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New Derivatives of Phosphonate Compounds with Enhanced Anti-viral Activity

Detailed Technology Description

A series of novel derivatives of phosphonate compounds has been synthesized. These novel compounds have demonstrated enhanced activity against poxviruses and herpes viruses in tissue culture cells when compared with the unmodified parent molecules. When evaluated against existing alkoxyalkyl analogs of phosphonates, the new compounds are easier and faster to synthesize while retaining the increased bioavailability demonstrated by the alkoxyalkyl phosphonate analogs.

Supplementary Information

Patent Number: US7652001B2
Application Number: US200553198A
Inventor: Hostetler, Karl Y. | Wan, W. Brad
Priority Date: 5 Feb 2004
Priority Number: US7652001B2
Application Date: 7 Feb 2005
Publication Date: 26 Jan 2010
IPC Current: A01N005700 | A01N005710 | A61K003166 | A61K0031675 | A61K00317072 | A61K00317076 | C07D027900 | C07D028500 | C07D029500 | C07F000902 | C07F00096512 | C07F00096558 | C07F00096561 | C07F00096571 | C07H001904
US Class: 514075 | 514143 | 544003 | 568008
Assignee Applicant: The Regents of the University of Californian Diego
Title: Pharmacologically active agents containing esterified phosphonates and methods for use thereof
Usefulness: Pharmacologically active agents containing esterified phosphonates and methods for use thereof
Summary: (I) Are useful to treat viral infections (caused by influenza, hepatitis B/C virus, cytomegalovirus, varicella zoster virus, herpes simplex virus types and 2, Epstein-Barr virus, herpes type 6 and type 8, varicella zoster virus, retroviral infections, orthopox viruses, vaccinia, ebola virus, adenovirus and papilloma virus) such as orthopox viral infection (e.g. smallpox, cowpox, camelpox or monkeypox) and herpes viral infection, growing neoplasm, hepatitis viral infection, and cancer (e.g. lung, head and neck squamous, colorectal, prostate, breast, cervical, childhood, esophageal, kidney, liver, oral, pancreatic and skin cancer, acute lymphocytic leukemia, adult acute myeloid leukemia, adult non-Hodgkin's lymphoma, brain tumors, childhood sarcoma, chronic lymphocytic leukemia, chronic myeloid leukemia, hairy cell leukemia, multiple myeloma, neuroblastoma, and primary central nervous system lymphoma) in mammals. (I) Are also useful to modulate cell proliferation, and to treat disease associated with bone metabolism such as osteoporosis (preferred), metastatic bone cancers, Paget's disease, osteogenesis imperfecta, fibrous dysplasia, rheumatoid arthritis, hyperparathyroidism, algodystrophy, stemo-costoclavicular hyperostosis, Gaucher's disease, Engleman's disease, certain non-skeletal disorders or periodontal disease (all claimed). The ability of (I) to treat cancer was tested using biological assays. The results showed that (I) exhibited a median effective concentration value of 1.6 ± 1.3 μM against vaccinia virus.
Novelty: New ester compounds useful as squalene synthase inhibitors for treating e.g. orthopox viral infection, herpes viral infection, growing neoplasm, hepatitis viral infection and cancer

Industry

Disease Diagnostic/Treatment

Sub Category

Cancer/Tumor

Application No.

7652001

Others

Additional Technologies by these Inventors

• New Drug Derivatives for Promoting Oral Delivery to the Lung
• Derivatives of Novel Nucleoside Phosphonates with Anti-viral Activity
• New Antiviral Compounds

Tech ID/UC Case

19687/2004-100-0

Related Cases

2004-100-0

*Abstract

None

*IP Issue Date

Jan 26, 2010

*Principal Investigator

Name: Karl Hostetler

Department:

Name: Karl Hostetler

Department:

Name: W. Brad Wan

Department:

Country/Region

USA