ECSP20046463A - Compuestos, composiciones y métodos para tratar enfermedades que involucren tejidos con enfermedades ácidas o hipóxicas - Google Patents

Compuestos, composiciones y métodos para tratar enfermedades que involucren tejidos con enfermedades ácidas o hipóxicas

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Publication number
ECSP20046463A
ECSP20046463A ECSENADI202046463A ECDI202046463A ECSP20046463A EC SP20046463 A ECSP20046463 A EC SP20046463A EC SENADI202046463 A ECSENADI202046463 A EC SENADI202046463A EC DI202046463 A ECDI202046463 A EC DI202046463A EC SP20046463 A ECSP20046463 A EC SP20046463A
Authority
EC
Ecuador
Prior art keywords
compounds
compositions
acidic
methods
diseases
Prior art date
Application number
ECSENADI202046463A
Other languages
English (en)
Inventor
Daniel Richard Marshall
Yana Reshetnyak
Don Engleman
Oleg Andreev
Johanna Marie Csengery
Robert A Volkmann
Dalton King
Original Assignee
Cybrexa 1 Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cybrexa 1 Inc filed Critical Cybrexa 1 Inc
Publication of ECSP20046463A publication Critical patent/ECSP20046463A/es

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    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
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    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/6425—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent the peptide or protein in the drug conjugate being a receptor, e.g. CD4, a cell surface antigen, i.e. not a peptide ligand targeting the antigen, or a cell surface determinant, i.e. a part of the surface of a cell
    • 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
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
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    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/092—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
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    • C07D401/06—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 only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D471/06—Peri-condensed systems
    • 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
    • C07D471/16—Peri-condensed systems
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    • 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
    • C07D487/06—Peri-condensed systems
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    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/1048—Glycosyltransferases (2.4)
    • C12N9/1077—Pentosyltransferases (2.4.2)
    • C—CHEMISTRY; METALLURGY
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    • C12Y—ENZYMES
    • C12Y204/00—Glycosyltransferases (2.4)
    • C12Y204/02—Pentosyltransferases (2.4.2)
    • C12Y204/0203—NAD+ ADP-ribosyltransferase (2.4.2.30), i.e. tankyrase or poly(ADP-ribose) polymerase

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Abstract

Compuestos para el tratamiento de enfermedades con tejidos con enfermedad ácida o hipóxica y composiciones farmacéuticas que comprenden los compuestos, así como métodos para preparar y usar los compuestos y las composiciones.
ECSENADI202046463A 2018-01-05 2020-08-04 Compuestos, composiciones y métodos para tratar enfermedades que involucren tejidos con enfermedades ácidas o hipóxicas ECSP20046463A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862613931P 2018-01-05 2018-01-05
US201862758264P 2018-11-09 2018-11-09

Publications (1)

Publication Number Publication Date
ECSP20046463A true ECSP20046463A (es) 2020-12-31

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ECSENADI202046463A ECSP20046463A (es) 2018-01-05 2020-08-04 Compuestos, composiciones y métodos para tratar enfermedades que involucren tejidos con enfermedades ácidas o hipóxicas

Country Status (18)

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US (2) US10933069B2 (es)
EP (1) EP3735297A1 (es)
JP (2) JP7356450B2 (es)
KR (1) KR20200121800A (es)
CN (1) CN111989137A (es)
AU (1) AU2019205325A1 (es)
BR (1) BR112020013672A2 (es)
CA (1) CA3088858A1 (es)
CL (1) CL2020001797A1 (es)
CR (1) CR20200334A (es)
EC (1) ECSP20046463A (es)
IL (1) IL275754A (es)
MA (1) MA51524A (es)
MX (1) MX2020007060A (es)
PE (1) PE20211305A1 (es)
PH (1) PH12020551043A1 (es)
TW (1) TWI820077B (es)
WO (1) WO2019136298A1 (es)

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Publication number Priority date Publication date Assignee Title
CA3066384A1 (en) * 2017-06-09 2018-12-13 Rhode Island Council On Postsecondary Education Linked and other ph-triggered compounds
CN111757882B (zh) 2018-01-05 2023-08-22 Ac免疫有限公司 用于治疗、减轻或预防与Tau聚集体相关的病症的化合物
AU2019205325A1 (en) 2018-01-05 2020-08-13 Cybrexa 1, Inc. Compounds, compositions, and methods for treatment of diseases involving acidic or hypoxic diseased tissues
BR112022000297A2 (pt) 2019-07-10 2022-03-15 Cybrexa 3 Inc Conjugados de peptídeos de agentes de alvo de microtúbulos como terapêuticos
MX2022000449A (es) 2019-07-10 2022-04-25 Cybrexa 2 Inc Conjugados peptídicos de citotoxinas como terapéuticos.
CN112939966B (zh) * 2019-12-10 2023-03-24 武汉光谷亚太医药研究院有限公司 嘧啶衍生物、其制备及应用
WO2021150792A1 (en) 2020-01-21 2021-07-29 Micurx Pharmaceuticals, Inc. Novel compounds and composition for targeted therapy of kidney-associated cancers
CN111285936A (zh) * 2020-03-11 2020-06-16 北京双赢科创生物科技有限公司 靶向肿瘤的酸性敏感纳米肽段及其应用
JP2024503380A (ja) 2021-01-08 2024-01-25 サイブレクサ 2,インコーポレイテッド コンジュゲート連結部分を調製するための方法
WO2022155172A1 (en) 2021-01-13 2022-07-21 Cybrexa 3, Inc. Peptide conjugates of therapeutics
CN115137818B (zh) * 2021-03-31 2023-06-27 华南师范大学 谷胱甘肽激活的光敏剂-化疗药一体化分子前药及其应用
EP4319755A4 (en) 2021-04-08 2025-03-26 Board of Regents, The University of Texas System Compounds and methods for theranostic targeting of parp activity
JP2024516825A (ja) 2021-04-29 2024-04-17 サイブレクサ 2,インコーポレイテッド トポイソメラーゼi阻害剤のペプチドコンジュゲートの投与レジメン
KR102677962B1 (ko) * 2022-03-02 2024-06-25 고려대학교 산학협력단 루카파립의 개선된 제조방법
CN116640229B (zh) * 2023-04-10 2024-01-30 中国人民解放军总医院第五医学中心 一种低pH靶向性CAR-T细胞的构建及应用
CN117815402A (zh) * 2023-09-28 2024-04-05 国家纳米科学中心 一种靶向stat3蛋白的偶联药物及其应用
CN117843713A (zh) * 2023-12-18 2024-04-09 上海亲合力生物医药科技股份有限公司 基于肿瘤微环境激活的激酶抑制剂、组合物及应用

Family Cites Families (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0841924T3 (da) * 1995-08-02 2003-02-10 Univ Newcastle Ventures Ltd Benzimidazolforbindelser
MY132496A (en) * 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
TR200101239T2 (tr) 1998-11-03 2001-11-21 Basf Aktiengesellschaft İkameli-2-fenilbenzimidazoller, üretimleri ve kullanımları
EP1140936B1 (en) * 1999-01-11 2004-03-17 Agouron Pharmaceuticals, Inc. Tricyclic inhibitors of poly(adp-ribose) polymerases
DE19920936A1 (de) 1999-05-07 2000-11-09 Basf Ag Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung
ECSP003637A (es) 1999-08-31 2002-03-25 Agouron Pharma Inhibidores triciclicos de poli (adp-ribosa) polimerasas
WO2001041534A2 (en) 1999-12-13 2001-06-14 Eli Lilly And Company Pseudomycin phosphate prodrugs
US7151102B2 (en) 2000-10-30 2006-12-19 Kudos Pharmaceuticals Limited Phthalazinone derivatives
GEP20074230B (en) 2002-03-20 2007-11-12 Bristol Myers Squibb Co Phosphate prodrugs of fluorooxindoles
DE60335359D1 (de) 2002-04-30 2011-01-27 Kudos Pharm Ltd Phthalazinonderivate
US7449464B2 (en) 2003-03-12 2008-11-11 Kudos Pharmaceuticals Limited Phthalazinone derivatives
JP2006522088A (ja) 2003-03-31 2006-09-28 ファイザー・インク ポリ(adp−リボース)ポリメラーゼの三環系阻害剤の塩
MXPA06000993A (es) 2003-07-25 2006-08-31 Cancer Rec Tech Ltd Inhbidores triciclicos de parp.
GB0317466D0 (en) 2003-07-25 2003-08-27 Univ Sheffield Use
SG150548A1 (en) 2003-12-01 2009-03-30 Kudos Pharm Ltd Dna damage repair inhibitors for treatment of cancer
CA2581025C (en) 2004-09-22 2011-06-07 Pfizer Inc. Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6h-azepino[5,4,3-cd]indol-6-one
CA2580833C (en) 2004-09-22 2010-12-21 Pfizer, Inc. Method of preparing poly(adp-ribose) polymerases inhibitors
JP2008513435A (ja) 2004-09-22 2008-05-01 ファイザー・インク ポリ(adp−リボース)ポリメラーゼ阻害剤を含む治療用組成物
WO2006078816A2 (en) 2005-01-18 2006-07-27 The Board Of Governors For Higher Education Selective delivery of molecules into cells or marking of cells in diseased tissue regions using environmentally senstive transmembrane peptide
US9707302B2 (en) 2013-07-23 2017-07-18 Immunomedics, Inc. Combining anti-HLA-DR or anti-Trop-2 antibodies with microtubule inhibitors, PARP inhibitors, bruton kinase inhibitors or phosphoinositide 3-kinase inhibitors significantly improves therapeutic outcome in cancer
CN101316834A (zh) 2005-09-29 2008-12-03 艾博特公司 在2位取代有苯基的1h-苯并咪唑-4-甲酰胺是强效parp抑制剂
SI2338487T1 (sl) * 2006-01-17 2014-01-31 Abbott Laboratories Kombinacijska terapija z inhibitorji PARP
WO2007131133A2 (en) 2006-05-04 2007-11-15 Genentech, Inc. Methods and compositions relating to zpa polypeptides
UY30639A1 (es) 2006-10-17 2008-05-31 Kudos Pharm Ltd Derivados sustituidos de 2h-ftalazin-1-ona, sus formas cristalinas, proceso de preparacion y aplicaciones
BRPI0806245B1 (pt) 2007-01-10 2022-01-25 Msd Italia S.R.L. Compostos de fórmula i e seus usos
WO2008114114A2 (en) 2007-03-16 2008-09-25 Pfizer Products Inc. Poly(adp-ribose) polymerases inhibitor for treating ophthalmic condition
US8067613B2 (en) 2007-07-16 2011-11-29 Abbott Laboratories Benzimidazole poly(ADP ribose)polymerase inhibitors
PE20100083A1 (es) * 2008-06-05 2010-02-17 Janssen Pharmaceutica Nv Combinaciones de drogas que comprenden un inhibidor de dgat y un agonista de ppar
US9353140B2 (en) 2009-11-25 2016-05-31 Academia Sinica BQC-G, a tumor-selective anti-cancer prodrug
ES2607806T5 (es) 2010-02-12 2024-10-07 Pfizer Sales y polimorfos de 8-fluoro-2-{4-[(metilamino}metil]fenil}-1,3,4,5-tetrahidro-6H-azepino[5,4,3-cd]indol-6-ona
CA3032186C (en) 2010-07-13 2022-04-26 Council on Postsecondary Education, State of Rhode Island and Providence Plantations Environmentally sensitive composition comprising a ph triggered peptide and uses thereof
US8846081B2 (en) * 2010-08-13 2014-09-30 Rhode Island Board Of Governors For Higher Education Liposome compositions and methods of use thereof
CN105813653B (zh) 2013-12-19 2020-06-26 西雅图基因公司 与目标-药物偶联物并用的亚甲基氨基甲酸酯连接物
JP6663350B2 (ja) 2014-01-16 2020-03-11 クロヴィス・オンコロジー,インコーポレーテッド ヘテロ接合性の喪失を示す乳癌または卵巣癌の患者を治療するためのparp阻害剤の使用
PL3099717T3 (pl) 2014-01-31 2019-10-31 Novartis Ag Cząsteczki przeciwciała dla TIM-3 i ich zastosowanie
EP3164420A4 (en) * 2014-06-30 2018-05-23 Tarveda Therapeutics, Inc. Targeted conjugates and particles and formulations thereof
KR20170043597A (ko) 2014-08-22 2017-04-21 클로비스 온콜로지 인코포레이티드 루카파립의 고 용량 강도 정제
PL3204018T3 (pl) * 2014-10-07 2022-01-03 Immunomedics, Inc. Neoadiuwantowe zastosowanie koniugatów przeciwciało-lek
JO3705B1 (ar) 2014-11-26 2021-01-31 Bayer Pharma AG إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية
KR102407261B1 (ko) 2015-02-27 2022-07-06 서울대학교산학협력단 나노 항암제형 및 그 제조 방법
MA43354A (fr) * 2015-10-16 2018-08-22 Genentech Inc Conjugués médicamenteux à pont disulfure encombré
CA3003283A1 (en) 2015-11-24 2017-06-01 Theravance Biopharma R&D Ip, Llc Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease
KR102498258B1 (ko) 2016-01-20 2023-02-10 삼성디스플레이 주식회사 표시 장치
US20170267727A1 (en) * 2016-03-04 2017-09-21 Lehigh University Conjugates of pH Low Insertion Peptide and Monomethyl Auristatins in the Treatment of Solid Tumors
GB201608885D0 (en) * 2016-05-20 2016-07-06 Univ Birmingham Treatment
WO2017210608A1 (en) 2016-06-02 2017-12-07 Yale University Compositions and methods for targeting and treating homologous recombination-deficient tumors
US10040831B2 (en) * 2016-12-19 2018-08-07 Morehouse School Of Medicine Compositions and methods for treating diseases by inhibiting exosome release
CA3066384A1 (en) 2017-06-09 2018-12-13 Rhode Island Council On Postsecondary Education Linked and other ph-triggered compounds
AU2019205325A1 (en) 2018-01-05 2020-08-13 Cybrexa 1, Inc. Compounds, compositions, and methods for treatment of diseases involving acidic or hypoxic diseased tissues
CN109232719B (zh) 2018-09-21 2021-06-29 中国科学院理化技术研究所 一种pH响应的抗菌肽及其制备方法和应用
MX2022000449A (es) 2019-07-10 2022-04-25 Cybrexa 2 Inc Conjugados peptídicos de citotoxinas como terapéuticos.
BR112022000297A2 (pt) 2019-07-10 2022-03-15 Cybrexa 3 Inc Conjugados de peptídeos de agentes de alvo de microtúbulos como terapêuticos

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