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 (55)
| 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 |
| RU2304140C2 (ru) | 2001-12-27 | 2007-08-10 | Дайити Фармасьютикал Ко., Лтд. | ИНГИБИТОРЫ ПРОДУЦИРОВАНИЯ / СЕКРЕЦИИ β-АМИЛОИДНОГО БЕЛКА |
| 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 |
| RU2336270C2 (ru) | 2003-06-30 | 2008-10-20 | Дайити Фармасьютикал Ко., Лтд. | Гетероциклические метилсульфоновые производные |
| CA2539042A1 (en) * | 2003-09-24 | 2005-04-07 | Merck Sharp & Dohme Limited | Gamma-secretase inhibitors |
| EP1888050B1 (de) | 2005-05-17 | 2012-03-21 | Merck Sharp & Dohme Ltd. | Cis-4-[(4-chlorophenyl)sulfonyl]-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 |
| US20080058316A1 (en) | 2006-02-27 | 2008-03-06 | The Johns Hopkins University | Cancer treatment with gama-secretase inhibitors |
| EP2094836B1 (de) | 2006-11-15 | 2016-06-08 | Massachusetts Eye & Ear Infirmary | Erzeugung von innerohrzellen |
| AU2008215948A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of AD and related conditions |
| US8461389B2 (en) | 2008-04-18 | 2013-06-11 | University College Dublin, National University Of Ireland, Dublin | Psycho-pharmaceuticals |
| HUE043090T2 (hu) * | 2008-06-09 | 2019-08-28 | Univ Muenchen Ludwig Maximilians | Gyógyszerek fehérjék aggregálódásának gátlására olyan betegségeknél, amelyek fehérje-aggregálódással és/vagy neurodegeneratív megbetegedésekkel függnek össze |
| CA2743436C (en) | 2008-11-24 | 2017-10-31 | 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 |
| US8691825B2 (en) | 2009-04-01 | 2014-04-08 | Merck Sharp & Dohme Corp. | Inhibitors of AKT activity |
| EP2488028B1 (de) | 2009-10-14 | 2020-08-19 | Merck Sharp & Dohme Corp. | Substituierte piperidine zur erhöhung der p53-aktivität und ihre verwendung |
| US8907098B2 (en) * | 2009-12-17 | 2014-12-09 | Merck Patent Gmbh | Inhibitors of sphingosine kinase |
| WO2011163330A1 (en) | 2010-06-24 | 2011-12-29 | Merck Sharp & Dohme Corp. | Novel heterocyclic compounds as erk inhibitors |
| CN107090456B (zh) | 2010-08-02 | 2022-01-18 | 瑟纳治疗公司 | 使用短干扰核酸的RNA干扰介导的联蛋白（钙粘蛋白关联蛋白质），β1基因表达的抑制 |
| JP2013537423A (ja) | 2010-08-17 | 2013-10-03 | メルク・シャープ・エンド・ドーム・コーポレイション | 低分子干渉核酸（ｓｉＮＡ）を用いたＢ型肝炎ウイルス（ＨＢＶ）遺伝子発現のＲＮＡ干渉媒介性阻害 |
| WO2012030685A2 (en) | 2010-09-01 | 2012-03-08 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| EP2615916B1 (de) | 2010-09-16 | 2017-01-04 | Merck Sharp & Dohme Corp. | Kondensierte pyrazolderivate als neue erk-hemmer |
| DK2632472T3 (en) | 2010-10-29 | 2018-03-19 | Sirna Therapeutics Inc | RNA INTERFERENCE-MEDIATED INHIBITION OF GENE EXPRESSION USING SHORT INTERFERRING NUCLEIC ACIDS (SINA) |
| WO2012087772A1 (en) | 2010-12-21 | 2012-06-28 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| WO2013063214A1 (en) | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| EP2844261B1 (de) | 2012-05-02 | 2018-10-17 | Sirna Therapeutics, Inc. | Sina-zusammensetzungen |
| 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 |
| HK1211875A1 (en) | 2012-09-07 | 2016-06-03 | Massachusetts Eye & Ear Infirmary | Treating hearing loss |
| CN105050598B (zh) | 2012-09-28 | 2018-04-27 | 默沙东公司 | 作为erk抑制剂的新型化合物 |
| RS56680B1 (sr) | 2012-11-28 | 2018-03-30 | Merck Sharp & Dohme | Kompozicije i postupci za lečenje kancera |
| US8846657B2 (en) | 2012-12-20 | 2014-09-30 | 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 |
| EP3041938A1 (de) | 2013-09-03 | 2016-07-13 | Moderna Therapeutics, Inc. | Kreisförmige polynukleotide |
| WO2016022776A2 (en) | 2014-08-06 | 2016-02-11 | Massachusetts Eye And Ear Infirmary | Increasing atoh1 life to drive sensorineural hair cell differentiantion |
| US11185536B2 (en) | 2015-12-04 | 2021-11-30 | 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 |
| CA3024424A1 (en) | 2016-05-16 | 2017-11-23 | The General Hospital Corporation | Human airway stem cells in lung epithelial engineering |
| US10975084B2 (en) | 2016-10-12 | 2021-04-13 | Merck Sharp & Dohme Corp. | KDM5 inhibitors |
| 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 |
| US11098059B2 (en) | 2017-11-08 | 2021-08-24 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| EP3706742B1 (de) | 2017-11-08 | 2023-03-15 | Merck Sharp & Dohme LLC | Prmt5-inhibitoren |
| CA3108388A1 (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 |
| EP3833668B1 (de) | 2018-08-07 | 2025-03-19 | Merck Sharp & Dohme LLC | Prmt5-inhibitoren |
| WO2020033285A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2021126728A1 (en) | 2019-12-17 | 2021-06-24 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| 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 |
| JP7589247B2 (ja) | 2019-12-17 | 2024-11-25 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｐｒｍｔ５阻害剤 |
| GEAP202516720A (en) | 2022-09-02 | 2025-07-10 | Merck Sharp & Dohme Llc | Exatecan-derived topoisomerase-1 inhibitors pharmaceutical compositions, and uses thereof |
| IL320396A (en) | 2022-10-25 | 2025-06-01 | Merck Sharp & Dohme Llc | Charge-linkers of anti-drug conjugates derived from extacan, pharmaceutical compositions, and uses thereof |
| US20240207425A1 (en) | 2022-12-14 | 2024-06-27 | Merck Sharp & Dohme Llc | Auristatin linker-payloads, pharmaceutical compositions, and uses thereof |
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 |
| HU225960B1 (en) | 1997-02-27 | 2008-01-28 | Takeda Pharmaceutical | Amine compounds, their production and use |
| US7365196B2 (en) | 2000-03-20 | 2008-04-29 | Merck Sharp & Dohme Ltd. | Sulphonamido-substituted bridged bicycloalkyl derivatives |
| DE60112957T2 (de) | 2000-11-02 | 2006-05-18 | Merck Sharp & Dohme Ltd., Hoddesdon | Sulfamide als gamma-secretase-inhibitoren |
| 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 |
| GB0209997D0 (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 AU AU2003229932A patent/AU2003229932B2/en not_active Ceased
- 2003-04-24 AT AT03722769T patent/ATE435219T1/de not_active IP Right Cessation
- 2003-04-24 EP EP03722769A patent/EP1503998B1/de 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
- 2003-04-24 US US10/512,810 patent/US7041689B2/en not_active Expired - Lifetime
-
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 |
|---|---|
| US20080070895A1 (en) | 2008-03-20 |
| WO2003093252A1 (en) | 2003-11-13 |
| AU2003229932A1 (en) | 2003-11-17 |
| US20060173054A1 (en) | 2006-08-03 |
| DE60328182D1 (de) | 2009-08-13 |
| US20050182109A1 (en) | 2005-08-18 |
| EP1503998B1 (de) | 2009-07-01 |
| AU2003229932B2 (en) | 2008-12-11 |
| EP1503998A1 (de) | 2005-02-09 |
| CA2484159A1 (en) | 2003-11-13 |
| US7282513B2 (en) | 2007-10-16 |
| CA2484159C (en) | 2011-02-22 |
| US7041689B2 (en) | 2006-05-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |