PE20142185A1 - Pirrolidina-2-carboxamidas sustituidas - Google Patents
Pirrolidina-2-carboxamidas sustituidasInfo
- Publication number
- PE20142185A1 PE20142185A1 PE2014001419A PE2014001419A PE20142185A1 PE 20142185 A1 PE20142185 A1 PE 20142185A1 PE 2014001419 A PE2014001419 A PE 2014001419A PE 2014001419 A PE2014001419 A PE 2014001419A PE 20142185 A1 PE20142185 A1 PE 20142185A1
- Authority
- PE
- Peru
- Prior art keywords
- chloro
- phenyl
- pyrrolidine
- lower alkyl
- substitute
- Prior art date
Links
- 150000003857 carboxamides Chemical class 0.000 title 1
- -1 4-CHLORO-2-FLUORPHENYL Chemical class 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- SLRMQYXOBQWXCR-UHFFFAOYSA-N 2154-56-5 Chemical class [CH2]C1=CC=CC=C1 SLRMQYXOBQWXCR-UHFFFAOYSA-N 0.000 abstract 1
- 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 abstract 1
- 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
-
- 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
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/572—Five-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Polyethers (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE: X ES H, F, CL, ENTRE OTROS; Y ES H, F, CL, ENTRE OTROS; Z ES ALCOXI INFERIOR; R1 ES ALQUILO INFERIOR, ALQUENILO INFERIOR, ARILO, ENTRE OTROS; R2 ES FENILO SUSTITUIDO; R3 ES H, ALQUILO INFERIOR O ALQUILO INFERIOR SUSTITUIDO; R4 SE ELIJE DE II, DONDE R5 ES ALQUILO INFERIOR, HETEROCICLO, CICLOALQUILO ENTRE OTROS Y R6 ES H O BENCILO. SON COMPUESTOS PREFERIDOS: 4-((2R,3S,4R,5S)-3-(3-CLORO-2-FLUORFENIL)-4-(4-CLORO-2-FLUORFENIL)-4-CIANO-5-NEOPENTILPIRROLIDINA-2-CARBOXAMIDO)-3-METOXIBENZOATO DE 1-(ETIL(ISOPROPIL)CARBAMOILOXI)ETILO; 4-{[(2R,3S,4R,5S)-3-(3-CLORO-2-FLUOR-FENIL)-4-(4-CLORO-2-FLUOR-FENIL)-4-CIANO-5-(2,2-DIMETIL-PROPIL)-PIRROLIDINA-2-CARBONIL]-AMINO}-3-METOXI-BENZOATO DE DI-TERT-BUTOXI-FOSFORILOXIMETILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN INHIBIDOR DE LA MDM2 Y ES UTIL EN EL TRATAMIENTO DEL CANCER.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261611200P | 2012-03-15 | 2012-03-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20142185A1 true PE20142185A1 (es) | 2014-12-29 |
Family
ID=47844360
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2014001419A PE20142185A1 (es) | 2012-03-15 | 2013-03-12 | Pirrolidina-2-carboxamidas sustituidas |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US8993614B2 (es) |
| EP (1) | EP2825528B1 (es) |
| JP (1) | JP6125546B2 (es) |
| KR (1) | KR20140138165A (es) |
| CN (1) | CN104271554B (es) |
| AR (1) | AR090328A1 (es) |
| AU (1) | AU2013203662B2 (es) |
| BR (1) | BR112014018959A8 (es) |
| CA (1) | CA2860781A1 (es) |
| CL (1) | CL2014001858A1 (es) |
| CO (1) | CO6990736A2 (es) |
| CR (1) | CR20140399A (es) |
| DK (1) | DK2825528T3 (es) |
| EA (1) | EA025557B1 (es) |
| ES (1) | ES2634290T3 (es) |
| HK (1) | HK1200830A1 (es) |
| HU (1) | HUE032864T2 (es) |
| IL (1) | IL234173A (es) |
| MX (1) | MX2014010942A (es) |
| NZ (1) | NZ626505A (es) |
| PE (1) | PE20142185A1 (es) |
| PH (1) | PH12014501542A1 (es) |
| PL (1) | PL2825528T3 (es) |
| SG (1) | SG11201404344XA (es) |
| SI (1) | SI2825528T1 (es) |
| TW (1) | TWI586648B (es) |
| UA (1) | UA113541C2 (es) |
| WO (1) | WO2013135648A1 (es) |
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| CN107540594A (zh) | 2012-05-30 | 2018-01-05 | 霍夫曼-拉罗奇有限公司 | 取代的吡咯烷‑2‑甲酰胺 |
| 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 |
| SG11201510654WA (en) * | 2013-06-24 | 2016-01-28 | Hoffmann La Roche | Stable intravenous formulation |
| WO2015000945A1 (en) * | 2013-07-03 | 2015-01-08 | F. Hoffmann-La Roche Ag | Mrna-based gene expression for personalizing patient cancer therapy with an mdm2 antagonist |
| AR097584A1 (es) | 2013-09-12 | 2016-03-23 | Hoffmann La Roche | Terapia de combinación de anticuerpos contra el csf-1r humano y anticuerpos contra el pd-l1 humano |
| DK3077004T3 (da) * | 2013-12-05 | 2020-04-27 | Hoffmann La Roche | Hidtil ukendt kombinationsbehandling af akut myeloid leukæmi (AML) |
| US9657351B2 (en) | 2013-12-06 | 2017-05-23 | Hoffman-La Roche Inc. | MRNA-based gene expression for personalizing patient cancer therapy with an MDM2 antagonist |
| JP6621761B2 (ja) * | 2014-04-15 | 2019-12-18 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 薬学的に活性な化合物の固体形態 |
| CA2946164A1 (en) * | 2014-05-22 | 2015-11-26 | The University Of Sydney | Omega-3 analogues |
| US20170227544A1 (en) * | 2014-10-10 | 2017-08-10 | Hoffmann-La Roche Inc. | Methods for personalizing patient cancer therapy with an mdm2 antagonist |
| CN104496822B (zh) * | 2014-12-15 | 2016-10-26 | 扬州三友合成化工有限公司 | 一种1-氯乙基环己基丙基碳酸酯的制备方法 |
| MA42043A (fr) | 2015-05-07 | 2018-03-14 | Agenus Inc | Anticorps anti-ox40 et procédés d'utilisation de ceux-ci |
| CN116063542A (zh) | 2015-12-02 | 2023-05-05 | 阿吉纳斯公司 | 抗体和其使用方法 |
| 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 |
| EP3498712B1 (en) * | 2016-08-08 | 2024-01-03 | Jiangsu Yayo Biotechnology Co. Ltd | Spirocyclic indolone polyethylene glycol carbonate compound, composition, preparation method and use thereof |
| CN107698598B (zh) * | 2016-08-08 | 2019-06-21 | 肖飞 | 螺环吲哚酮聚乙二醇碳酸酯类化合物和其组合物、制备方法及用途 |
| CN109790220A (zh) | 2016-08-25 | 2019-05-21 | 豪夫迈·罗氏有限公司 | 与巨噬细胞激活剂组合的抗csf-1r抗体的间歇给药 |
| CA3041340A1 (en) | 2016-11-09 | 2018-05-17 | Agenus Inc. | Anti-ox40 antibodies, anti-gitr antibodies, and methods of use thereof |
| EP3558360A1 (en) | 2016-12-22 | 2019-10-30 | F. Hoffmann-La Roche AG | Treatment of tumors with an anti-csf-1r antibody in combination with an anti-pd-l1 antibody after failure of anti-pd-l1/pd1 treatment |
| CN111511361A (zh) * | 2017-12-20 | 2020-08-07 | 安杰斯制药公司 | 作为多激酶抑制剂的胺基碳酸盐及尿素化合物 |
| CN114230561B (zh) * | 2020-09-09 | 2024-03-19 | 中国人民解放军海军军医大学 | 一种mdm2抑制剂类小分子化合物及用途 |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
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| JPH0720857B2 (ja) | 1988-08-11 | 1995-03-08 | テルモ株式会社 | リポソームおよびその製法 |
| DE69120141T2 (de) | 1990-03-28 | 1996-11-28 | Shuji Kojima | Polymerkombiniertes Arzneimittel zur Magenbehandlung und Verfahren zu dessen Herstellung |
| US5681811A (en) | 1993-05-10 | 1997-10-28 | Protein Delivery, Inc. | Conjugation-stabilized therapeutic agent compositions, delivery and diagnostic formulations comprising same, and method of making and using the same |
| GB9317618D0 (en) | 1993-08-24 | 1993-10-06 | Royal Free Hosp School Med | Polymer modifications |
| KR100361933B1 (ko) | 1993-09-08 | 2003-02-14 | 라 졸라 파마슈티칼 컴파니 | 화학적으로정의된비중합성결합가플랫폼분자및그것의콘주게이트 |
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| DE4435087A1 (de) | 1994-09-30 | 1996-04-04 | Deutsches Krebsforsch | Konjugat zur Behandlung von Infektions-, Autoimmun- und Hauterkrankungen |
| AU5773798A (en) | 1997-01-29 | 1998-08-18 | Polymasc Pharmaceuticals Plc | Pegylation process |
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| JP4991037B2 (ja) | 2004-04-01 | 2012-08-01 | カーディオム ファーマ コーポレイション | イオンチャネル調節化合物を含む薬物結合体 |
| TW200616604A (en) | 2004-08-26 | 2006-06-01 | Nicholas Piramal India Ltd | Nitric oxide releasing prodrugs containing bio-cleavable linker |
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| SG176463A1 (en) | 2005-02-22 | 2011-12-29 | Univ Michigan | Small molecule inhibitors of mdm2 and uses thereof |
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| WO2008109783A2 (en) | 2007-03-06 | 2008-09-12 | The Regents Of The University Of California | Detecting spin perturbations using magnetic resonance imaging |
| JP2008308690A (ja) | 2007-06-13 | 2008-12-25 | Bio-Cancer Treatment Internatl Ltd | ポリ（エチレングリコール）機能性誘導体およびその製造方法 |
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| ES2398342T3 (es) | 2008-09-18 | 2013-03-15 | F. Hoffmann-La Roche Ag | Pirrolidina-2-carboxamidas sustituidas |
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| US20110118283A1 (en) | 2009-11-17 | 2011-05-19 | Qingjie Ding | Substituted Pyrrolidine-2-Carboxamides |
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| CN101991860B (zh) | 2010-11-08 | 2013-06-19 | 中国药科大学 | 泊洛沙姆-羧酸类药物偶联物及其制备方法与应用 |
| NZ611866A (en) | 2010-11-12 | 2015-04-24 | Univ Michigan | Spiro-oxindole mdm2 antagonists |
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| EP2678042B1 (en) | 2011-02-23 | 2018-05-09 | The Board of Trustees of the University of Illionis | Amphiphilic dendron-coils, micelles thereof and uses |
| CN102247602B (zh) | 2011-06-13 | 2013-01-02 | 中山大学 | 一种超分子水凝胶双重药物载体及其制备方法和应用 |
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-
2013
- 2013-03-05 US US13/785,267 patent/US8993614B2/en not_active Expired - Fee Related
- 2013-03-12 AU AU2013203662A patent/AU2013203662B2/en not_active Ceased
- 2013-03-12 MX MX2014010942A patent/MX2014010942A/es unknown
- 2013-03-12 HU HUE13708466A patent/HUE032864T2/en unknown
- 2013-03-12 BR BR112014018959A patent/BR112014018959A8/pt not_active IP Right Cessation
- 2013-03-12 JP JP2014561405A patent/JP6125546B2/ja active Active
- 2013-03-12 EA EA201491623A patent/EA025557B1/ru not_active IP Right Cessation
- 2013-03-12 EP EP13708466.1A patent/EP2825528B1/en active Active
- 2013-03-12 ES ES13708466.1T patent/ES2634290T3/es active Active
- 2013-03-12 PE PE2014001419A patent/PE20142185A1/es not_active Application Discontinuation
- 2013-03-12 DK DK13708466.1T patent/DK2825528T3/en active
- 2013-03-12 WO PCT/EP2013/054920 patent/WO2013135648A1/en active Application Filing
- 2013-03-12 CN CN201380021271.9A patent/CN104271554B/zh not_active Expired - Fee Related
- 2013-03-12 CA CA2860781A patent/CA2860781A1/en not_active Abandoned
- 2013-03-12 SI SI201330703T patent/SI2825528T1/sl unknown
- 2013-03-12 KR KR20147025671A patent/KR20140138165A/ko not_active Application Discontinuation
- 2013-03-12 SG SG11201404344XA patent/SG11201404344XA/en unknown
- 2013-03-12 NZ NZ626505A patent/NZ626505A/en not_active IP Right Cessation
- 2013-03-12 PL PL13708466T patent/PL2825528T3/pl unknown
- 2013-03-13 AR ARP130100814A patent/AR090328A1/es unknown
- 2013-03-14 TW TW102109122A patent/TWI586648B/zh not_active IP Right Cessation
- 2013-12-03 UA UAA201411036A patent/UA113541C2/uk unknown
-
2014
- 2014-06-25 CO CO14137196A patent/CO6990736A2/es active IP Right Grant
- 2014-07-03 PH PH12014501542A patent/PH12014501542A1/en unknown
- 2014-07-14 CL CL2014001858A patent/CL2014001858A1/es unknown
- 2014-08-18 IL IL234173A patent/IL234173A/en not_active IP Right Cessation
- 2014-08-26 CR CR20140399A patent/CR20140399A/es unknown
-
2015
- 2015-02-09 HK HK15101410.3A patent/HK1200830A1/xx not_active IP Right Cessation
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