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 |
|---|---|---|---|---|
| ES2248397T3 (es) * | 2000-11-02 | 2006-03-16 | MERCK SHARP & DOHME LTD. | Sulfamidas como inhibidores de la gamma-secretasa. |
| 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 |
| DE60328182D1 (de) * | 2002-05-01 | 2009-08-13 | Merck Sharp & Dohme | Heteroaryl substituierte spirocyclische sulfamide zur hemmung von gamma sekretase |
| 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 |
| WO2005030731A1 (en) * | 2003-09-24 | 2005-04-07 | Merck Sharp & Dohme Limited | Gamma-secretase inhibitors |
| US8362075B2 (en) | 2005-05-17 | 2013-01-29 | Merck Sharp & Dohme Corp. | Cyclohexyl sulphones for treatment of cancer |
| 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 |
| EP2121633A2 (de) | 2007-02-12 | 2009-11-25 | Merck & Co., Inc. | Piperazinderivate zur behandlung von alzheimer-krankheit und verwandten leiden |
| US8461389B2 (en) | 2008-04-18 | 2013-06-11 | University College Dublin, National University Of Ireland, Dublin | Psycho-pharmaceuticals |
| WO2010000372A2 (en) * | 2008-06-09 | 2010-01-07 | Ludwig-Maximilians-Universität München | New drug for inhibiting aggregation of proteins involved in diseases linked to protein aggregation and/or neurodegenerative diseases |
| US10143711B2 (en) | 2008-11-24 | 2018-12-04 | 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 |
| WO2010114780A1 (en) | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| JP5099731B1 (ja) | 2009-10-14 | 2012-12-19 | メルク・シャープ・アンド・ドーム・コーポレーション | ｐ５３活性を増大する置換ピペリジン及びその使用 |
| AU2010341229A1 (en) * | 2009-12-17 | 2012-08-02 | Merck Patent Gmbh | Sphingosine kinase inhibitors |
| EP2584903B1 (de) | 2010-06-24 | 2018-10-24 | Merck Sharp & Dohme Corp. | Neue heterozyklische verbindungen als erk-hemmer |
| AU2011285909B2 (en) | 2010-08-02 | 2016-11-10 | Sirna Therapeutics, Inc. | RNA interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (CTNNB1) gene expression using short interfering nucleic acid (siNA) |
| EP2606134B1 (de) | 2010-08-17 | 2019-04-10 | Sirna Therapeutics, Inc. | Rna-interferenz-vermittelte hemmung der hepatitis b-virus (hbv)-genexpression mittels kurzer interferierender nukleinsäure (sina) |
| 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 |
| EP3766975A1 (de) | 2010-10-29 | 2021-01-20 | Sirna Therapeutics, Inc. | Rna-interferenz-vermittelte inhibition von genexpression unter verwendung kurzer interferierender nukleinsäure (sina) |
| EP2654748B1 (de) | 2010-12-21 | 2016-07-27 | Merck Sharp & Dohme Corp. | Indazolderivate als erk-hemmer |
| WO2013063214A1 (en) | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| EP3358013B1 (de) | 2012-05-02 | 2020-06-24 | Sirna Therapeutics, Inc. | Sina-zusammensetzungen |
| US20150209406A1 (en) | 2012-09-07 | 2015-07-30 | Massachusetts Eye And Ear Infirmary | Methods and compositions for regenerating hair cells and/or supporting cells |
| EP3970725B1 (de) | 2012-09-07 | 2025-08-20 | Massachusetts Eye & Ear Infirmary | Ein gamma-sekretase-inhibitor zur behandlung von gehörverlust |
| KR20150060724A (ko) | 2012-09-28 | 2015-06-03 | 머크 샤프 앤드 돔 코포레이션 | Erk 억제제인 신규 화합물 |
| DK2925888T3 (en) | 2012-11-28 | 2017-12-18 | Merck Sharp & Dohme | COMPOSITIONS AND METHODS OF CANCER TREATMENT |
| EP2935263B1 (de) | 2012-12-20 | 2018-12-05 | Merck Sharp & Dohme Corp. | Substituierte imidazopyridine als hdm2 inhibitoren |
| US9540377B2 (en) | 2013-01-30 | 2017-01-10 | 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 |
| US20170314027A1 (en) | 2014-08-06 | 2017-11-02 | 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 |
| CA3013038A1 (en) | 2016-01-29 | 2017-08-03 | Massachusetts Eye And Ear Infirmary | Expansion and differentiation of inner ear supporting cells and methods of use thereof |
| WO2017200762A2 (en) | 2016-05-16 | 2017-11-23 | The General Hospital Corporation | Human airway stem cells in lung epithelial engineering |
| WO2018071283A1 (en) | 2016-10-12 | 2018-04-19 | Merck Sharp & Dohme Corp. | Kdm5 inhibitors |
| CN110337291A (zh) | 2016-12-16 | 2019-10-15 | 帕珀莱恩医疗公司 | 治疗耳蜗突触病变的方法 |
| US11098059B2 (en) | 2017-11-08 | 2021-08-24 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| WO2019094311A1 (en) | 2017-11-08 | 2019-05-16 | 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 |
| BR112021002267A8 (pt) | 2018-08-07 | 2023-02-07 | Merck Sharp & Dohme | Inibidores de prmt5 |
| EP4076459B1 (de) | 2019-12-17 | 2026-04-29 | 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 |
| BR112022012015A2 (pt) | 2019-12-17 | 2022-08-30 | Merck Sharp & Dohme Llc | Inibidores de prmt5 |
| CA3160153A1 (en) | 2019-12-17 | 2021-06-24 | Michelle Machacek | Prmt5 inhibitors |
| KR20250053961A (ko) | 2022-09-02 | 2025-04-22 | 머크 샤프 앤드 돔 엘엘씨 | 엑사테칸-유래 토포이소머라제-1 억제제 제약 조성물 및 그의 용도 |
| TW202432099A (zh) | 2022-10-25 | 2024-08-16 | 美商默沙東有限責任公司 | 源自依克沙替康(exatecan)之adc連接子-載藥(payload)、醫藥組合物及其用途 |
| IL321395A (en) | 2022-12-14 | 2025-08-01 | Merck Sharp & Dohme Llc | Auristatin cargo-linkers, pharmaceutical compounds, and their uses |
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 |
| EP0971878B1 (de) | 1997-02-27 | 2008-03-26 | Takeda Pharmaceutical Company Limited | Aminderivate, ihre herstellung und verwendung als inhibitoren der produktion von amyloid-beta |
| CA2404125C (en) * | 2000-03-20 | 2011-01-25 | Merck Sharp & Dohme Limited | Sulphonamido-substituted bridged bicycloalkyl derivatives |
| ES2248397T3 (es) * | 2000-11-02 | 2006-03-16 | MERCK SHARP & DOHME LTD. | Sulfamidas como inhibidores de la gamma-secretasa. |
| GB0209997D0 (en) | 2002-05-01 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
| DE60328182D1 (de) * | 2002-05-01 | 2009-08-13 | Merck Sharp & Dohme | Heteroaryl substituierte spirocyclische sulfamide zur hemmung von gamma sekretase |
| GB0209991D0 (en) * | 2002-05-01 | 2002-06-12 | Merck Sharp & Dohme | Therapeutic agents |
-
2003
- 2003-04-24 DE DE60328182T patent/DE60328182D1/de not_active Expired - Lifetime
- 2003-04-24 AT AT03722769T patent/ATE435219T1/de not_active IP Right Cessation
- 2003-04-24 WO PCT/GB2003/001763 patent/WO2003093252A1/en not_active Ceased
- 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 EP EP03722769A patent/EP1503998B1/de not_active Expired - Lifetime
- 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 |
|---|---|
| CA2484159A1 (en) | 2003-11-13 |
| AU2003229932B2 (en) | 2008-12-11 |
| US20050182109A1 (en) | 2005-08-18 |
| CA2484159C (en) | 2011-02-22 |
| US7041689B2 (en) | 2006-05-09 |
| EP1503998B1 (de) | 2009-07-01 |
| AU2003229932A1 (en) | 2003-11-17 |
| WO2003093252A1 (en) | 2003-11-13 |
| US7282513B2 (en) | 2007-10-16 |
| US20060173054A1 (en) | 2006-08-03 |
| DE60328182D1 (de) | 2009-08-13 |
| US20080070895A1 (en) | 2008-03-20 |
| EP1503998A1 (de) | 2005-02-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |