ATE435219T1 - Heteroaryl substituierte spirocyclische sulfamide zur hemmung von gamma sekretase - Google Patents
Heteroaryl substituierte spirocyclische sulfamide zur hemmung von gamma sekretaseInfo
- Publication number
- ATE435219T1 ATE435219T1 AT03722769T AT03722769T ATE435219T1 AT E435219 T1 ATE435219 T1 AT E435219T1 AT 03722769 T AT03722769 T AT 03722769T AT 03722769 T AT03722769 T AT 03722769T AT E435219 T1 ATE435219 T1 AT E435219T1
- Authority
- AT
- Austria
- Prior art keywords
- sulfamides
- heteroaryl substituted
- gamma secretase
- substituted spirocyclic
- inhibit gamma
- Prior art date
Links
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 title abstract 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0209996A GB0209996D0 (en) | 2002-05-01 | 2002-05-01 | Therapeutic agents |
| GB0223873A GB0223873D0 (en) | 2002-10-14 | 2002-10-14 | Therapeutic agents |
| US42460802P | 2002-11-07 | 2002-11-07 | |
| PCT/GB2003/001763 WO2003093252A1 (en) | 2002-05-01 | 2003-04-24 | Heteroaryl substituted spirocyclic sulfamides for inhibition of gamma secretase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE435219T1 true ATE435219T1 (de) | 2009-07-15 |
Family
ID=29407321
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT03722769T ATE435219T1 (de) | 2002-05-01 | 2003-04-24 | Heteroaryl substituierte spirocyclische sulfamide zur hemmung von gamma sekretase |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US7041689B2 (de) |
| EP (1) | EP1503998B1 (de) |
| AT (1) | ATE435219T1 (de) |
| AU (1) | AU2003229932B2 (de) |
| CA (1) | CA2484159C (de) |
| DE (1) | DE60328182D1 (de) |
| WO (1) | WO2003093252A1 (de) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60112957T2 (de) * | 2000-11-02 | 2006-05-18 | Merck Sharp & Dohme Ltd., Hoddesdon | Sulfamide als gamma-secretase-inhibitoren |
| US7399775B2 (en) | 2001-12-27 | 2008-07-15 | Daiichi Pharmaceutical Co., Ltd. | β-amyloid protein production/secretion inhibitor |
| GB0209995D0 (en) * | 2002-05-01 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
| CA2484159C (en) * | 2002-05-01 | 2011-02-22 | Merck Sharp & Dohme Limited | Heteroaryl substituted spirocyclic sulfamides for inhibition of gamma secretase |
| GB0225475D0 (en) * | 2002-11-01 | 2002-12-11 | Merck Sharp & Dohme | Therapeutic agents |
| US7521481B2 (en) * | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| GB0308318D0 (en) * | 2003-04-10 | 2003-05-14 | Merck Sharp & Dohme | Therapeutic agents |
| PL379466A1 (pl) | 2003-06-30 | 2006-09-18 | Daiichi Sankyo Company , Limited | Heterocykliczne pochodne metylosulfonu |
| WO2005030731A1 (en) * | 2003-09-24 | 2005-04-07 | Merck Sharp & Dohme Limited | Gamma-secretase inhibitors |
| ATE550019T1 (de) | 2005-05-17 | 2012-04-15 | Merck Sharp & Dohme | Cis-4-ä(4-chlorophenyl)sulfonylü-4-(2,5- difluorophenyl)cyclohexanepropansäure zur behandlug von krebs |
| US8242103B2 (en) | 2005-05-19 | 2012-08-14 | Merck Sharp & Dohme Limited | Sulphamides for treatment of cancer |
| EP2198863A1 (de) | 2006-02-27 | 2010-06-23 | The Johns Hopkins University | Krebsbehandlung mit gamma-sekretasehemmern |
| WO2008076556A2 (en) | 2006-11-15 | 2008-06-26 | Massachusetts Eye & Ear Infirmary | Generation of inner ear cells |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| WO2009128057A2 (en) | 2008-04-18 | 2009-10-22 | UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al | Psycho-pharmaceuticals |
| ES2714453T3 (es) * | 2008-06-09 | 2019-05-28 | Univ Muenchen Ludwig Maximilians | Fármacos para inhibir la agregación de proteínas implicadas en enfermedades relacionadas con enfermedades neurodegenerativas y/o agregación de proteínas |
| WO2010060088A2 (en) | 2008-11-24 | 2010-05-27 | Massachusetts Eye & Ear Infirmary | Pathways to generate hair cells |
| TWI519530B (zh) | 2009-02-20 | 2016-02-01 | 艾伯維德國有限及兩合公司 | 羰醯胺化合物及其作為鈣蛋白酶（ｃａｌｐａｉｎ）抑制劑之用途 |
| EP2413932A4 (de) | 2009-04-01 | 2012-09-19 | Merck Sharp & Dohme | Hemmer der akt-aktivität |
| CA2777043C (en) | 2009-10-14 | 2015-12-15 | Schering Corporation | Substituted piperidines that increase p53 activity and the uses thereof |
| BR112012014884A2 (pt) * | 2009-12-17 | 2016-03-22 | Merck Patent Gmbh | inibidores de esfingosina quinase |
| EP2584903B1 (de) | 2010-06-24 | 2018-10-24 | Merck Sharp & Dohme Corp. | Neue heterozyklische verbindungen als erk-hemmer |
| CN103068980B (zh) | 2010-08-02 | 2017-04-05 | 瑟纳治疗公司 | 使用短干扰核酸（siNA）的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1（CTNNB1）基因表达的抑制 |
| RU2745848C2 (ru) | 2010-08-17 | 2021-04-01 | Сирна Терапьютикс, Инк. | ОПОСРЕДУЕМОЕ РНК-ИНТЕРФЕРЕНЦИЕЙ ИНГИБИРОВАНИЕ ЭКСПРЕССИИ ГЕНОВ ВИРУСА ГЕПАТИТА B (HBV) С ПРИМЕНЕНИЕМ МАЛОЙ ИНТЕРФЕРИРУЮЩЕЙ НУКЛЕИНОВОЙ КИСЛОТЫ (миНК) |
| EP2613782B1 (de) | 2010-09-01 | 2016-11-02 | Merck Sharp & Dohme Corp. | Indazolderivate als erk-hemmer |
| US9242981B2 (en) | 2010-09-16 | 2016-01-26 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel ERK inhibitors |
| 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 (de) | 2011-10-27 | 2018-04-04 | Merck Sharp & Dohme Corp. | Neue verbindungen als erk-hemmer |
| EP3919620A1 (de) | 2012-05-02 | 2021-12-08 | Sirna Therapeutics, Inc. | Zusammensetzungen mit kurzer interferierender nukleinsäure (sina) |
| EP2892506B1 (de) | 2012-09-07 | 2021-11-03 | Massachusetts Eye & Ear Infirmary | Behandlung von gehörverlust mit dem gamma-secretase inhibitor ly411575 |
| CA2884309A1 (en) | 2012-09-07 | 2014-03-13 | Massachusetts Eye And Ear Infirmary | Methods and compositions for regenerating hair cells and/or supporting cells from differentiated cochlear cells or differentiated utricular cells by modulation of notch and cmyc activity |
| CA2882950A1 (en) | 2012-09-28 | 2014-04-03 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| SMT201700595T1 (it) | 2012-11-28 | 2018-03-08 | Merck Sharp & Dohme | Composizioni e metodi per trattare il cancro |
| WO2014100065A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| WO2015034925A1 (en) | 2013-09-03 | 2015-03-12 | Moderna Therapeutics, Inc. | Circular polynucleotides |
| WO2016022776A2 (en) | 2014-08-06 | 2016-02-11 | Massachusetts Eye And Ear Infirmary | Increasing atoh1 life to drive sensorineural hair cell differentiantion |
| WO2017096233A1 (en) | 2015-12-04 | 2017-06-08 | Massachusetts Eye And Ear Infirmary | Treatment of hearing loss by inhibition of casein kinase 1 |
| CN109219439B (zh) | 2016-01-29 | 2022-09-20 | 马萨诸塞眼科耳科诊所 | 内耳支持细胞的扩增和分化及其使用方法 |
| KR102362222B1 (ko) | 2016-05-16 | 2022-02-11 | 더 제너럴 하스피탈 코포레이션 | 폐 상피 공학에서 인간 기도 줄기 세포 |
| US10975084B2 (en) | 2016-10-12 | 2021-04-13 | Merck Sharp & Dohme Corp. | KDM5 inhibitors |
| EP3554502A4 (de) | 2016-12-16 | 2021-01-06 | Pipeline Therapeutics, Inc. | Verfahren zur behandlung von cochlea-synaptopathie |
| EP3706742B1 (de) | 2017-11-08 | 2023-03-15 | Merck Sharp & Dohme LLC | Prmt5-inhibitoren |
| WO2019094312A1 (en) | 2017-11-08 | 2019-05-16 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2020033285A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| CA3108388A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2020033282A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| EP3833667B1 (de) | 2018-08-07 | 2024-03-13 | Merck Sharp & Dohme LLC | Prmt5-inhibitoren |
| EP4076460B1 (de) | 2019-12-17 | 2026-01-21 | Merck Sharp & Dohme LLC | 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidin]-derivate als prmt5 inhibitoren zur behandlung von krebs |
| ES3074517T3 (en) | 2019-12-17 | 2026-07-21 | Merck Sharp & Dohme Llc | 4-(3,4-dihydroisoquinolin-2(1h)-yl)-3-hydroxypiperidine derivatives as prmt5 inhibitors for the treatment of cancer and sickle cell disease |
| EP4076459B1 (de) | 2019-12-17 | 2026-04-29 | Merck Sharp & Dohme LLC | Prmt5-inhibitoren |
| ES3022307T3 (en) | 2019-12-17 | 2025-05-28 | Merck Sharp & Dohme Llc | 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 |
| KR20250079227A (ko) | 2022-10-25 | 2025-06-04 | 머크 샤프 앤드 돔 엘엘씨 | 엑사테칸-유래 adc 링커-페이로드, 제약 조성물, 및 그의 용도 |
| KR20250116773A (ko) | 2022-12-14 | 2025-08-01 | 머크 샤프 앤드 돔 엘엘씨 | 아우리스타틴 링커-페이로드, 제약 조성물, 및 그의 용도 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3406184A (en) * | 1966-05-04 | 1968-10-15 | Du Pont | Addition compounds of norbornadienes and quadricyclenes with bis(trifluoromethyl) thioketene and their s-oxides and s-dioxides |
| US3715362A (en) * | 1970-08-17 | 1973-02-06 | Lilly Co Eli | Tetracyclic aziridine and method for its preparation |
| US5703129A (en) * | 1996-09-30 | 1997-12-30 | Bristol-Myers Squibb Company | 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production |
| WO1998038156A1 (en) | 1997-02-27 | 1998-09-03 | Takeda Chemical Industries, Ltd. | Amine compounds, their production and use as amyloid-beta production inhibitors |
| JP2003528076A (ja) * | 2000-03-20 | 2003-09-24 | メルク シャープ エンド ドーム リミテッド | スルホンアミド置換架橋ビシクロアルキル誘導体 |
| DE60112957T2 (de) | 2000-11-02 | 2006-05-18 | Merck Sharp & Dohme Ltd., Hoddesdon | Sulfamide als gamma-secretase-inhibitoren |
| GB0209997D0 (en) | 2002-05-01 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
| CA2484159C (en) * | 2002-05-01 | 2011-02-22 | Merck Sharp & Dohme Limited | Heteroaryl substituted spirocyclic sulfamides for inhibition of gamma secretase |
| GB0209991D0 (en) * | 2002-05-01 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
-
2003
- 2003-04-24 CA CA2484159A patent/CA2484159C/en not_active Expired - Fee Related
- 2003-04-24 EP EP03722769A patent/EP1503998B1/de not_active Expired - Lifetime
- 2003-04-24 AT AT03722769T patent/ATE435219T1/de not_active IP Right Cessation
- 2003-04-24 AU AU2003229932A patent/AU2003229932B2/en not_active Ceased
- 2003-04-24 US US10/512,810 patent/US7041689B2/en not_active Expired - Lifetime
- 2003-04-24 DE DE60328182T patent/DE60328182D1/de not_active Expired - Lifetime
- 2003-04-24 WO PCT/GB2003/001763 patent/WO2003093252A1/en not_active Ceased
-
2006
- 2006-03-02 US US11/366,866 patent/US7282513B2/en not_active Expired - Lifetime
-
2007
- 2007-09-07 US US11/899,844 patent/US20080070895A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20060173054A1 (en) | 2006-08-03 |
| AU2003229932B2 (en) | 2008-12-11 |
| WO2003093252A1 (en) | 2003-11-13 |
| EP1503998B1 (de) | 2009-07-01 |
| CA2484159A1 (en) | 2003-11-13 |
| US20050182109A1 (en) | 2005-08-18 |
| AU2003229932A1 (en) | 2003-11-17 |
| US7282513B2 (en) | 2007-10-16 |
| US7041689B2 (en) | 2006-05-09 |
| EP1503998A1 (de) | 2005-02-09 |
| DE60328182D1 (de) | 2009-08-13 |
| US20080070895A1 (en) | 2008-03-20 |
| CA2484159C (en) | 2011-02-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |