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Stimulus-Triggered Metalloenzyme Inhibitors

详细技术说明

Matrix metalloproteinases (MMPs) are a class of zinc-dependent hydrolytic enzymes that function in the degradation and restructuring of extracellular proteins. Overexpression of MMPs has been associated with a variety of diseases, including cancer, arthritis, and cardiovascular disease. Commercialization of MMP inhibitors (MMPi) has not been successful, as the inhibition of MMPs systemically has resulted in adverse events such as musculoskeletal syndrome. The researchers have approached this problem by developing prodrug MMPi or "proinhibitors" that are triggered in a localized fashion, minimizing the systemic effects of the drugs. A protected zinc-binding group was used to develop the proinhibitor. The researchers demonstrated that it is possible to protect the MMPi, activate it through an enzymatic reaction, and inhibit MMPs in a controlled manner. The ability to create MMP proinhibitors may provide a new approach to MMPi therapy of disease.

*Abstract

None

*IP Issue Date

Nov 18, 2014

*Principal Investigation

Name: Seth Cohen

Department:

Name: Jody Major-Jourden

Department:

附加资料

Patent Number: US20110312905A1
Application Number: US13166796A
Inventor: Cohen, Seth M. | Major Jourden, Jody L.
Priority Date: 22 Jun 2010
Priority Number: US20110312905A1
Application Date: 22 Jun 2011
Publication Date: 22 Dec 2011
IPC Current: A61K003170 | A61P000900 | A61P001902 | A61P002500 | A61P003500 | C07H001500 | C12N000999
US Class: 514027 | 435184 | 5360041 | 5360174
Assignee Applicant: The Regents of the University of California
Title: STIMULUS-TRIGGERED PRODRUGS
Usefulness: STIMULUS-TRIGGERED PRODRUGS
Summary: (A1) are useful for treating a disease (claimed) comprising: Alzheimer's disease, Parkinson's disease, osteoporosis, inflammatory diseases, osteoarthritis, rheumatoid arthritis, stroke, aneurysm, cardiovascular disease, hypertension, depression, anxiety, glaucoma, HIV or AIDS, neurodegeneration, Addison's Disease, frailty, muscle frailty, inflammatory diseases, asthma, rhinitis, adrenal function related ailments, viral infection, immunodeficiency, immunomodulation, autoimmune diseases, allergies or wound healing; autoimmune diseases in which a subject's immune system irregularly responds to at least one component (e.g. biomolecule, protein, cell, tissue, organ, etc.) of the subject including acute disseminated encephalomyelitis, allergic asthma, autoimmune hepatitis, dermatomyositis, Graves' disease; inflammatory diseases comprising arthritis, psoriatic arthritis, juvenile idiopathic arthritis, multiple sclerosis, systemic lupus erythematosus (SLE), myasthenia gravis, juvenile onset diabetes, diabetes mellitus type 1, etc; cardiovascular disease or condition affecting the heart or blood vessels, comprising coronary artery disease, congenital heart disease, arrhythmogenic right ventricular cardiomyopathy, ischemic heart disease, heart failure, hypertensive heart disease, left ventricular hypertrophy; cancer e.g. cancer of the brain, breast, cervix, colon, head and neck, liver, kidney, lung, non-small cell lung, melanoma, mesothelioma, ovary, sarcoma, stomach, uterus, anemia, embolism and medulloblastoma; and skin related diseases comprising e.g. acne and eczema.
Novelty: New substituted phenyl compounds are matrix metalloprotease inhibitors used for treating disease e.g. Alzheimer's disease, cancer, cardiovascular disease, allergies, asthma, osteoarthritis, inflammatory and cardiovascular diseases

主要类别

诊断/治疗

细分类别

人类免疫缺陷病毒

申请号码

8889638

其他

Additional Technologies by these Inventors

• Novel Matrix Metalloproteinase Inhibitors

Tech ID/UC Case

19944/2010-123-0

Related Cases

2010-123-0

国家/地区

美国