BR0215156A - Cis-imidazolinas como inibidores de mdm 2 - Google Patents
Cis-imidazolinas como inibidores de mdm 2Info
- Publication number
- BR0215156A BR0215156A BR0215156-1A BR0215156A BR0215156A BR 0215156 A BR0215156 A BR 0215156A BR 0215156 A BR0215156 A BR 0215156A BR 0215156 A BR0215156 A BR 0215156A
- Authority
- BR
- Brazil
- Prior art keywords
- mdm
- cis
- inhibitors
- imidazolines
- formula
- Prior art date
Links
- 239000012819 MDM2-Inhibitor Substances 0.000 title abstract 2
- 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 abstract 1
- 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 abstract 1
- 230000001028 anti-proliverative effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 230000003993 interaction Effects 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D233/22—Radicals substituted by oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D233/26—Radicals substituted by carbon atoms having three bonds to hetero atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
"CIS-IMIDAZOLINAS COMO INIBIDORES DE MDM 2". A presente invenção refere-se a compostos de acordo com a fórmula I e fórmula II e seus sais e ésteres farmaceuticamente aceitáveis, contendo as designações fornecidas aí e que inibem a interação de proteína MDM2 com peptídeo semelhante a p53 e tem atividade antiproliferativa (I) (II).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34172901P | 2001-12-18 | 2001-12-18 | |
| US39087602P | 2002-06-21 | 2002-06-21 | |
| PCT/EP2002/013905 WO2003051360A1 (en) | 2001-12-18 | 2002-12-09 | Cis-imidazolines as mdm2 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0215156A true BR0215156A (pt) | 2004-10-19 |
Family
ID=26992633
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0215156-1A BR0215156A (pt) | 2001-12-18 | 2002-12-09 | Cis-imidazolinas como inibidores de mdm 2 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US6617346B1 (pt) |
| EP (1) | EP1463501B1 (pt) |
| JP (1) | JP4361798B2 (pt) |
| KR (1) | KR100640707B1 (pt) |
| CN (1) | CN1604778A (pt) |
| AR (1) | AR037882A1 (pt) |
| AT (1) | ATE397925T1 (pt) |
| AU (1) | AU2002361986B2 (pt) |
| BR (1) | BR0215156A (pt) |
| CA (1) | CA2468783A1 (pt) |
| DE (1) | DE60227108D1 (pt) |
| ES (1) | ES2307822T3 (pt) |
| MX (1) | MXPA04005880A (pt) |
| PA (1) | PA8561801A1 (pt) |
| PE (1) | PE20030717A1 (pt) |
| PL (1) | PL370909A1 (pt) |
| RU (1) | RU2312101C2 (pt) |
| TW (1) | TW200301696A (pt) |
| UY (1) | UY27586A1 (pt) |
| WO (1) | WO2003051360A1 (pt) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004253245B2 (en) * | 2003-06-17 | 2010-02-11 | F. Hoffmann-La Roche Ag | CIS-imidazolines as MDM2 inhibitors |
| US7132421B2 (en) | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
| JP4814228B2 (ja) * | 2004-05-18 | 2011-11-16 | エフ.ホフマン−ラ ロシュ アーゲー | 新規cis−イミダゾリン |
| EP1758579A1 (en) * | 2004-05-29 | 2007-03-07 | 7TM Pharma A/S | Crth2 receptor ligands for medicinal uses |
| US7893278B2 (en) * | 2004-06-17 | 2011-02-22 | Hoffman-La Roche Inc. | CIS-imidazolines |
| KR100944301B1 (ko) * | 2005-02-22 | 2010-02-24 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | Mdm2의 소분자 억제제 및 이의 용도 |
| US7759383B2 (en) | 2005-02-22 | 2010-07-20 | The Regents Of The University Of Michigan | Small molecule inhibitors of MDM2 and the uses thereof |
| JP4870778B2 (ja) | 2005-12-01 | 2012-02-08 | エフ.ホフマン−ラ ロシュ アーゲー | 抗ガン剤として使用されるp53およびmdm2タンパク質間の相互作用の阻害剤としての2,4,5−トリフェニルイミダゾリン誘導体 |
| KR101015073B1 (ko) * | 2006-01-18 | 2011-02-16 | 에프. 호프만-라 로슈 아게 | Mdm2 억제제로서의시스-4,5-비아릴-2-헤테로시클릭-이미다졸린 |
| 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 |
| US8222288B2 (en) | 2006-08-30 | 2012-07-17 | The Regents Of The University Of Michigan | Small molecule inhibitors of MDM2 and the uses thereof |
| AU2007332493A1 (en) | 2006-12-14 | 2008-06-19 | Daiichi Sankyo Company, Limited | Imidazothiazole derivatives |
| US7625895B2 (en) * | 2007-04-12 | 2009-12-01 | Hoffmann-Le Roche Inc. | Diphenyl-dihydro-imidazopyridinones |
| RU2487127C2 (ru) * | 2007-10-09 | 2013-07-10 | Ф.Хоффманн-Ля Рош Аг | Хиральные цис-имидазолины |
| EP2224961A1 (en) * | 2007-11-26 | 2010-09-08 | The Research Foundation of the State University of New York | Small molecule cancer treatments that cause necrosis in cancer cells but do not affect normal cells |
| 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 |
| PL2380892T3 (pl) | 2009-01-16 | 2014-08-29 | Daiichi Sankyo Co Ltd | Pochodna imidazotiazolowa mająca strukturę pierścienia proliny |
| UA107814C2 (uk) | 2009-11-12 | 2015-02-25 | Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган | Спірооксіндольні антагоністи мdм2 |
| US10159669B2 (en) * | 2010-03-02 | 2018-12-25 | Ian H. Chan | Individual and combination of mdivi-1 and nutlin-3 for topical or intravitreal ophthalmic use |
| WO2012047587A2 (en) * | 2010-09-27 | 2012-04-12 | Serrata, Llc | Mdm2 inhibitors for treatment of ocular conditions |
| WO2012045018A1 (en) | 2010-09-30 | 2012-04-05 | St. Jude Children's Research Hospital | Aryl-substituted imidazoles |
| FR2967072B1 (fr) | 2010-11-05 | 2013-03-29 | Univ Dundee | Procede pour ameliorer la production de virus et semences vaccinales influenza |
| JP2014500870A (ja) | 2010-11-12 | 2014-01-16 | ザ、リージェンツ、オブ、ザ、ユニバーシティ、オブ、ミシガン | スピロ−オキシインドールmdm2アンタゴニスト |
| SG193002A1 (en) | 2011-03-10 | 2013-09-30 | Daiichi Sankyo Co Ltd | Dispiropyrrolidine derivative |
| WO2012155066A2 (en) | 2011-05-11 | 2012-11-15 | Shaomeng Wang | Spiro-oxindole mdm2 antagonists |
| KR101384683B1 (ko) * | 2011-10-27 | 2014-04-11 | 한국생명공학연구원 | mdm2-결합 모티프를 포함하는 펩타이드 및 이의 용도 |
| US9937178B2 (en) | 2011-12-07 | 2018-04-10 | Duke University | Methods of identifying and using MDM2 inhibitors |
| TWI586668B (zh) | 2012-09-06 | 2017-06-11 | 第一三共股份有限公司 | 二螺吡咯啶衍生物之結晶 |
| KR102196882B1 (ko) | 2012-12-20 | 2020-12-30 | 머크 샤프 앤드 돔 코포레이션 | Hdm2 억제제로서의 치환된 이미다조피리딘 |
| IL286427B2 (en) | 2014-01-28 | 2024-08-01 | Mayo Found Medical Education & Res | Inhibitors bcl-2 anti-apoptotic protein family members for treatment of non cancer pulmonary disease or an opthalmic disease |
| US20190269675A1 (en) | 2014-01-28 | 2019-09-05 | Buck Institute for Research and Aging | Treatment of parkinson's disease and other conditions caused or mediated by senescent astrocytes using small molecule senolytic agents |
| US10328058B2 (en) | 2014-01-28 | 2019-06-25 | Mayo Foundation For Medical Education And Research | Treating atherosclerosis by removing senescent foam cell macrophages from atherosclerotic plaques |
| US20170216286A1 (en) | 2014-01-28 | 2017-08-03 | Mayo Foundation For Medical Education And Research | Killing senescent cells and treating senescence-associated conditions using a src inhibitor and a flavonoid |
| TWI750129B (zh) * | 2015-08-03 | 2021-12-21 | 瑞士商諾華公司 | 作為血液學毒性生物標記之gdf-15 |
| SG11201808728QA (en) | 2016-04-06 | 2018-11-29 | Univ Michigan Regents | Mdm2 protein degraders |
| US10759808B2 (en) | 2016-04-06 | 2020-09-01 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| 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 |
| CN110088081A (zh) | 2017-06-16 | 2019-08-02 | 尤尼蒂生物技术公司 | 制备用于药物用途的对映纯顺式-咪唑啉化合物的合成方法 |
| US12239720B2 (en) | 2018-04-06 | 2025-03-04 | Oncolyze, Inc. | Compositions for use in lysis of selective cancer cells |
| CN112912143A (zh) | 2018-10-08 | 2021-06-04 | 美国密歇根州立大学试剂中心 | 小分子mdm2蛋白降解剂 |
| KR20230005160A (ko) | 2020-03-19 | 2023-01-09 | 카이메라 쎄라퓨틱스 인코포레이티드 | Mdm2 분해제 및 이의 용도 |
| 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 (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GR75287B (pt) * | 1980-07-25 | 1984-07-13 | Ciba Geigy Ag | |
| JPH02101065A (ja) * | 1988-10-06 | 1990-04-12 | Tanabe Seiyaku Co Ltd | イミダゾリン誘導体及びその製法 |
| US5474998A (en) | 1990-08-17 | 1995-12-12 | E. I. Du Pont De Nemours And Company | Arthropodicidal pyrazolines, pyrazolidines and hydrazines |
| GB2351082A (en) * | 1999-06-18 | 2000-12-20 | Lilly Forschung Gmbh | Synthesis of Cyclic Substituted Amidines |
-
2002
- 2002-12-09 AT AT02796582T patent/ATE397925T1/de not_active IP Right Cessation
- 2002-12-09 CN CNA028252292A patent/CN1604778A/zh active Pending
- 2002-12-09 ES ES02796582T patent/ES2307822T3/es not_active Expired - Lifetime
- 2002-12-09 CA CA002468783A patent/CA2468783A1/en not_active Abandoned
- 2002-12-09 BR BR0215156-1A patent/BR0215156A/pt not_active IP Right Cessation
- 2002-12-09 KR KR1020047009612A patent/KR100640707B1/ko not_active Expired - Fee Related
- 2002-12-09 PL PL02370909A patent/PL370909A1/xx not_active Application Discontinuation
- 2002-12-09 AU AU2002361986A patent/AU2002361986B2/en not_active Ceased
- 2002-12-09 JP JP2003552293A patent/JP4361798B2/ja not_active Expired - Fee Related
- 2002-12-09 DE DE60227108T patent/DE60227108D1/de not_active Expired - Lifetime
- 2002-12-09 MX MXPA04005880A patent/MXPA04005880A/es active IP Right Grant
- 2002-12-09 RU RU2004122404/04A patent/RU2312101C2/ru not_active IP Right Cessation
- 2002-12-09 WO PCT/EP2002/013905 patent/WO2003051360A1/en not_active Ceased
- 2002-12-09 EP EP02796582A patent/EP1463501B1/en not_active Expired - Lifetime
- 2002-12-11 US US10/316,696 patent/US6617346B1/en not_active Expired - Fee Related
- 2002-12-13 PE PE2002001225A patent/PE20030717A1/es not_active Application Discontinuation
- 2002-12-17 UY UY27586A patent/UY27586A1/es not_active Application Discontinuation
- 2002-12-17 PA PA20028561801A patent/PA8561801A1/es unknown
- 2002-12-17 AR ARP020104913A patent/AR037882A1/es not_active Application Discontinuation
- 2002-12-18 TW TW091136524A patent/TW200301696A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20040068289A (ko) | 2004-07-30 |
| WO2003051360A1 (en) | 2003-06-26 |
| ATE397925T1 (de) | 2008-07-15 |
| MXPA04005880A (es) | 2004-09-13 |
| RU2004122404A (ru) | 2005-05-27 |
| EP1463501B1 (en) | 2008-06-11 |
| EP1463501A1 (en) | 2004-10-06 |
| JP4361798B2 (ja) | 2009-11-11 |
| CN1604778A (zh) | 2005-04-06 |
| DE60227108D1 (de) | 2008-07-24 |
| UY27586A1 (es) | 2003-06-30 |
| RU2312101C2 (ru) | 2007-12-10 |
| JP2005515210A (ja) | 2005-05-26 |
| KR100640707B1 (ko) | 2006-10-31 |
| AR037882A1 (es) | 2004-12-09 |
| ES2307822T3 (es) | 2008-12-01 |
| AU2002361986A1 (en) | 2003-06-30 |
| CA2468783A1 (en) | 2003-06-26 |
| TW200301696A (en) | 2003-07-16 |
| PA8561801A1 (es) | 2003-07-28 |
| PL370909A1 (en) | 2005-05-30 |
| US6617346B1 (en) | 2003-09-09 |
| PE20030717A1 (es) | 2003-08-28 |
| AU2002361986B2 (en) | 2008-04-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 9A ANUI DADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: NAO APRESENTADA A GUIA DE CUMPRIMENTO DE EXIGENCIA. REFERENTE A 9A ANUIDADE. |