AR037882A1 - Cis-imidazolinas - Google Patents
Cis-imidazolinasInfo
- Publication number
- AR037882A1 AR037882A1 ARP020104913A ARP020104913A AR037882A1 AR 037882 A1 AR037882 A1 AR 037882A1 AR P020104913 A ARP020104913 A AR P020104913A AR P020104913 A ARP020104913 A AR P020104913A AR 037882 A1 AR037882 A1 AR 037882A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently
- heteroatom
- ch2och2ch3
- ch2och3
- alkoxy
- Prior art date
Links
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)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se proporcionan compuestos, sales y ésteres farmacéuticamente aceptables de los mismos, que inhiben la interacción de la proteína MDM2 con un péptido similar a p53 y que presentan una actividad antiproliferativa. También se reivindica una composición farmacéutica, uso y procedimiento. Reivindicación 1: Un compuesto de la fórmula (1) y las sales y ésteres farmacéuticamente aceptables del mismo, en la que Z1, Z2 y Z3, con independencia entre sí, significan alcoxi C1-6, -CH2OCH3 o -CH2OCH2CH3, o bien uno de Z1, Z2, y Z3 es -H y los dos restantes, con independencia entre sí, son alquilo C1-6, alcoxi C1-6, -Cl, -Br, -F, -CF3, -CH2OCH3, -CH2OCH2CH3, -OCH2CH2R1, -CH2-morfolino, -OR2, -CH2R2, -OCH2-CF3, -OCH(CH3)CH2OH o -COOQ, en las que Q significa -H o alquilo C1-6, o uno de Z1, Z2 y Z3 es -H y los dos restantes junto con los dos átomos de carbono y los enlaces entre ellos y el anillo bencénico, al que están eventualmente sustituidos, forman un anillo insaturado o saturado de 5 o 6 eslabones que contiene por lo menos un heteroátomo elegido entre S, N, y O, en las que R1 significa -F, -OCH3, -N(CH3)2 o un anillo insaturado de 5 eslabones que contiene por lo menos un heteroátomo, eligiéndose dicho heteroátomo entre S, N y O, R2 es un anillo saturado de 3 a 6 eslabones e Y1 e Y2, con independencia entre sí, son -Cl, -Br, -NO2, -C=N o -C=CH.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34172901P | 2001-12-18 | 2001-12-18 | |
| US39087602P | 2002-06-21 | 2002-06-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR037882A1 true AR037882A1 (es) | 2004-12-09 |
Family
ID=26992633
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020104913A AR037882A1 (es) | 2001-12-18 | 2002-12-17 | Cis-imidazolinas |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US6617346B1 (es) |
| EP (1) | EP1463501B1 (es) |
| JP (1) | JP4361798B2 (es) |
| KR (1) | KR100640707B1 (es) |
| CN (1) | CN1604778A (es) |
| AR (1) | AR037882A1 (es) |
| AT (1) | ATE397925T1 (es) |
| AU (1) | AU2002361986B2 (es) |
| BR (1) | BR0215156A (es) |
| CA (1) | CA2468783A1 (es) |
| DE (1) | DE60227108D1 (es) |
| ES (1) | ES2307822T3 (es) |
| MX (1) | MXPA04005880A (es) |
| PA (1) | PA8561801A1 (es) |
| PE (1) | PE20030717A1 (es) |
| PL (1) | PL370909A1 (es) |
| RU (1) | RU2312101C2 (es) |
| TW (1) | TW200301696A (es) |
| UY (1) | UY27586A1 (es) |
| WO (1) | WO2003051360A1 (es) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0411597A (pt) * | 2003-06-17 | 2006-08-29 | Hoffmann La Roche | cis-imidazolinas como inibidores de mdm2 |
| US7132421B2 (en) | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
| AU2005243465B2 (en) * | 2004-05-18 | 2011-08-25 | F. Hoffmann-La Roche Ag | Novel CIS-imidazolines |
| WO2005115382A1 (en) * | 2004-05-29 | 2005-12-08 | 7Tm Pharma A/S | Crth2 receptor ligands for medicinal uses |
| US7893278B2 (en) * | 2004-06-17 | 2011-02-22 | Hoffman-La Roche Inc. | CIS-imidazolines |
| NZ561215A (en) | 2005-02-22 | 2010-12-24 | Univ Michigan | Small molecule inhibitors of MDM2 and uses thereof |
| CN101160314B (zh) | 2005-02-22 | 2012-05-23 | 密执安州立大学董事会 | Mdm2的小分子抑制剂以及其应用 |
| BRPI0619236A2 (pt) | 2005-12-01 | 2011-09-20 | Hoffmann La Roche | derivados de 2,4,5-trifenil imidazolina, composição farmacêutica que os compreende, uso e processo para a sìntese dos mesmos |
| AU2007207052B2 (en) * | 2006-01-18 | 2012-07-12 | F. Hoffmann-La Roche Ag | CIS-4, 5-biaryl-2-heterocyclic-imidazolines as MDM2 inhibitors |
| WO2008014216A1 (en) | 2006-07-28 | 2008-01-31 | St. Jude Children's Research Hospital | Method for treating ocular cancer |
| US8470785B2 (en) | 2006-07-28 | 2013-06-25 | 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 |
| EP2325180A1 (en) * | 2007-10-09 | 2011-05-25 | F. Hoffmann-La Roche AG | Chiral CIS-imidazolines |
| 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 |
| AU2010205201A1 (en) | 2009-01-16 | 2011-08-04 | Daiichi Sankyo Company,Limited | Imidazothiazole derivative having proline ring structure |
| KR20120099462A (ko) | 2009-11-12 | 2012-09-10 | 더 리젠츠 오브 더 유니버시티 오브 미시건 | 스피로-옥신돌 ｍｄｍ2 길항제 |
| 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 |
| US20130225603A1 (en) * | 2010-09-27 | 2013-08-29 | 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 |
| SG190230A1 (en) | 2010-11-12 | 2013-06-28 | Univ Michigan | Spiro-oxindole mdm2 antagonists |
| US8629133B2 (en) | 2011-03-10 | 2014-01-14 | Daiichi Sankyo Company, Limited | Dispiropyrrolidine derivatives |
| SG194873A1 (en) | 2011-05-11 | 2013-12-30 | Sanofi Sa | Spiro-oxindole mdm2 antagonists |
| KR101384683B1 (ko) * | 2011-10-27 | 2014-04-11 | 한국생명공학연구원 | ｍｄｍ２－결합 모티프를 포함하는 펩타이드 및 이의 용도 |
| CA2858565A1 (en) | 2011-12-07 | 2013-07-04 | 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 |
| RU2690663C2 (ru) | 2012-12-20 | 2019-06-05 | Мерк Шарп И Доум Корп. | Замещенные имидазопиридины в качестве ингибиторов hdm2 |
| WO2015116735A1 (en) | 2014-01-28 | 2015-08-06 | Mayo Foundation For Medical Education And Research | Methods and combinations for killing senescent cells and for treating senescence-associated diseases and disorders |
| 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 |
| AU2015211021B2 (en) | 2014-01-28 | 2020-07-02 | Buck Institute For Research On Aging | Methods and compositions for killing senescent cells and for treating senescence-associated diseases and disorders |
| 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 |
| US10759808B2 (en) | 2016-04-06 | 2020-09-01 | The Regents Of The University Of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| SG11201808728QA (en) | 2016-04-06 | 2018-11-29 | Univ Michigan Regents | Mdm2 protein degraders |
| PL3458101T3 (pl) | 2016-05-20 | 2021-05-31 | F. Hoffmann-La Roche Ag | Koniugaty PROTAC-przeciwciało i sposoby ich stosowania |
| JP6848055B2 (ja) | 2017-06-16 | 2021-03-24 | ユニティ バイオテクノロジー インコーポレイテッド | 薬学的使用のための鏡像異性的に純粋なシス‐イミダゾリン化合物を生成するための合成方法 |
| MX2021003999A (es) | 2018-10-08 | 2021-06-23 | Univ Michigan Regents | Moleculas de bajo peso molecular degradadoras de la proteina mdm2. |
| IL296451A (en) | 2020-03-19 | 2022-11-01 | Kymera Therapeutics Inc | mdm2 joints and their uses |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 BR BR0215156-1A patent/BR0215156A/pt not_active IP Right Cessation
- 2002-12-09 JP JP2003552293A patent/JP4361798B2/ja not_active Expired - Fee Related
- 2002-12-09 AT AT02796582T patent/ATE397925T1/de not_active IP Right Cessation
- 2002-12-09 DE DE60227108T patent/DE60227108D1/de not_active Expired - Lifetime
- 2002-12-09 CN CNA028252292A patent/CN1604778A/zh active Pending
- 2002-12-09 EP EP02796582A patent/EP1463501B1/en not_active Expired - Lifetime
- 2002-12-09 MX MXPA04005880A patent/MXPA04005880A/es active IP Right Grant
- 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 WO PCT/EP2002/013905 patent/WO2003051360A1/en active IP Right Grant
- 2002-12-09 KR KR1020047009612A patent/KR100640707B1/ko not_active IP Right Cessation
- 2002-12-09 RU RU2004122404/04A patent/RU2312101C2/ru not_active IP Right Cessation
- 2002-12-09 ES ES02796582T patent/ES2307822T3/es not_active Expired - Lifetime
- 2002-12-09 CA CA002468783A patent/CA2468783A1/en not_active Abandoned
- 2002-12-11 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 PA PA20028561801A patent/PA8561801A1/es unknown
- 2002-12-17 AR ARP020104913A patent/AR037882A1/es not_active Application Discontinuation
- 2002-12-17 UY UY27586A patent/UY27586A1/es not_active Application Discontinuation
- 2002-12-18 TW TW091136524A patent/TW200301696A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DE60227108D1 (de) | 2008-07-24 |
| KR100640707B1 (ko) | 2006-10-31 |
| JP2005515210A (ja) | 2005-05-26 |
| CA2468783A1 (en) | 2003-06-26 |
| TW200301696A (en) | 2003-07-16 |
| MXPA04005880A (es) | 2004-09-13 |
| RU2004122404A (ru) | 2005-05-27 |
| EP1463501A1 (en) | 2004-10-06 |
| WO2003051360A1 (en) | 2003-06-26 |
| US6617346B1 (en) | 2003-09-09 |
| AU2002361986B2 (en) | 2008-04-10 |
| UY27586A1 (es) | 2003-06-30 |
| PA8561801A1 (es) | 2003-07-28 |
| PL370909A1 (en) | 2005-05-30 |
| ATE397925T1 (de) | 2008-07-15 |
| RU2312101C2 (ru) | 2007-12-10 |
| JP4361798B2 (ja) | 2009-11-11 |
| BR0215156A (pt) | 2004-10-19 |
| KR20040068289A (ko) | 2004-07-30 |
| CN1604778A (zh) | 2005-04-06 |
| ES2307822T3 (es) | 2008-12-01 |
| PE20030717A1 (es) | 2003-08-28 |
| EP1463501B1 (en) | 2008-06-11 |
| AU2002361986A1 (en) | 2003-06-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |