ARNOLD GLAZIER, M.D.
Medical Practice at Brandeis Rd, Newton, MA

2003003, Feb 13, 2003

Jun 24, 2002

10/179610

Arnold Glazier - Newton MA, US

Drug Innovation & Design, Incorporated - Waltham MA

A61K039/395, C12N015/85

424/178100, 435/455000

The present invention relates to the compositions, methods, and applications of a new approach to pattern recognition based targeting by which an exponential amplification of effector response can be specifically obtained at a targeted cells. The purpose of this invention is to enable the selective delivery of large quantities of an array of effector molecules to target cells for diagnostic or therapeutic purposes. The invention is comprised of two components designated as “Compound 1” and “Compound 2”: Compound 1 is comprised of a cell binding agent and a masked female adaptor. Compound 2 is comprised of a male ligand, an effector agent, and two or more masked female receptors. The male ligand is selected to bind with high affinity to the female adaptor. Compound 1 can bind with high affinity to the target cell and the female receptor can then be unmasked by an enzyme enriched at the tumor cell. The male ligand of Compound 2 can then bind to the unmasked female adaptor bound to the target cell. The masked female adaptor on the bound Compound 2 can then be specifically unmasked. One receptor has in effect become two. Two new molecules of Compound 2 can bind to the unmasked adaptors receptors. After unmasking two receptors in effect become four. The process can continue in an explosive exponential like fashion resulting in enormous amplification of the number of effector molecules specifically deposited at the target cell.

2007017, Jul 26, 2007

Nov 7, 2006

11/593938

Arnold Glazier - Newton MA, US

A61K 51/00, A61K 38/16, C07K 14/00, C07K 9/00

424001110, 424178100, 514012000, 514015000, 514007000, 514008000, 530322000

The present invention relates to the compositions, methods, and applications of a new approach to pattern recognition based targeting by which an exponential amplification of effector response can be specifically obtained at a targeted cells. The purpose of this invention is to enable the selective delivery of large quantities of an array of effector molecules to target cells for diagnostic or therapeutic purposes. The invention is comprised of two components designated as “Compound 1” and “Compound 2”: Compound 1 is comprised of a cell binding agent and a masked female adaptor. Compound 2 is comprised of a male ligand, an effector agent, and two or more masked female receptors. The male ligand is selected to bind with high affinity to the female adaptor. Compound 1 can bind with high affinity to the target cell and the female receptor can then be unmasked by an enzyme enriched at the tumor cell. The male ligand of Compound 2 can then bind to the unmasked female adaptor bound to the target cell. The masked female adaptor on the bound Compound 2 can then be specifically unmasked. One receptor has in effect become two. Two new molecules of Compound 2 can bind to the unmasked adaptors receptors. After unmasking two receptors in effect become four. The process can continue in an explosive exponential like fashion resulting in enormous amplification of the number of effector molecules specifically deposited at the target cell.

5274162, Dec 28, 1993

Dec 13, 1991

7/808030

Arnold Glazier - Newton MA

A01N 4716, A01N 4102, A01N 3734, A61K 31445, C07F 902

558166

The composition, methods of synthesis, and applications of a new class of tumor selective antineoplastic drugs is described. These novel antineoplastic agents are of the general structure: A-C-B. The agents are designed with two key functionalities: a trigger which toxifies the drug; (A) and a deactivator which detoxifies the drug (B) The trigger is selected such that it is activated by an enzyme which is present in elevated levels in the tumor. The deactivator is selected such that it is actuated by an enzyme ubiquitous to all tissues. The fate of the drug in a given cell is then determined by the ratio of the enzymatic activity that triggers toxication to the enzymatic activity which detoxifies the drug. The partitioning of the drug between toxic metabolite and nontoxic metabolite defines the resulting specificity of cytotoxic effect. The application of this invention is exemplified by a new class of antineoplastic drugs which are designed to be selectively toxic for tumor cells bearing the enzyme guanidinobenzoatase.

2003013, Jul 24, 2003

Dec 15, 2000

09/738625

Arnold Glazier - Newton MA, US

Drug Innovation & Design, Inc.

A61K039/395

424/178100

The present invention relates to the compositions, methods, and applications of a novel approach to selective cellular targeting. The purpose of this invention is to enable the selective delivery and/or selective activation of effector molecules to target cells for diagnostic or therapeutic purposes. The present invention relates to multi-functional prodrugs or targeting vehicles wherein each functionality is capable of enhancing targeting selectivity, affinity, intracellular transport, activation or detoxification. The present invention also relates to ultra-low dose, multiple target, multiple drug chemotherapy and targeted immunotherapy for cancer treatment.

6214811, Apr 10, 2001

Feb 28, 2000

9/514552

Arnold Glazier - Newton MA
Milka Yanachkova - Newton MA
Ivan Yanachkov - Newton MA

Drug Innovation & Design, Inc. - Waltham MA

A61K 31675, C07F 965

514 81

Disclosed are novel prodrugs represented by the following structural formula; ##STR1## Z is oxygen or sulfur; Y is, together with a hydroxy group, acyclovir or an analog of acyclovir; A is a substituted benzyl group with one or more protected hydroxy or protected amine groups in the ortho or para positions, relative to the phosphate ester, which can be converted in vivo to a hydroxy or amino group. Also disclosed is a method of treating a viral infection in an individual or animal. The method comprises administering to the individual or animal a therapeutically effective amount of a prodrug represented by structural formula shown above.

6031096, Feb 29, 2000

May 15, 1998

9/080064

Arnold Glazier - Newton MA
Milka Yanachkova - Newton MA
Ivan Yanachkov - Newton MA

Drug Innovation & Design, Inc. - Waltham MA

C07D47318

544244

Disclosed are novel prodrugs represented by the following structural formula: ##STR1## Z is oxygen or sulfur; Y is, together with a hydroxy group, acyclovir or an analog of acyclovir; A is a substituted benzyl group with one or more protected hydroxy or protected amine groups in the ortho or para positions, relative to the phosphate ester, which can be converted in vivo to a hydroxy or amino group. Also disclosed is a method of treating a viral infection in an individual or animal. The method comprises administering to the individual or animal a therapeutically effective amount of a prodrug represented by structural formula shown above.

5627165, May 6, 1997

Sep 23, 1994

8/310972

Arnold Glazier - Newton MA

Drug Innovation & Design, Inc. - Newton MA

A61K 3166, A61K 3170

514 75

The composition and methods of synthesis of phosphorus prodrugs are described. These methods can be used to convert negatively charged phosphorous bearing drugs into neutrally charged; lipid soluble prodrugs which are able to passively diffuse into cells and into tissues in vivo. Prodrugs for a variety of antiviral and anti-leukemic agents are described.

2011020, Aug 18, 2011

Oct 22, 2009

13/125536

Arnold Glazier - Newton MA, US

A61K 31/409, A61K 31/407, A61K 9/00, A61P 27/02

424429, 514411

The present invention relates to method for the treatment or prevention and of proliferative eye diseases including but not limited to: age related macular degeneration associated proliferative retinopathy, proliferative diabetic retinopathy, proliferative vitreoretinopathy, posterior capsular opacification, scaring and fibrosis after glaucoma filtration surgery, uveal melanoma, and retinoblastoma. The method comprises contacting cells in the eye by means of intra-ocular injection or infusion, with a drug that irreversibly inhibits cellular proliferation without causing extensive tissue necrosis or cytotoxicity. In a preferred embodiment the drug is bizelesin.

5789608, Aug 4, 1998

Dec 11, 1996

8/763412

Arnold Glazier - Newton MA

Drug Innovation and Design, Inc. - Needham MA

C07D41300

554116

The composition and methods of synthesis of phosphorus prodrugs are described. These methods can be used to convert negatively charged phosphorous bearing drugs into neutrally charged; lipid soluble prodrugs which are able to passively diffuse into cells and into tissues in vivo. Prodrugs for a variety of antiviral and anti-leukemic agents are described.