Abstract: The invention relates to the method of use of compounds with B3-agonist activity for inhibiting uterine contractions, preventing or slowing down premature labor, or for the treatment and/or prophylaxis of dysmenorrhea.

Abstract: Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula R1—L—NHSO2R2  I in which R1 represents an unsubstituted or substituted aromatic or heteroaromatic group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R3R4N in which R3 and R4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are at

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: This invention relates to new aminopiperazine derivatives having the potentiation of the cholinergic activity, etc., and represented by general formula [I]. wherein R1 is lower alkyl, etc., R2 is aryl, etc., A is or —SO2—, Q is —N═CH—, etc., X is lower alkylene, etc., and R3 and R4 are taken together to form lower alkylene, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and a pharmaceutical composition comprising the same.

Abstract: Prostaglandin agonists of formula (I), in which, for example, A is a sulphonyl or acyl group, B is N or CH, M contains a ring and K and Q are linking groups, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits useful for the treatment of bone disorders including osteoporosis.

Abstract: Nimesulide topical formulations are provided in the form of liquid crystals. The emulsifier cetylstearyl glycoside is used, and constituents of the lipid phase such as caprylic/capric triglycerides and jojoba oil, consistence factors such as cetylstearyl alcohol. Also disclosed is a process for the preparation thereof. The formulations have advantages such as higher stability, better release and absorption of nimesulide, and a higher bioavailability of the active ingredient.

Abstract: The present invention provides compounds having the Formula I The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.

Abstract: The invention discloses a safer Antiarrhythmic drug with controlled Beta Adrenergic activity which comprises a combination of dextro- and laevo-rotatory isomers of sotalol as active ingredients, pharmaceutical compositions with said combination as active ingredients and its preparation and use of the said combination in the treatment of cardiac ailments in mammals including human beings.

Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eac

Abstract: The present invention describes a process for the preparation of aqueous formulations containing azithromycin for ophthalmic use, as well any formulations obtained by this process and their topical use in the ocular bacterial infections, more preferably in the treatment of conjunctivitis, keratitis and blepharitis.

Abstract: Hydrazine derivatives of the formula wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula -Z-aryl, -Z-heterocyclyl or —(CH2)n—, CH═CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each repres

Abstract: The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.

Abstract: Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.

Abstract: Descriptive summary: use of a compound with the formula (I) where R1 is a hydrogen atom, a C1-2 alkyl group, a C1-2 fluoroalkyl group or a C1-2 perfluoroalkyl group and R2, R3 and R4, which may be the same or different, all represent a hydrogen atom, a straight- or branched-chain C1-4 alkyl group or a C3-4 cycloalkyl group, and R5 is a hydrogen atom, a halogen such as fluorine or chlorine, a C1-4 alkyl group or a straight- or branched-chain C1-4 alkoxy group to manufacture a medicinal agent which can be used to treat ejaculation problems such as retrograde ejaculation or aspermia.

Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II: Ar1—W—Ar2—X—Q  II The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.

Abstract: Pharmaceutical composition containing nimesulide in a hydroalcoholic solution and a mixture of traditional vehicles and excipients for local use and application to the oral and rhinopharyngeal cavity for the treatment of inflammation of oral and rhinopharyngeal mucosae.

Abstract: &agr;-Amino acid amides of formula (I) wherein the substituents are defined as follows: n is a number zero or one; R1 to R7 are as defined herein; R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl; R9 is C3-C8cycloalkyl; a C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl group substituted by one or more halogen atoms; or a group (a) wherein p and q are identical or different and are each independently of the other a number zero or one; and R13, R14, R15 and R16 are identical or different and are each independently of the others hydrogen or C1-C4alkyl; X is hydrogen, in which case p and q must have the value zero; phenyl, unsubstituted or mono- or poly-substituted by halogen, nitro, cyano, carboxy, C2-C6alkenyl, C2-C6alkenyl, C1-C6haloalkyl, C3-C6alkenyloxy, C3-C6alkynyloxy, C3-C7cycloalkyl, C1-C6haloalkoxy, C1-C6alkylthio, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl, C3-C6alkynyloxycarbonyl, C1-C6or by C1-C6alkoxy, cyano, —COOR17; —COR18 or a group (b) wherein R17 and R21 are each independently of the other

Abstract: The present invention provides a method of treatment of a disease associated with neurodegeneration by administering a therapeutically effective amount of a compound of the general formula wherein Ar1 is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by hydroxy, lower alkoxy, nitro, amino or methanesulfonamide; Ar2 is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by lower alkyl or halogen; X is C, CH, C(OH) or N; Y is —CH2−, CH or O; Z —CH2—, —CH(CH3)— or —C(CH3)2—; R1 is hydrogen, lower alkyl or acetyl; A is C═O or —(CHR2)n—, wherein R2 is hydrogen, lower alkyl or hydroxy-lower alkyl; B is —(CH2)n—, O, —CH(OH)(CH2)n—, —CH(CH2OH)(CH2)n—, —(CH2)n CH(OH)— or —CH(CH2OH)—; - - - may be a bond; and n is 0-4, or pharmaceutically acceptable acid addition salts thereof.

Abstract: The subject invention concerns novel materials and methods for the treatment and/or prevention of autoimmune disease. In a specific embodiment, elevated production of prostaglandin synthase-2 (PGS-2) is correlated with autoimmune dysfunction.

Abstract: A compound of formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are as defined in the description, R.sup.2 being an aromatic group, useful in the treatment and condition selected from the group consisting of the group meningitis and salpingitis, septic shock, disseminated intravascular coagulation, and/or adult respiratory distress syndrome, acute or chronic inflammation, arthritis, cholangitis, colitis, encephalitis, endocarditis, glomerulonephritis, hepatitis, myocarditis, pancreatitis, pericarditis, reperfusion injury, vasculitis, acute and delayed hypersensitivity, graft rejection, and graft-versus-host disease, auto-immune diseases including Type 1 diabetes mellitus and multiple sclerosis, periodonate diseases, interstitial pulmonary fibrosis, cirrhosis, systemic sclerosis, keloid formation tumors which produce IL-1 as an autocrine growth factor, cachexia, Alzeimer's disease, percussion injury, depression, atherosclerosis, osteoporosis in a mammal, including human.

Abstract: The present invention provides compounds having the of the formula I: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: A Parenteral Water-miscible non-intensely colored injectable composition of Non-steroidal anti-inflammatory drugs is disclosed. The invention utilizes solubilization techniques to achieve sufficiently high concentrations of Nimesulide suitable to deliver therapeutic doses in conveniently small volumes using water and without any salt form or complexing agent of Nimesulide. In the composition of the invention all the ingredients of the base are hydrophillic. The hydrophillic base serves the advantage of better miscibility with body fluids, faster drug disposition and better compatibility with the tissue environment.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The invention provides a method for treating, preventing, or reducing the risk of developing a condition selected from the group consisting of acute coronary ischemic syndrome, thrombosis, thromboembolism, thrombotic occlusion and reocclusion, restenosis, transient ischemic attack, and first or subsequent thrombotic stroke, in a patient, comprising administering to the patient a therapeutically effective amount of an antiplatelet agent in combination with a therapeutically effective amount of a COX-2 inhibitor. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a COX-2 inhibitor, or a pharmaceutically acceptable salt thereof, and an antiplatelet agent, or a pharmaceutically acceptable salt thereof.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: The invention relates to the substantially pure dofetilide polymorphs P162, P162a and P143, and to processes for the preparation of, compositions containing and to the uses of, such polymorphs.

Abstract: The present invention is directed to new therapeutic uses of compounds of formula: ##STR1## wherein X and Y are oxygen, sulfur, or (CR'R").sub.n wherein n is 1 to 4; R is hydrogen, alkyl, or benzyl; R.sub.1 and R.sub.2 are phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, an alkyl chain, adamantyl, or a cycloalkyl group. The uses are cerebrovascular disease such as stroke, peripheral vascular diseases, and restenosis.

Abstract: The instant invention is new compounds of Formula I ##STR1## their use as cerebrovascular agents in diseases such as stroke, peripheral vascular disease, restenosis, and as agents for regulating plasma cholesterol concentrations, for treating hypercholesterolemia and atherosclerosis, and for lowering the serum or plasma level of Lp(a). A pharmaceutical composition is also claimed.

Abstract: Compounds of formula I ##STR1## in which R(1) to R(8) and X have the meanings indicated in the specification, are useful for the production of medicaments having K.sup.+ channel-blocking action; in particular for the production of a medicament for the treatment or prophylaxis of stimulated gastric acid secretion; of ulcers of the stomach and of the intestinal region; of reflux esophagitis; of diarrhea; of all types of arrhythmias, including ventricular and supraventricular arrhythmias; and of reentry arrhythmias and for the prophylaxis of sudden heart death as a result of ventricular fibrillation.

Abstract: Methods are provided for conducting surgical procedures in a patient wherein, during the surgical procedure, autonomous ventricular electrical conductivity and escape beats are reversibly and transiently suppressed to facilitate the surgical procedure. Also provided are compositions which are capable of inducing ventricular asystole in a patient. The compositions may include an AV node blocker. In one embodiment, compositions including an atrioventricular (AV) node blocker and a .beta.-blocker are provided, wherein the .beta.-blocker is present in an amount sufficient to substantially reduce the amount of AV node blocker required to induce ventricular asystole in the patient. The compositions and methods may be used for inducing temporary ventricular asystole in a beating heart, and to facilitate the performance of a variety of surgical techniques, including minimally invasive microsurgical techniques.

Abstract: The present invention relates to the compounds of formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

Abstract: A novel composition for increasing the bioavailability of Non-steroidal Anti-inflammatory Drugs (NSAIDs), particularly those belonging to the category which exhibits its activity by selectively inhibiting cyclooxygenases-II (COX-II) and/or lipooxygenases, is disclosed. The composition is characterized in having clinically significant increased bioavailability when compared to the known compositions of the drugs. The pharmaceutical compositions comprise NSAIDs and Piperine, as herein disclosed. Enhanced bioavailability of NSAIDs results in the reduction of both dosages and dose-related side effects.

Abstract: Compounds of the formula (I) in which A is oxygen, sulphur or NH; B is a group of the formula (IIa) or (IIb); and the other variables have the meaning given in claim 1, may be used as inhibitors of the enzyme cyclooxygenase II ##STR1##

Abstract: This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula I. ##STR1## wherein A, R.sup.2 and R.sup.3 are as described in the specification.

Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: The subject invention concerns novel materials and methods for the treatment and/or prevention of autoimmune disease. In a specific embodiment, elevated production of prostaglandin synthase-2 (PGS-2) is correlated with autoimmune dysfunction.

Abstract: Compounds of formula (I) and pharmacologically acceptable salts thereof wherein: n is 1 to 3, R is an alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is alkyl, R.sub.3 is an alkyl; b) alkyl substituted with an aryl, heteroaryl or cycloalkyl; c) alkyl substituted with one to eight fluorine atoms; d) cycloalkyl; e) alkenyl; f) alkyl substituted with one to three hydroxy, acyloxy or alkoxy substituents, and where the sum of carbons in R.sub.2 and R.sub.3 is greater than five br where R.sub.2 and R.sub.3 with the nitrogen atom form a saturated heterocyclic group having one nitrogen and form 4-8 carbon atoms or a 4-substituted piperazine group in which the 4-substituent can be alkyl, aryl, benzyl, or heteroaryl, and X is hydrogen, hydroxy, alkoxy, alkyl, carbon trifluoride or a halogen, or compounds of formula (I') and pharmacologically acceptable salts thereof wherein: n is 1 to 3, R is an alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is an alkyl, R.sub.

Abstract: An antiinflammatory agent for external use, containing nimesulide as the active ingredient dispersed in the base component and being well absorbable, safe and discoloration-free.

Abstract: There is disclosed a novel amino alcohol amine derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.

Abstract: The present invention provides a compound of the formula: ##STR1## Such compounds are useful for inhibiting prostaglandin synthesis. Pharmaceutical compositions and methods for inhibiting prostaglandin synthesis are also disclosed.

Abstract: Compounds of the formula ##STR1## or pharmaceutically acceptable salts thereof wherein: A is a bond, --(CH.sub.2).sub.n -- or --CH(B)--, where n is an integer of 1 to 3 and B is --CN, --CON(R.sup.9)R.sup.9' or --CO.sub.2 R.sup.7 ;R.sup.1 is lower alkyl, aryl or arylalkyl;R.sup.2 is hydrogen, hydroxy, alkoxy, --CH.sub.2 OH, cyano, --C(O)OR.sup.7, --CO.sub.2 H, --CONH.sub.2, tetrazole, --CH.sub.2 NH.sub.2 or halogen; ##STR2## R.sup.3 is hydrogen, alkyl, heterocycle or R.sup.4 is hydrogen, alkyl or B;R.sup.5, R.sup.5', R.sup.8, R.sup.8' or R.sup.8" are independently hydrogen, alkoxy, lower alkyl, halogen, --OH, --CN, --(CH.sub.2).sub.n NR.sup.6 COR.sup.7, --CON(R.sup.6)R.sup.6', --CON(R.sup.6)OR.sup.6', --CO.sub.2 R.sup.6, --SR.sup.7, --SOR.sup.7, --SO.sub.2 R.sup.7, --N(R.sup.6)SO.sub.2 R.sup.1, --N(R.sup.6)R.sup.6', --NR.sup.6 COR.sup.7, --OCH.sub.2 CON(R.sup.6)R.sup.6', --OCH.sub.2 CO.sub.2 R.sup.7 or aryl; orR.sup.5 and R.sup.5' or R.sup.8 and R.sup.