Methods for introducing a sulfhydryl amino or hydroxyl groups to a compound
US5017693A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 19, 1989 |
| Grant date | May 21, 1991 |
| Priority date | — |
| Expiry date | Dec 19, 2009 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K2123/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of target cell an agent free of its targeting molecular carrier. A diagnostically therapeutically effective dose of a cleavable conjugate is administered to a warm-blooded animal such as man. Another aspect of the invention provides methods for isolating a compound. The compound binds covalently to a solid phase which has been derivatized with the linkers describ…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.