CA2777043C - Substituted piperidines that increase p53 activity and the uses thereof - Google Patents

Substituted piperidines that increase p53 activity and the uses thereof Download PDF

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Publication number
CA2777043C
CA2777043C CA2777043A CA2777043A CA2777043C CA 2777043 C CA2777043 C CA 2777043C CA 2777043 A CA2777043 A CA 2777043A CA 2777043 A CA2777043 A CA 2777043A CA 2777043 C CA2777043 C CA 2777043C
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CA
Canada
Prior art keywords
cr8r8
alkyl
compound
cycloalkyl
group
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.)
Expired - Fee Related
Application number
CA2777043A
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English (en)
French (fr)
Other versions
CA2777043A1 (en
Inventor
Stephane L. Bogen
Yao Ma
Yaolin Wang
Brian Robert Lahue
Latha G. Nair
Manami Shizuka
Matthew Ernst Voss
Margarita Kirova-Snover
Weidong Pan
Yuan Tian
Bheemashankar A. Kulkarni
Craig R. Gibeau
Yuan Liu
Giovanna Scapin
Diane Rindgen
Ronald J. Doll
Timothy J. Guzi
Danny J. Hicklin
Amin Nomeir
Cynthia Seidel-Dugan
Gerald W. Shipps, Jr.
Malcolm Maccoss
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Publication of CA2777043A1 publication Critical patent/CA2777043A1/en
Application granted granted Critical
Publication of CA2777043C publication Critical patent/CA2777043C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
CA2777043A 2009-10-14 2010-10-05 Substituted piperidines that increase p53 activity and the uses thereof Expired - Fee Related CA2777043C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US25160309P 2009-10-14 2009-10-14
US61/251,603 2009-10-14
US25246809P 2009-10-16 2009-10-16
US61/252,468 2009-10-16
PCT/US2010/051403 WO2011046771A1 (en) 2009-10-14 2010-10-05 SUBSTITUTED PIPERIDINES THAT INCREASE p53 ACTIVITY AND THE USES THEREOF

Publications (2)

Publication Number Publication Date
CA2777043A1 CA2777043A1 (en) 2011-04-21
CA2777043C true CA2777043C (en) 2015-12-15

Family

ID=43876442

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2777043A Expired - Fee Related CA2777043C (en) 2009-10-14 2010-10-05 Substituted piperidines that increase p53 activity and the uses thereof

Country Status (28)

Country Link
US (2) US8859776B2 (enExample)
EP (1) EP2488028B1 (enExample)
JP (2) JP5099731B1 (enExample)
KR (1) KR101485645B1 (enExample)
CN (2) CN104945382B (enExample)
AR (1) AR078622A1 (enExample)
AU (1) AU2010307198C9 (enExample)
BR (1) BR112012008849A2 (enExample)
CA (1) CA2777043C (enExample)
CL (1) CL2012000949A1 (enExample)
CO (1) CO6531452A2 (enExample)
CR (1) CR20120183A (enExample)
EA (1) EA023838B1 (enExample)
GT (1) GT201200111A (enExample)
IL (1) IL219125A0 (enExample)
IN (1) IN2012DN03085A (enExample)
MA (1) MA33745B1 (enExample)
MX (1) MX2012004377A (enExample)
MY (1) MY174452A (enExample)
NI (1) NI201200059A (enExample)
NZ (1) NZ599343A (enExample)
PE (1) PE20121172A1 (enExample)
PH (1) PH12012500713A1 (enExample)
TN (1) TN2012000129A1 (enExample)
TW (1) TWI507405B (enExample)
UA (1) UA109417C2 (enExample)
WO (1) WO2011046771A1 (enExample)
ZA (2) ZA201202667B (enExample)

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NZ717373A (en) 2010-06-03 2017-11-24 Pharmacyclics Llc The use of inhibitors of bruton’s tyrosine kinase (btk)
SG2014011654A (en) 2011-08-30 2014-08-28 Chdi Foundation Inc Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
EA027451B1 (ru) 2011-08-30 2017-07-31 Схди Фаундейшн, Инк. Ингибиторы кинуренин-3-монооксигеназы, фармацевтические композиции и их применение
EP2771008A4 (en) * 2011-10-28 2015-04-08 Merck Sharp & Dohme MACROCYCLES FOR INCREASING P53 ACTIVITY AND USES THEREOF
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SG11201408679XA (en) * 2012-06-26 2015-01-29 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
US10954567B2 (en) 2012-07-24 2021-03-23 Pharmacyclics Llc Mutations associated with resistance to inhibitors of Bruton's Tyrosine Kinase (BTK)
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