ATE302753T1 - Sulfamide als gamma-secretase-inhibitoren - Google Patents
Sulfamide als gamma-secretase-inhibitorenInfo
- Publication number
- ATE302753T1 ATE302753T1 AT01978652T AT01978652T ATE302753T1 AT E302753 T1 ATE302753 T1 AT E302753T1 AT 01978652 T AT01978652 T AT 01978652T AT 01978652 T AT01978652 T AT 01978652T AT E302753 T1 ATE302753 T1 AT E302753T1
- Authority
- AT
- Austria
- Prior art keywords
- sulfamides
- gamma secretase
- secretase inhibitors
- gamma
- secretase
- Prior art date
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- C07—ORGANIC CHEMISTRY
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- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- 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
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- A—HUMAN NECESSITIES
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- C07C307/04—Diamides of sulfuric acids
- C07C307/08—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to carbon atoms of rings other than six-membered aromatic rings
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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/36—Oxygen or sulfur atoms
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
- C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
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- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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- C07C2602/00—Systems containing two condensed rings
- C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
- C07C2602/44—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing eight carbon atoms
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- C07C2602/00—Systems containing two condensed rings
- C07C2602/36—Systems containing two condensed rings the rings having more than two atoms in common
- C07C2602/46—Systems containing two condensed rings the rings having more than two atoms in common the bicyclo ring system containing nine carbon atoms
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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- C07C2603/56—Ring systems containing bridged rings
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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| PCT/GB2001/004817 WO2002036555A1 (en) | 2000-11-02 | 2001-10-29 | Sulfamides as gamma-secretase inhibitors |
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| MXPA05012323A (es) | 2003-05-16 | 2006-01-30 | Merck Sharp & Dohme | Sulfonamidas ciclicas para la inhibicion de gama-secretasa. |
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| US9656991B2 (en) | 2007-04-18 | 2017-05-23 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| WO2009035522A1 (en) * | 2007-09-14 | 2009-03-19 | Albert Einstein College Of Medicine Of Yeshiva University | Use of gamma secretase inhibitors and notch pathway inhibitors for treatment and prevention of renal disease |
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| EP2291181B9 (en) | 2008-04-18 | 2013-09-11 | University College Dublin National University Of Ireland, Dublin | Captodiamine for the treatment of depression symptoms |
| CA2743436C (en) | 2008-11-24 | 2017-10-31 | Massachusetts Eye & Ear Infirmary | Pathways to generate hair cells |
| WO2010114780A1 (en) | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| ES2548913T3 (es) | 2009-09-11 | 2015-10-21 | Probiodrug Ag | Derivados heterocíclicos como inhibidores de glutaminil ciclasa |
| MY174452A (en) | 2009-10-14 | 2020-04-19 | Schering Corp | Substituted piperidines that increase p53 activity and the uses thereof |
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| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| CA2789440C (en) | 2010-03-10 | 2020-03-24 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
| JP5945532B2 (ja) | 2010-04-21 | 2016-07-05 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤としてのベンゾイミダゾール誘導体 |
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| 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 |
| US9260471B2 (en) | 2010-10-29 | 2016-02-16 | Sirna Therapeutics, Inc. | RNA interference mediated inhibition of gene expression using short interfering nucleic acids (siNA) |
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| US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
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| EP3970725B1 (en) | 2012-09-07 | 2025-08-20 | Massachusetts Eye & Ear Infirmary | A gamma secretase inhibitor for treating hearing loss |
| 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 |
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| WO2021126729A1 (en) | 2019-12-17 | 2021-06-24 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| AU2020408148B2 (en) | 2019-12-17 | 2025-04-24 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| US20230108114A1 (en) | 2019-12-17 | 2023-04-06 | Merck Sharp & Dohme Llc | Prmt5 inhibitors |
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| 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 |
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| 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 |
| DE69839305T2 (de) | 1997-02-27 | 2009-04-09 | Takeda Pharmaceutical Co. Ltd. | Aminderivate, ihre herstellung und verwendung als inhibitoren der produktion von amyloid-beta |
| EP1254108A1 (en) * | 2000-01-24 | 2002-11-06 | MERCK SHARP & DOHME LTD. | Gamma-secretase inhibitors |
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| JP2002037731A (ja) * | 2000-05-19 | 2002-02-06 | Takeda Chem Ind Ltd | βセクレターゼ阻害剤 |
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| ATE435219T1 (de) * | 2002-05-01 | 2009-07-15 | Merck Sharp & Dohme | Heteroaryl substituierte spirocyclische sulfamide zur hemmung von gamma sekretase |
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- 2001-10-29 US US10/415,751 patent/US7138400B2/en not_active Expired - Lifetime
- 2001-10-29 EP EP01978652A patent/EP1334085B1/en not_active Expired - Lifetime
- 2001-10-29 CA CA2427206A patent/CA2427206C/en not_active Expired - Fee Related
- 2001-10-29 ES ES01978652T patent/ES2248397T3/es not_active Expired - Lifetime
- 2001-10-29 AT AT01978652T patent/ATE302753T1/de not_active IP Right Cessation
- 2001-10-29 DE DE60112957T patent/DE60112957T2/de not_active Expired - Lifetime
- 2001-10-29 WO PCT/GB2001/004817 patent/WO2002036555A1/en not_active Ceased
-
2006
- 2006-03-22 JP JP2006078136A patent/JP4495686B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP2004513108A (ja) | 2004-04-30 |
| JP4495686B2 (ja) | 2010-07-07 |
| AU2002210747B2 (en) | 2006-06-01 |
| ES2248397T3 (es) | 2006-03-16 |
| CA2427206C (en) | 2011-06-28 |
| EP1334085A1 (en) | 2003-08-13 |
| CA2427206A1 (en) | 2002-05-10 |
| AU1074702A (en) | 2002-05-15 |
| US20040049038A1 (en) | 2004-03-11 |
| WO2002036555A1 (en) | 2002-05-10 |
| DE60112957T2 (de) | 2006-05-18 |
| DE60112957D1 (de) | 2005-09-29 |
| US7138400B2 (en) | 2006-11-21 |
| JP2006241163A (ja) | 2006-09-14 |
| JP3880051B2 (ja) | 2007-02-14 |
| EP1334085B1 (en) | 2005-08-24 |
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| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |