IN2012DN02487A - - Google Patents

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Publication number
IN2012DN02487A
IN2012DN02487A IN2487DEN2012A IN2012DN02487A IN 2012DN02487 A IN2012DN02487 A IN 2012DN02487A IN 2487DEN2012 A IN2487DEN2012 A IN 2487DEN2012A IN 2012DN02487 A IN2012DN02487 A IN 2012DN02487A
Authority
IN
India
Prior art keywords
enantiomers
esters
useful
formula
pharmaceutically acceptable
Prior art date
Application number
Inventor
David Joseph Bartkovits
Xin-Jie Chu
Jin-Jun Liu
Tina Morgan Ross
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 IN2012DN02487A publication Critical patent/IN2012DN02487A/en

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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)

Abstract

There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.
IN2487DEN2012 2009-10-14 2010-10-11 IN2012DN02487A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25141309P 2009-10-14 2009-10-14
US34562610P 2010-05-18 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
IN2012DN02487A true IN2012DN02487A (en) 2015-08-28

Family

ID=43567698

Family Applications (1)

Application Number Title Priority Date Filing Date
IN2487DEN2012 IN2012DN02487A (en) 2009-10-14 2010-10-11

Country Status (12)

Country Link
US (1) US8017607B2 (en)
EP (1) EP2488491A1 (en)
JP (1) JP2013507416A (en)
KR (1) KR20120081210A (en)
CN (1) CN102548963A (en)
AU (1) AU2010305914A1 (en)
BR (1) BR112012008485A2 (en)
CA (1) CA2774512A1 (en)
IL (1) IL218018A0 (en)
IN (1) IN2012DN02487A (en)
MX (1) MX2012003982A (en)
WO (1) WO2011045257A1 (en)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8889632B2 (en) 2007-01-31 2014-11-18 Dana-Farber Cancer Institute, Inc. Stabilized p53 peptides and uses thereof
US8592377B2 (en) 2007-03-28 2013-11-26 President And Fellows Of Harvard College Stitched polypeptides
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
WO2012021876A2 (en) 2010-08-13 2012-02-16 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
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
SG193002A1 (en) 2011-03-10 2013-09-30 Daiichi Sankyo Co Ltd Dispiropyrrolidine derivative
CN108929375A (en) 2011-10-18 2018-12-04 爱勒让治疗公司 Peptidomimetic macrocyclic compound
WO2013123267A1 (en) 2012-02-15 2013-08-22 Aileron Therapeutics, Inc. Triazole-crosslinked and thioether-crosslinked peptidomimetic macrocycles
RU2642299C2 (en) 2012-02-15 2018-01-24 Эйлерон Терапьютикс, Инк. p53 PEPTIDOMIMETIC MACROCYCLES
TWI586668B (en) 2012-09-06 2017-06-11 第一三共股份有限公司 Crystals of dispiropyrrolidine derivative
US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
BR112015013611A2 (en) 2012-12-20 2017-11-14 Merck Sharp & Dohme compound and pharmaceutical composition
AU2015320545C1 (en) 2014-09-24 2020-05-14 Aileron Therapeutics, Inc. Peptidomimetic macrocycles and formulations thereof
KR20170058424A (en) 2014-09-24 2017-05-26 에일러론 테라퓨틱스 인코포레이티드 Peptidomimetic macrocycles and uses thereof
MX2017011834A (en) 2015-03-20 2018-04-11 Aileron Therapeutics Inc Peptidomimetic macrocycles and uses thereof.
EP3347372A4 (en) 2015-09-10 2019-09-04 Aileron Therapeutics, Inc. PEPTIDOMIMETIC MACROCYCLES AS MODULATORS OF MCL-1
CN109152843A (en) 2016-05-20 2019-01-04 豪夫迈·罗氏有限公司 PROTAC antibody conjugates and methods of using the same
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)

* Cited by examiner, † Cited by third party
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
MX2007010272A (en) 2005-02-22 2008-03-12 Univ Michigan Small molecule inhibitors of mdm2 and uses thereof.
AU2007207052B2 (en) 2006-01-18 2012-07-12 F. Hoffmann-La Roche Ag CIS-4, 5-biaryl-2-heterocyclic-imidazolines as MDM2 inhibitors
KR20090042779A (en) 2006-06-30 2009-04-30 쉐링 코포레이션 Substituted piperidine and its use to increase P53 activity
MY160424A (en) 2008-09-18 2017-03-15 Hoffmann La Roche Substituted pyrrolidine-2-carboxyamides.

Also Published As

Publication number Publication date
IL218018A0 (en) 2012-04-30
US20110086854A1 (en) 2011-04-14
JP2013507416A (en) 2013-03-04
BR112012008485A2 (en) 2019-09-24
MX2012003982A (en) 2012-05-08
CA2774512A1 (en) 2011-04-21
US8017607B2 (en) 2011-09-13
KR20120081210A (en) 2012-07-18
EP2488491A1 (en) 2012-08-22
AU2010305914A1 (en) 2012-03-08
WO2011045257A1 (en) 2011-04-21
CN102548963A (en) 2012-07-04

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