JP2004531517A5 - - Google Patents
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- Publication number
- JP2004531517A5 JP2004531517A5 JP2002579421A JP2002579421A JP2004531517A5 JP 2004531517 A5 JP2004531517 A5 JP 2004531517A5 JP 2002579421 A JP2002579421 A JP 2002579421A JP 2002579421 A JP2002579421 A JP 2002579421A JP 2004531517 A5 JP2004531517 A5 JP 2004531517A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- halogen
- alkoxy
- compound according
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- -1 amino, carbamoyl Chemical group 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 208000024827 Alzheimer disease Diseases 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 239000000470 constituent Substances 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000003367 polycyclic group Chemical group 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 150000001408 amides Chemical group 0.000 claims 1
- 230000006933 amyloid-beta aggregation Effects 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002148 esters Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0108592.7A GB0108592D0 (en) | 2001-04-05 | 2001-04-05 | Therapeutic agents |
| PCT/GB2001/003778 WO2002081433A1 (en) | 2001-04-05 | 2001-08-21 | Sulphones which modulate the action of gamma secretase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004531517A JP2004531517A (ja) | 2004-10-14 |
| JP2004531517A5 true JP2004531517A5 (https=) | 2008-10-02 |
Family
ID=9912330
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002579421A Pending JP2004531517A (ja) | 2001-04-05 | 2001-08-21 | γ−セクレターゼの作用を調節するスルホン |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7411004B2 (https=) |
| EP (1) | EP1379496B1 (https=) |
| JP (1) | JP2004531517A (https=) |
| AT (1) | ATE400550T1 (https=) |
| AU (1) | AU2001282313B2 (https=) |
| CA (1) | CA2442885C (https=) |
| DE (1) | DE60134788D1 (https=) |
| GB (1) | GB0108592D0 (https=) |
| WO (1) | WO2002081433A1 (https=) |
Families Citing this family (50)
| 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 |
| CN100562516C (zh) | 2001-12-27 | 2009-11-25 | 第一制药株式会社 | β-淀粉样蛋白产生和分泌的抑制剂 |
| DE10201392A1 (de) * | 2002-01-16 | 2003-07-31 | Bayer Ag | Phenylsulfoxide und-sulfone |
| GB0223039D0 (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 |
| GB0308318D0 (en) * | 2003-04-10 | 2003-05-14 | Merck Sharp & Dohme | Therapeutic agents |
| EP1638951B1 (en) * | 2003-05-16 | 2008-02-13 | MERCK SHARP & DOHME LTD. | Cyclohexyl sulphones as gamma-secretase inhibitors |
| CA2526487A1 (en) | 2003-06-30 | 2005-01-06 | Daiichi Pharmaceutical Co., Ltd. | Heterocyclic methyl sulfone derivative |
| CN100378072C (zh) * | 2003-06-30 | 2008-04-02 | 第一制药株式会社 | 杂环甲基砜衍生物 |
| AR047666A1 (es) * | 2004-02-20 | 2006-02-01 | Merck Sharp & Dohme | Sintesis estereoselectiva del acido ciclohexanopropanoico 4,4-disubstituido |
| US8114886B2 (en) | 2005-04-08 | 2012-02-14 | Daiichi Sankyo Company, Limited | Pyridylmethylsulfone derivative |
| WO2006123182A2 (en) | 2005-05-17 | 2006-11-23 | Merck Sharp & Dohme Limited | Cyclohexyl sulphones for treatment of cancer |
| CA2676715A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperazine derivatives for treatment of ad and related conditions |
| TW200920362A (en) | 2007-09-11 | 2009-05-16 | Daiichi Sankyo Co Ltd | Alkylsulfone derivatives |
| KR101595238B1 (ko) | 2007-12-21 | 2016-02-18 | 리간드 파마슈티칼스 인코포레이티드 | 선택적 안드로겐 수용체 조절제(sarm) 및 이의 용도 |
| WO2009128057A2 (en) | 2008-04-18 | 2009-10-22 | UNIVERSITY COLLEGE DUBLIN, NATIONAL UNIVERSITY OF IRELAND, DUBLIN et al | Psycho-pharmaceuticals |
| WO2010114780A1 (en) | 2009-04-01 | 2010-10-07 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| US8859776B2 (en) | 2009-10-14 | 2014-10-14 | Merck Sharp & Dohme Corp. | Substituted piperidines that increase p53 activity and the uses thereof |
| US8999957B2 (en) | 2010-06-24 | 2015-04-07 | Merck Sharp & Dohme Corp. | Heterocyclic compounds as ERK inhibitors |
| CA2805265A1 (en) | 2010-08-02 | 2012-02-09 | Merck Sharp & Dohme Corp. | Rna interference mediated inhibition of catenin (cadherin-associated protein), beta 1 (ctnnb1) gene expression using short interfering nucleic acid (sina) |
| WO2012024170A2 (en) | 2010-08-17 | 2012-02-23 | Merck Sharp & Dohme Corp. | 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 |
| 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) |
| EP2654748B1 (en) | 2010-12-21 | 2016-07-27 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| EP2770987B1 (en) | 2011-10-27 | 2018-04-04 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| WO2013165816A2 (en) | 2012-05-02 | 2013-11-07 | Merck Sharp & Dohme Corp. | SHORT INTERFERING NUCLEIC ACID (siNA) COMPOSITIONS |
| WO2014052563A2 (en) | 2012-09-28 | 2014-04-03 | Merck Sharp & Dohme Corp. | Novel compounds that are erk inhibitors |
| ME02925B (me) | 2012-11-28 | 2018-04-20 | Merck Sharp & Dohme | Kompozicije i postupci za liječenje kancera |
| TW201429969A (zh) | 2012-12-20 | 2014-08-01 | Merck Sharp & Dohme | 作爲hdm2抑制劑之經取代咪唑吡啶 |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| US20160194368A1 (en) | 2013-09-03 | 2016-07-07 | Moderna Therapeutics, Inc. | Circular polynucleotides |
| EP3094323A4 (en) | 2014-01-17 | 2017-10-11 | Ligand Pharmaceuticals Incorporated | Methods and compositions for modulating hormone levels |
| US10975084B2 (en) | 2016-10-12 | 2021-04-13 | Merck Sharp & Dohme Corp. | KDM5 inhibitors |
| US10947234B2 (en) | 2017-11-08 | 2021-03-16 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| EP3706747B1 (en) | 2017-11-08 | 2025-09-03 | Merck Sharp & Dohme LLC | Prmt5 inhibitors |
| WO2020033288A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| EP3833669A4 (en) | 2018-08-07 | 2022-05-11 | Merck Sharp & Dohme Corp. | PRMT5 INHIBITORS |
| WO2020033282A1 (en) | 2018-08-07 | 2020-02-13 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| US11981701B2 (en) | 2018-08-07 | 2024-05-14 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| AU2020257397B2 (en) | 2019-04-19 | 2026-02-26 | Ligand Pharmaceuticals Inc. | Crystalline forms and methods of producing crystalline forms of a compound |
| US12595248B2 (en) | 2019-12-17 | 2026-04-07 | Merck Sharp & Dohme Llc | PRMT5 inhibitors |
| CN115003303B (zh) | 2019-12-17 | 2024-03-08 | 默沙东公司 | Prmt5抑制剂 |
| EP4076460B1 (en) | 2019-12-17 | 2026-01-21 | Merck Sharp & Dohme LLC | 1,4-dihydro-2h-spiro[isoquinoline-3,4'-piperidine derivatives as prmt5 inhibitors for the treatment of cancer |
| 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 |
| JP7595854B2 (ja) * | 2020-05-25 | 2024-12-09 | 地方独立行政法人大阪産業技術研究所 | [6,6]メタノフラーレン誘導体の製造方法 |
| JP2025511436A (ja) | 2022-09-02 | 2025-04-16 | メルク・シャープ・アンド・ドーム・エルエルシー | エキサテカン由来トポイソメラーゼ-1阻害薬医薬組成物及びその使用 |
| CN120417935A (zh) | 2022-10-25 | 2025-08-01 | 默沙东有限责任公司 | 依喜替康衍生的adc接头-载荷及其药物组合物和用途 |
| US20240207425A1 (en) | 2022-12-14 | 2024-06-27 | Merck Sharp & Dohme Llc | Auristatin linker-payloads, pharmaceutical compositions, and uses thereof |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3016403A (en) * | 1955-07-29 | 1962-01-09 | Searle & Co | 1-aryl-3-hydroxypropyl sulfones and processes |
| JPS537691A (en) * | 1976-07-09 | 1978-01-24 | Yoshitomi Pharmaceut Ind Ltd | Piperazines |
| DE2735314A1 (de) * | 1977-08-05 | 1979-02-22 | Basf Ag | Alpha-azolylsulfide und deren derivate |
| US4675316A (en) * | 1978-03-10 | 1987-06-23 | Rohm And Haas Company | Substituted azoylmethylarylsulfides and derivatives and pesticidal use thereof |
| DE2821829A1 (de) * | 1978-05-19 | 1979-11-22 | Basf Ag | Mittel zur regulierung des pflanzenwachstums |
| JPS5626847A (en) | 1979-08-13 | 1981-03-16 | Sagami Chem Res Center | Preparation of substituted salicylic acid derivative |
| JPS5716840A (en) * | 1980-07-03 | 1982-01-28 | Sagami Chem Res Center | Phneylacetic acid derivative |
| US4379921A (en) * | 1980-08-21 | 1983-04-12 | Sumitomo Chemical Company, Limited | Production of triazolylvinyl ketones |
| FR2593178B1 (fr) * | 1986-01-20 | 1988-04-29 | Esteve Labor Dr | Derives de 2-benzimidazolylalkylthio (ou sulfinyle ou sulfonyle) leur preparation et leur application en tant que medicaments. |
| JPS62181260A (ja) * | 1986-02-06 | 1987-08-08 | Nippon Kayaku Co Ltd | ピリジン誘導体およびそれを有効成分とする農園芸用殺菌剤 |
| JP3582070B2 (ja) * | 1994-08-11 | 2004-10-27 | 日本曹達株式会社 | フェニルエタン誘導体及びそれを用いた感熱記録材料 |
| ES2194209T3 (es) * | 1996-07-22 | 2003-11-16 | Monsanto Co | Inhibidores de metaloproteasa de tiol sulfona. |
| 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 |
| WO2000050391A1 (en) | 1999-02-26 | 2000-08-31 | Merck & Co., Inc. | Novel sulfonamide compounds and uses thereof |
| SE9901901D0 (sv) * | 1999-05-26 | 1999-05-26 | Astra Ab | Compounds |
| CN100562516C (zh) | 2001-12-27 | 2009-11-25 | 第一制药株式会社 | β-淀粉样蛋白产生和分泌的抑制剂 |
| DE10201392A1 (de) | 2002-01-16 | 2003-07-31 | Bayer Ag | Phenylsulfoxide und-sulfone |
-
2001
- 2001-04-05 GB GBGB0108592.7A patent/GB0108592D0/en not_active Ceased
- 2001-08-21 CA CA2442885A patent/CA2442885C/en not_active Expired - Fee Related
- 2001-08-21 EP EP01960923A patent/EP1379496B1/en not_active Expired - Lifetime
- 2001-08-21 DE DE60134788T patent/DE60134788D1/de not_active Expired - Lifetime
- 2001-08-21 AU AU2001282313A patent/AU2001282313B2/en not_active Ceased
- 2001-08-21 AT AT01960923T patent/ATE400550T1/de not_active IP Right Cessation
- 2001-08-21 WO PCT/GB2001/003778 patent/WO2002081433A1/en not_active Ceased
- 2001-08-21 US US10/473,767 patent/US7411004B2/en not_active Expired - Fee Related
- 2001-08-21 JP JP2002579421A patent/JP2004531517A/ja active Pending
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