CA2774512A1 - Novel n-substituted-pyrrolidines as inhibitors of mdm2-p-53 interactions - Google Patents
Novel n-substituted-pyrrolidines as inhibitors of mdm2-p-53 interactions Download PDFInfo
- Publication number
- CA2774512A1 CA2774512A1 CA2774512A CA2774512A CA2774512A1 CA 2774512 A1 CA2774512 A1 CA 2774512A1 CA 2774512 A CA2774512 A CA 2774512A CA 2774512 A CA2774512 A CA 2774512A CA 2774512 A1 CA2774512 A1 CA 2774512A1
- Authority
- CA
- Canada
- Prior art keywords
- phenyl
- chloro
- fluoro
- coch2
- dimethyl
- 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.)
- Abandoned
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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)
- Pyrrole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25141309P | 2009-10-14 | 2009-10-14 | |
| US61/251,413 | 2009-10-14 | ||
| US34562610P | 2010-05-18 | 2010-05-18 | |
| US61/345,626 | 2010-05-18 | ||
| PCT/EP2010/065159 WO2011045257A1 (en) | 2009-10-14 | 2010-10-11 | Novel n-substituted-pyrrolidines as inhibitors of mdm2-p-53 interactions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2774512A1 true CA2774512A1 (en) | 2011-04-21 |
Family
ID=43567698
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2774512A Abandoned CA2774512A1 (en) | 2009-10-14 | 2010-10-11 | Novel n-substituted-pyrrolidines as inhibitors of mdm2-p-53 interactions |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8017607B2 (Direct) |
| EP (1) | EP2488491A1 (Direct) |
| JP (1) | JP2013507416A (Direct) |
| KR (1) | KR20120081210A (Direct) |
| CN (1) | CN102548963A (Direct) |
| AU (1) | AU2010305914A1 (Direct) |
| BR (1) | BR112012008485A2 (Direct) |
| CA (1) | CA2774512A1 (Direct) |
| IL (1) | IL218018A0 (Direct) |
| IN (1) | IN2012DN02487A (Direct) |
| MX (1) | MX2012003982A (Direct) |
| WO (1) | WO2011045257A1 (Direct) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008095063A1 (en) | 2007-01-31 | 2008-08-07 | Dana-Farber Cancer Institute, Inc. | Stabilized p53 peptides and uses thereof |
| ES2430067T3 (es) | 2007-03-28 | 2013-11-18 | President And Fellows Of Harvard College | Polipéptidos cosidos |
| US8354444B2 (en) * | 2008-09-18 | 2013-01-15 | Hoffmann-La Roche Inc. | Substituted pyrrolidine-2-carboxamides |
| US20110118283A1 (en) * | 2009-11-17 | 2011-05-19 | Qingjie Ding | Substituted Pyrrolidine-2-Carboxamides |
| DK2603600T3 (da) | 2010-08-13 | 2019-03-04 | Aileron Therapeutics Inc | Peptidomimetiske makrocyklusser |
| WO2012076513A1 (en) * | 2010-12-09 | 2012-06-14 | F. Hoffmann-La Roche Ag | 3-cyano-1-hydroxymethyl-2-phenylpyrrolidine derivatives as inhibitors of mdm2-p53 interactions useful for the treatment of cancer |
| CA2829188C (en) | 2011-03-10 | 2016-10-18 | Daiichi Sankyo Company, Limited | Dispiropyrrolidine derivatives |
| CA2852468A1 (en) | 2011-10-18 | 2013-04-25 | Aileron Therapeutics, Inc. | Peptidomimetic macrocyles |
| SG10201606775YA (en) | 2012-02-15 | 2016-10-28 | Aileron Therapeutics Inc | Peptidomimetic macrocycles |
| HK1205454A1 (en) | 2012-02-15 | 2015-12-18 | Aileron Therapeutics, Inc. | Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles |
| 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 |
| CA2887285A1 (en) | 2012-11-01 | 2014-05-08 | Aileron Therapeutics, Inc. | Disubstituted amino acids and methods of preparation and use thereof |
| 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 |
| SG10201902598VA (en) | 2014-09-24 | 2019-04-29 | Aileron Therapeutics Inc | Peptidomimetic macrocycles and formulations thereof |
| JP2017533889A (ja) | 2014-09-24 | 2017-11-16 | エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. | ペプチド模倣大環状分子およびその使用 |
| JP2018516844A (ja) | 2015-03-20 | 2018-06-28 | エルロン・セラピューティクス・インコーポレイテッドAileron Therapeutics,Inc. | ペプチド模倣大環状分子およびその使用 |
| EP3347372A4 (en) | 2015-09-10 | 2019-09-04 | Aileron Therapeutics, Inc. | PEPTIDOMIMETIC MACROCYCLES AS MODULATORS OF MCL-1 |
| JP2019522633A (ja) | 2016-05-20 | 2019-08-15 | ジェネンテック, インコーポレイテッド | Protac抗体コンジュゲート及び使用方法 |
| 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 (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0947511A1 (en) | 1998-03-30 | 1999-10-06 | F. Hoffmann-La Roche Ag | Derivatives of phenoxy acetic acid and of phenoxymethyl tetrazole having antitumor activity |
| SK822002A3 (en) | 1999-07-21 | 2002-09-10 | Astrazeneca Ab | New compounds |
| WO2005099687A2 (en) | 2004-04-09 | 2005-10-27 | President And Fellows Of Harvard College | Analogs of salinosporamide a |
| US7423051B2 (en) | 2004-07-15 | 2008-09-09 | Hoffmann-La Roche Inc. | 2,6-diaminopyridine derivatives |
| CA2752738C (en) | 2005-02-22 | 2014-05-27 | The Regents Of The University Of Michigan | Small molecule inhibitors of mdm2 and uses thereof |
| JP2009523751A (ja) | 2006-01-18 | 2009-06-25 | エフ.ホフマン−ラ ロシュ アーゲー | Mdm2阻害剤としてのシス−4,5−ビアリール−2−ヘテロサイクリック−イミダゾリン |
| JP2009542666A (ja) | 2006-06-30 | 2009-12-03 | シェーリング コーポレイション | P53活性を増加させる置換ピペリジンおよびその使用 |
| MX2011002976A (es) | 2008-09-18 | 2011-04-11 | Hoffmann La Roche | Pirrolidina-2-carboxamidas sustituidas. |
-
2010
- 2010-10-06 US US12/898,974 patent/US8017607B2/en not_active Expired - Fee Related
- 2010-10-11 CN CN2010800461741A patent/CN102548963A/zh active Pending
- 2010-10-11 IN IN2487DEN2012 patent/IN2012DN02487A/en unknown
- 2010-10-11 BR BR112012008485A patent/BR112012008485A2/pt not_active IP Right Cessation
- 2010-10-11 CA CA2774512A patent/CA2774512A1/en not_active Abandoned
- 2010-10-11 KR KR1020127012100A patent/KR20120081210A/ko not_active Ceased
- 2010-10-11 JP JP2012533592A patent/JP2013507416A/ja active Pending
- 2010-10-11 AU AU2010305914A patent/AU2010305914A1/en not_active Abandoned
- 2010-10-11 WO PCT/EP2010/065159 patent/WO2011045257A1/en not_active Ceased
- 2010-10-11 MX MX2012003982A patent/MX2012003982A/es not_active Application Discontinuation
- 2010-10-11 EP EP10768450A patent/EP2488491A1/en not_active Withdrawn
-
2012
- 2012-02-09 IL IL218018A patent/IL218018A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20110086854A1 (en) | 2011-04-14 |
| BR112012008485A2 (pt) | 2019-09-24 |
| IN2012DN02487A (Direct) | 2015-08-28 |
| US8017607B2 (en) | 2011-09-13 |
| AU2010305914A1 (en) | 2012-03-08 |
| CN102548963A (zh) | 2012-07-04 |
| WO2011045257A1 (en) | 2011-04-21 |
| MX2012003982A (es) | 2012-05-08 |
| EP2488491A1 (en) | 2012-08-22 |
| IL218018A0 (en) | 2012-04-30 |
| KR20120081210A (ko) | 2012-07-18 |
| JP2013507416A (ja) | 2013-03-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20131011 |