5118684 Piperdine derivative and pharmaceutical composition

New Patents

tx

Structure m which A, B, and C are hydrogen, halogen, or amdo, D ~s hydrogen, halogen, azldo, or OH; A and B or C and D can be replaced with a double bond, R is an aldohexose, aldohexosamme, or N-acetyl aldohexosamme, W is O or S, X is O, S, or CH2, Y is a purlne or pynrmdme base, Z is C, S, or O, and whereto when Z is S or O, A and C are not present The compounds of tlus mverntlon have enhanced pharmaceutical or biological actlwty or mcreased mtracellular absorpUon compared to the corresponding parent nucleoslde as a function of the 5'-dlphosphohexose moiety Many of these compounds have anUwral, mcludmg ant~-HIV, act~wty Others have anUbactenal actw~ty In one embodiment, the invenUon ~s a method to treat HIV mfect~on and opportumsUc mfecUons concomitantly

alkyl group or a benzyl group), a group of the formula See Patent for Chemtcal Structure a group of the formula See Patent for Chemtcal Structure a group of the formula -OCH2CH2CH = or a group of the formula See Patent for Chemtcal Structure the nng A denotes a group of the formula See Patent for Chemtcal Structure a group of the formula See Patent for Chemtcal Structure a group of the formula See Patent for Chemtcal Structure or a group of the formula See Patent for Chemtcal Structure and R2 denotes a hydrogen atom, a lower alkyl group, a substituted or unsubstltuted benzyl group, a substituted or unsubsUtuted benzoyl group, a pyndyl group, a 2-hydroxyethyl group, a pyndylmetyl group or a group of the formula See Patent for Chemical Structure (whereto Z represents a halogen atom)

5118684

5118687

PIPERDINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION

1-OXA-2-OXO-8-AZASPIRO (4,5) DECANE DERIVATIVES, PHARM ACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME

Hach~ro Sug~moto, Takaharu Nakamura, Yutaka Tsuchlya, Hlroyulo Suguml, Kunizou H1gurashl, Nono Kanbc, Yoshlharu Yamamshx, H1roo Ogura, S ~ n Arakl, Atsuhlko Kubota, M1chlko Ohtakc, Klyoml Tamatsu, Usl~ku, Japan asslgncd to Elsm Co Lid A novel plpendme derivative is defined by the formula (I), including a sit thereof, See Patent for Chemzcal Structure (I) whereto R1 denotes a umvalent group derived from one selected among substatuted or unsubst~tuted benzene, pyndme, pyrazme, mdole, anthraqumone, qumohne, substatuted or unsubstatuted phthahnude, homophthalinude, pyndmecarboxyhc acid lmlde, pyridme N-oxtde, pyramnedlcarboxyhc acld Imide, naphthalenedicarboxyhc acid imlde, substltuted or unsubstltuted qumazolinedlone, 1,8naphthahmlde, blcyclo (222) oct-5-ene-2,3dlcarboxyhc acld Imide and pyromerylimldc, X denotes a group of the formula -(CH2)n-, a group of the formula -O(CH2)n-, a group of the formula -S(CH2)n-, a group of the formula NH(CH2)n-, a group of the formula SO2NH(CH2)n-, a group of the formula See Patent for Chemtcal Structure a group of the formula See Patent for Chemtcal Structure a group of the formula See Patent for Chemwal Structure a group of the formula -CH2NH(CH2)n-, a group of the formula See Patent for Chemtcal Structure (m all the above formulas, n is an integer of 1 t h r o u g h 7 and R3 represents a lower GP 23/6---U

Edit Toth, Jozsef Torley, Laszlo Szporny, Bela K~ss, Egon KarpaU, Eva Palos,, G r o o D o r a , Istvan Laszlovszky, Zsolt Szombathelyl, Adam Sarkach, AmkoCsomor Katahn Gere, BodoMihaly , Judl Laszy, Zsolt SzenUrmay, Budapest, Hungary assigned to Pdchter Gedeon Vegyeszet~ Gyar Rt The invention relates to novel compounds loxa-2-oxo-8- of the formula (I), See Patent for Chemzcal Structure (I) whereto X means oxygen or an ) N R group, whereto R stands for hydrogen, a Cl-12alkyl, C3-6cycloalkyl, carbocyclic C6-10aryl or carbocychc C6-10aryl-Cl0-4alkyl group, the lattertwo groups are opuonally substltuted on their aromatic molety by one or more, same or differenthalogen(s), one or more CI-4alkyl or CI-4alkoxy group(s), RI and R2 together represent a methylene group or, when X stands for an ) N R group, whereto R m as defined above, one of RI and R2 may represent a hydroxyl group whereas the other is a methyl group; R3 stands for hydrogen or a phenyl group opUonally subsUtuted by one or more halogen(s), one or more CI-4alkyl or CI4alkoxy or hydroxyl group(s), R4 means hydrogen, one or more halogen(s), CI-4alkyl, CI4alkoxy, hydroxyl or tnhalomethyl group(s); and n m I,2 or 3 as well as thelracid addltlon and quaternary ammomum salts