JP2006501292A5 - - Google Patents
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- Publication number
- JP2006501292A5 JP2006501292A5 JP2004540927A JP2004540927A JP2006501292A5 JP 2006501292 A5 JP2006501292 A5 JP 2006501292A5 JP 2004540927 A JP2004540927 A JP 2004540927A JP 2004540927 A JP2004540927 A JP 2004540927A JP 2006501292 A5 JP2006501292 A5 JP 2006501292A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halogen
- substituents
- cor
- con
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 36
- 125000001424 substituent group Chemical group 0.000 claims description 25
- 229910052736 halogen Inorganic materials 0.000 claims description 18
- 150000002367 halogens Chemical class 0.000 claims description 16
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 6
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 claims description 5
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 4
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 125000002252 acyl group Chemical group 0.000 claims description 2
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- -1 methylenedioxy, difluoromethylenedioxy Chemical group 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- ILVXOBCQQYKLDS-UHFFFAOYSA-N pyridine N-oxide Chemical compound [O-][N+]1=CC=CC=C1 ILVXOBCQQYKLDS-UHFFFAOYSA-N 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 238000006467 substitution reaction Methods 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims description 2
- 125000003302 alkenyloxy group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 description 2
- 0 CC(CC1)CCC1([Al])S(*)(=O)=O Chemical compound CC(CC1)CCC1([Al])S(*)(=O)=O 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0223039.9A GB0223039D0 (en) | 2002-10-04 | 2002-10-04 | Therapeutic compounds |
| PCT/GB2003/004102 WO2004031137A1 (en) | 2002-10-04 | 2003-09-25 | Cyclohexyl sulphone derivatives as gamma-secretase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006501292A JP2006501292A (ja) | 2006-01-12 |
| JP2006501292A5 true JP2006501292A5 (enExample) | 2010-03-18 |
| JP4653485B2 JP4653485B2 (ja) | 2011-03-16 |
Family
ID=9945313
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004540927A Expired - Fee Related JP4653485B2 (ja) | 2002-10-04 | 2003-09-25 | ガンマ−セクレターゼインヒビターとしてのシクロヘキシルスルホン誘導体 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US7101895B2 (enExample) |
| EP (1) | EP1551797B1 (enExample) |
| JP (1) | JP4653485B2 (enExample) |
| AT (1) | ATE354562T1 (enExample) |
| AU (1) | AU2003267614B2 (enExample) |
| CA (1) | CA2500964C (enExample) |
| DE (1) | DE60312016T2 (enExample) |
| ES (1) | ES2280774T3 (enExample) |
| GB (1) | GB0223039D0 (enExample) |
| WO (1) | WO2004031137A1 (enExample) |
Families Citing this family (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0108591D0 (en) | 2001-04-05 | 2001-05-23 | Merck Sharp & Dohme | Therapeutic agents |
| GB0120347D0 (en) | 2001-08-21 | 2001-10-17 | Merck Sharp & Dohme | Therapeutic agents |
| AU2002367147A1 (en) | 2001-12-27 | 2003-07-15 | Daiichi Pharmaceutical Co., Ltd. | Beta-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS |
| US7521481B2 (en) | 2003-02-27 | 2009-04-21 | Mclaurin Joanne | Methods of preventing, treating and diagnosing disorders of protein aggregation |
| CA2526487A1 (en) | 2003-06-30 | 2005-01-06 | Daiichi Pharmaceutical Co., Ltd. | Heterocyclic methyl sulfone derivative |
| AR047666A1 (es) * | 2004-02-20 | 2006-02-01 | Merck Sharp & Dohme | Sintesis estereoselectiva del acido ciclohexanopropanoico 4,4-disubstituido |
| US20090215775A1 (en) * | 2005-05-17 | 2009-08-27 | Huw David Lewis | Sulphonamido-Substituted Cyclohexyl Sulphones for Treatment of Cancer |
| 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 |
| WO2006131713A1 (en) * | 2005-06-06 | 2006-12-14 | Merck Sharp & Dohme Limited | Cyclohexanesulfonyl derivatives as glyt1 inhibitors to treat schizophrenia |
| GB0513747D0 (en) * | 2005-07-06 | 2005-08-10 | Merck Sharp & Dohme | Therapeutic compounds |
| AU2007207481B2 (en) * | 2006-01-20 | 2012-08-23 | Merck Sharp & Dohme Corp. | Carbocyclic and heterocyclic arylsulfones as gamma secretase inhibitors |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| JP2010509919A (ja) | 2006-11-15 | 2010-04-02 | マサチューセッツ・アイ・アンド・イア・インファーマリー | 内耳細胞の生成 |
| SI2091948T1 (sl) | 2006-11-30 | 2012-07-31 | Probiodrug Ag | Novi inhibitorji glutaminil ciklaze |
| AU2008215948A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of AD and related conditions |
| EA200901140A1 (ru) | 2007-03-01 | 2010-04-30 | Пробиодруг Аг | Новое применение ингибиторов глутаминилциклазы |
| EP2142514B1 (en) | 2007-04-18 | 2014-12-24 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
| EP2435416B1 (en) * | 2007-07-05 | 2016-03-30 | Merck Sharp & Dohme Corp. | Tetrahydropyranochromene gamma secretase inhibitors |
| PE20090447A1 (es) * | 2007-07-17 | 2009-04-18 | Schering Corp | Bencensulfonil-cromano, tiocromano, tetrahidronaftaleno e inhibidores relacionados de la gamma secretasa |
| 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 |
| EP2291181B9 (en) | 2008-04-18 | 2013-09-11 | University College Dublin National University Of Ireland, Dublin | Captodiamine for the treatment of depression symptoms |
| EP2381936B2 (en) | 2008-11-24 | 2020-02-12 | Massachusetts Eye & Ear Infirmary | Pathways to generate auditory hair cells |
| EP2393776B1 (en) * | 2009-02-06 | 2014-05-14 | Merck Sharp & Dohme Corp. | Novel trifluoromethylsulfonamide gamma secretase inhibitor |
| WO2010114780A1 (en) | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| CN102695546B (zh) | 2009-09-11 | 2014-09-10 | 前体生物药物股份公司 | 作为谷氨酰胺酰环化酶抑制剂的杂环衍生物 |
| WO2011046771A1 (en) | 2009-10-14 | 2011-04-21 | Schering Corporation | SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF |
| WO2011107530A2 (en) | 2010-03-03 | 2011-09-09 | Probiodrug Ag | Novel inhibitors |
| SG183229A1 (en) | 2010-03-10 | 2012-09-27 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
| EP2560953B1 (en) | 2010-04-21 | 2016-01-06 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
| US8999957B2 (en) | 2010-06-24 | 2015-04-07 | Merck Sharp & Dohme Corp. | Heterocyclic compounds as ERK inhibitors |
| 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) |
| EP4079856A1 (en) | 2010-08-17 | 2022-10-26 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of hepatitis b virus (hbv) gene expression using short interfering nucleic acid (sina) |
| WO2012030685A2 (en) | 2010-09-01 | 2012-03-08 | Schering Corporation | Indazole derivatives useful as erk inhibitors |
| EP2615916B1 (en) | 2010-09-16 | 2017-01-04 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel erk inhibitors |
| EP3327125B1 (en) | 2010-10-29 | 2020-08-05 | Sirna Therapeutics, Inc. | Rna interference mediated inhibition of gene expression using short interfering nucleic acids (sina) |
| US9351965B2 (en) | 2010-12-21 | 2016-05-31 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as ERK inhibitors |
| WO2012123563A1 (en) | 2011-03-16 | 2012-09-20 | Probiodrug Ag | Benz imidazole derivatives as inhibitors of glutaminyl cyclase |
| EP2770987B1 (en) | 2011-10-27 | 2018-04-04 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| EP3453762B1 (en) | 2012-05-02 | 2021-04-21 | Sirna Therapeutics, Inc. | Short interfering nucleic acid (sina) compositions |
| HK1211875A1 (en) | 2012-09-07 | 2016-06-03 | Massachusetts Eye & Ear Infirmary | Treating hearing loss |
| AU2013312305B2 (en) | 2012-09-07 | 2018-06-28 | Massachusetts Eye And Ear Infirmary | Methods and compositions for regenerating hair cells and/or supporting cells |
| AU2013323508B2 (en) | 2012-09-28 | 2017-11-02 | Merck Sharp & Dohme Corp. | Novel compounds that are ERK inhibitors |
| EP2925888B1 (en) | 2012-11-28 | 2017-10-25 | Merck Sharp & Dohme Corp. | Compositions and methods for treating cancer |
| CA2895504A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| EP2951180B1 (en) | 2013-01-30 | 2018-05-02 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| US8859286B2 (en) | 2013-03-14 | 2014-10-14 | Viacyte, Inc. | In vitro differentiation of pluripotent stem cells to pancreatic endoderm cells (PEC) and endocrine cells |
| WO2015034925A1 (en) | 2013-09-03 | 2015-03-12 | Moderna Therapeutics, Inc. | Circular polynucleotides |
| US9708253B2 (en) * | 2014-01-06 | 2017-07-18 | Bristol-Myers Squibb Company | Cyclohexyl sulfone RORγ modulators |
| WO2016007775A1 (en) | 2014-07-11 | 2016-01-14 | Genentech, Inc. | Notch pathway inhibition |
| WO2016022776A2 (en) | 2014-08-06 | 2016-02-11 | Massachusetts Eye And Ear Infirmary | Increasing atoh1 life to drive sensorineural hair cell differentiantion |
| MX2018000999A (es) | 2015-07-24 | 2018-11-09 | Oncotracker Inc | Moduladores de gamma secretasa para el tratamiento de disfuncion del sistema inmunologico. |
| US11185536B2 (en) | 2015-12-04 | 2021-11-30 | Massachusetts Eye And Ear Infirmary | Treatment of hearing loss by inhibition of casein kinase 1 |
| AU2017212655B2 (en) | 2016-01-29 | 2024-01-18 | Decibel Therapeutics, Inc. | Expansion and differentiation of inner ear supporting cells and methods of use thereof |
| AU2017268078B2 (en) | 2016-05-16 | 2023-03-02 | The General Hospital Corporation | Human airway stem cells in lung epithelial engineering |
| EP3525785B1 (en) | 2016-10-12 | 2025-08-27 | Merck Sharp & Dohme LLC | Kdm5 inhibitors |
| AU2017376109A1 (en) | 2016-12-16 | 2019-07-11 | Pipeline Therapeutics, Inc. | Methods of treating cochlear synaptopathy |
| AU2018222749B2 (en) | 2017-02-17 | 2024-04-18 | Fred Hutchinson Cancer Center | Combination therapies for treatment of BCMA-related cancers and autoimmune disorders |
| DK3461819T3 (da) | 2017-09-29 | 2020-08-10 | Probiodrug Ag | Inhibitorer af glutaminylcyklase |
| US11098059B2 (en) | 2017-11-08 | 2021-08-24 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| EP3706742B1 (en) | 2017-11-08 | 2023-03-15 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2020033288A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| EP3833668B1 (en) | 2018-08-07 | 2025-03-19 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| US11981701B2 (en) | 2018-08-07 | 2024-05-14 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| WO2021126728A1 (en) | 2019-12-17 | 2021-06-24 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2021126729A1 (en) | 2019-12-17 | 2021-06-24 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US20230108452A1 (en) | 2019-12-17 | 2023-04-06 | Merck Sharp & Dohme Llc | Prmt5 inhibitors |
| CN111205264A (zh) * | 2020-02-25 | 2020-05-29 | 成都睿智化学研究有限公司 | 一种合成同位羟基和甲磺酰甲基化合物的新方法 |
| BR112022018987A2 (pt) | 2020-03-26 | 2022-11-01 | Seagen Inc | Métodos de tratamento de mieloma múltiplo |
| PE20251401A1 (es) | 2022-09-02 | 2025-05-22 | Merck Sharp And Dohme Llc | Inhibidores de topoisomerasa-1 derivados de exatecan composiciones farmaceuticas y sus usos |
| AU2023366166A1 (en) | 2022-10-25 | 2025-05-01 | Merck Sharp & Dohme Llc | Exatecan-derived adc linker-payloads, pharmaceutical compositions, and uses thereof |
| WO2024129628A1 (en) | 2022-12-14 | 2024-06-20 | Merck Sharp & Dohme Llc | Auristatin linker-payloads, pharmaceutical compositions, and uses thereof |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2802013A (en) * | 1954-02-12 | 1957-08-06 | Searle & Co | 2-(oxo and imino)-3-(phenyl and halophenyl)-tetrahydrofuransulfones and processes for the manufacture thereof |
| US2812330A (en) * | 1956-05-02 | 1957-11-05 | Searle & Co | Sulfone derivatives of 2, 6-piperidinedione |
| JPS5625149A (en) | 1979-08-08 | 1981-03-10 | Sagami Chem Res Center | Keto ester derivative and its preparation |
| JPS5626866A (en) | 1979-08-13 | 1981-03-16 | Sagami Chem Res Center | Unsaturated ketoester derivative and its preparation |
| JPS5626847A (en) | 1979-08-13 | 1981-03-16 | Sagami Chem Res Center | Preparation of substituted salicylic acid derivative |
| CA2191924A1 (en) * | 1995-12-05 | 1997-06-06 | Kevin Felsenstein | 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of .beta.-amyloid protein production |
| EP0863134A1 (en) | 1997-03-07 | 1998-09-09 | Merck Frosst Canada Inc. | 2-(3,5-difluorophenyl)-3-(4-(methyl-sulfonyl)phenyl)-2-cyclopenten-1-one useful as an inhibitor of cyclooxygenase-2 |
| HRP990246A2 (en) * | 1998-08-07 | 2000-06-30 | Du Pont Pharm Co | Succinoylamino benzodiazepines as inhibitors of a beta protein production |
| CN1348442A (zh) | 1999-02-26 | 2002-05-08 | 默克公司 | 新的磺胺化合物及其应用 |
| AU2001240861B2 (en) * | 2000-03-20 | 2006-03-30 | Merck Frosst Canada Ltd | Sulphonamido-substituted bridged bicycloalkyl derivatives |
| GB0108592D0 (en) | 2001-04-05 | 2001-05-23 | Merck Sharp & Dohme | Therapeutic agents |
| GB0108591D0 (en) * | 2001-04-05 | 2001-05-23 | Merck Sharp & Dohme | Therapeutic agents |
| WO2003013527A1 (en) * | 2001-08-03 | 2003-02-20 | Schering Corporation | Sulfonamide derivatives as gamma secretase inhibitors |
| AU2002324123B2 (en) | 2001-08-21 | 2007-07-12 | Merck Sharp & Dohme (Uk) Limited | Novel cyclohexyl sulphones |
| AU2002367147A1 (en) | 2001-12-27 | 2003-07-15 | Daiichi Pharmaceutical Co., Ltd. | Beta-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS |
| DE10201392A1 (de) * | 2002-01-16 | 2003-07-31 | Bayer Ag | Phenylsulfoxide und-sulfone |
| GB0218041D0 (en) | 2002-08-02 | 2002-09-11 | Merck Sharp & Dohme | Chemical process |
| JP3092689U (ja) * | 2002-09-10 | 2003-03-20 | 船井電機株式会社 | 光ピックアップ |
| GB0223038D0 (en) * | 2002-10-04 | 2002-11-13 | Merck Sharp & Dohme | Therapeutic compounds |
| GB0223040D0 (en) | 2002-10-04 | 2002-11-13 | Merck Sharp & Dohme | Therapeutic compounds |
| DE10254875A1 (de) | 2002-11-25 | 2004-06-03 | Bayer Healthcare Ag | Phenylsulfoxid und -sulfon-Derivate |
| GB0304524D0 (en) * | 2003-02-27 | 2003-04-02 | Merck Sharp & Dohme | Therapeutic agents |
| NZ542797A (en) | 2003-05-16 | 2007-12-21 | Merck Sharp & Dohme | Cyclohexyl sulfones comprising an additional fused ring cyclic sulfonamide group suitable for inhibition of gamma-secretase |
| CA2526487A1 (en) | 2003-06-30 | 2005-01-06 | Daiichi Pharmaceutical Co., Ltd. | Heterocyclic methyl sulfone derivative |
| GB0323258D0 (en) * | 2003-10-04 | 2003-11-05 | Merck Sharp & Dohme | Therapeutic compounds |
-
2002
- 2002-10-04 GB GBGB0223039.9A patent/GB0223039D0/en not_active Ceased
-
2003
- 2003-09-25 AT AT03748306T patent/ATE354562T1/de not_active IP Right Cessation
- 2003-09-25 ES ES03748306T patent/ES2280774T3/es not_active Expired - Lifetime
- 2003-09-25 WO PCT/GB2003/004102 patent/WO2004031137A1/en not_active Ceased
- 2003-09-25 EP EP03748306A patent/EP1551797B1/en not_active Expired - Lifetime
- 2003-09-25 CA CA2500964A patent/CA2500964C/en not_active Expired - Fee Related
- 2003-09-25 AU AU2003267614A patent/AU2003267614B2/en not_active Ceased
- 2003-09-25 JP JP2004540927A patent/JP4653485B2/ja not_active Expired - Fee Related
- 2003-09-25 DE DE60312016T patent/DE60312016T2/de not_active Expired - Lifetime
- 2003-10-06 US US10/679,557 patent/US7101895B2/en not_active Expired - Fee Related