CN105884905A - 同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途 - Google Patents

同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途 Download PDF

Info

Publication number
CN105884905A
CN105884905A CN201610294789.5A CN201610294789A CN105884905A CN 105884905 A CN105884905 A CN 105884905A CN 201610294789 A CN201610294789 A CN 201610294789A CN 105884905 A CN105884905 A CN 105884905A
Authority
CN
China
Prior art keywords
lys
compound
obzl
arg
ala
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201610294789.5A
Other languages
English (en)
Chinese (zh)
Inventor
彭师奇
赵明
蒋雪云
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shanghai Is Bright Along Bio Tech Ltd
Original Assignee
Shanghai Is Bright Along Bio Tech Ltd
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
Priority claimed from CN 201210323951 external-priority patent/CN102898506A/zh
Priority claimed from CN2012103238493A external-priority patent/CN102875644A/zh
Priority claimed from CN2012103238506A external-priority patent/CN102898505A/zh
Priority claimed from CN2012103238489A external-priority patent/CN102887941A/zh
Application filed by Shanghai Is Bright Along Bio Tech Ltd filed Critical Shanghai Is Bright Along Bio Tech Ltd
Publication of CN105884905A publication Critical patent/CN105884905A/zh
Pending legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C07K5/0817—Tripeptides with the first amino acid being basic the first amino acid being Arg
    • 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
    • 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
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K47/54—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 an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K47/69—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6921—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere
    • A61K47/6927—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores
    • A61K47/6929—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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores the form being a nanoparticle, e.g. an immuno-nanoparticle
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/28—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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745—Blood coagulation or fibrinolysis factors
    • C07K14/75—Fibrinogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C07K5/0823—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp and Pro-amino acid; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/01—Fusion polypeptide containing a localisation/targetting motif

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Toxicology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Nanotechnology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
CN201610294789.5A 2012-09-05 2013-03-05 同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途 Pending CN105884905A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
CN2012103239513 2012-09-05
CN 201210323951 CN102898506A (zh) 2012-09-05 2012-09-05 Rpak/咪唑啉/rgd三元缀合物及其制备方法和用途
CN2012103238493A CN102875644A (zh) 2012-09-05 2012-09-05 Grpak/咪唑啉/rgd三元缀合物及其制备方法和用途
CN2012103238506A CN102898505A (zh) 2012-09-05 2012-09-05 Arpak/咪唑啉/rgd三元缀合物及其制备方法和用途
CN2012103238489 2012-09-05
CN2012103238489A CN102887941A (zh) 2012-09-05 2012-09-05 Pak/咪唑啉/rgd三元缀合物及其制备方法和用途
CN2012103238493 2012-09-05
CN2012103238506 2012-09-05
CN201310068532.4A CN103665107B (zh) 2012-09-05 2013-03-05 同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201310068532.4A Division CN103665107B (zh) 2012-09-05 2013-03-05 同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途

Publications (1)

Publication Number Publication Date
CN105884905A true CN105884905A (zh) 2016-08-24

Family

ID=50236496

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201310068532.4A Active CN103665107B (zh) 2012-09-05 2013-03-05 同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途
CN201610294789.5A Pending CN105884905A (zh) 2012-09-05 2013-03-05 同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201310068532.4A Active CN103665107B (zh) 2012-09-05 2013-03-05 同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途

Country Status (14)

Country Link
US (2) US20150290339A1 (enExample)
EP (1) EP2894160B1 (enExample)
JP (2) JP6212123B2 (enExample)
KR (1) KR20150048871A (enExample)
CN (2) CN103665107B (enExample)
AU (1) AU2013312689B2 (enExample)
BR (1) BR112015004854A2 (enExample)
CA (1) CA2884057A1 (enExample)
MX (1) MX2015002848A (enExample)
PH (1) PH12015500465B1 (enExample)
RU (1) RU2604193C2 (enExample)
TW (1) TWI568747B (enExample)
WO (1) WO2014036821A1 (enExample)
ZA (1) ZA201500316B (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110577584A (zh) * 2018-06-08 2019-12-17 首都医科大学 1S-甲基-β-四氢咔啉酰-K(RPAK)-RGDV,其合成,活性和应用
CN110577576A (zh) * 2018-06-08 2019-12-17 首都医科大学 1S-甲基-β-四氢咔啉酰-K(GRPAK)-RGDV,其合成,活性和应用
CN113121641A (zh) * 2021-03-11 2021-07-16 武汉英纳氏药业有限公司 一类多功能多肽及其在医药领域的应用

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2847934T3 (es) * 2013-06-05 2021-08-04 Shanghai Lumosa Therapeutics Co Ltd Nuevos compuestos que tienen actividades triples de trombólisis, antitrombóticos y captadores de radicales, y síntesis, nanoestructura y uso de los mismos
CN105218638A (zh) * 2014-06-11 2016-01-06 首都医科大学 Rgds修饰的吲哚喹嗪，其制备，纳米结构，活性和应用
CN105218634A (zh) * 2014-06-11 2016-01-06 首都医科大学 Yigsr修饰的吲哚喹嗪,其制备,纳米结构,活性和应用
CN104151375B (zh) * 2014-07-16 2016-04-20 南京农业大学 一种昆仑雪菊酚苷化合物及其制备方法和用途
CN104402821A (zh) * 2014-12-04 2015-03-11 贾正平 具有抗缺氧损伤活性的氮氧自由基类化合物及其制备和应用
CN105884862B (zh) * 2014-12-16 2019-09-13 首都医科大学 RGD四肽修饰的β-咔啉酰-色氨酸，其制备，纳米结构，活性及应用
CN105859832A (zh) * 2015-01-19 2016-08-17 复旦大学 以rgd为活性中心的多肽及其在制备治疗缺血性脑卒中靶向药物中的应用
CN106279363B (zh) * 2015-06-23 2020-01-17 首都医科大学 五甲氧色胺基羰丙酰-grpak肽,其制备,活性和应用
CN106317194B (zh) * 2015-06-23 2019-07-26 首都医科大学 环组氨酰-karpak,其合成,血栓相关活性及应用
CN106317187B (zh) * 2015-06-23 2019-07-12 首都医科大学 五甲氧色胺基羰丙酰-pak肽,其制备,活性和应用
CN106317189B (zh) * 2015-06-23 2019-07-12 首都医科大学 五甲氧色胺基羰丙酰-rpak肽,其制备,活性和应用
CN112812152B (zh) * 2015-06-23 2022-09-02 首都医科大学 Glu-Leu-Phe-Tyr-Val五肽的合成及抗炎应用
CN106317199B (zh) * 2015-06-24 2019-09-13 首都医科大学 The-GRPAKRGDV十肽,其制备,活性及应用
CN106317198B (zh) * 2015-06-24 2019-09-17 首都医科大学 GRPAK-The-RGDV，其制备，活性及应用
CN106336450B (zh) * 2015-07-13 2019-09-13 首都医科大学 RGDV-The-GRPAK十肽，其制备，活性及应用
CN106349333B (zh) * 2015-07-13 2019-09-17 首都医科大学 The-K(KAPRG)RGDV十一肽，其制备，活性及应用
FR3042192B1 (fr) * 2015-10-09 2017-12-08 Inst Europeen De Biologie Cellulaire Peptides utiles dans le traitement preventif et curatif de l'alopecie
CN106608904B (zh) * 2015-10-22 2020-07-28 彭莉 1-羟基-2-(氧乙酰基十肽苯基)-四甲基咪唑啉,其合成,活性及应用
CN107459553B (zh) * 2016-06-03 2021-06-08 首都医科大学 左旋维c-2-氧乙酰-pak,其合成,活性和应用
CN108976280B (zh) * 2017-05-30 2021-09-24 首都医科大学 脂肪胺修饰的ldv,其合成,活性和应用
CN112010928B (zh) * 2019-05-30 2022-04-22 首都医科大学 乙基pak修饰的双咔啉并哌嗪二酮,其制备,活性和应用
CN112175041B (zh) * 2019-06-18 2023-01-13 首都医科大学 乙基qrpak修饰的双咔啉并哌嗪二酮,其制备,活性和应用
ES3017234T3 (en) 2019-09-25 2025-05-12 Lumosa Therapeutics Co Ltd Pharmaceutical composition comprising thrombolytic peptide-tetrahydroisoquinoline conjugate
CN115403653B (zh) * 2022-05-19 2024-08-06 首都医科大学 D(+)-β-(3,4-二羟基苯基)-乳酰-Pro-Ala-Lys,其合成及应用
WO2025241148A1 (zh) * 2024-05-23 2025-11-27 骏蓦(北京)生物科技有限公司 化合物及其制备方法和应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101085806A (zh) * 2006-06-07 2007-12-12 韩苏 一种合成方式及其产物的用途
WO2007146049A2 (en) * 2006-06-06 2007-12-21 Abbott Cardiovascular Systems Inc. Morphology profiles for control of agent release rates from polymer matrices
WO2008023378A1 (en) * 2006-08-23 2008-02-28 Yeda Research And Development Co. Ltd Conjugates of rgd peptides and porphyrin or (bacterio)chlorophyll photosynthesizers and their uses

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0665853T3 (da) * 1992-10-02 2002-11-04 Diatide Inc Multimere polyvalente antitrombotiske midler
CN1055479C (zh) 1995-06-13 2000-08-16 北京医科大学 心血管活性多肽以及它们的合成和在医学中的应用
RU2214416C2 (ru) * 2001-12-10 2003-10-20 Государственный научный центр вирусологии и биотехнологии "Вектор" Rgd-содержащие пептиды
CN1231494C (zh) * 2002-10-18 2005-12-14 一泰医药研究（深圳）有限公司 咪唑啉取代的苯氧乙酰寡肽类化合物，它们的合成及在医学中的应用
CN1231495C (zh) * 2002-10-18 2005-12-14 一泰医药研究（深圳）有限公司 咪唑啉取代的苯氧乙酰寡肽类衍生物，它们的合成及在医学中的应用
CN100404513C (zh) 2004-09-03 2008-07-23 首都医科大学 2-取代-4,4,5,5-四甲基-1-氧咪唑啉、及其合成和应用
CN1326839C (zh) 2004-09-03 2007-07-18 首都医科大学 2－取代－4,4,5,5－四甲基－1－羟基咪唑啉，及其合成和应用
CN100404514C (zh) 2004-09-03 2008-07-23 首都医科大学 2-取代苯基-4,4,5,5-四甲基-1,3-二氧基咪唑啉，它们的制备及在药物制备中的应用
CN1978462B (zh) * 2005-11-30 2010-04-21 首都医科大学 咪唑啉修饰的氨基酸,其合成方法及在多肽标记中的应用
CN101190941B (zh) * 2006-11-30 2010-12-01 首都医科大学 具有溶血栓活性的多肽、其制备方法及应用
CN101190940B (zh) * 2006-11-30 2012-06-06 首都医科大学 具有靶向抗血栓活性的多肽、其制备方法和应用
CN101318993B (zh) 2007-06-04 2011-12-07 北京大学 以3S-四氢-β-咔啉-3-羧酸为连接臂的杂交肽、其制备方法及应用
CN102120757B (zh) 2007-06-04 2013-03-27 北京大学 以3S-四氢-β-咔啉-3-羧酸为连接臂的杂交肽、其制备方法及应用
CN101591376A (zh) * 2008-05-30 2009-12-02 首都医科大学 具有溶栓活性的寡肽及其制备方法和应用
CN102477076B (zh) 2010-11-30 2014-04-16 首都医科大学 用于溶血栓的寡肽化合物及其制备方法和应用
CN102477075B (zh) 2010-11-30 2013-08-14 首都医科大学 用于抗血栓的寡肽及其制备方法和应用
CN102477072B (zh) * 2010-11-30 2014-06-18 首都医科大学 用于溶血栓的寡肽化合物及其制备方法和应用
CN102485747B (zh) 2010-12-01 2013-09-25 首都医科大学 具有靶向性溶血栓活性的寡肽、其制备方法和应用
CN102485746B (zh) * 2010-12-01 2014-05-07 首都医科大学 具有靶向性溶血栓活性的寡肽、其制备方法和应用
CN102485748B (zh) 2010-12-01 2013-09-25 首都医科大学 具有靶向性溶血栓活性的寡肽、其制备方法和应用
CN102796046B (zh) 2011-05-26 2015-03-04 首都医科大学 2–(4-羟基)苯甲酰氨基酸-4,4,5,5-四甲基-1,3-二氧基咪唑啉及其制备方法和应用
CN102807605B (zh) 2011-06-03 2014-06-04 首都医科大学 Nα-(1,3-二氧-4,4,5,5-四甲基咪唑啉-2-苯基-4’-氧乙酰基)-Nω-脂肪酰基-Lys-Arg-Gly-Asp-Phe、其制备方法和应用
CN102807604B (zh) 2011-06-03 2014-06-04 首都医科大学 Nα-(1,3-二氧-4,4,5,5-四甲基咪唑啉-2-苯基-4’-氧乙酰基)-Nω-脂肪酰基-Lys-Arg-Gly-Asp-Val、其制备方法和应用
CN103159835B (zh) 2011-12-13 2015-03-25 首都医科大学 Lys及寡肽修饰的姜黄素衍生物、其合成及在医学中的应用
CN102887941A (zh) * 2012-09-05 2013-01-23 永光制药有限公司 Pak/咪唑啉/rgd三元缀合物及其制备方法和用途
CN102898505A (zh) * 2012-09-05 2013-01-30 永光制药有限公司 Arpak/咪唑啉/rgd三元缀合物及其制备方法和用途
CN102898507B (zh) 2012-09-05 2015-05-27 上海晟顺生物科技有限公司 溶栓寡肽-咪唑啉二元缀合物及其制备方法和用途
CN102875644A (zh) * 2012-09-05 2013-01-16 永光制药有限公司 Grpak/咪唑啉/rgd三元缀合物及其制备方法和用途
CN102898506A (zh) * 2012-09-05 2013-01-30 永光制药有限公司 Rpak/咪唑啉/rgd三元缀合物及其制备方法和用途

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007146049A2 (en) * 2006-06-06 2007-12-21 Abbott Cardiovascular Systems Inc. Morphology profiles for control of agent release rates from polymer matrices
CN101085806A (zh) * 2006-06-07 2007-12-12 韩苏 一种合成方式及其产物的用途
WO2008023378A1 (en) * 2006-08-23 2008-02-28 Yeda Research And Development Co. Ltd Conjugates of rgd peptides and porphyrin or (bacterio)chlorophyll photosynthesizers and their uses

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
YIN-YE WANG 等: "The Antithrombotic Effects of P6A and its Derivatives", 《JOURNAL OF CHINESE PHARMACEUTICAL SCIENCES》 *
张桂娟 等: "P6A及类似物修饰的咪唑啉的合成、自由基清除和溶栓活性研究", 《首都医科大学学报》 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110577584A (zh) * 2018-06-08 2019-12-17 首都医科大学 1S-甲基-β-四氢咔啉酰-K(RPAK)-RGDV,其合成,活性和应用
CN110577576A (zh) * 2018-06-08 2019-12-17 首都医科大学 1S-甲基-β-四氢咔啉酰-K(GRPAK)-RGDV,其合成,活性和应用
CN113121641A (zh) * 2021-03-11 2021-07-16 武汉英纳氏药业有限公司 一类多功能多肽及其在医药领域的应用
WO2022188878A1 (zh) 2021-03-11 2022-09-15 武汉英纳氏药业有限公司 一类多功能多肽及其在医药领域的应用
CN113121641B (zh) * 2021-03-11 2022-11-01 武汉英纳氏药业有限公司 一类多功能多肽及其在医药领域的应用

Also Published As

Publication number Publication date
RU2604193C2 (ru) 2016-12-10
US10806798B2 (en) 2020-10-20
KR20150048871A (ko) 2015-05-07
EP2894160A4 (en) 2016-04-13
JP2015529209A (ja) 2015-10-05
AU2013312689B2 (en) 2017-03-30
CN103665107B (zh) 2017-07-14
ZA201500316B (en) 2017-09-27
CA2884057A1 (en) 2014-03-13
TWI568747B (zh) 2017-02-01
US20150290339A1 (en) 2015-10-15
CN103665107A (zh) 2014-03-26
AU2013312689A1 (en) 2015-03-19
JP6212123B2 (ja) 2017-10-11
TW201410708A (zh) 2014-03-16
JP2017206540A (ja) 2017-11-24
MX2015002848A (es) 2015-05-15
BR112015004854A2 (pt) 2020-04-22
EP2894160B1 (en) 2019-03-13
WO2014036821A1 (zh) 2014-03-13
EP2894160A1 (en) 2015-07-15
RU2015112025A (ru) 2016-10-27
US20180264126A1 (en) 2018-09-20
PH12015500465A1 (en) 2015-04-20
PH12015500465B1 (en) 2015-04-20

Similar Documents

Publication Publication Date Title
CN105884905A (zh) 同时具溶血栓、清除自由基和血栓靶向功能的新颖化合物及其制备方法和用途
JP2015529209A5 (enExample)
CN102887941A (zh) Pak/咪唑啉/rgd三元缀合物及其制备方法和用途
CN102875644A (zh) Grpak/咪唑啉/rgd三元缀合物及其制备方法和用途
AU650020B2 (en) Method for increasing blood-brain barrier permeability
CN102898505A (zh) Arpak/咪唑啉/rgd三元缀合物及其制备方法和用途
CA3226532A1 (en) Lipidated peptide inhibitors of interleukin-23 receptor
CN102898507B (zh) 溶栓寡肽-咪唑啉二元缀合物及其制备方法和用途
JP7280619B2 (ja) ペプチド組成物
JP6510500B2 (ja) 血栓溶解、抗血栓及びフリーラジカル消去の３つの活性を有する新規の化合物、その合成、ナノ構造と応用
CN102898506A (zh) Rpak/咪唑啉/rgd三元缀合物及其制备方法和用途
JP2001514659A (ja) ドラスタチン−１５誘導体とタキサンとの併用
CN102477072B (zh) 用于溶血栓的寡肽化合物及其制备方法和应用
JPH06179696A (ja) 血液凝固阻害ペプチド及び血栓症治療剤
CN106317193A (zh) 含Tyr-Val片段的肽,其合成、活性和应用
CN106608901A (zh) 二羟基二甲基四氢异喹啉-3-甲酰-Lys(Ala-Lys),其合成,活性及应用
CN106432413A (zh) 五甲氧色胺基羰丙酰-k(pak),其制备,活性和应用
CN106589060A (zh) N-(pak)-2,3-二羟基异喹啉-7-甲酰-rgdv/f,其合成,活性及应用

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20160824

WD01 Invention patent application deemed withdrawn after publication