PE20121532A1 - Pirrolidina-2-carboxamidas sustituidas - Google Patents

Pirrolidina-2-carboxamidas sustituidas

Info

Publication number
PE20121532A1
PE20121532A1 PE2012001184A PE2012001184A PE20121532A1 PE 20121532 A1 PE20121532 A1 PE 20121532A1 PE 2012001184 A PE2012001184 A PE 2012001184A PE 2012001184 A PE2012001184 A PE 2012001184A PE 20121532 A1 PE20121532 A1 PE 20121532A1
Authority
PE
Peru
Prior art keywords
phenyl
fluoro
chloro
cyane
pyrrolidin
Prior art date
Application number
PE2012001184A
Other languages
English (en)
Inventor
David Joseph Bartkovitz
Xin-Jie Chu
Quinjie Ding
Nan Jiang
Jin-Jun Liu
Tina Morgan Ross
Jing Zhang
Zhuming Zhang
Original Assignee
Hoffmann La Roche
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20121532A1 publication Critical patent/PE20121532A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO SELECCIONADO ENTRE: ESTER TERC-BUTILICO DEL ACIDO [2-(4-{[(2R,3S,4R,5S)-4-(4-CLORO-2-FLUORO-FENIL)-3-(3-CLORO-2-FLUORO-FENIL)-4-CIANO-5-(2,2-DIMETIL-PROPIL)-PIRROLIDIN-2-CARBONIL]-AMINO}-FENIL)-ETIL]-CARBAMICO QUIRAL; ACIDO 1-(4-{[(2R,3S,4R,5S)-4-(4-CLORO-2-FLUORO-FENIL)-3-(3-CLORO-2-FLUORO-FENIL)-4-CIANO-5-(2,2-DIMETIL-PROPIL)-PIRROLIDIN-2-CARBONIL]-AMINO}-FENIL)-PIPERIDIN-4-CARBOXILICO; ACIDO 5-{[(2R,3S,4R,5S)-4-(4-CLORO-2-FLUORO-FENIL)-3-(3-CLORO-2-FLUORO-FENIL)-4-CIANO-5-(2,2-DIMETIL-PROPIL)-PIRROLIDIN-2-CARBONIL]-AMINO}-PIRAZIN-2-CARBOXILICO; ACIDO 4-{[(2R,3S,4R,5S)-4-(4-CLORO-2-FLUORO-FENIL)-3-(3-CLORO-2-FLUORO-FENIL)-4-CIANO-5-(2,2-DIMETIL-PROPIL)-PIRROLIDIN-2-CARBONIL]-AMINO}-3-METOXI-BENZOICO; ACIDO 4-{[(2R,3S,4R,5S)-4-(4-CLORO-2-FLUORO-FENIL)-3-(3-CLORO-2-FLUORO-FENIL)-4-CIANO-5-(2,2-DIMETIL-PROPIL)-PIRROLIDIN-2-CARBONIL]-AMINO}-2-TRIFLUOROMETIL-BENZOICO; ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UTIL PARA EL TRATAMIENTO DE TUMORES DE MAMA, COLON, PULMON Y PROSTATA
PE2012001184A 2010-02-09 2011-02-04 Pirrolidina-2-carboxamidas sustituidas PE20121532A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12/702,402 US8354444B2 (en) 2008-09-18 2010-02-09 Substituted pyrrolidine-2-carboxamides

Publications (1)

Publication Number Publication Date
PE20121532A1 true PE20121532A1 (es) 2012-11-26

Family

ID=43608850

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012001184A PE20121532A1 (es) 2010-02-09 2011-02-04 Pirrolidina-2-carboxamidas sustituidas

Country Status (32)

Country Link
US (1) US8354444B2 (es)
EP (1) EP2534132B1 (es)
JP (1) JP5612710B2 (es)
KR (1) KR101461298B1 (es)
CN (1) CN102753522B (es)
AR (2) AR080143A1 (es)
AU (1) AU2011214506C1 (es)
BR (1) BR112012019672B1 (es)
CA (1) CA2788236C (es)
CL (1) CL2012002189A1 (es)
CR (1) CR20120410A (es)
CY (1) CY1119049T1 (es)
DK (1) DK2534132T3 (es)
EC (1) ECSP12012083A (es)
ES (1) ES2629439T3 (es)
HK (1) HK1171452A1 (es)
HR (1) HRP20170903T1 (es)
HU (1) HUE034816T2 (es)
LT (1) LT2534132T (es)
MX (1) MX2012009186A (es)
MY (1) MY165238A (es)
NZ (1) NZ601422A (es)
PE (1) PE20121532A1 (es)
PL (1) PL2534132T3 (es)
PT (1) PT2534132T (es)
RS (1) RS56163B1 (es)
RU (1) RU2564022C2 (es)
SG (1) SG182763A1 (es)
SI (1) SI2534132T1 (es)
TW (1) TWI401243B (es)
UA (1) UA107954C2 (es)
WO (1) WO2011098398A1 (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7303676B2 (en) * 2003-02-13 2007-12-04 Zenon Technology Partnership Supported biofilm apparatus and process
GB0811643D0 (en) 2008-06-25 2008-07-30 Cancer Rec Tech Ltd New therapeutic agents
US8354444B2 (en) 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
MX2012004377A (es) 2009-10-14 2012-06-01 Merck Sharp & Dohme Piperidinas sustituidas que aumentan la actividad de p53 y sus usos.
US8088815B2 (en) * 2009-12-02 2012-01-03 Hoffman-La Roche Inc. Spiroindolinone pyrrolidines
US20120010235A1 (en) * 2010-07-12 2012-01-12 Xin-Jie Chu N-substituted pyrrolidines
US8709419B2 (en) 2010-08-17 2014-04-29 Hoffmann-La Roche, Inc. Combination therapy
US9295669B2 (en) 2010-12-14 2016-03-29 Hoffman La-Roche Inc. Combination therapy for proliferative disorders
SI2684880T1 (en) 2011-03-10 2018-08-31 Daiichi Sankyo Company, Limited DERIVAT DISPIROPYROLIDINE
US8987274B2 (en) 2011-10-28 2015-03-24 Merck Sharp & Dohme Corp Macrocycles that increase p53 activity and the uses thereof
WO2013096150A1 (en) 2011-12-21 2013-06-27 Merck Sharp & Dohme Corp. Substituted piperidines as hdm2 inhibitors
US8993614B2 (en) * 2012-03-15 2015-03-31 F. Hoffmann-La Roche Ag Substituted pyrrolidine-2-carboxamides
US20130245089A1 (en) * 2012-03-19 2013-09-19 Hoffmann-La Roche Inc. Method for administration
US9216170B2 (en) 2012-03-19 2015-12-22 Hoffmann-La Roche Inc. Combination therapy for proliferative disorders
US20140200255A1 (en) * 2012-03-19 2014-07-17 Brian Higgins Method for administration
JP6067108B2 (ja) 2012-05-30 2017-01-25 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 置換ピロリジン−2−カルボキサミド
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
US8846657B2 (en) 2012-12-20 2014-09-30 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
JP6192244B2 (ja) * 2013-01-22 2017-09-06 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 改良されたバイオアベイラビリティを有する薬学的組成物
ES2630392T3 (es) * 2013-02-21 2017-08-21 F. Hoffmann-La Roche Ag Síntesis asimétrica de una pirrolidina-2-carboxamida sustituida
WO2014158638A1 (en) * 2013-03-13 2014-10-02 Dow Agrosciences Llc Preparation of certain (substituted phenyl)-triazolyl-(substituted phenyl) molecules, and intermediates and insecticides related thereto
WO2014202497A1 (en) * 2013-06-19 2014-12-24 F. Hoffmann-La Roche Ag Combination of ro5503781, capecitabine and oxaliplantin for cancer therapy
CA2912816A1 (en) * 2013-06-19 2014-12-24 F. Hoffmann-La Roche Ag Combination of ro5503781 and capecitabine for cancer therapy
JP6346945B2 (ja) * 2013-06-24 2018-06-20 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 安定な静脈内製剤
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
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
BR112016023767A2 (pt) * 2014-04-15 2017-08-15 Hoffmann La Roche forma sólida, composição farmacêutica, compostos, métodos, composições e utilizações
CA2945527C (en) 2014-04-17 2022-05-17 The Regents Of The University Of Michigan Mdm2 inhibitors and therapeutic methods using the same
JP6162646B2 (ja) * 2014-05-27 2017-07-12 信越化学工業株式会社 3,5−ジメチルドデカン酸の製造方法
JP6608439B2 (ja) * 2014-10-10 2019-11-20 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Mdm2アンタゴニストによる患者のがん治療を個別化するための方法
RS61759B9 (sr) * 2015-03-30 2021-11-30 Mission Therapeutics Ltd Jedinjenja 1-cijano-pirolidina kao inhibitori usp30
GB201517216D0 (en) 2015-09-29 2015-11-11 Cancer Res Technology Ltd And Astex Therapeutics Ltd Pharmaceutical compounds
GB201517217D0 (en) 2015-09-29 2015-11-11 Astex Therapeutics Ltd And Cancer Res Technology Ltd Pharmaceutical compounds
PL3458101T3 (pl) 2016-05-20 2021-05-31 F. Hoffmann-La Roche Ag Koniugaty PROTAC-przeciwciało i sposoby ich stosowania
KR102122469B1 (ko) 2016-11-01 2020-06-12 주식회사 엘지화학 변성 공액디엔계 중합체 및 이의 제조방법
CA3048088C (en) 2016-12-30 2021-05-04 Oriental (Luzhou) Agrochemicals. Co., Ltd. Method for preparing 2-(cyclohexenylidene) malonic acid derivatives and uses thereof
GB201704965D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
GB201704966D0 (en) 2017-03-28 2017-05-10 Astex Therapeutics Ltd Pharmaceutical compounds
UY37806A (es) 2017-07-11 2020-01-31 Vertex Pharma Carboxamidas como moduladores de los canales de sodio
CN108586195A (zh) * 2017-12-27 2018-09-28 北京汇康博源医药科技有限公司 一种5-羟基-7,7-二甲基-2h-茚酮的制备方法
WO2019213106A1 (en) 2018-04-30 2019-11-07 Teva Pharmaceuticals International Gmbh Solid state forms of idasanutlin
CR20220316A (es) 2019-12-06 2022-10-07 Vertex Pharma Tetrahidrofuranos sustituidos como moduladores de canales de sodio
CN117794920A (zh) 2021-06-04 2024-03-29 沃泰克斯药物股份有限公司 N-(羟烷基(杂)芳基)四氢呋喃甲酰胺作为钠通道调节剂
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same
CN116459225B (zh) * 2023-04-26 2023-11-10 东莞市金美济药业有限公司 一种艾拉戈克钠片及其制备工艺

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4732902A (en) 1986-05-23 1988-03-22 Hoffmann-La Roche Inc. Pyrroloisoquinolinyl-dimethyloxoalkyl alkonoates and their use as antipsychotic agents
TW394760B (en) 1993-09-07 2000-06-21 Hoffmann La Roche Novel Carboxamides, process for their preparation and pharmaceutical composition containing the same
DE69824433D1 (en) 1997-08-28 2004-07-15 Biovitrum Ab Proteintyrosinphosphatase inhibitoren
US6482921B1 (en) 1999-01-28 2002-11-19 Essential Therapeutics, Inc. Uridyl peptide antibiotic (UPA) derivatives, their synthesis and use
US6531494B1 (en) 2001-08-29 2003-03-11 Pharmacia Corporation Gem-substituted αvβ3 antagonists
US6916833B2 (en) * 2003-03-13 2005-07-12 Hoffmann-La Roche Inc. Substituted piperidines
CN1294120C (zh) * 2003-10-21 2007-01-10 山东大学 吡咯烷类基质金属蛋白酶抑制剂及其应用
US7550487B2 (en) * 2004-03-26 2009-06-23 Hoffmann-La Roche Inc. Pyrrolidine-3,4-dicarboxamide derivatives
US7759383B2 (en) * 2005-02-22 2010-07-20 The Regents Of The University Of Michigan Small molecule inhibitors of MDM2 and the uses thereof
CA2752738C (en) 2005-02-22 2014-05-27 The Regents Of The University Of Michigan Small molecule inhibitors of mdm2 and uses thereof
JP2008546684A (ja) 2005-06-17 2008-12-25 アストラゼネカ アクチボラグ トロンビン阻害性2−オキソ−1,2,5,6−テトラヒドロピリジン誘導体
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
CN101553219B (zh) 2006-12-06 2013-04-24 塞诺菲-安万特股份有限公司 作为TAFIa抑制剂的脲和磺酰胺衍生物
TW200911787A (en) 2007-07-03 2009-03-16 Astrazeneca Ab New aza-bicyclohexane compounds useful as inhibitors of thrombin
JO2704B1 (en) * 2007-09-21 2013-03-03 جانسين فارماسوتيكا ان في Interference inhibition factors between MD2 and B53
US8134001B2 (en) * 2007-12-14 2012-03-13 Hoffmann-La Roche Inc. Spiroindolinone derivatives
NZ589671A (en) 2008-06-06 2012-03-30 Sanofi Aventis Macrocyclic urea and sulfamide derivatives as inhibitors of tafia
JP2011525487A (ja) 2008-06-23 2011-09-22 アストラゼネカ アクチボラグ トロンビン阻害剤としての使用のための新規複素環式カルボキサミド
GB0811643D0 (en) * 2008-06-25 2008-07-30 Cancer Rec Tech Ltd New therapeutic agents
US8354444B2 (en) 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
NZ591024A (en) 2008-09-18 2013-01-25 Hoffmann La Roche Substituted pyrrolidine-2-carboxamides
US8017607B2 (en) 2009-10-14 2011-09-13 Hoffmann-La Roche Inc. N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions

Also Published As

Publication number Publication date
JP5612710B2 (ja) 2014-10-22
HRP20170903T1 (hr) 2017-09-08
HK1171452A1 (en) 2013-03-28
BR112012019672B1 (pt) 2020-11-17
AR080143A1 (es) 2012-03-14
AU2011214506A1 (en) 2012-08-16
HUE034816T2 (en) 2018-02-28
CR20120410A (es) 2012-09-05
AR114159A2 (es) 2020-07-29
KR20120119922A (ko) 2012-10-31
AU2011214506B2 (en) 2014-04-17
SG182763A1 (en) 2012-08-30
CA2788236C (en) 2015-01-20
US20100152190A1 (en) 2010-06-17
NZ601422A (en) 2014-07-25
CY1119049T1 (el) 2018-01-10
LT2534132T (lt) 2017-07-10
ECSP12012083A (es) 2012-09-28
UA107954C2 (en) 2015-03-10
TWI401243B (zh) 2013-07-11
CN102753522A (zh) 2012-10-24
WO2011098398A1 (en) 2011-08-18
TW201136892A (en) 2011-11-01
EP2534132B1 (en) 2017-04-26
JP2013518921A (ja) 2013-05-23
DK2534132T3 (en) 2017-07-10
CL2012002189A1 (es) 2012-11-23
MX2012009186A (es) 2012-08-23
MY165238A (en) 2018-03-14
ES2629439T3 (es) 2017-08-09
CN102753522B (zh) 2013-11-27
CA2788236A1 (en) 2011-08-18
BR112012019672A2 (pt) 2016-05-03
SI2534132T1 (sl) 2017-08-31
PT2534132T (pt) 2017-06-26
PL2534132T3 (pl) 2017-09-29
RU2564022C2 (ru) 2015-09-27
EP2534132A1 (en) 2012-12-19
US8354444B2 (en) 2013-01-15
KR101461298B1 (ko) 2014-11-28
RU2012138257A (ru) 2014-03-20
RS56163B1 (sr) 2017-11-30
AU2011214506C1 (en) 2014-07-17

Similar Documents

Publication Publication Date Title
PE20121532A1 (es) Pirrolidina-2-carboxamidas sustituidas
PE20110151A1 (es) Derivados de 3-hidroxi metil-1h-[1,2,4]triazolil-1-ilo como antagonistas muscarinicos y agonistas beta2-adrenergicos
PE20142185A1 (es) Pirrolidina-2-carboxamidas sustituidas
PE20141322A1 (es) Ciclopropilaminas como inhibidores de desmetilasa 1 especifica de lisina
PE20151335A1 (es) Composicion farmaceutica con biodisponibilidad mejorada
CL2008001047A1 (es) Compuestos derivados de difenil-dihidro-imidazopiridinonas; inhibidores de mdm2-p53;composicion farmaceutica;y uso para preparar un medicamento destinado al tratamiento o control de tumores solidos,tales como:tumores de mama.de colon,de pulmon o de prostata.
TN2014000398A1 (en) New indanyloxydihydrobenzofuranylacetic acid derivatives and their use as gpr40 receptor agonists
TR201203989T1 (tr) Ksantin oksidaz inhibitörleri olarak etkin olan yeni bileşikler, bunları hazırlamaya yönelik yöntem ve bunları içeren farmasötik bileşim.
PE20140966A1 (es) Quinazolincarboxamida azetidinas
PE20140831A1 (es) Nuevo derivado de 1,2,3,4-tetrahidroquinolina util para el tratamiento de diabetes
PE20170502A1 (es) ACIDO 4-(3-FLUORO-3-(2-(5,6,7,8-TETRAHIDRO-1,8-NAFTIRIDIN-2-IL)ETIL)PIRROLIDIN-1-IL)-3-(3-(2-METOXIETOXI)FENIL)BUTANOICO COMO ANTAGONISTA DE INTEGRINA aVß6
PH12015501116A1 (en) New indanyloxydihydrobenzofuranylacetic acids
NZ612119A (en) Use of sigma ligands in bone cancer pain
MX2014001671A (es) Compuestos fungicidas de 1-{2-[2-halo-4-(4-halogen-fenoxi)-fenil]- 2-aluiniloxi-etil}-1h[1,2,4]triazol sustituidos.
AR082600A1 (es) Polimorfos cristalinos de la sal de besilato de n-(3-(5-fluor-2-(4-(2-metoxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida, composiciones farmaceuticas que los contienen y uso de los mismos para tratar canceres, enfermedades autoinmunes y oseas, entre otras
EA201290952A1 (ru) Химические соединения
NZ601121A (en) 5-alkynyl-pyrimidines
PE20091400A1 (es) Derivados de n-(2-amino-fenil)-amida como inhibidores de hdac
EA201200046A1 (ru) Новые соединения, фармацевтическая композиция и связанные с ними способы
PE20170914A1 (es) 1-[2-(aminometil)bencil]-2-tioxo-1,2,3,5-tetrahidro-4h-pirrolo[3,2-d]pirimidin-4-onas como inhibidores de mieloperoxidasa
PE20210859A1 (es) Inhibidores de triazol glicolato oxidasa
GEP20156319B (en) Asymmetric ureas and medical uses thereof
PE20142399A1 (es) Compuestos de pirazol como inhibidores de sglt1
EA201891506A1 (ru) Индолиноновые соединения и их применение в лечении фиброзных заболеваний
EP4249005A3 (en) 18f-labeled triazole containing psma inhibitors

Legal Events

Date Code Title Description
FG Grant, registration