Classifications

• • 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
  • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
  • A61K31/4035—Isoindoles, e.g. phthalimide
• • 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
  • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
• • 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
  • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
• • 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

Definitions

• Cerebral infarction is definitively treated by recanalization of an obstructed site; however, resupply of blood flow to a site damaged by cerebral infarction may cause hemorrhagic cerebral infarction and worsen life and functional prognosis.
• thrombolytic therapy by intravenous administration of a thrombolytic agent, rt-PA, and mechanical thrombectomy by endovascular surgery, are known.
• the rt-PA currently used as a first-choice drug can be administered to patients by 4.5 hours after onset.
• the agent has a strong thrombolytic effect but likely causes a hemorrhagic side effect.
• Other than application timing, strict restrictions are present.
• the percentage of allowable patients for administration is less than 10% of the whole cerebral infarction patients.
• SMTP Stachybotrys Microspora Triprenyl Phenol
• SMTP compounds which refer to a group of compounds having a triprenyl phenol skeleton and produced by filamentous fungi, are known to have a thrombolysis promoter effect and an angiogenesis inhibitory effect (Patent Literatures 1 to 3).
• SMTP compounds induce a conformational change of plasminogen and consequently promote thrombolysis. Because of this, induction of excessive plasmin production can be avoided and risk of developing a hemorrhagic side effect is lessened (Non Patent Literature 1).
• SMTP compounds inhibit soluble epoxy hydrolase (sEH) to thereby produce an anti-inflammatory activity (Non Patent Literature 2) and an antioxidant activity, bringing a cerebroprotective action.
• Non Patent Literature 2 soluble epoxy hydrolase 2
• Non Patent Literature 3 an antioxidant activity 3
• a method for reducing a hemorrhagic risk in cerebral infarction comprising administering Compound I or a salt thereof to a subject.
• a method for treating cerebral infarction comprising administering Compound I or a salt thereof to a subject, wherein risk of a hemorrhagic side effect is low.
• the risk of a hemorrhagic side effect is low in comparison with, for example, an existing cerebral infarction drug (for example, tPA).
• Figure 7 shows mRS original score on Day 90 after administration between a placebo group and (TMS-007 1 mg-administration group) FAS group.
• Compound I has a thrombolytic effect, an anti-inflammatory effect and an antioxidant effect. As a result that Compound I exerts a cell protective effect and a neuroprotective effect in addition to the thrombolytic effect, and produces a preventive or therapeutic effect against ischemic damage such as cerebral infarction.
• a drug, t-PA, widely used as a cerebral infarction drug is considered to show clinical utility mainly due to thrombolytic effect.
• Other compounds such as desmoteplase and tenecteplase have been developed as a thrombolytic agent, are proteins similarly to t-PA.
• a lower molecular compound having an effect to remove thrombi of cerebral infarction patients has not been known (Mican et ah, Computational and Structural Biotechnology Journal, Vol.17, 2019, Pages 917-938; Nikitin et ak, J Stroke. 2021; 23 (1): 12-36).

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• Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Chemical & Material Sciences (AREA)
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• Pharmacology & Pharmacy (AREA)
• Medicinal Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Epidemiology (AREA)
• Urology & Nephrology (AREA)
• Vascular Medicine (AREA)
• Cardiology (AREA)
• Heart & Thoracic Surgery (AREA)
• Diabetes (AREA)
• Hematology (AREA)
• Dermatology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicinal Preparation (AREA)

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• 2022
  • 2022-05-10 US US18/289,399 patent/US20240238248A1/en active Pending
  • 2022-05-10 AU AU2022275263A patent/AU2022275263A1/en active Pending
  • 2022-05-10 CN CN202280033982.7A patent/CN117295497A/zh active Pending
  • 2022-05-10 BR BR112023023534A patent/BR112023023534A2/pt unknown
  • 2022-05-10 CA CA3216137A patent/CA3216137A1/en active Pending
  • 2022-05-10 JP JP2023570055A patent/JP2024525998A/ja active Pending
  • 2022-05-10 WO PCT/US2022/028488 patent/WO2022240810A1/en not_active Ceased
  • 2022-05-10 KR KR1020237038570A patent/KR20240005749A/ko active Pending
  • 2022-05-10 EP EP22733771.4A patent/EP4337193A1/en active Pending

Patent Citations (5)

Non-Patent Citations (11)

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