A (https=) |
| NO (1) | NO324324B1 (https=) |
| NZ (1) | NZ525854A (https=) |
| PE (1) | PE20020802A1 (https=) |
| PL (1) | PL212199B1 (https=) |
| PT (1) | PT1341531E (https=) |
| SI (1) | SI1341531T1 (https=) |
| SK (1) | SK288065B6 (https=) |
| TW (1) | TWI305204B (https=) |
| UA (1) | UA74849C2 (https=) |
| WO (1) | WO2002047671A2 (https=) |
| ZA (1) | ZA200303789B (https=) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7468365B2 (en) | 2000-11-17 | 2008-12-23 | Eli Lilly And Company | Lactam compound |
| UA74849C2 (en) * | 2000-11-17 | 2006-02-15 | Lilly Co Eli | Lactam |
| AU2006234441B2 (en) | 2005-04-08 | 2011-07-07 | Daiichi Sankyo Company, Limited | Pyridylmethylsulfone derivative |
| ES2382814T3 (es) | 2005-05-17 | 2012-06-13 | Merck Sharp & Dohme Ltd. | Ácido cis-4-[(4-clorofenil)sulfonil]-4-(2,5-difluorofenil)ciclohexanopropanoico para el tratamiento del cáncer |
| JP5198877B2 (ja) | 2006-01-31 | 2013-05-15 | 株式会社エーピーアイ コーポレーション | ベンゾアゼピノン類の製造方法 |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| JP2010533723A (ja) * | 2007-07-16 | 2010-10-28 | ワイス・エルエルシー | βアミロイド生成の阻害剤 |
| JP5385904B2 (ja) | 2007-08-14 | 2014-01-08 | イーライ リリー アンド カンパニー | γ−セクレターゼ阻害剤 |
| TW200920362A (en) | 2007-09-11 | 2009-05-16 | Daiichi Sankyo Co Ltd | Alkylsulfone derivatives |
| EP2222636B1 (en) | 2007-12-21 | 2013-04-10 | Ligand Pharmaceuticals Inc. | Selective androgen receptor modulators (sarms) and uses thereof |
| EP2291181B9 (en) | 2008-04-18 | 2013-09-11 | University College Dublin National University Of Ireland, Dublin | Captodiamine for the treatment of depression symptoms |
| WO2010114780A1 (en) | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| PE20121172A1 (es) | 2009-10-14 | 2012-09-05 | Merck Sharp & Dohme | Piperidinas sustituidas con actividad en la hdm2 |
| WO2011163330A1 (en) | 2010-06-24 | 2011-12-29 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| EP3330377A1 (en) | 2010-08-02 | 2018-06-06 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina) |
| US9029341B2 (en) | 2010-08-17 | 2015-05-12 | Sirna Therapeutics, Inc. | RNA interference mediated inhibition of hepatitis B virus (HBV) gene expression using short interfering nucleic acid (siNA) |
| EP2613782B1 (en) | 2010-09-01 | 2016-11-02 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| US9242981B2 (en) | 2010-09-16 | 2016-01-26 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel ERK inhibitors |
| WO2012040444A2 (en) * | 2010-09-24 | 2012-03-29 | Bristol-Myers Squibb Company | Treatment of patients with incipient alzheimer's disease |
| WO2012058210A1 (en) | 2010-10-29 | 2012-05-03 | Merck Sharp & Dohme Corp. | RNA INTERFERENCE MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERING NUCLEIC ACIDS (siNA) |
| WO2012087772A1 (en) | 2010-12-21 | 2012-06-28 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| EP2770987B1 (en) | 2011-10-27 | 2018-04-04 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| CN102690231B (zh) * | 2012-04-11 | 2014-07-09 | 南京友杰医药科技有限公司 | 治疗阿尔茨海默病潜在药物司马西特的合成方法 |
| US20150299696A1 (en) | 2012-05-02 | 2015-10-22 | Sirna Therapeutics, Inc. | SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS |
| US20150209406A1 (en) | 2012-09-07 | 2015-07-30 | Massachusetts Eye And Ear Infirmary | Methods and compositions for regenerating hair cells and/or supporting cells |
| US20150209367A1 (en) | 2012-09-07 | 2015-07-30 | Massachusetts Eye & Ear Infirmary | Treating Hearing Loss |
| RU2660429C2 (ru) | 2012-09-28 | 2018-07-06 | Мерк Шарп И Доум Корп. | Новые соединения, которые являются ингибиторами erk |
| RS56680B1 (sr) | 2012-11-28 | 2018-03-30 | Merck Sharp & Dohme | Kompozicije i postupci za lečenje kancera |
| KR102196882B1 (ko) | 2012-12-20 | 2020-12-30 | 머크 샤프 앤드 돔 코포레이션 | Hdm2 억제제로서의 치환된 이미다조피리딘 |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| JP6319912B2 (ja) | 2013-04-19 | 2018-05-09 | 国立大学法人 岡山大学 | アミロイドβ蛋白質により誘発される認知障害の治療剤およびアルツハイマー病治療薬、ならびにこれらに関連する治療方法および病態解析方法 |
| WO2015034925A1 (en) | 2013-09-03 | 2015-03-12 | Moderna Therapeutics, Inc. | Circular polynucleotides |
| US10441567B2 (en) | 2014-01-17 | 2019-10-15 | Ligand Pharmaceuticals Incorporated | Methods and compositions for modulating hormone levels |
| US11370823B2 (en) | 2014-10-29 | 2022-06-28 | Massachusetts Eye And Ear Infirmary | Efficient delivery of therapeutic molecules to cells of the inner ear |
| JP6840774B2 (ja) | 2016-05-16 | 2021-03-10 | ザ ジェネラル ホスピタル コーポレイション | 肺上皮エンジニアリングにおけるヒト気道幹細胞 |
| EP3525785B1 (en) | 2016-10-12 | 2025-08-27 | Merck Sharp & Dohme LLC | Kdm5 inhibitors |
| EP3706747B1 (en) | 2017-11-08 | 2025-09-03 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| US10947234B2 (en) | 2017-11-08 | 2021-03-16 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| WO2019148067A1 (en) | 2018-01-26 | 2019-08-01 | Massachusetts Eye And Ear Infirmary | Treatment of hearing loss |
| US12173026B2 (en) | 2018-08-07 | 2024-12-24 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| US11981701B2 (en) | 2018-08-07 | 2024-05-14 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| US12552826B2 (en) | 2018-08-07 | 2026-02-17 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| EP3833668B1 (en) | 2018-08-07 | 2025-03-19 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2020214834A1 (en) | 2019-04-19 | 2020-10-22 | Ligand Pharmaceuticals Inc. | Crystalline forms and methods of producing crystalline forms of a compound |
| US12441730B2 (en) | 2019-12-17 | 2025-10-14 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| US12595248B2 (en) | 2019-12-17 | 2026-04-07 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| BR112022012015A2 (pt) | 2019-12-17 | 2022-08-30 | Merck Sharp & Dohme Llc | Inibidores de prmt5 |
| WO2021126731A1 (en) | 2019-12-17 | 2021-06-24 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US20240116945A1 (en) | 2022-09-02 | 2024-04-11 | Merck Sharp & Dohme Llc | Exatecan-derived topoisomerase-1 inhibitors pharmaceutical compositions, and uses thereof |
| WO2024091437A1 (en) | 2022-10-25 | 2024-05-02 | Merck Sharp & Dohme Llc | Exatecan-derived adc linker-payloads, pharmaceutical compositions, and uses thereof |
| GEAP202516798A (en) | 2022-12-14 | 2025-10-27 | Merck Sharp & Dohme Llc | Auristatin linker-payloads, pharmaceutical compositions, and uses thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0001232A3 (en) * | 1996-12-23 | 2001-02-28 | Elan Pharmaceuticals Inc San F | Cycloalkyl, lactam, lactone derivatives and their thio analogues inhibiting betha-amyloid peptide release and/or its synthesis and pharmaceutical compositions containing the compounds |
| JP2002518481A (ja) * | 1998-06-22 | 2002-06-25 | エラン ファーマシューティカルズ，インコーポレイテッド | β−アミロイドペプチドの放出および／またはその合成を阻害するための化合物 |
| JP2003513958A (ja) * | 1999-11-09 | 2003-04-15 | イーライ・リリー・アンド・カンパニー | β−アミロイドペプチド放出および／またはその合成を阻害するために有用なβ−アミノ酸化合物 |
| EP1345955B1 (en) * | 2000-11-17 | 2008-08-20 | Eli Lilly And Company | Lactam dipeptide and its use in inhibiting beta-amyloid peptide release |
| UA74849C2 (en) * | 2000-11-17 | 2006-02-15 | Lilly Co Eli | Lactam |
| UA77165C2 (en) * | 2000-11-17 | 2006-11-15 | Lilly Co Eli | (n)-((s)-2-hydroxy-3-methyl-butyryl)-1-(l-alaninyl)-(s)-1-amino-3-methyl-4,5,6,7-tetrahydro-2h-3-benzazepin-2-one dihydrate, processes for manufacturing and pharmaceutical composition |
-
2001
- 2001-05-11 UA UA2003054408A patent/UA74849C2/uk unknown
- 2001-11-05 WO PCT/US2001/027799 patent/WO2002047671A2/en not_active Ceased
- 2001-11-05 DK DK01989070T patent/DK1341531T3/da active
- 2001-11-05 NZ NZ525854A patent/NZ525854A/en not_active IP Right Cessation
- 2001-11-05 DZ DZ013453A patent/DZ3453A1/fr active
- 2001-11-05 AU AU4319202A patent/AU4319202A/xx active Pending
- 2001-11-05 CN CNA018221009A patent/CN1486184A/zh active Pending
- 2001-11-05 EA EA200300580A patent/EA005954B1/ru not_active IP Right Cessation
- 2001-11-05 PT PT01989070T patent/PT1341531E/pt unknown
- 2001-11-05 BR BR0115427-3A patent/BR0115427A/pt not_active IP Right Cessation
- 2001-11-05 EP EP01989070A patent/EP1341531B1/en not_active Expired - Lifetime
- 2001-11-05 JP JP2002549245A patent/JP4116437B2/ja not_active Expired - Fee Related
- 2001-11-05 CZ CZ20031351A patent/CZ20031351A3/cs unknown
- 2001-11-05 HR HR20030383A patent/HRP20030383B1/xx not_active IP Right Cessation
- 2001-11-05 CA CA2427227A patent/CA2427227C/en not_active Expired - Fee Related
- 2001-11-05 US US10/416,771 patent/US20050261495A1/en not_active Abandoned
- 2001-11-05 HU HU0301842A patent/HU228117B1/hu not_active IP Right Cessation
- 2001-11-05 IL IL15596001A patent/IL155960A0/xx unknown
- 2001-11-05 MX MXPA03004292A patent/MXPA03004292A/es active IP Right Grant
- 2001-11-05 AU AU2002243192A patent/AU2002243192B2/en not_active Ceased
- 2001-11-05 DE DE60126132T patent/DE60126132T2/de not_active Expired - Lifetime
- 2001-11-05 ES ES01989070T patent/ES2278804T3/es not_active Expired - Lifetime
- 2001-11-05 PL PL362688A patent/PL212199B1/pl unknown
- 2001-11-05 KR KR1020037006721A patent/KR100819679B1/ko not_active Expired - Fee Related
- 2001-11-05 SI SI200130701T patent/SI1341531T1/sl unknown
- 2001-11-05 SK SK559-2003A patent/SK288065B6/sk not_active IP Right Cessation
- 2001-11-12 TW TW090128005A patent/TWI305204B/zh not_active IP Right Cessation
- 2001-11-14 AR ARP010105312A patent/AR035927A1/es not_active Application Discontinuation
- 2001-11-15 MY MYPI20015236A patent/MY134559A/en unknown
- 2001-11-16 PE PE2001001142A patent/PE20020802A1/es not_active Application Discontinuation
-
2003
- 2003-05-13 EC EC2003004600A patent/ECSP034600A/es unknown
- 2003-05-15 ZA ZA200303789A patent/ZA200303789B/en unknown
- 2003-05-15 IL IL155960A patent/IL155960A/en not_active IP Right Cessation
- 2003-05-16 NO NO20032236A patent/NO324324B1/no not_active IP Right Cessation
-
2007
- 2007-03-09 CY CY20071100331T patent/CY1106366T1/el unknown
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