EA010160B1 - Новые гетероциклические соединения - ингибиторы hsp90 и способы их получения - Google Patents

Новые гетероциклические соединения - ингибиторы hsp90 и способы их получения Download PDF

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Publication number
EA010160B1
EA010160B1 EA200600594A EA200600594A EA010160B1 EA 010160 B1 EA010160 B1 EA 010160B1 EA 200600594 A EA200600594 A EA 200600594A EA 200600594 A EA200600594 A EA 200600594A EA 010160 B1 EA010160 B1 EA 010160B1
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EA
Eurasian Patent Office
Prior art keywords
sun
aryl
substituents
dimethyl
heteroaryl
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EA200600594A
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English (en)
Russian (ru)
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EA200600594A1 (ru
Inventor
Сринивас Р. Касибхатла
Маркус Ф. Боем
Кевин Д. Хонг
Марко А. Биамонт
Джиандонг Ши
Жан-Ив Лё Бразидек
Лин Жанг
Дэвид Херст
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Конформа Терапьютикс Корпорейшн
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Publication of EA200600594A1 publication Critical patent/EA200600594A1/ru
Publication of EA010160B1 publication Critical patent/EA010160B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P3/00—Drugs for disorders of the metabolism
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P37/02—Immunomodulators
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    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA200600594A 2003-09-18 2004-09-20 Новые гетероциклические соединения - ингибиторы hsp90 и способы их получения EA010160B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US50413503P 2003-09-18 2003-09-18
US59146704P 2004-07-26 2004-07-26
PCT/US2004/031248 WO2005028434A2 (en) 2003-09-18 2004-09-20 Novel heterocyclic compounds as hsp90-inhibitors

Publications (2)

Publication Number Publication Date
EA200600594A1 EA200600594A1 (ru) 2006-10-27
EA010160B1 true EA010160B1 (ru) 2008-06-30

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EA200600594A EA010160B1 (ru) 2003-09-18 2004-09-20 Новые гетероциклические соединения - ингибиторы hsp90 и способы их получения

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US (8) US7138401B2 (US07138402-20061121-C00173.png)
EP (2) EP1670802A4 (US07138402-20061121-C00173.png)
JP (1) JP2007505933A (US07138402-20061121-C00173.png)
KR (1) KR20060070572A (US07138402-20061121-C00173.png)
CN (1) CN101906106A (US07138402-20061121-C00173.png)
AU (2) AU2004274507B2 (US07138402-20061121-C00173.png)
BR (1) BRPI0414533A (US07138402-20061121-C00173.png)
CA (1) CA2539548A1 (US07138402-20061121-C00173.png)
EA (1) EA010160B1 (US07138402-20061121-C00173.png)
IL (1) IL174375A0 (US07138402-20061121-C00173.png)
MX (1) MXPA06002997A (US07138402-20061121-C00173.png)
NO (1) NO20061396L (US07138402-20061121-C00173.png)
NZ (1) NZ546611A (US07138402-20061121-C00173.png)
WO (1) WO2005028434A2 (US07138402-20061121-C00173.png)

Families Citing this family (181)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6992188B1 (en) * 1995-12-08 2006-01-31 Pfizer, Inc. Substituted heterocyclic derivatives
CN101928288B (zh) * 2000-11-02 2013-09-11 斯隆-凯特林癌症研究所 结合hsp90的小分子组合物
AU2002315389A1 (en) * 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof
US20070129334A1 (en) * 2001-10-30 2007-06-07 Conforma Therapeutics Corporation Orally Active Purine-Based Inhibitors of Heat Shock Protein 90
JP4397691B2 (ja) * 2001-10-30 2010-01-13 コンフォーマ・セラピューティクス・コーポレイション Ｈｓｐ９０阻害活性を有するプリン類似体
KR20060070572A (ko) * 2003-09-18 2006-06-23 콘포마 세러퓨틱스 코포레이션 Ｈｓｐ90-저해제로서의 신규 헤테로시클릭 화합물
AU2005302000A1 (en) * 2004-11-02 2006-05-11 Conforma Therapeutics Corporation Methods and compositions for treating chronic lymphocytic leukemia
WO2006050373A2 (en) * 2004-11-02 2006-05-11 The Regents Of The University Of California Methods and compositions for modulating apoptosis
US8212012B2 (en) * 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues having modified sugar moieties
US9120774B2 (en) 2004-11-03 2015-09-01 University Of Kansas Novobiocin analogues having modified sugar moieties
NZ561939A (en) 2005-03-30 2011-03-31 Conforma Therapeutics Corp Alkynyl pyrrolopyrimidines and related analogs as HSP90-inhibitors
PT2332909E (pt) * 2005-04-13 2014-12-17 Astex Therapeutics Ltd Derivados de hidroxibenzamida e sua utilização como inibidores de hsp90
JP2008536867A (ja) * 2005-04-14 2008-09-11 ノバルティス ヴァクシンズ アンド ダイアグノスティクス， インコーポレイテッド 増殖疾患を処置する際に有用なｈｓｐ９０インヒビターとしての２−アミノ−キナゾリン−５−オン
WO2006124897A2 (en) * 2005-05-13 2006-11-23 Lexicon Genetics Incorporated Methods and compositions for improving cognition
US7932257B2 (en) * 2005-07-22 2011-04-26 Sunesis Pharmaceuticals, Inc. Substituted pyrazolo[4,3-d]pyrimidines as aurora kinase inhibitors
CN101304748A (zh) * 2005-08-22 2008-11-12 加利福尼亚大学董事会 Tlr激动剂
EP1926734A1 (en) 2005-08-22 2008-06-04 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
JP2009506036A (ja) * 2005-08-24 2009-02-12 レキシコン・ファーマシューティカルズ・インコーポレーテッド ピロロピリジン、ピロロピリミジンおよびピラゾロピリジン化合物、それらを含む組成物、ならびにそれらの使用方法
US20070105874A1 (en) * 2005-09-23 2007-05-10 Conforma Therapeutics Corporation Anti-Tumor Methods Using Multi Drug Resistance Independent Synthetic HSP90 Inhibitors
WO2007058879A2 (en) * 2005-11-10 2007-05-24 Smithkline Beecham Corporation Inhibitors of akt activity
JP2009517342A (ja) * 2005-11-10 2009-04-30 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性の阻害剤
EP1962863A4 (en) * 2005-12-22 2010-11-24 Conforma Therapeutics Corp ORALLY ACTIVE PURINE INHIBITORS OF THERMAL SHOCK PROTEIN 90
EP2012791A4 (en) * 2006-02-07 2010-09-22 Conforma Therapeutics Corp 7,9-DIHYDRO-PURIN-8-ONE AND RELATED ANALOGUES AS INHIBITORS OF HSP90
US8658633B2 (en) * 2006-02-16 2014-02-25 Massachusetts Eye And Ear Infirmary Methods and compositions for treating conditions of the eye
EP2038041A4 (en) 2006-05-12 2010-02-17 Myriad Genetics Inc THERAPEUTIC COMPOUNDS AND THEIR USE AGAINST CANCER
EP2700638A1 (en) * 2006-05-31 2014-02-26 The Regents Of the University of California Purine analogs
US10336757B2 (en) * 2006-06-30 2019-07-02 Sloan-Kettering Institute For Cancer Research Treatment of neurodegenerative diseases through inhibition of HSP90
US20080009508A1 (en) * 2006-07-10 2008-01-10 Lucie Szucova 6,9-Disubstituted Purine Derivatives And Their Use For Treating Skin
DK1887359T3 (da) * 2006-08-03 2009-03-02 Cellzome Ag Fremgangsmåde til identifikation af PI3K-interagerende molekyler og til rensning af PI3K
KR101485199B1 (ko) 2006-09-19 2015-01-22 다이이찌 산쿄 가부시키가이샤 피라졸로피리미딘 유도체
WO2008045529A1 (en) * 2006-10-12 2008-04-17 Serenex, Inc. Purine and pyrimidine derivatives for treatment of cancer and inflammatory diseases
CL2007002994A1 (es) * 2006-10-19 2008-02-08 Wyeth Corp Compuestos derivados heterociclicos que contienen sulfamoilo, inhibidores de hsp90; composicion farmaceutica; y uso para el tratamiento del cancer, tal como cancer de mama, de colon y prostata, entre otros.
FR2907453B1 (fr) * 2006-10-24 2008-12-26 Sanofi Aventis Sa Nouveaux derives du fluorene,compositions les contenant et utilisation
GB0622084D0 (en) * 2006-11-06 2006-12-13 Chroma Therapeutics Ltd Inhibitors of HSP90
CA2676658A1 (en) * 2007-01-30 2008-08-07 Biogen Idec Ma Inc. Modulators of mitotic kinases
RU2009132605A (ru) * 2007-02-01 2011-03-10 Астразенека Аб (Se) Производные 5,6,7,8-тетрагидроптеридина в качестве ингибиторов hsp90
ES2456964T3 (es) 2007-02-07 2014-04-24 The Regents Of The University Of California Conjugados de agonistas de TLR sintéticos y usos de los mismos
KR101313804B1 (ko) * 2007-03-20 2013-10-01 쿠리스 인코퍼레이션 Ｈｓｐ９０ 억제제로서의 융합된 아미노 피리딘
MX2009010667A (es) 2007-04-12 2010-02-24 Joyant Pharmaceuticals Inc Dimeros y trimeros mimeticos de smac utiles como agentes anti-cancer.
US8143265B2 (en) * 2007-04-16 2012-03-27 Meharry Medical College Method of treating atherosclerosis
US7960353B2 (en) * 2007-05-10 2011-06-14 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
DE102007028521A1 (de) * 2007-06-21 2008-12-24 Merck Patent Gmbh Indazolamidderivate
EP2200653A2 (en) 2007-09-10 2010-06-30 University of Massachusetts Mitochondria-targeted anti-tumour agents
US8119616B2 (en) * 2007-09-10 2012-02-21 Curis, Inc. Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety
US20110160232A1 (en) 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
US7960420B2 (en) 2007-12-21 2011-06-14 Joyant Pharmaceuticals, Inc Diazonamide analogs with improved solubility
US8895701B2 (en) * 2008-01-05 2014-11-25 Sloan-Kettering Institute For Cancer Research Peptide-conjugated oligonucleotide therapeutic and method of making and using same
EA201001264A1 (ru) * 2008-02-07 2011-04-29 Дзе Регентс Оф Дзе Юниверсити Оф Калифорния Способ лечения заболеваний мочевого пузыря с помощью активатора tlr7
US8190543B2 (en) * 2008-03-08 2012-05-29 Tokyo Electron Limited Autonomous biologically based learning tool
WO2009114470A2 (en) * 2008-03-10 2009-09-17 Curis, Inc. Tetrahydroindole and tetrahdyroindazole as hsp90 inhibitors containing a zinc binding moiety
WO2009114874A2 (en) * 2008-03-14 2009-09-17 Intellikine, Inc. Benzothiazole kinase inhibitors and methods of use
US8637542B2 (en) 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
JP5123429B2 (ja) 2008-04-29 2013-01-23 ジョイアント ファーマスーティカルズ、インク． インドリン抗癌剤
LT5623B (lt) 2008-04-30 2010-01-25 Biotechnologijos Institutas, , 5-aril-4-(5-pakeistieji 2,4-dihidroksifenil)-1,2,3-tiadiazolai kaip hsp90 šaperono slopikliai ir tarpiniai junginiai jiems gauti
EP2273882A4 (en) * 2008-05-13 2011-07-13 Poniard Pharmaceuticals Inc BIOACTIVE COMPOUNDS FOR THE TREATMENT OF CANCER AND NEURODEEGENERATIVE DISEASES
US8153619B2 (en) 2008-05-22 2012-04-10 Joyant Pharmaceuticals, Inc. Diazonamide analogs
BRPI0915231A2 (pt) 2008-07-08 2018-06-12 Intellikine Inc compostos inibidores de quinase e métodos de uso
US20100022635A1 (en) * 2008-07-28 2010-01-28 University Of Kansas Heat shock protein 90 inhibitor dosing methods
GB0819102D0 (en) * 2008-10-17 2008-11-26 Chroma Therapeutics Ltd Pyrrolo-pyrimidine compounds
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
EP2373317B1 (en) * 2008-11-25 2016-12-14 Merck Sharp & Dohme Corp. 4-amino-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one or 4-amino-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one derivatives as activators of the soluble guanylat cyclase for the treatment of cardiovascular diseases
MX2011007612A (es) 2009-01-16 2012-01-20 Curis Inc Aminopiridinas fusionadas para el tratamiento de tumores del cerebro.
WO2010088924A1 (en) 2009-02-06 2010-08-12 Telormedix Sa Pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof suitable for local administration
SG173617A1 (en) * 2009-02-11 2011-09-29 Univ California Toll-like receptor modulators and treatment of diseases
MX2011008677A (es) 2009-02-25 2011-09-08 Daiichi Sankyo Co Ltd Derivados de pirazolopirimidina triciclicos.
DK2770327T3 (en) * 2009-03-30 2017-08-28 Nordic Bioscience As BIOMARKERING ASSAY FOR FIBROSE
WO2010117425A1 (en) * 2009-03-31 2010-10-14 Biogen Idec Ma Inc. Certain substituted pyrimidines, pharmaceutical compositions thereof, and methods for their use
JP5677425B2 (ja) 2009-06-29 2015-02-25 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉ３ｋ阻害剤としてのピリミジノン
WO2011004610A1 (ja) * 2009-07-10 2011-01-13 大鵬薬品工業株式会社 アザ二環式化合物又はその塩
MX2012002066A (es) 2009-08-17 2012-03-29 Intellikine Inc Compuestos heterociclicos y usos de los mismos.
US20110082098A1 (en) * 2009-09-30 2011-04-07 University Of Kansas Novobiocin analogues and treatment of polycystic kidney disease
NZ599138A (en) 2009-10-07 2014-06-27 Sloan Kettering Inst Cancer Purine derivatives useful as hsp90 inhibitors
EP2784076A1 (en) 2009-10-28 2014-10-01 Joyant Pharmaceuticals, Inc. Dimeric SMAC mimetics
US20110130711A1 (en) * 2009-11-19 2011-06-02 Follica, Inc. Hair growth treatment
WO2011075643A1 (en) * 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
US8680108B2 (en) * 2009-12-18 2014-03-25 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
AR079545A1 (es) 2009-12-21 2012-02-01 Bayer Cropscience Ag Tienilpiri(mi)dinilazol
CA2796311A1 (en) 2010-04-14 2011-10-20 Incyte Corporation Fused derivatives as pi3k.delta. inhibitors
AU2011247358B2 (en) 2010-04-30 2014-10-30 Urogen Pharma Ltd. Phospholipid drug analogs
US9050319B2 (en) 2010-04-30 2015-06-09 Telormedix, Sa Phospholipid drug analogs
WO2011146313A1 (en) * 2010-05-19 2011-11-24 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
JPWO2012026433A1 (ja) 2010-08-23 2013-10-28 第一三共株式会社 三環性ピラゾロピリミジン誘導体のフリー体結晶
TW201213333A (en) 2010-08-23 2012-04-01 Daiichi Sankyo Co Ltd Crystal forms of tricyclic pyrazolopyrimidine derivative
WO2012064744A2 (en) 2010-11-08 2012-05-18 Lycera Corporation Tetrahydroquinoline and related bicyclic compounds for inhibition of rorϒ activity and the treatment of disease
WO2012083181A1 (en) * 2010-12-16 2012-06-21 Indiana University Research And Technology Corporation Alpha helix mimetics and methods for using
NZ609448A (en) 2010-12-16 2015-07-31 Hoffmann La Roche Tricyclic pi3k inhibitor compounds and methods of use
EP2655374B1 (en) 2010-12-20 2019-10-23 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US8362023B2 (en) 2011-01-19 2013-01-29 Hoffmann-La Roche Inc. Pyrazolo pyrimidines
JP5766820B2 (ja) * 2011-02-09 2015-08-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｐｉ３キナーゼ阻害剤としての複素環化合物
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
AU2012240079B2 (en) 2011-04-05 2017-05-18 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
CN103582642B (zh) 2011-04-05 2021-05-11 索隆-基特林癌症研究协会 Hsp90抑制剂
WO2012145255A2 (en) 2011-04-22 2012-10-26 Joyant Pharmaceuticals, Inc. Diazonamide analogs
JP2014515368A (ja) 2011-05-26 2014-06-30 第一三共株式会社 プロテインキナーゼ阻害剤としての複素環化合物
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
ITTO20110652A1 (it) * 2011-07-20 2013-01-21 Medestea Res & Production S P A Composto derivato dall'adenina avente azione immuno-modulante, antinfiammatoria e antidolorifica
KR102507287B1 (ko) 2011-09-02 2023-03-07 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
CA2850617A1 (en) 2011-10-03 2013-04-11 The University Of North Carolina At Chapel Hill Pyrrolopyrimidine compounds for the treatment of cancer
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US9394315B2 (en) 2012-05-08 2016-07-19 Lycera Corporation Tetrahydro[1,8]naphthyridine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease
US9657033B2 (en) 2012-05-08 2017-05-23 Lycera Corporation Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease
WO2013172872A1 (en) * 2012-05-15 2013-11-21 Calasia Pharmaceuticals, Inc. Pyrimidine diamine derivatives as inhibitors of cytosolic hsp90
WO2013177168A1 (en) 2012-05-22 2013-11-28 The University Of North Carolina At Chapel Hill Pyrimidine compounds for the treatment of cancer
ME03300B (me) 2012-06-13 2019-07-20 Incyte Holdings Corp Supsтituisana triciklična jedinjenja као inhibiтori fgfr
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
EP2904119B1 (en) 2012-10-02 2020-06-17 The General Hospital Corporation d/b/a Massachusetts General Hospital Methods relating to dna-sensing pathway related conditions
JP2015531395A (ja) 2012-10-04 2015-11-02 ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ ピロロ［３，２−ｃ］ピリジントロポミオシン関連キナーゼ阻害剤
CN103724269B (zh) * 2012-10-11 2016-12-21 中国科学院上海药物研究所 苯基1,2-异噁唑或苯基1,2-吡唑类化合物及其用途
WO2014062774A1 (en) 2012-10-17 2014-04-24 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
EP2925752A4 (en) 2012-11-27 2016-06-01 Univ North Carolina PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
PL3808749T3 (pl) 2012-12-07 2023-07-10 Vertex Pharmaceuticals Incorporated Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
EP2970288A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
AU2014228822A1 (en) 2013-03-15 2015-10-01 Memorial Sloan-Kettering Cancer Center HSP90-targeted cardiac imaging and therapy
WO2014145576A2 (en) * 2013-03-15 2014-09-18 Northwestern University Substituted pyrrolo(2,3-d)pyrimidines for the treatment of cancer
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2014153509A1 (en) 2013-03-22 2014-09-25 Millennium Pharmaceuticals, Inc. Combination of catalytic mtorc 1/2 inhibitors and selective inhibitors of aurora a kinase
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
CN112472699A (zh) 2013-07-26 2021-03-12 种族肿瘤学公司 改善比生群及衍生物的治疗益处的组合方法
AU2014306417C1 (en) 2013-08-16 2019-07-25 Memorial Sloan-Kettering Cancer Center Selective Grp94 inhibitors and uses thereof
JP6543252B2 (ja) 2013-12-06 2019-07-10 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ ＡＴＲキナーゼ阻害剤として有用な２−アミノ−６−フルオロ−Ｎ−［５−フルオロ−ピリジン−３−イル］ピラゾロ［１，５−ａ］ピリミジン−３−カルボキサミド化合物、その調製、その異なる固体形態および放射性標識された誘導体
US9663502B2 (en) 2013-12-20 2017-05-30 Lycera Corporation 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease
US9783511B2 (en) 2013-12-20 2017-10-10 Lycera Corporation Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease
US9809561B2 (en) 2013-12-20 2017-11-07 Merck Sharp & Dohme Corp. Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease
CN106132422A (zh) 2014-02-27 2016-11-16 莱斯拉公司 使用视黄酸受体相关孤儿受体γ的激动剂的过继细胞疗法＆相关治疗方法
ES2548927B1 (es) * 2014-03-21 2016-08-11 Universidad De Granada Derivados de purina como inhibidores de Dapk-1
WO2015157125A1 (en) 2014-04-11 2015-10-15 The University Of North Carolina At Chapel Hill Therapuetic uses of selected pyrazolopyrimidine compounds with anti-mer tyrosine kinase activity
AU2015256190B2 (en) 2014-05-05 2019-08-15 Lycera Corporation Tetrahydroquinoline sulfonamide and related compounds for use as agonists of rory and the treatment of disease
EP3209641A4 (en) 2014-05-05 2018-06-06 Lycera Corporation Benzenesulfonamido and related compounds for use as agonists of ror and the treatement of disease
MX2016015874A (es) 2014-06-05 2017-03-27 Vertex Pharma Derivados radiomarcadores de un compuesto de 2-amino-6-fluoro-n-[5 -fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida util como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparacion de tal compuesto y diferentes formas solidas del mismo.
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
PT3157566T (pt) 2014-06-17 2019-07-11 Vertex Pharma Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr
CA2961499A1 (en) 2014-09-17 2016-03-24 Memorial Sloan Kettering Cancer Center Hsp90-targeted inflammation and infection imaging and therapy
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
KR101713638B1 (ko) * 2014-11-18 2017-03-08 한국과학기술연구원 신규한 피롤로 피리미딘 유도체 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물
JP2018510135A (ja) 2015-02-11 2018-04-12 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ＲＯＲγＴ阻害剤としての置換ピラゾール化合物及びその使用
EA038045B1 (ru) 2015-02-20 2021-06-28 Инсайт Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
PE20180129A1 (es) 2015-02-27 2018-01-18 Incyte Corp Sales de inhibidor de pi3k y procesos de preparacion
CA2982847A1 (en) 2015-05-05 2016-11-10 Lycera Corporation Dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of ror.gamma. and the treatment of disease
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
KR20180025894A (ko) 2015-06-11 2018-03-09 라이세라 코퍼레이션 Rory의 작용제로서 사용하기 위한 아릴 디히드로-2h-벤조[b][1,4]옥사진 술폰아미드 및 관련 화합물 및 질환의 치료
CA3217238A1 (en) * 2015-07-20 2017-01-26 Genzyme Corporation Colony stimulating factor-1 receptor (csf-1r) inhibitors
CA3000684A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
EP3368539B1 (en) 2015-10-27 2020-12-02 Merck Sharp & Dohme Corp. Substituted indazole compounds as ror gamma t inhibitors and uses thereof
WO2017075178A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
EP3368535B1 (en) 2015-10-27 2020-12-02 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
US11697851B2 (en) 2016-05-24 2023-07-11 The Regents Of The University Of California Early ovarian cancer detection diagnostic test based on mRNA isoforms
KR101896616B1 (ko) * 2016-10-11 2018-09-07 한국과학기술연구원 2-아미노 퓨린 유도체 화합물, 이를 제조하는 방법, 및 이의 용도
WO2018079988A1 (ko) * 2016-10-26 2018-05-03 울산과학기술원 Trap1 저해제로서 유용한 화합물 및 이를 포함하는 항암용 조성물
CN109311897B (zh) 2017-03-20 2021-07-20 福马治疗股份有限公司 作为丙酮酸激酶(pkr)活化剂的吡咯并吡咯组合物
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US10472361B2 (en) 2017-08-16 2019-11-12 Bristol-Myers Squibb Company Toll-like receptor 7 (TLR7) agonists having a benzotriazole moiety, conjugates thereof, and methods and uses therefor
JOP20180094A1 (ar) 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
CN107857763A (zh) * 2017-11-28 2018-03-30 江苏杏睿生物科技有限公司 一种邻硝基芳酰化衍生物类化合物、制备方法及其应用
FR3075794A1 (fr) * 2017-12-21 2019-06-28 Galderma Research & Development Nouveaux composes inhibiteurs de mtor
FR3075795A1 (fr) 2017-12-21 2019-06-28 Galderma Research & Development Nouveaux composes inhibiteurs de mtor
IL276802B2 (en) 2018-03-09 2023-09-01 Recurium Ip Holdings Llc Transduced 2,1-dihydro-3h-pyrazolo[4,3-d]pyrimidine-3-ones
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
EA202092649A1 (ru) 2018-05-04 2021-06-21 Инсайт Корпорейшн Соли ингибитора fgfr
US20200129485A1 (en) 2018-09-19 2020-04-30 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
US20230055923A1 (en) 2018-09-19 2023-02-23 Forma Therapeutics, Inc. Activating pyruvate kinase r
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclyl heterocycles as fgr suppressors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR102516260B1 (ko) * 2020-07-10 2023-03-31 울산과학기술원 Trap1 선택적 억제제로서의 화합물 및 이를 포함하는 암 예방 또는 치료용 조성물
JP2024500919A (ja) 2020-12-23 2024-01-10 ジェンザイム・コーポレーション 重水素化コロニー刺激因子－１受容体（ｃｓｆ－１ｒ）阻害剤
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CN115925724A (zh) * 2022-11-16 2023-04-07 成都中医药大学 一种具有抗炎作用的腺嘌呤类化合物及其制备方法与应用
CN116332940A (zh) * 2023-02-14 2023-06-27 广西民族大学 一种7-脱氮嘌呤衍生物及其制备方法和应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0151528A2 (en) * 1984-02-02 1985-08-14 Merck & Co. Inc. 5-(Amino or substituted amino)-1,2,3-triazoles
US4772606A (en) * 1985-08-22 1988-09-20 Warner-Lambert Company Purine derivatives
US4923885A (en) * 1988-08-19 1990-05-08 Merck & Co., Inc. 5-amino-1-(4-naphthoylbenzyl)-1,2,3-triazole-4-carboxamides and analogs as antiproliferative agents
US5002950A (en) * 1986-10-24 1991-03-26 Warner-Lambert Co. 7-deazaguanines as immunomodulators
US5110818A (en) * 1988-10-06 1992-05-05 Ciba-Geigy Corporation Anticonvulsive substituted-9-benzyl-9h-purines
US5656629A (en) * 1995-03-10 1997-08-12 Sanofi Winthrop, Inc. 6-substituted pyrazolo (3,4-d)pyrimidin-4-ones and compositions and methods of use thereof
WO2001038584A2 (en) * 1999-11-23 2001-05-31 Epoch Biosciences, Inc. Non-aggregating, non-quenching oligomers comprising nucleotide analogues; methods of synthesis and use thereof
WO2002055083A1 (en) * 2001-01-10 2002-07-18 Vernalis Research Limited TRIAZOLO[4,5-d] PYRIMIDINE DERIVATIVES AND THEIR USE AS PURINERGIC RECEPTOR ANTAGONISTS

Family Cites Families (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB884151A (en) 1957-12-06 1961-12-06 Ciba Ltd New pyrazolo-pyrimidines substituted in the pyrazole nucleus, and process for their manufacture
IL64501A (en) 1980-12-22 1985-07-31 Astra Laekemedel Ab 9-substituted 4-hydroxybutyl guanine derivatives,their preparation and antiviral use
US4699877A (en) 1982-11-04 1987-10-13 The Regents Of The University Of California Methods and compositions for detecting human tumors
US4921859A (en) 1983-10-31 1990-05-01 Warner-Lambert Company Purine derivatives
US5098906A (en) 1983-10-31 1992-03-24 Warner-Lambert Company Purine derivatives
US4806642A (en) 1984-10-05 1989-02-21 Warner-Lambert Company Purine derivatives
US4547573A (en) 1983-12-02 1985-10-15 Ici Pharma Process for preparing cephalosporin derivatives
US4748177A (en) 1984-03-26 1988-05-31 Warner-Lambert Company Guanine derivatives
US4617304A (en) 1984-04-10 1986-10-14 Merck & Co., Inc. Purine derivatives
IT1196261B (it) * 1984-09-20 1988-11-16 Pierrel Spa Derivati nucleosidici e purinici 8-sostituiti
ZA857647B (en) * 1984-10-12 1986-05-28 Warner Lambert Co Purine derivatives
IL76546A (en) 1984-10-12 1988-12-30 Warner Lambert Co 9-(heteroarylalkyl)-6-purine(thi)one derivatives,their preparation and pharmaceutical compositions containing them
JO1406B1 (en) 1984-11-02 1986-11-30 سميث كلاين اند فرينش لابوراتوريز ليمتد Chemical compounds
US5217866A (en) 1985-03-15 1993-06-08 Anti-Gene Development Group Polynucleotide assay reagent and method
DE3650699T2 (de) 1985-03-15 1999-04-15 Antivirals Inc Immunotestmittel für Polynukleotid und Verfahren
IL78643A0 (en) 1985-05-02 1986-08-31 Wellcome Found Purine derivatives,their preparation and pharmaceutical compositions containing them
GB8515934D0 (en) 1985-06-24 1985-07-24 Janssen Pharmaceutica Nv (4-piperidinomethyl and-hetero)purines
US4918162A (en) 1986-05-06 1990-04-17 The Regents Of The University Of California Assays and antibodies for N-MYC proteins
DE3623099C3 (de) * 1986-07-09 1998-08-13 Spoetzl Markus Dipl Ing Fh Blasformmaschine
US4968603A (en) * 1986-12-31 1990-11-06 The Regents Of The University Of California Determination of status in neoplastic disease
US5204353A (en) 1987-04-07 1993-04-20 Ciba-Geigy Corporation 3-benzyl-3H-1,2,3-triazolo[4,5-d]pyrimidines, compositions thereof, and method of treating epilepsy therewith
JPH0821101B2 (ja) 1987-07-21 1996-03-04 三洋電機株式会社 硬貨選別装置
SE8801729D0 (sv) 1988-05-06 1988-05-06 Astra Ab Purine derivatives for use in therapy
US5332744A (en) 1989-05-30 1994-07-26 Merck & Co., Inc. Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists
DE69116750T2 (de) 1990-07-04 1996-11-14 Merrell Dow Pharma 9-Purinyl-Phosphonsäurederivate
GB9020931D0 (en) 1990-09-26 1990-11-07 Wellcome Found Heterocyclic compounds
DE69230349T2 (de) 1991-03-05 2000-07-27 Ajinomoto Kk Cyclopropanderivat
US5939420A (en) 1991-04-08 1999-08-17 Duquesne University Of The Holy Ghost Pyrrolo 2,3d!derivatives
WO1992021032A1 (en) * 1991-05-24 1992-11-26 The Regents Of The University Of California Methods for the detection of bcr-abl and abnormal abl proteins in leukemia patients
US6025126A (en) * 1991-10-28 2000-02-15 Arch Development Corporation Methods and compositions for the detection of chromosomal aberrations
CA2093403C (en) 1992-04-08 1999-08-10 Fumio Suzuki Therapeutic agent for parkinson's disease
JPH0680670A (ja) 1992-09-03 1994-03-22 Ajinomoto Co Inc シクロプロパン誘導体及びその製造法
US6005107A (en) 1992-12-23 1999-12-21 Biochem Pharma, Inc. Antiviral compounds
GB9226879D0 (en) * 1992-12-23 1993-02-17 Iaf Biochem Int Anti-viral compounds
US6444656B1 (en) * 1992-12-23 2002-09-03 Biochem Pharma, Inc. Antiviral phosphonate nucleotides
US5744492A (en) 1993-09-17 1998-04-28 United States Of America Method for inhibiting angiogenesis
US5602156A (en) * 1993-09-17 1997-02-11 The United States Of America As Represented By The Department Of Health And Human Services Method for inhibiting metalloproteinase expression
GB9402161D0 (en) * 1994-02-04 1994-03-30 Wellcome Found Chloropyrimidine intermediates
JP3769737B2 (ja) 1994-03-30 2006-04-26 味の素株式会社 シクロプロパン誘導体及びその製造法
US5932566A (en) * 1994-06-16 1999-08-03 Pfizer Inc. Ansamycin derivatives as antioncogene and anticancer agents
US5994361A (en) 1994-06-22 1999-11-30 Biochem Pharma Substituted purinyl derivatives with immunomodulating activity
US5525606A (en) 1994-08-01 1996-06-11 The United States Of America As Represented By The Department Of Health And Human Services Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
JPH0841035A (ja) 1994-08-05 1996-02-13 Ajinomoto Co Inc シクロプロパン誘導体及びその製造法
US5846749A (en) 1994-10-12 1998-12-08 The Regents Of The University Of California Quantitative measurement of tissue protein identified by immunohistochemistry and standardized protein determination
JPH08208687A (ja) 1994-11-25 1996-08-13 Sankyo Co Ltd グリセリルオリゴヌクレオチド
US6177460B1 (en) * 1995-04-12 2001-01-23 The Procter & Gamble Company Method of treatment for cancer or viral infections
JPH0920776A (ja) 1995-06-30 1997-01-21 Nippon Paper Ind Co Ltd 新規なプリンヌクレオシド誘導体、その製造方法及びその誘導体を有効成分とする抗ウイルス剤
JPH09169758A (ja) 1995-10-18 1997-06-30 Nippon Paper Ind Co Ltd 新規なプリンヌクレオシド誘導体、その製造方法、及びそれを用いた抗ウイルス剤
JPH1025294A (ja) * 1996-03-26 1998-01-27 Akira Matsuda 縮合ヘテロ環誘導体、その製造法及びそれを含有する悪性腫瘍治療剤
AU698419B2 (en) 1996-07-03 1998-10-29 Dainippon Sumitomo Pharma Co., Ltd. A novel purine derivative
US6723727B1 (en) * 1996-12-20 2004-04-20 Hoechst Aktiengesellschaft Substituted purine derivatives, processes for their preparation, their use, and compositions comprising them
WO1998039344A1 (en) 1997-03-07 1998-09-11 Metabasis Therapeutics, Inc. Novel purine inhibitors of fructose-1,6-bisphosphatase
US5861503A (en) * 1997-04-30 1999-01-19 The Regents Of The University Of California Process for producing 8-fluoropurines
JP4903922B2 (ja) 1997-05-14 2012-03-28 スローン − ケッタリング インスティチュート フォー キャンサー リサーチ 選択された蛋白質を分解する複合化合物
CN1268137A (zh) 1997-07-03 2000-09-27 杜邦药品公司 治疗神经失调的咪唑并嘧啶和咪唑并吡啶
EP1017394B1 (en) 1997-07-12 2005-12-07 Cancer Research Technology Limited Cyclin dependent kinase inhibiting purine derivatives
GB9717849D0 (en) 1997-08-23 1997-10-29 Seal Sands Chemicals Limited Preparation of pyridene derivatives
AUPO912997A0 (en) 1997-09-11 1997-10-02 Commonwealth Scientific And Industrial Research Organisation Antiviral agents
US5968921A (en) * 1997-10-24 1999-10-19 Orgegon Health Sciences University Compositions and methods for promoting nerve regeneration
DE69824632T2 (de) 1997-11-12 2005-06-09 Mitsubishi Chemical Corp. Purinderivate und medikamente, welche dieselben als aktiven bestandteil enthalten
TW572758B (en) 1997-12-22 2004-01-21 Sumitomo Pharma Type 2 helper T cell-selective immune response inhibitors comprising purine derivatives
WO1999051223A1 (en) 1998-04-03 1999-10-14 University Of Pittsburgh Of The Commonwealth System Of Higher Education Benzoquinoid ansamycins for the treatment of cardiac arrest and stroke
US5985060A (en) 1998-07-25 1999-11-16 Breed Automotive Technology, Inc. Gas generant compositions containing guanidines
SI20022A (sl) 1998-07-29 2000-02-29 Kemijski inštitut Alkilno substituirani purinovi derivati in njihova priprava
JP2000072773A (ja) 1998-08-28 2000-03-07 Zeria Pharmaceut Co Ltd プリン誘導体
US6369092B1 (en) * 1998-11-23 2002-04-09 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted benzimidazole derivatives
JP2002539076A (ja) * 1999-01-06 2002-11-19 ユニバーシティ・オブ・サザン・カリフォルニア 新脈管形成抑制のための方法および組成物
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
DK1150982T3 (da) 1999-02-01 2005-12-27 Cv Therapeutics Inc Purininhibitorer af cylkineafhængig kinase 2 og 1kB-alfa
FR2790702B1 (fr) 1999-03-08 2001-07-20 Sidel Sa Unite de moulage et machine d'extrusion-soufflage munie d'une telle unite
US6174875B1 (en) * 1999-04-01 2001-01-16 University Of Pittsburgh Benzoquinoid ansamycins for the treatment of cardiac arrest and stroke
WO2000068230A1 (en) 1999-05-05 2000-11-16 Darwin Discovery Limited 9-(1,2,3,4-tetrahydronaphthalen-1-yl)-1,9-dihydropurin-6-one derivatives as pde7 inhibitors
AU2728201A (en) 1999-12-21 2001-07-03 Sugen, Inc. 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors
US20030187261A1 (en) 2000-01-07 2003-10-02 Libor Havlicek Purine derivatives, process for their preparation and use thereof
AU2001247759A1 (en) 2000-03-24 2001-10-08 Duke University Characterization of grp94-ligand interactions and purification, screening, and therapeutic methods relating thereto
WO2001081346A2 (en) 2000-04-25 2001-11-01 Icos Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
US6887853B2 (en) 2000-06-29 2005-05-03 The Trustees Of Boston University Use of geldanamycin and related compounds for treatment of fibrogenic disorders
US6946456B2 (en) 2000-07-28 2005-09-20 Sloan-Kettering Institute For Cancer Research Methods for treating cell proliferative disorders and viral infections
US6613089B1 (en) 2000-10-25 2003-09-02 Sdgi Holdings, Inc. Laterally expanding intervertebral fusion device
WO2002036171A1 (en) 2000-11-02 2002-05-10 Sloan Kettering Institute For Cancer Research Methods for enhancing the efficacy of cytotoxic agents through the use of hsp90 inhibitors
CN101928288B (zh) * 2000-11-02 2013-09-11 斯隆-凯特林癌症研究所 结合hsp90的小分子组合物
GB0100623D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds IV
GB0100621D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds VI
MY141789A (en) * 2001-01-19 2010-06-30 Lg Chem Investment Ltd Novel acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same.
EP1423080A4 (en) 2001-03-01 2009-06-03 Conforma Therapeutics Corp PROCESS FOR TREATING PROLIFERATIVE GENETIC DISORDERS WITH HSP90 INHIBITORS
CA2377054C (en) * 2001-03-16 2006-09-05 Susan M. Boyetchko Biocontrol of weeds using pseudomonas compositions
JP4331944B2 (ja) 2001-04-17 2009-09-16 大日本住友製薬株式会社 新規アデニン誘導体
US20020156277A1 (en) * 2001-04-20 2002-10-24 Fick David B. Synthesis and methods of use of purine analogues and derivatives
US20030022864A1 (en) 2001-04-24 2003-01-30 Ishaq Khalid S. 9-[(5-dihydroxyboryl)-pentyl] purines, useful as an inhibitor of inflammatory cytokines
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
WO2002094196A2 (en) 2001-05-23 2002-11-28 Sloan Kettering Institute For Cancer Research Method of treatment for cancers associated with elevated
PE20030008A1 (es) 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
US6949522B2 (en) 2001-06-22 2005-09-27 Pharmasset, Inc. β-2′- or 3′-halonucleosides
DE60205376T2 (de) 2001-06-27 2006-04-06 Cyclacel Ltd. 2,6,9-substituierte purinderivate und ihre verwendung bei der behandlung proliferativer krankheiten
US6962991B2 (en) 2001-09-12 2005-11-08 Epoch Biosciences, Inc. Process for the synthesis of pyrazolopyrimidines
DE60225307T2 (de) 2001-09-24 2009-03-19 Conforma Therapeutics Corp., San Diego Verfahren zur herstellung von 17-allyl-amino-geldanamycin (17-aag) und anderer ansamycine
DE60230818D1 (de) 2001-09-24 2009-02-26 Imp Innovations Ltd Pyy3-36 zur zur reduzierung oder vorbeugung von fettleibigkeit
JP2003113181A (ja) 2001-10-04 2003-04-18 Sumika Fine Chemicals Co Ltd ６−ハロプリンの製造方法
JP4397691B2 (ja) 2001-10-30 2010-01-13 コンフォーマ・セラピューティクス・コーポレイション Ｈｓｐ９０阻害活性を有するプリン類似体
EP1450784A4 (en) 2001-11-09 2005-02-09 Conforma Therapeutics Corp HSP90-INHIBITABLE ZEARALANOL COMPOUNDS AND METHOD FOR THEIR PREPARATION AND USE
GB0219746D0 (en) * 2002-08-23 2002-10-02 Inst Of Ex Botany Ascr Azapurine derivatives
AU2003267145A1 (en) * 2002-09-13 2004-04-30 Irm, Llc Highly specific modulators of gtpases for target validation
US7601694B2 (en) * 2003-02-20 2009-10-13 New York University CLK-peptide and SLK-peptide
US7560458B2 (en) * 2003-07-16 2009-07-14 Janssen Pharmaceutica, N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
CA2531232A1 (en) * 2003-07-16 2005-02-10 Janssen Pharmaceutica N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
KR20060070572A (ko) 2003-09-18 2006-06-23 콘포마 세러퓨틱스 코포레이션 Ｈｓｐ90-저해제로서의 신규 헤테로시클릭 화합물
US20080081817A1 (en) * 2004-07-23 2008-04-03 Tanabe Seiyaku Co., Ltd. Nitrogenous Fused Bicyclic Compound
US20070105874A1 (en) * 2005-09-23 2007-05-10 Conforma Therapeutics Corporation Anti-Tumor Methods Using Multi Drug Resistance Independent Synthetic HSP90 Inhibitors
WO2016146042A1 (en) 2015-03-13 2016-09-22 Acro Biotech Co., Ltd. Zinc binding fusion protein of glutathione s-transferase and metallothionein

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0151528A2 (en) * 1984-02-02 1985-08-14 Merck & Co. Inc. 5-(Amino or substituted amino)-1,2,3-triazoles
US4772606A (en) * 1985-08-22 1988-09-20 Warner-Lambert Company Purine derivatives
US5002950A (en) * 1986-10-24 1991-03-26 Warner-Lambert Co. 7-deazaguanines as immunomodulators
US4923885A (en) * 1988-08-19 1990-05-08 Merck & Co., Inc. 5-amino-1-(4-naphthoylbenzyl)-1,2,3-triazole-4-carboxamides and analogs as antiproliferative agents
US5110818A (en) * 1988-10-06 1992-05-05 Ciba-Geigy Corporation Anticonvulsive substituted-9-benzyl-9h-purines
US5656629A (en) * 1995-03-10 1997-08-12 Sanofi Winthrop, Inc. 6-substituted pyrazolo (3,4-d)pyrimidin-4-ones and compositions and methods of use thereof
WO2001038584A2 (en) * 1999-11-23 2001-05-31 Epoch Biosciences, Inc. Non-aggregating, non-quenching oligomers comprising nucleotide analogues; methods of synthesis and use thereof
WO2002055083A1 (en) * 2001-01-10 2002-07-18 Vernalis Research Limited TRIAZOLO[4,5-d] PYRIMIDINE DERIVATIVES AND THEIR USE AS PURINERGIC RECEPTOR ANTAGONISTS

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
ASHWELL. "An improved route to Guanines Substituted al N-9". J. Chem. Soc. Chem. Commun., 1990, pp. 955-956. See compound 2f *
BENNETT et al. "Synthesis and antiviral activity of some acyclic and C-acyclic pyrrolo[2,3-d]pyrimidine nucleoside analogs". J. Med. Chem. 1990, Vol. 33, No. 8, pp. 2162-2173. See compounds 37, 38, 41, 42, 49, 57, 50 and 58 *
CHENG et al. "Rearrangement of 4-Amino-6-chloro-l-methylpyrazolo (3,4-d)pyrimidine in Basic Solution". J. Org. Chem. 1959, Vol. 24, pp. 1570-1571. See compound II *
GANGJEE et al. "Design, Synthesis, and X-ray Crystal Structure of a Potent Dual Inhibitor of Thymidylate Synthase and Dihydrofolate Reductase as an Antitumor Agent". J. Amer. Chem. Soc. 2000, Vol. 43, No. 21, pp. 3837-3851. See compound 9 *
GUILLARME et al. "Rapid access to acyclic nucleosides via conjugate addition". Tetrahedron. Vol. 59, Issue 12, 17 March 2003, pp. 2177-2184. See 13 and 4e *
KOZAI. "Synthesis and Biological Activity of 9-(2,6-Difluorobenzyl)-9H-purines Bearing Chlorine". Chem. Pharm. Bull. 1999. Vol. 47, No. 4,p. 574. See 2a *
MALLORY et al. "Pyrimido[4,5-c]pyridazines. 3. Preferential formation of 8-amino-1H-pyrimido[4,5-c]-1.2-diazepin-6(7H)-ones by cyclizations with .alpha.,.gamma.-dioxo esters". J. Organic Chem. 1982, Vol. 47, pp. 667-674 *
QUINTELA et al. "Pyrazolopyrimidines: synthesis, effect on histamine release from rat peritoneal mast cells and cytotoxic activity". European. J. Med. Chem. 2001, Vol. 36, pp. 321-332. See 3a, 3b, 4e and 4a *

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