ATE323717T1 - Piperazin-4-phenyl-derivate als inhibitoren der wechselwirkung zwischen mdm2 und mdm2 - Google Patents
Piperazin-4-phenyl-derivate als inhibitoren der wechselwirkung zwischen mdm2 und mdm2Info
- Publication number
- ATE323717T1 ATE323717T1 AT99944688T AT99944688T ATE323717T1 AT E323717 T1 ATE323717 T1 AT E323717T1 AT 99944688 T AT99944688 T AT 99944688T AT 99944688 T AT99944688 T AT 99944688T AT E323717 T1 ATE323717 T1 AT E323717T1
- Authority
- AT
- Austria
- Prior art keywords
- 4alkyl
- mdm2
- formula
- piperazine
- inhibitors
- Prior art date
Links
- 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 title abstract 3
- 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 title abstract 3
- 230000003993 interaction Effects 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000003396 thiol group Chemical group [H]S* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—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
- C07D295/16—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 acylated on ring nitrogen atoms
- C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/20—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D417/02—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
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0815—Tripeptides with the first amino acid being basic
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9819860.9A GB9819860D0 (en) | 1998-09-12 | 1998-09-12 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE323717T1 true ATE323717T1 (de) | 2006-05-15 |
Family
ID=10838741
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT99944688T ATE323717T1 (de) | 1998-09-12 | 1999-09-07 | Piperazin-4-phenyl-derivate als inhibitoren der wechselwirkung zwischen mdm2 und mdm2 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US6770627B1 (de) |
| EP (1) | EP1112284B1 (de) |
| JP (1) | JP2002524570A (de) |
| AT (1) | ATE323717T1 (de) |
| AU (1) | AU5751299A (de) |
| DE (1) | DE69930947T2 (de) |
| GB (1) | GB9819860D0 (de) |
| WO (1) | WO2000015657A1 (de) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7129242B2 (en) | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
| US7122544B2 (en) | 2000-12-06 | 2006-10-17 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto |
| CA2438272A1 (en) | 2001-03-02 | 2002-10-10 | John Macor | Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same |
| WO2003075917A1 (en) | 2002-03-08 | 2003-09-18 | Signal Pharmaceuticals, Inc. | Combination therapy for treating, preventing or managing proliferative disorders and cancers |
| GB0215650D0 (en) * | 2002-07-05 | 2002-08-14 | Cyclacel Ltd | Bisarylsufonamide compounds |
| AU2004212928A1 (en) | 2003-02-13 | 2004-09-02 | Bioveris Corporation | Deazaflavin compounds and methods of use thereof |
| US6916833B2 (en) | 2003-03-13 | 2005-07-12 | Hoffmann-La Roche Inc. | Substituted piperidines |
| WO2005112922A2 (en) * | 2004-04-22 | 2005-12-01 | Samaritan Pharmaceuticals | Benzamide compounds |
| AU2006305538B2 (en) | 2005-10-21 | 2012-06-28 | Idorsia Pharmaceuticals Ltd | Piperazine derivatives as antimalarial agents |
| WO2007107545A1 (en) | 2006-03-22 | 2007-09-27 | Janssen Pharmaceutica N.V. | Cyclic-alkylaminederivatives as inhibitors of the interaction between mdm2 and p53 |
| US8232298B2 (en) | 2006-03-22 | 2012-07-31 | Janssen Pharmaceutica N.V. | Inhibitors of the interaction between MDM2 and P53 |
| BRPI0713119A2 (pt) | 2006-06-30 | 2012-04-17 | Schering Corp | piperidinas substituìdas que aumentam a atividade de p53 e os usos destas |
| US8470785B2 (en) | 2006-07-28 | 2013-06-25 | St. Jude Children's Research Hospital | Method for treating ocular cancer |
| WO2008014216A1 (en) | 2006-07-28 | 2008-01-31 | St. Jude Children's Research Hospital | Method for treating ocular cancer |
| WO2008018778A1 (en) * | 2006-08-10 | 2008-02-14 | Korea Research Institute Of Bioscience And Biotechnology | New heterocyclic compounds containing nitrogen atoms or pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical composition comprising the same for treatment of cancer |
| EP2066318B1 (de) | 2006-09-21 | 2010-05-12 | F. Hoffmann-Roche AG | Oxindolderivate als antikrebsmittel |
| AU2007332493A1 (en) | 2006-12-14 | 2008-06-19 | Daiichi Sankyo Company, Limited | Imidazothiazole derivatives |
| US7723372B2 (en) * | 2008-03-19 | 2010-05-25 | Hoffman-La Roche Inc. | Spiroindolinone derivatives |
| WO2009151069A1 (ja) | 2008-06-12 | 2009-12-17 | 第一三共株式会社 | ４，７－ジアザスピロ［２．５］オクタン環構造を有するイミダゾチアゾール誘導体 |
| PE20121172A1 (es) | 2009-10-14 | 2012-09-05 | Merck Sharp & Dohme | Piperidinas sustituidas con actividad en la hdm2 |
| US8088815B2 (en) | 2009-12-02 | 2012-01-03 | Hoffman-La Roche Inc. | Spiroindolinone pyrrolidines |
| US8889688B2 (en) | 2010-01-05 | 2014-11-18 | Actelion Pharmaceuticals Ltd. | Piperazines as antimalarial agents |
| US8288431B2 (en) | 2010-02-17 | 2012-10-16 | Hoffmann-La Roche Inc. | Substituted spiroindolinones |
| US8217044B2 (en) | 2010-04-28 | 2012-07-10 | Hoffmann-La Roche Inc. | Spiroindolinone pyrrolidines |
| US8987274B2 (en) | 2011-10-28 | 2015-03-24 | Merck Sharp & Dohme Corp | Macrocycles that increase p53 activity and the uses thereof |
| US9062071B2 (en) | 2011-12-21 | 2015-06-23 | Merck Sharp & Dohme Corp. | Substituted piperidines as HDM2 inhibitors |
| KR102196882B1 (ko) | 2012-12-20 | 2020-12-30 | 머크 샤프 앤드 돔 코포레이션 | Hdm2 억제제로서의 치환된 이미다조피리딘 |
| WO2014120748A1 (en) | 2013-01-30 | 2014-08-07 | Merck Sharp & Dohme Corp. | 2,6,7,8 substituted purines as hdm2 inhibitors |
| CN105189485B (zh) | 2013-03-15 | 2017-10-24 | 埃科特莱茵药品有限公司 | 作为抗疟剂的新型丙烯酰胺衍生物 |
| WO2015004610A1 (en) | 2013-07-11 | 2015-01-15 | Adamed Sp. Z O.O. | 1,5-dihydropyrrol-2-one derivatives as inhibitors of p53-mdm2/mdm4 protein-protein interaction |
| CN103954601A (zh) * | 2014-05-20 | 2014-07-30 | 中国科学技术大学 | 一种mdm2拮抗剂的检验试剂盒及其制备方法 |
| CN118436801A (zh) | 2016-05-20 | 2024-08-06 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| CN110183348B (zh) * | 2019-06-18 | 2022-06-03 | 中国医科大学 | N-(3-硝基-4-烷氧基苯甲酰基)氨基酸类化合物、制备方法及其用途 |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE423858C (de) | 1925-05-11 | 1926-01-11 | Raduner & Co Akt Ges Fa | Verfahren zum Appretieren von Faserstoffen |
| FR2518088B1 (fr) | 1981-12-16 | 1987-11-27 | Roques Bernard | Nouveaux derives d'aminoacides, et leur application therapeutique |
| JP2769578B2 (ja) | 1989-10-13 | 1998-06-25 | 大塚製薬株式会社 | バソプレシン拮抗剤 |
| CA2056799C (en) | 1990-11-30 | 2002-01-01 | Hiroshi Ikawa | 1,4-dihydropyridine derivatives and methods of producing the same |
| US5411860A (en) | 1992-04-07 | 1995-05-02 | The Johns Hopkins University | Amplification of human MDM2 gene in human tumors |
| JPH05294915A (ja) | 1992-04-21 | 1993-11-09 | Yamanouchi Pharmaceut Co Ltd | タキキニン拮抗剤 |
| DK0610487T3 (da) | 1992-09-03 | 2000-05-15 | Boehringer Ingelheim Pharma | Nye aminosyrederivater, fremgangsmåde til deres fremstilling og farmaceutiske præparater indeholdende disse forbindelser |
| WO1994007496A1 (en) | 1992-10-07 | 1994-04-14 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| AU690275B2 (en) | 1994-05-07 | 1998-04-23 | Boehringer Ingelheim International Gmbh | Neurokinine (tachykinine) antagonists |
| US5777112A (en) | 1994-06-13 | 1998-07-07 | Merck & Co., Inc | Piperazine compounds promote release of growth hormone |
| US5770377A (en) | 1994-07-20 | 1998-06-23 | University Of Dundee | Interruption of binding of MDM2 and P53 protein and therapeutic application thereof |
| US5607936A (en) | 1994-09-30 | 1997-03-04 | Merck & Co., Inc. | Substituted aryl piperazines as neurokinin antagonists |
| JP3127732B2 (ja) | 1994-10-18 | 2001-01-29 | トヨタ自動車株式会社 | トリミング方法及びその装置 |
| KR0173034B1 (ko) | 1995-04-28 | 1999-03-30 | 성재갑 | 선택적 트롬빈 억제제 |
| FR2738151B1 (fr) | 1995-09-04 | 1997-09-26 | Rhone Poulenc Rorer Sa | Antagonistes de l'activite oncogenique de la proteine mdm2, et leur utilisation dans le traitement des cancers |
| DE69625622T2 (de) | 1995-10-25 | 2003-08-14 | Senju Pharmaceutical Co., Ltd. | Angiogenese Inhibitoren |
| GB9601724D0 (en) | 1996-01-29 | 1996-03-27 | Merck Sharp & Dohme | Therapeutic agents |
| AU2393997A (en) | 1996-04-05 | 1997-10-29 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Alpha1-adrenergic receptor antagonists |
| EP0958305B1 (de) * | 1996-07-05 | 2008-06-04 | Cancer Research Technology Limited | Hemmer der interaktion zwischen p53 und mdm2 |
| SK285631B6 (sk) | 1996-09-10 | 2007-05-03 | Dr. Karl Thomae Gmbh | Modifikované aminokyseliny, farmaceutický prostriedok s ich obsahom a ich použitie |
| AU5522498A (en) | 1996-12-13 | 1998-07-03 | Merck & Co., Inc. | Substituted aryl piperazines as modulators of chemokine receptor activity |
-
1998
- 1998-09-12 GB GBGB9819860.9A patent/GB9819860D0/en not_active Ceased
-
1999
- 1999-09-07 AU AU57512/99A patent/AU5751299A/en not_active Abandoned
- 1999-09-07 WO PCT/GB1999/002957 patent/WO2000015657A1/en not_active Ceased
- 1999-09-07 AT AT99944688T patent/ATE323717T1/de not_active IP Right Cessation
- 1999-09-07 DE DE69930947T patent/DE69930947T2/de not_active Expired - Fee Related
- 1999-09-07 JP JP2000570195A patent/JP2002524570A/ja active Pending
- 1999-09-07 EP EP99944688A patent/EP1112284B1/de not_active Expired - Lifetime
- 1999-09-07 US US09/786,702 patent/US6770627B1/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| DE69930947T2 (de) | 2006-12-28 |
| JP2002524570A (ja) | 2002-08-06 |
| AU5751299A (en) | 2000-04-03 |
| WO2000015657A1 (en) | 2000-03-23 |
| EP1112284A1 (de) | 2001-07-04 |
| DE69930947D1 (de) | 2006-05-24 |
| US6770627B1 (en) | 2004-08-03 |
| GB9819860D0 (en) | 1998-11-04 |
| EP1112284B1 (de) | 2006-04-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |