KR101099206B1 - 신규한 글루타미닐 시클라제 저해제 - Google Patents

신규한 글루타미닐 시클라제 저해제 Download PDF

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KR101099206B1
KR101099206B1 KR1020067017874A KR20067017874A KR101099206B1 KR 101099206 B1 KR101099206 B1 KR 101099206B1 KR 1020067017874 A KR1020067017874 A KR 1020067017874A KR 20067017874 A KR20067017874 A KR 20067017874A KR 101099206 B1 KR101099206 B1 KR 101099206B1
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phenyl
methyl
group
compound
inhibitors
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Korean (ko)
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KR20060125884A (ko
Inventor
슈테판 쉴링
미르코 부흐홀츠
앙드레 요하네스 니스트로이
한스-울리히 데무트
울리히 하이저
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프로비오드룩 아게
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Priority claimed from US10/838,993 external-priority patent/US7371871B2/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/61—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P5/00—Drugs for disorders of the endocrine 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020067017874A 2004-02-05 2005-02-04 신규한 글루타미닐 시클라제 저해제 Expired - Fee Related KR101099206B1 (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US54213304P 2004-02-05 2004-02-05
US60/542,133 2004-02-05
US10/838,993 US7371871B2 (en) 2003-05-05 2004-05-05 Inhibitors of glutaminyl cyclase
US10/838,993 2004-05-05
US63436404P 2004-12-08 2004-12-08
US60/634,364 2004-12-08
PCT/EP2005/001153 WO2005075436A2 (en) 2004-02-05 2005-02-04 Novel inhibitors of glutaminyl cyclase

Publications (2)

Publication Number Publication Date
KR20060125884A KR20060125884A (ko) 2006-12-06
KR101099206B1 true KR101099206B1 (ko) 2011-12-27

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ID=40253652

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KR1020067017874A Expired - Fee Related KR101099206B1 (ko) 2004-02-05 2005-02-04 신규한 글루타미닐 시클라제 저해제

Country Status (9)

Country Link
US (2) US7304086B2 (https=)
EP (1) EP1713780B1 (https=)
JP (1) JP4996926B2 (https=)
KR (1) KR101099206B1 (https=)
CN (1) CN1918131B (https=)
AU (1) AU2005210004B2 (https=)
BR (1) BRPI0507485A (https=)
CA (1) CA2554809C (https=)
WO (1) WO2005075436A2 (https=)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
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JP4279784B2 (ja) * 2002-12-04 2009-06-17 エーザイ・アール・アンド・ディー・マネジメント株式会社 １，３−ジヒドロ−イミダゾール縮合環化合物
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7732162B2 (en) * 2003-05-05 2010-06-08 Probiodrug Ag Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases
US8338120B2 (en) 2003-05-05 2012-12-25 Probiodrug Ag Method of treating inflammation with glutaminyl cyclase inhibitors
KR20110059664A (ko) * 2003-05-05 2011-06-02 프로비오드룩 아게 글루타미닐 및 글루타메이트 사이클라제의 이펙터의 용도
JP4806628B2 (ja) * 2003-05-05 2011-11-02 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤
KR20060041309A (ko) 2003-08-13 2006-05-11 다케다 야쿠힌 고교 가부시키가이샤 ４-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도
US7790734B2 (en) 2003-09-08 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7667044B2 (en) 2003-11-03 2010-02-23 Probiodrug Ag Compounds for the treatment of neurological disorders
EP1824846A2 (en) * 2003-11-03 2007-08-29 Probiodrug AG Novel compounds for the treatment of neurological disorders
US20100099721A1 (en) * 2003-11-03 2010-04-22 Probiodrug Ag Novel compounds for the treatment of neurological disorders
US20050171112A1 (en) * 2003-11-03 2005-08-04 Probiodrug Ag Combinations useful for the treatment of neuronal disorders
US7304086B2 (en) 2004-02-05 2007-12-04 Probiodrug Ag Inhibitors of glutaminyl cyclase
CN102127057A (zh) * 2004-03-15 2011-07-20 武田药品工业株式会社 二肽基肽酶抑制剂
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KR100650278B1 (ko) * 2004-12-27 2006-11-27 김성진 엔-아릴 엔' 모르폴리노/ 피페리디노 티오카르바마이드유도체를 유효성분으로 함유하는 당뇨병, 당뇨병 합병증,인슐린저항성 및 그로 인한 인슐린 저항성 증후군의 예방및 치료용 약학적 조성물
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CN101360723A (zh) 2005-09-16 2009-02-04 武田药品工业株式会社 制备嘧啶二酮衍生物的方法
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US8889709B2 (en) 2006-09-21 2014-11-18 Probiodrug Ag Use of isoQC inhibitors in the treatment and prevention of inflammatory diseases or conditions
BRPI0718507A2 (pt) * 2006-09-21 2013-11-12 Probiodrug Ag Genes relacionados à glutaminil ciclase
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US9277737B2 (en) 2006-09-21 2016-03-08 Probiodrug Ag Mouse models carrying a knock-out mutation of the QPCTL-gene
US8420684B2 (en) * 2006-11-09 2013-04-16 Probiodrug Ag Inhibitors of glutaminyl cyclase
JP5599614B2 (ja) * 2006-11-09 2014-10-01 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
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US9126987B2 (en) * 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
KR100867978B1 (ko) * 2006-12-12 2008-11-10 이화여자대학교 산학협력단 이중 작용기를 가지는 새로운 이온성 액체 및 그의제조방법
JP2010516235A (ja) * 2007-01-19 2010-05-20 プロビオドルグ エージー アルツハイマー病及び他のｑｐｃｔ関連障害の治療のためのインビボスクリーニングモデル
GB2447017A (en) * 2007-03-01 2008-09-03 Probiodrug Ag New use for inhibitors of glutaminyl peptide cyclotransferinase
BRPI0808170A2 (pt) * 2007-03-01 2014-07-08 Probiodrug Ag Uso de inibidores de glutaminil ciclase
AU2008220785B2 (en) * 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
US7803810B2 (en) * 2007-03-09 2010-09-28 Probiodrug Ag Inhibitors
WO2008114800A2 (en) * 2007-03-13 2008-09-25 Takeda Pharmaceutical Company Limited Solid preparation comprising 2- [ [6- [ (3r) -3-amino-1-piperidinyl] -3, 4-dihydro-3-methyl-2, 4-dioxo-1 (2h) -pyrimidinyl] methyl] -4-fluorobenzonitrile
US8093236B2 (en) * 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
JP5675343B2 (ja) * 2007-04-18 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としての尿素誘導体
DK2142515T3 (da) * 2007-04-18 2014-06-23 Probiodrug Ag Nitrovinyl-diaminderivater som glutaminyl-cyclase-inhibitorer
WO2008128982A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Thioxoquinazolinone derivatives as glutaminyl cyclase inhibitors
WO2008128983A1 (en) * 2007-04-18 2008-10-30 Probiodrug Ag Cyano-guanidine derivatives as glutaminyl cyclase inhibitors
JP5667440B2 (ja) * 2007-04-18 2015-02-12 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体
JP5675340B2 (ja) * 2007-04-18 2015-02-25 プロビオドルグ エージー 新規阻害剤
JP5676249B2 (ja) * 2007-04-20 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体
US8524654B2 (en) * 2007-05-21 2013-09-03 The Uab Research Foundation Prolyl endopeptidase inhibitors for reducing or preventing neutrophilic inflammation
CA2696934A1 (en) * 2007-09-12 2010-02-16 Probiodrug Ag Transgenic mice
NZ586665A (en) * 2008-01-14 2011-12-22 Probiodrug Ag MOUSE MODELS CARRYING A KNOCK-OUT MUTATION OF THE GLUTAMINYL CYCLASE GENE (Qpct)
EP2320942B1 (en) 2008-07-21 2018-03-14 Probiodrug AG Diagnostic antibody assay
CN103983787A (zh) * 2008-07-31 2014-08-13 前体生物药物股份公司 作为神经退行性疾病诊断/预后指示物的谷氨酰胺酰环化酶
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JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
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EP2537029A1 (en) 2010-02-18 2012-12-26 Probiodrug AG Methods of diagnosing inflammatory diseases by determining pyroglutamate-modified mcp-1 and screening methods for inhibitors of glutaminyl cyclase
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
JP5688745B2 (ja) 2010-03-10 2015-03-25 プロビオドルグ エージー グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
US8409837B2 (en) 2010-08-19 2013-04-02 Probiodrug Ag Crystal structure of glutaminyl cyclase
CN106243023A (zh) * 2010-09-03 2016-12-21 福马Tm有限责任公司 用于抑制nampt的胍化合物和组合物
US9868728B2 (en) 2010-10-29 2018-01-16 Emory University Quinazoline derivatives, compositions, and uses related thereto
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