Lupane triterpenoid derivatives
Patent 5643884 Issued on July 1, 1997. Estimated Expiration Date: 
July 1, 2014. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
July 1, 2014. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent References18ଲ-Glycyrrhetinic acid amides useful as antiulcer agents 3ଲ-Hydroxy-18ଲ-olean-9-en-30-oic acids Glycyrrhetinic acid derivatives Derivatives of triterpenoid acids as inhibitors of cell-adhesion molecules ELAM-1 (E-selectin) and LECAM-1 (L-selectin) Derivatives of triterpenoid acids and uses thereof Patent #: 5527890 InventorsAssigneeApplicationNo. 105095 filed on 08/09/1993US Classes:514/26, Cyclopentanohydrophenanthrene ring system514/25, O-glycoside514/53, Dissacharide514/61, Tri- or tetrasaccharide514/169, Cyclopentanohydrophenanthrene ring system DOAI514/172, Hetero ring containing514/176, Nitrogen containing hetero ring514/178, Oxygen single bonded to a ring carbon of the cyclopentanohydrophenanthrene ring system536/4.1, O- or S- Glycosides536/5, Cyclopentanohydrophenanthrene ring system536/18.7, Nitrogen containing536/123.1, Polysaccharides536/123.13Disaccharides (e.g., maltose, sucrose, lactose, formaldehyde lactose, etc.)ExaminersPrimary: Hollinden, Gary E.Assistant: Chapman, Lara E. Attorney, Agent or FirmInternational ClassesA61K 031/705C07J 017/00 AbstractThis invention relates generally to the field of medicinal chemistry, and more specifically to derivatives of a subclass of triterpenoid acids that have multi-medicament properties, that is derivatives of the lupane, betulinic acid, formulations containing such, and their use to prevent or treat certain diseases, and preferably to derivatives or analogues of betulinic acid, that have the following structural formula (1): ##STR1## wherein: Y is OR1, NR12, O- M1 ;R1 is H, LOWER ALKYL,M1 is Na+, K+, Mg++, Ca++ ions;each R2 is independently CH2 OR1 or CH3 ;each R3 is independently H, CH3, lower alkyl, COY, CH2 OH, CH2 OCH2 CH=CH2, CH2 OSO3- M1 ;each Z is independently NHR12, NR1 Ac, NR1 Bz, H, OCH3, lower alkyl, OH, OSO3- M1, OCH2 CH=CH2, OCH2 CO2 H or O-glucoside;each X is independently O, S, NR1 or NR21each W is independently C=O, C=CR12, CR1 CR13, CR1 -CR12 OR1, COR1 -CR1 OR1, COR1 CR12 OR1, CR1 CR12 NR12, CR1 CR12 OCR1 COY, CHR4 ;R4 is H, OH, OSO3- M1, or NH(CH2)nNH2, where n=1-8, or NH-Ph-NH2 where Ph=an phenyl or naphthyl rings substituted with up to 3 amine functionalities and the remaining substitutions can be H, R1, R2 or COY;R5 and R6 are independently H, CH3, or taken together form a 5 or 6 membered carbocyclic ring.Other References
Field of SearchAttached to cyclopentano-hydrophenanthrene (e.g., cholesterol, bile acid, steroids, cholane), hormone, or neurotransmitter, or other secreted growth regulatory factor, differentiation factor, or intercellular mediator (e.g., T3, T4, insulin, human chorionic gonadotropin, intragonadal regulatory protein, Mullerian inhibiting substance, inhibin, epidermal growth factor, nerve growth factor, dopamine, norepinephrine); derivative thereofAttached to carbohydrate compound; derivative thereof (e.g., DNA, nucleotide, nucleoside, sugar, starch, tannin, saccharide, polysaccharide, cellulose, O-, N- and S-glycoside, vitamin B12) Cyclopentanohydrophenanthrene ring system Oxygen containing six-membered hetero ring (e.g., oxathiane, etc.) Nitrogen containing The hetero ring is six-membered Chalcogen or nitrogen attached directly to the hetero ring by nonionic bonding Plural chalcogens bonded directly to the hetero ring Nitrogen attached directly or indirectly to the hetero ring by acyclic nonionic bonding Nitrogen bonded directly to the hetero ring The additional ring is one of the cyclos in a polycyclo ring system Cyclopentanohydrophenanthrene ring system Dissacharide Additional ring containing The hetero ring is six-membered |
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