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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Animal Behavior & Ethology (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (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)
- Medicinal Preparation (AREA)
- Hydrogenated Pyridines (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)
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA74849C2 (en) * | 2000-11-17 | 2006-02-15 | Lilly Co Eli | Lactam |
| US7468365B2 (en) | 2000-11-17 | 2008-12-23 | Eli Lilly And Company | Lactam compound |
| EP1867636B1 (en) | 2005-04-08 | 2013-06-05 | Daiichi Sankyo Company, Limited | Pyridylmethylsulfone derivative |
| WO2006123182A2 (en) | 2005-05-17 | 2006-11-23 | Merck Sharp & Dohme Limited | Cyclohexyl sulphones for treatment of cancer |
| 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 |
| CL2008002060A1 (es) * | 2007-07-16 | 2008-11-21 | Wyeth Corp | Compuestos derivados de sulfonamida, inhibidores de la produccion de beta amiloide; metodo de preparacion; composicion farmaceutica; kit farmaceutico; y uso en el tratamiento de enfermedades tales como alzheimer, angiopatia amiloide, sindrome de down, entre otras. |
| CA2694209C (en) | 2007-08-14 | 2013-09-17 | Eli Lilly And Company | Azepine derivatives as gamma-secretase inhibitors |
| TW200920362A (en) | 2007-09-11 | 2009-05-16 | Daiichi Sankyo Co Ltd | Alkylsulfone derivatives |
| ES2413504T3 (es) | 2007-12-21 | 2013-07-16 | Ligand Pharmaceuticals Inc. | Moduladores selectivos del receptor de andrógeno (SARM) y usos de los mismos |
| 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 |
| MY174452A (en) | 2009-10-14 | 2020-04-19 | Schering Corp | Substituted piperidines that increase p53 activity and the uses thereof |
| US8999957B2 (en) | 2010-06-24 | 2015-04-07 | Merck Sharp & Dohme Corp. | Heterocyclic compounds as ERK inhibitors |
| US8518907B2 (en) | 2010-08-02 | 2013-08-27 | Merck Sharp & Dohme Corp. | RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA) |
| EP3587574B1 (en) | 2010-08-17 | 2022-03-16 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina) |
| US8946216B2 (en) | 2010-09-01 | 2015-02-03 | 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 |
| US9260471B2 (en) | 2010-10-29 | 2016-02-16 | Sirna Therapeutics, Inc. | RNA interference mediated inhibition of gene expression using short interfering nucleic acids (siNA) |
| EP2654748B1 (en) | 2010-12-21 | 2016-07-27 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| US9023865B2 (en) | 2011-10-27 | 2015-05-05 | Merck Sharp & Dohme Corp. | 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 |
| EP3919620A1 (en) | 2012-05-02 | 2021-12-08 | Sirna Therapeutics, Inc. | Short interfering nucleic acid (sina) compositions |
| EP3970725B1 (en) | 2012-09-07 | 2025-08-20 | Massachusetts Eye & Ear Infirmary | A gamma secretase inhibitor for treating hearing loss |
| JP6486272B2 (ja) | 2012-09-07 | 2019-03-20 | マサチューセッツ・アイ・アンド・イア・インファーマリー | 有毛細胞および／または支持細胞再生のための方法および組成物 |
| JP6280554B2 (ja) | 2012-09-28 | 2018-02-14 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | Ｅｒｋ阻害剤である新規化合物 |
| DK2925888T3 (en) | 2012-11-28 | 2017-12-18 | Merck Sharp & Dohme | COMPOSITIONS AND METHODS OF CANCER TREATMENT |
| AR094116A1 (es) | 2012-12-20 | 2015-07-08 | Merck Sharp & Dohme | Imidazopiridinas sustituidas como inhibidores de hdm2 |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| US20160067306A1 (en) | 2013-04-19 | 2016-03-10 | National University Corporation Hokkaido University | Treatment agent for cognitive impairment induced by amyloid beta-protein, therapeutic agent for alzheimer's disease, and treatment method and pathological analysis method related to these |
| US20160194368A1 (en) | 2013-09-03 | 2016-07-07 | Moderna Therapeutics, Inc. | Circular polynucleotides |
| EP3613418A1 (en) | 2014-01-17 | 2020-02-26 | Ligand Pharmaceuticals, Inc. | Methods and compositions for modulating hormone levels |
| EP3212773B1 (en) | 2014-10-29 | 2021-09-15 | Massachusetts Eye and Ear Infirmary | Efficient delivery of therapeutic molecules to cells of the inner ear |
| EP3458076A4 (en) | 2016-05-16 | 2020-01-22 | The General Hospital Corporation | HUMAN RESPIRATORY STEM CELLS IN BREEDING LUNG EPITHEL |
| EP3525785B1 (en) | 2016-10-12 | 2025-08-27 | Merck Sharp & Dohme LLC | Kdm5 inhibitors |
| US10947234B2 (en) | 2017-11-08 | 2021-03-16 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| EP3706747B1 (en) | 2017-11-08 | 2025-09-03 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| US11590152B2 (en) | 2018-01-26 | 2023-02-28 | Massachusetts Eye And Ear Infirmary | Treatment of hearing loss |
| WO2020033284A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US11993602B2 (en) | 2018-08-07 | 2024-05-28 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| EP3833355A4 (en) | 2018-08-07 | 2022-05-11 | Merck Sharp & Dohme Corp. | PRMT5 INHIBITORS |
| BR112021020864A2 (pt) | 2019-04-19 | 2021-12-14 | Ligand Pharm Inc | Formas cristalinas e métodos de produção de formas cristalinas de um composto |
| US20230108114A1 (en) | 2019-12-17 | 2023-04-06 | Merck Sharp & Dohme Llc | Prmt5 inhibitors |
| AU2020408148B2 (en) | 2019-12-17 | 2025-04-24 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| WO2021126729A1 (en) | 2019-12-17 | 2021-06-24 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| CN120225528A (zh) | 2022-09-02 | 2025-06-27 | 默沙东有限责任公司 | 依喜替康衍生的拓扑异构酶-1抑制剂药物组合物及其用途 |
| CR20250146A (es) | 2022-10-25 | 2025-05-26 | Merck Sharp & Dohme Llc | Enlazadores-cargas útiles de adc derivados de exatecán, composiciones farmacéuticas, y usos de los mismos |
| CN120359051A (zh) | 2022-12-14 | 2025-07-22 | 默沙东有限责任公司 | 奥瑞他汀接头-载荷、药物组合物及其用途 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2272305A1 (en) * | 1996-12-23 | 1998-07-02 | Elan Pharmaceuticals, Inc. | Cycloalkyl, lactam, lactone and related compounds as .beta.-amyloid peptide release inhibitors |
| WO1999067219A1 (en) * | 1998-06-22 | 1999-12-29 | Elan Pharmaceuticals, Inc. | Compounds for inhibiting beta-amyloid peptide release and/or its synthesis |
| WO2001034571A1 (en) * | 1999-11-09 | 2001-05-17 | Eli Lilly And Company | β-AMINOACID COMPOUNDS USEFUL FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS |
| 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 |
| UA74849C2 (en) * | 2000-11-17 | 2006-02-15 | Lilly Co Eli | Lactam |
| CA2425558C (en) * | 2000-11-17 | 2012-01-03 | Eli Lilly And Company | Lactam compound |
-
2001
- 2001-05-11 UA UA2003054408A patent/UA74849C2/uk unknown
- 2001-11-05 MX MXPA03004292A patent/MXPA03004292A/es active IP Right Grant
- 2001-11-05 DE DE60126132T patent/DE60126132T2/de not_active Expired - Lifetime
- 2001-11-05 HR HR20030383A patent/HRP20030383B1/xx not_active IP Right Cessation
- 2001-11-05 DZ DZ013453A patent/DZ3453A1/fr active
- 2001-11-05 DK DK01989070T patent/DK1341531T3/da active
- 2001-11-05 CA CA2427227A patent/CA2427227C/en not_active Expired - Fee Related
- 2001-11-05 AU AU2002243192A patent/AU2002243192B2/en not_active Ceased
- 2001-11-05 SK SK559-2003A patent/SK288065B6/sk not_active IP Right Cessation
- 2001-11-05 HU HU0301842A patent/HU228117B1/hu not_active IP Right Cessation
- 2001-11-05 NZ NZ525854A patent/NZ525854A/en not_active IP Right Cessation
- 2001-11-05 JP JP2002549245A patent/JP4116437B2/ja not_active Expired - Fee Related
- 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 KR KR1020037006721A patent/KR100819679B1/ko not_active Expired - Fee Related
- 2001-11-05 PT PT01989070T patent/PT1341531E/pt unknown
- 2001-11-05 IL IL15596001A patent/IL155960A0/xx unknown
- 2001-11-05 SI SI200130701T patent/SI1341531T1/sl unknown
- 2001-11-05 BR BR0115427-3A patent/BR0115427A/pt not_active IP Right Cessation
- 2001-11-05 WO PCT/US2001/027799 patent/WO2002047671A2/en not_active Ceased
- 2001-11-05 CZ CZ20031351A patent/CZ20031351A3/cs unknown
- 2001-11-05 ES ES01989070T patent/ES2278804T3/es not_active Expired - Lifetime
- 2001-11-05 US US10/416,771 patent/US20050261495A1/en not_active Abandoned
- 2001-11-05 EP EP01989070A patent/EP1341531B1/en not_active Expired - Lifetime
- 2001-11-05 PL PL362688A patent/PL212199B1/pl unknown
- 2001-11-05 AU AU4319202A patent/AU4319202A/xx active Pending
- 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 IL IL155960A patent/IL155960A/en not_active IP Right Cessation
- 2003-05-15 ZA ZA200303789A patent/ZA200303789B/en unknown
- 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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Legal Events
| Date | Code | Title | Description |
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| FA | Abandonment or withdrawal |