Betulinol derivatives

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C552S500000, C424S178100, C424S193100, C514S002600, C514S345000, C514S387000

Reexamination Certificate

active

06890533

ABSTRACT:
The present invention is directed to betulinol derivatives and betulinol-antibody conjugates having the formulae:andin-line-formulae description="In-line Formulae" end="lead"?HO-antibody-spacer-(A2)nin-line-formulae description="In-line Formulae" end="tail"?and, in particular, betulinol dimethyl ether. Methods for making and using these derivatives and conjugates, as well as a method for making and using betulonic aldehyde, are also disclosed.

REFERENCES:
patent: 4122166 (1978-10-01), Tribble et al.
patent: 4146615 (1979-03-01), Fauran et al.
patent: 4671958 (1987-06-01), Rodwell et al.
patent: 4749567 (1988-06-01), McNatty et al.
patent: 4801688 (1989-01-01), Laguzza et al.
patent: 5013547 (1991-05-01), Sweet et al.
patent: 5034223 (1991-07-01), Abrams et al.
patent: 5064823 (1991-11-01), Lee et al.
patent: 5144010 (1992-09-01), Erlanger et al.
patent: 5162218 (1992-11-01), Schultz
patent: 5166319 (1992-11-01), Wrasidlo
patent: 5272253 (1993-12-01), Koppel et al.
patent: 5328840 (1994-07-01), Coller
patent: 5399672 (1995-03-01), Jalalian et al.
patent: 5468888 (1995-11-01), Bouboutou et al.
patent: 5639656 (1997-06-01), Wright, Jr.
patent: 5643884 (1997-07-01), Anderson
patent: 5679828 (1997-10-01), Lee
Bejar, Int. J. Pharmacogn. 33, 25-32, 1995.*
Kochergina, Chem. Abstr. 106, 153022, 1987.*
Pokhilo, Chem. Abstr. 114, 98300, 1991.*
Pisha, Nature Medicine 1 (10) 1046-51, 1995.*
Macias, Phytochemistry 36, 1369-79, 1994.*
Kircher, Phytochemistry 19, 2707-12, 1980.*
House, “Modern Synthetic Reactions”, 2ndEd (W.A. Benjamin, Inc.) pp. 257-265 1972.*
The Merck Index, 11th Edition, entry 1212, p. 185 (betulin) 1989.*
Sheth et al., “Tumor-Inhibitory Agent fromHyptis emoryi(Labiatae),”Journal of Pharmaceutical Sciences, 61:1819 (1972).
Sheth et al., “Antitumor Agents fromAlnus oregona(Betulaceae),”Journal of Pharmaceutical Sciences, 62:139-140 (1973).
Ukkonen et al., “Birch Bark Extractives,”Kemia Kemi, 6:217-220 (1979).
Tomas et al., “A Cytotoxic Triterpenoid and Flavonoids fromCrossopteryx febrifuga,”Planta Medica, 54:266-267 (1988).
“Bark of Common Northern Birch Tree May Be Invaluable As a New Treatment for Melanoma,”The Medical Herald, pp. 4-5 (May 1995).
Lindgren et al., “Lupan-3β, 20 diol and Lupan-3β, 28-triol in Bank from Birch,Betula verrucosaErh.,”Acta Chem. Scand., 20:1720-1721 (1966).
Jaaskelainen, “Betulinol and Its Utilisation,”Papperi Ha Puu-Papper Orc Trä., 63:599-603 (1981).
Rathnam et al., “Daunorubicin Conjugates of Antibodies to CA-125 and Lutropin Receptor,” FASEB Journal, Experimental Biology 96, Washington, D.C. (Apr. 14-17, 1996) (abstract).
Suwa et al., “Epidermal Growth Factor Receptor-Dependent Cytotoxic Effect of Anti-EGFR Antibody-Ribonuclease Conjugate on Human Cancer Calls,”Anticancer Research19:4161-4166 (1999).
Takahashi et al., “Experimental Treatment of Malignant Gliomas with Human Monoclonal Antibody-Drug Conjugates,”Anticancer Research19:4151-4156 (1999).
Charles et al., “Atrophy of Cholinergic Basal Forebrain Neurons Following Excitotoxic Cortical Lesions is Reversed by Intravenous Administration of an NGF Conjugate,”Brain Research728:193-203 (1996).
Roy et al., “Targeting T Cells Against Brain Tumors with a Bispecific Ligand-Antibody Conjugate,”Int. J. Cancer76:761-766 (1998).
Harapanhalli et al., “Lysine-Directed Conjugation of Ethidium Homodimer to B72.3 Antibody: Retention of Immunoreactivity but Altered Tumor Targeting,”Nuclear Medicine&Biology25:267-278 (1998).
Crosasso et al., “Antitumoral Activity of Liposomes and Immunoliposomes Containing 5-Fluorouridine Prodrugs,”Journal of Pharmaceutical Sciences86:832-839 (1997).
Cheng, “Bystander Killing of Tumour Cells by Antibody-Targeted Enzymatic Activation of a Glucuronide Prodrug,”British Journal of Cancer79:1378-1385 (1999).
Chang et al., “Five Different Anti-Prostate-specific Membrane Antigen (PSMA) Antibodies Confirm PSMA Expression in Tumor-Associated Neovasculature,”Cancer Research59:3192-3198 (1999).
Oosterwijk et al., “Antibody Localization in Human Renal Cell Carcinoma: A Phase I Study of Monocolonal Antibody G250,”Journal of Clinical Oncology11:738-750 (1993).
Texter et al., “The Role of Monoclonal Antibody in the Management of Prostate Adenocarcinoma,”The Journal of Urology160:2393-2395 (1998).
Kaminski et al., “Radioimmunotherapy of B-Cell Lymphoma With [131I]Antigen-B1 (Anti-CD20) Antibody,”The New England Journal of Medicine329:459-465 (1993).
Houba et al., “Improved Characteristics of a Human β-Glucuronidase-Antibody Conjugate After Deglyconsylation for Use in Antibody-Directed Enzyme Prodrug,”Bioconjugate Chem., 7:606-611 (1996).
Wolfe et al., “Antibody-Directed Enzyme Prodrug Therapy With the T268G Mutant of Human Carboxypeptidase A1: In Vitro Studies With Prodrugs of Methotrexate and the Thymidylate Synthase Inhibitors GW1031 and GW1843,”Bioconjugate Chem., 10:38-48 (1999).
Somasundaram et al., “Development of a Trispecific Antibody Conjugate Directs Two Distinct Tumor-Associated Antigens to CD64 on Myeloid Effector Cells,”Human Antibodies, 9:47-54 (1999).
Nathan et al., “Hydrogels Based on Water-Soluble Poly(ether urethanes) Derived from L-Lysine and Poly(ethylene glycol),”Macromolecules, 25:4476-4484 (1992).
Nathan et al., “Copolymers of Lysine and Polyethylene Glycol: A New Family of Functionalized Drug Carriers,”Bioconjugate Chem., 4:54-62 (1993).
Poiani et al., “Conjugates of cis-4-Hydroxy-L-proline and Poly(PEG-Lys), a Water Soluble Poly(ether urethane): Synthesis and Evaluation of Antifibrotic Effects in Vitro and in Vivo,”Bioconjugate Chem., 5:621-630 (1994).
Vilaseca et al., “Protein Conjugates of Defined Structure: Synthesis and Use of a New Carrier Molecule,”Bioconjugate Chem., 4:515-520 (1993).
Haselgrübler et al., “Synthesis and Applications of a New Poly(ethylene glycol) Derivative for the Crosslinking of Amines With Thiols,”Bioconjugate Chem., 6:242-248 (1995).
Senter et al., “Poly(ethylene glycol)-Doxorubicin Conjugates Containing β-Lactamase-Sensitive Linkers,”Bioconjugate Chem., 6:389-394 (1995).
Sejbal et al., “Functionalization of Lupane with Chromium (VI) Oxide, a Remark on the Structure of Clerodone,”Collect. Czech. Chem. Commun. 61:1371-1379 (1996).
Pouzar et al., “Reduction and Steric Interaction of 12-Lupanone Derivatives,”Collection Czechoslov. Chem. Commun. 41:3452-3466 (1976).
Simonsen et al., “The Triterpenes and Their Derivatives,”The Terpenes, vol. 4, Ch. II, Alcohols, Cambridge University Press, pp. 287-369 (1957).

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Betulinol derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Betulinol derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Betulinol derivatives will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3406606

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.