CN111032039B - 用于预防和治疗医学障碍的化合物及其用途 - Google Patents

用于预防和治疗医学障碍的化合物及其用途 Download PDF

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CN111032039B
CN111032039B CN201880050555.3A CN201880050555A CN111032039B CN 111032039 B CN111032039 B CN 111032039B CN 201880050555 A CN201880050555 A CN 201880050555A CN 111032039 B CN111032039 B CN 111032039B
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compound
gal
compounds
galectin
binding
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CN111032039A (zh
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R·尼尔
E·佐默
P·G·特拉伯
J·M·约翰逊
R·乔治
S·谢克特尔
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Galectin Sciences LLC
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Galectin Sciences LLC
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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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • 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
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
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    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN201880050555.3A 2017-08-03 2018-08-03 用于预防和治疗医学障碍的化合物及其用途 Active CN111032039B (zh)

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Application Number Priority Date Filing Date Title
US201762540860P 2017-08-03 2017-08-03
US62/540,860 2017-08-03
PCT/US2018/045175 WO2019028357A1 (en) 2017-08-03 2018-08-03 COMPOUNDS FOR THE PREVENTION AND TREATMENT OF MEDICAL DISORDERS AND USES THEREOF

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CN111032039B true CN111032039B (zh) 2024-03-26

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US (2) US11583530B2 (enExample)
EP (1) EP3661502A4 (enExample)
JP (1) JP7498108B2 (enExample)
KR (1) KR102692840B1 (enExample)
CN (1) CN111032039B (enExample)
AU (1) AU2018309085B2 (enExample)
BR (1) BR112020001698A2 (enExample)
CA (1) CA3069745A1 (enExample)
IL (1) IL272097B2 (enExample)
MX (1) MX2020001256A (enExample)
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Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI744300B (zh) * 2016-03-23 2021-11-01 里爾中央醫學中心 改良性熱處理的血小板顆粒裂解液在製備用於治療神經系統疾病的組合物的用途
WO2019023247A1 (en) 2017-07-25 2019-01-31 Immutics, Inc. TREATMENT OF CANCER BY BLOCKING THE INTERACTION OF TIM-3 AND ITS LIGAND
BR112020001698A2 (pt) 2017-08-03 2020-07-21 Galectin Sciences, Llc compostos para prevenção e tratamento de distúrbios médicos e usos dos mesmos
EP3918323A4 (en) 2019-01-30 2022-12-28 TrueBinding, Inc. ANTI-GAL3 ANTIBODIES AND USES THEREOF
WO2021242776A2 (en) 2020-05-26 2021-12-02 Truebinding, Inc. Methods of treating inflammatory diseases by blocking galectin-3
CN113476442A (zh) * 2021-07-28 2021-10-08 上海交通大学医学院附属第九人民医院 化合物gb-0139在治疗心肌梗死后心肌过度纤维化的药物中的应用
GB2631509A (en) * 2023-07-04 2025-01-08 Univ Liverpool Compositions
GB2631507A (en) * 2023-07-04 2025-01-08 Univ Liverpool Compositions

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4428952A (en) * 1981-06-30 1984-01-31 Farmitalia Carlo Erba S.P.A. Substituted pyrrolo[2,1-b]quinazolines and pyrido[2,1-b]quinazolines useful for the treatment of or the prevention of gastrointestinal ulcers
WO2012158913A2 (en) * 2011-05-17 2012-11-22 Discoverybiomed Inc. Treating protein folding disorders with small molecule cftr correctors
CN106220631A (zh) * 2016-07-26 2016-12-14 中山大学 一种7位氟取代Isaindigotone衍生物及其制备方法和在制备抗癌药物中的应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL69274A (en) 1982-08-05 1986-08-31 Erba Farmitalia (substituted amino)derivatives of 3-benzylidene-pyrrolo(2,1-b)quinazolin-9-ones and 6-benzylidene-pyrido(2,1-b)quinazolin-11-ones,their preparation and pharmaceutical compositions containing them
SE0100172D0 (sv) * 2001-01-22 2001-01-22 Ulf Nilsson New inhibitors against galectins
WO2002060392A2 (en) 2001-01-31 2002-08-08 Synaptic Pharmaceutical Corporation Use of gal3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
IL157102A0 (en) 2001-01-31 2004-02-08 Synaptic Pharma Corp Use of gal3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
CN1556705B (zh) 2002-07-09 2010-04-28 埃科特莱茵药品有限公司 7,8,9,10-四氢-6H-氮杂卓并、6,7,8,9-四氢-吡啶并和2,3-二氢-2H-吡咯并[2,1-b]-喹唑啉酮衍生物
US7220775B2 (en) 2002-08-07 2007-05-22 H. Lundbeck A/S Compound useful for the treatment of neuropathic pain
DE10304141B4 (de) 2003-02-03 2006-03-09 Hf Arzneimittelforschung Gmbh Verfahren zur Herstellung von Chinazolin-Alkaloiden
CA2841897A1 (en) 2011-07-13 2013-01-17 Santen Pharmaceutical Co., Ltd. Novel compound having parp inhibitory activity
WO2016004093A2 (en) 2014-07-01 2016-01-07 Stealth Biotherapeutics Corp Therapeutic compositions including galectin-3 inhibitors and uses thereof
ES2858729T3 (es) 2015-01-30 2021-09-30 Galecto Biotech Ab Inhibidores de alfa-d-galactósido de galectinas
CN105272986A (zh) 2015-06-15 2016-01-27 厦门医学高等专科学校 一种可抑制乙酰胆碱酯酶活性的化合物或其制备方法和应用
BR112020001698A2 (pt) 2017-08-03 2020-07-21 Galectin Sciences, Llc compostos para prevenção e tratamento de distúrbios médicos e usos dos mesmos

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4428952A (en) * 1981-06-30 1984-01-31 Farmitalia Carlo Erba S.P.A. Substituted pyrrolo[2,1-b]quinazolines and pyrido[2,1-b]quinazolines useful for the treatment of or the prevention of gastrointestinal ulcers
WO2012158913A2 (en) * 2011-05-17 2012-11-22 Discoverybiomed Inc. Treating protein folding disorders with small molecule cftr correctors
CN106220631A (zh) * 2016-07-26 2016-12-14 中山大学 一种7位氟取代Isaindigotone衍生物及其制备方法和在制备抗癌药物中的应用

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
On the Synthesis and Reactivity of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-ones;Charlotte L. Sutherell et al.,;《synthesis》;20161219;第49卷(第01期);表3 *
Structure Activity Relationship of Arylidene Pyrrolo and Pyrido [2,1-b] Quinazolones as Cytotoxic Agents: Synthesis, SAR Studies, Biological Evaluation and Docking Studies;Veenu Mangla et al.,;《Medicinal chemistry》;20130601;第9卷(第5期);第642页，第645页，图4 *

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IL272097B1 (en) 2024-02-01
WO2019028357A1 (en) 2019-02-07
KR20200035982A (ko) 2020-04-06
IL272097B2 (en) 2024-06-01
JP2020529988A (ja) 2020-10-15
US11583530B2 (en) 2023-02-21
ZA202000375B (en) 2025-04-30
US20230116370A1 (en) 2023-04-13
EP3661502A1 (en) 2020-06-10
EP3661502A4 (en) 2020-12-02
US20200147088A1 (en) 2020-05-14
BR112020001698A2 (pt) 2020-07-21
JP7498108B2 (ja) 2024-06-11
MX2020001256A (es) 2020-08-17
IL272097A (en) 2020-03-31
CA3069745A1 (en) 2019-02-07
US12377102B2 (en) 2025-08-05
KR102692840B1 (ko) 2024-08-07
AU2018309085B2 (en) 2022-12-08
CN111032039A (zh) 2020-04-17
AU2018309085A1 (en) 2020-02-06

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