TWI507405B - 增加p53活性之經取代六氫吡啶及其用途 - Google Patents

增加p53活性之經取代六氫吡啶及其用途 Download PDF

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Publication number
TWI507405B
TWI507405B TW099134959A TW99134959A TWI507405B TW I507405 B TWI507405 B TW I507405B TW 099134959 A TW099134959 A TW 099134959A TW 99134959 A TW99134959 A TW 99134959A TW I507405 B TWI507405 B TW I507405B
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Taiwan
Prior art keywords
alkyl
group
compound
cancer
cycloalkyl
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TW099134959A
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English (en)
Chinese (zh)
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TW201124405A (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 & Dohme
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Publication of TWI507405B publication Critical patent/TWI507405B/zh

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    • 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • 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
    • C07D409/14Heterocyclic 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
TW099134959A 2009-10-14 2010-10-13 增加p53活性之經取代六氫吡啶及其用途 TWI507405B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25160309P 2009-10-14 2009-10-14
US25246809P 2009-10-16 2009-10-16

Publications (2)

Publication Number Publication Date
TW201124405A TW201124405A (en) 2011-07-16
TWI507405B true TWI507405B (zh) 2015-11-11

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Country Status (28)

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

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US8883785B2 (en) 2010-01-25 2014-11-11 Chdi Foundation, Inc. Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
KR101580714B1 (ko) 2010-06-03 2016-01-04 파마싸이클릭스 엘엘씨 브루톤 티로신 인산화효소(btk)의 억제제의 용도
US9428464B2 (en) 2011-08-30 2016-08-30 Chdi Foundation, Inc. Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
MY166890A (en) 2011-08-30 2018-07-24 Chdi Foundation Inc Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
WO2013062923A1 (en) * 2011-10-28 2013-05-02 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
EP2872161B1 (en) * 2012-06-26 2020-12-16 Del Mar Pharmaceuticals Dianhydrogalactitol for use in treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations
BR112015001690A2 (pt) 2012-07-24 2017-11-07 Pharmacyclics Inc mutações associadas com a resistência a inibidores da tirosina quinase de bruton (btk)
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
US9169214B2 (en) 2012-12-21 2015-10-27 The Board Of Trustees Of The Leland Stanford Junior University Compounds and compositions that bind and stabilize transthyretin and their use for inhibiting transthyretin amyloidosis and protein-protein interactions
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JP2017520610A (ja) 2014-07-17 2017-07-27 シーエイチディーアイ ファウンデーション,インコーポレーテッド Hiv関連障害を治療するための方法及び組成物
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US10085999B1 (en) 2017-05-10 2018-10-02 Arixa Pharmaceuticals, Inc. Beta-lactamase inhibitors and uses thereof
WO2018227129A1 (en) * 2017-06-09 2018-12-13 Regents Of The University Of Minnesota Skin care formulations and skin cancer treatment
CN111448182A (zh) 2017-10-02 2020-07-24 阿里萨制药有限公司 氨曲南衍生物及其用途
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EP3781156A4 (en) * 2018-04-16 2022-05-18 C4 Therapeutics, Inc. SPIROCYCLIC COMPOUNDS
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