Abstract: Disclosed is a method for decreasing NMDA receptor-mediated neuronal damage in a mammal by administering to the mammal a nitroso-compound that generates nitric-oxide or related redox species, in a concentration effective to effect neuroprotection. Also disclosed is a method for decreasing NMDA receptor-mediated neuronal damage in a mammal by administering to the mammal a nitroso-compound that generates nitric oxide (or a related redox species such as NO.sup.- or NO.sup.+ equivalent), or a physiologically concentration effective to cause such neuroprotection.

Abstract: The present invention provides a compound having the structure: ##STR1## wherein X, Y, and Z are independently H, Cl, Br, F, OCH.sub.3, I, or an alkyl group having 1 to 6 carbon atoms; and R is ##STR2## wherein n is 0 to 6, X' and Y' are independently H, Cl, F, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, OCH.sub.3, OH, CF.sub.3, OCF.sub.3, NO.sub.2, NH.sub.2, N(CH.sub.3).sub.2, NHCOCH.sub.3, NCS, NHCOCH.sub.2 Br, or N.sub.3, and (CH.sub.2).sub.n, if present, may be substituted with OH, OCH.sub.3, or an alkyl or alkenyl group having 1 to 3 carbon atoms. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier. The present invention further provides a method for treating a disease characterized by a dopamine deficiency which comprises administering to a subject in need of such treatment an amount of the pharmaceutical composition above effective to treat the disease.

Abstract: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or >CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.

Abstract: A compound of the formula ##STR1## wherein R is hydrogen or hydroxy, R.sup.1 and R.sup.2 taken together are a group of the formula --(CH.sub.2).sub.m -- and R.sup.7 is hydrogen or R.sup.1 and R.sup.7 taken together are a group of the formula --(CH.sub.2).sub.n -- and R.sup.2 is hydrogen; R.sup.3 is an aryl or aromatic heterocyclic group; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halogen, alkyl, hydroxy, alkoxy, haloalkyl, nitro, amino, acylamino, alkylthio, alkylsulfinyl or alkylsulfonyl; R.sup.8 is a group of the formula --(CH.sub.2).sub.p --R.sup.9 or --(CH.sub.2).sub.q --R.sup.10 ; R.sup.9 is hydrogen, alkylcarbonyl, aminoalkylcarbonyl, cyano, amidino, alkoxycarbonyl, aryloxycarbonyl, alkylsulfonyl, aminocarbonyl or aminothiocarbonyl; R.sup.

Abstract: Compounds for treating or preventing cerebrovascular diseases are disclosed. These compounds are 5-HT antagonists. More specifically, these compounds, when combined with pharmaceutically acceptable carriers or excipients and administered to animals including humans, are useful in treating or preventing cerebrovascular dementia.

Abstract: Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS curing agent containing the same as an effective ingredient.

Abstract: The present invention provides an antiproliferative p-heteroatom-substituted phenol compound having the structure formula ##STR1## wherein m is 0 to 3, n is 0 to 4 when Het is nitrogen, wherein R is selected from the group consisting of hydrogen, alkyl, arylmethyl and acyl; R.sup.1 is alkyl; R.sup.2 is selected from the group consisting of hydrogen and alkyl; R.sup.3 is selected from the group consisting of alkyl and acyl when Het is nitrogen, R.sup.4 is selected from the group consisting of hydrogen and alkyl; R.sup.5 is selected from the group consisting of hydrogen and alkyl; and R.sup.6 and R.sup.7 are selected from the group consisting of hydrogen, alkyl and R.sup.6 and R.sup.7 together may represent oxygen. Also provided are various methods for the treatment of a pathological cell proliferative disease comprising administering to an animal) a pharmacologically and therapeutically effective dose of a pharmaceutical composition comprising a p-heteroatom-substituted phenols or an analog thereof.

Abstract: Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.3, R.sup.4, and R.sup.6 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2) (1) R.sup.1 is X, R.sup.3 is X, or both R.sup.1 and R.sup.3 are X; and X is the dithiocarbamate containing moiety;and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

Abstract: A nitrogen-containing tricyclic compound represented by formula (I): ##STR1## a salt thereof, or a solvate of said compound or said salt, wherein R represents phenyl or naphthyl group which is unsubstituted or substituted at one to five sites with a group such as a halogen atom; a straight chain or branched alkyl group containing 1 to 10 carbon atoms which is unsubstituted or substituted with one or more halogen atoms; or the like; Y represents hydrogen atom; and Z represents a group such as hydrogen atom, hydroxyl group, or the like; or Y and Z together represent a group such as hydrazono group, hydroxyimino group, or the like which is unsubstituted or substituted with a particular group; and X.sup.1 -X.sup.2 .about.C.about.X.sup.3 represents CH--N--C.dbd.C or N--C.dbd.C--N; provided that when X.sup.1 -X.sup.2 .about.C.about.X.sup.3 represents N--C.dbd.

Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2##

Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonist and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.

Abstract: The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

Abstract: Compounds of the formula ##STR1## wherein the broken line represents an optional double bond; X is O, S, CH.sub.2 or CH.sub.2 CH.sub.2 ; R.sup.1 is selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkyl substituted with 1, 2 or 3 halogen atoms; R.sup.2 is selected from the group consisting of phenyl, substituted phenyl, heterocyclic groups, and substituted heterocyclic groups, said substituted phenyl and substituted heterocyclic groups being substituted with 1 or 2 substituents independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl, trifuluoromethyl, and halogen; R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, or trifluoromethyl, or R.sup.3 and R.sup.

Abstract: The present invention is drawn to methods for treating cerebral infarction by administering to a patient in need thereof an effective amount of a compound of the formulae (I, II or III): ##STR1##

Abstract: A sustained release medicinal preparation is produced by enclosing a macrocyclic compound represented by 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l)-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1 .0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone or 17-ethyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylviny l]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1 .0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone, into the fine particles generally called microspheres which arc made of biodegradable polymer. This preparation, when, for example, given by injection, appreciably improves the transferance of said macrocyclic compound into the blood. Further, this is also used as an agent suitable for topical administration.

Abstract: This invention provides a method of treating immune related anemia in a mammal which comprises administering rapamycin to said mammal orally, parenterally, intravascularly, intranasally, intrabronchially, transdermally, rectally.

Abstract: The present invention provides a disturbance-of-consciousness improving agent which is a highly effective and quick remedy and which can be administered orally. The disturbance-of-consciousness improving agent of the invention contains a sigma receptor agonist compound as an active ingredient.

Abstract: The present invention discloses compounds of the general formula: ##STR1## The compounds are highly isozyme selective protein kinase C beta-1 and beta-2 isozyme inhibitors. Accordingly, the present invention provides a method of selectively inhibiting protein kinase C isozymes beta-1, and beta-2. As isozyme selective inhibitors of beta-1 and beta-2, the compounds are therapeutically useful in treating conditions associated with diabetes mellitus and its complications, as well as other disease states associated with an elevation of the beta-1 and beta-2 isozyme.

Abstract: The invention relates to thiadiazole derivatives corresponding to the general formula ##STR1## in which Ar represents a nitrogen-containing aromatic heterocycle, in particular indolyl which is substituted or unsubstituted on the nitrogen atom with CO--(C.sub.1 -C.sub.4)alkyl; with (CH.sub.2).sub.n COR in which n represents 1 or 2 and R represents OR.sub.1 or NR.sub.1 R.sub.2 with R.sub.1 and R.sub.2, which may be identical or different, representing H or (C.sub.1 -C.sub.4)alkyl; with (C.sub.1 -C.sub.4) hydroxyalkyl; with (C.sub.2 -C.sub.6) alkoxyalkyl; tetrahydropyranyl; or with a --(CH.sub.2).sub.3 -- chain, the last carbon of which is attached to the phenyl ring of the indole to form a 6-membered ring;Z represents(a) the group ##STR2## where A and B, independently of each other, represent C, CH or N; and X.sub.1, X.sub.2, X.sub.3 and X.sub.4, which may be identical or different, represent H, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.

Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.

Abstract: The present invention relates to novel fused tricycylic nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated, conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof.

Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

Abstract: This invention relates to 5-chloro-2,3-dihydro-2,2-dimethylbenzofuran-7-carboxylic acid-octahydro-3-hydroxy-2,6-methano-2H-quinolizin-8-yl ester (I), a novel 5-HT.sub.3 -receptor antagonist, its method of preparation, and to its end-use application in the treatment or radio- and chemo-therapeutically-induced nausea and vomiting, in the treatment or pain associated with migraine, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses or the type manifested in patients suffering from schizophrenia and mania, for irritable bowel syndrome, and to combat drug abuse.

Abstract: The invention features methods of treating insulin-induced obesity, weight gain, and other conditions associated with hyperinsulinemia.

Abstract: Recurrent paroxysmal neuropsychiatric disorders selected from (1) acute dystonic reactions, (2) seizure disorders and (3) panic disorders may be treated by means of aerosol inhalation of (1) anticholinergic and/or antihistaminic agents, (2) benzodiazepines and (3) antihistaminic agents, respectively.

Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.

Abstract: This invention relates to compounds of the formula: ##STR1## which are useful as 5-HT.sub.4 agonists or antagonists and 5-HT.sub.3 antagonists.

Abstract: 1-Hetero substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: The invention relates to the use of magnesium-pyridoxal-5'-phosphate-glutaminate to prepare a pharmaceutical suitable for the reduction of LDL-bound peroxides and for the prophylaxis of vascular lesions resulting therefrom in the absence of hypercholesteraemia or hyperlipidaemia.

Abstract: Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O-- or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl orR.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl,andB is a saturated azabicyclic ring (e.g. tropanyl or quinuclidinyl) or a N-oxide thereofand their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.

Abstract: The pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl optionally unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula >C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, that can be used for the control or treatment of muscle tension, stress, insomnia, anxiety and/or convulsions.

Abstract: The compound (S)-1-[(10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quino-lizin-1-yl)c arbonyl]-3-ethoxypyrrolidine of the formula ##STR1## which has valuable pharmacological properties, is described. In particular, the compound of formula I has a non-sedating, hypnotic, that is, sleep-promoting, activity and can accordingly be used for the treatment of sleep disorders.

Abstract: Pharmacologically active compounds having anti-allergic properties corresponding to the formula I ##STR1## which can be mono- or disubstituted in the phenyl ring and their acid addition salts and/or S-mono- or dioxides of sulfur-containing compounds of the formula I are described, together with processes and intermediates for their preparation.

Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

Abstract: The invention relates to a method of treating cardiac ischemic disease using a compound of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkenyl or N,N-di(lower)alkylaminomethyl,R.sup.2 is hydrogen, lower alkyl or halogen,R.sup.3 is imidazolyl or pyridyl, each of which may have substituent(s) selected from lower alkyl and imino-protective group, andR.sup.4 is hydrogen, lower alkyl, lower alkenyl or hydroxy(lower)alkyl and R.sup.5 is hydrogen, hydroxy or lower alkanoyloxy, orR.sup.4 and R.sup.5 are linked together to form an additional bond,or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkoxy, halogen, amino, monoalkylamino, dialkylamino, acylamino and alkylsulfonylamino; R.sub.3 is selected from the group consisting of H, alkyl and cycloalkyl; X is NH or O; Z is selected from the group consisting of ##STR2## n and r are independently 1 or 2; p is 0 or 1; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositions which act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.

Abstract: Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C.dbd.O, C.dbd.S, C-SCH.sub.3, C.dbd.NH, C-NH.sub.2, C-NHCH.sub.3, C--NHCOOCH.sub.3, or C--NHCN. B is CH.sub.2, CH, C.dbd.O, N, NH or N--CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C.dbd.O, O, N, NH or N--CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.

Abstract: A pharmaceutical solution which contains the compound of the general formula having the immusuppreseive activity is disclosed.

Abstract: The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

Abstract: The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

Abstract: Insecticidal, acaricidal and herbicidal polycyclic 3-aryl-pyrrolidine-2,4-dione derivatives of the formula ##STR1## in which A represents the radical of a bi-, tri- or polycyclic system which is optionally interrupted by further hetero atoms or groups of hetero atoms,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number from 0-3, andG represents hydrogen or various organic radicals.

Abstract: Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O--or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl or R.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl,andB is a saturated azabicyclic ring (eg tropanyl or quinuclidinyl) or a N-oxide thereofand their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.

Abstract: Aminomacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by incorporation of a nitrogen substituent at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma.

Abstract: Macrolide compounds having the structure shown below ##STR1## wherein R.sup.1 is hydroxy or protected hydroxy, R.sup.2 is hydrogen, hydroxy or protected hydroxy, R.sup.3 is methyl, ethyl, propyl or allyl, R.sup.4 is hydroxy, methoxy or oxo, n is 1 or 2 and the symbol of a line and a dotted is a single bond or a double bond, provided that R.sup.2 is not protected hydroxy where R.sup.4 is hydroxy or oxo are used to treat hepatic disease and regenerate liver tissue by facilitating hypertrophy and hyperplasia of hepatocytes.

Abstract: There is described pyrroloquinoline derivatives of general formula: ##STR1## wherein R' is a C.sub.1 -C.sub.6 alkyl group, R.sup.2 is a group: ##STR2## or group: ##STR3## wherein R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined, or salt thereof. These compounds have an antimicrobial activity.

Abstract: The invention relates to compounds for treatment of nausea and vomiting, of the formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkenyl or N,N-di(lower)alkylaminomethyl,R.sup.2 is hydrogen, lower alkyl or halogen,R.sup.3 is imidazolyl or pyridyl, each of which may have substituent(s) selected from lower alkyl and imino-protective group, andR.sup.4 is hydrogen, lower alkyl, lower alkenyl or hydroxy(lower)alkyl and R.sup.5 is hydrogen, hydroxy or lower alkanoyloxy, orR.sup.4 and R.sup.5 are linked together to form an additional bond,or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, or a pharmaceutically acceptable cation;Y is cyclopropyl, ethyl or p-fluorophenyl, and X is hydrogen or fluoro, or X and Y taken together form a group ##STR2## wherein R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof. Also disclosed are antibacterial pharmaceutical compositions comprising the foregoing compounds, methods of using the compounds in treating bacterial infections, and intermediates for the preparation of the compounds.

Abstract: An azatetracycle compound useful as 5HT.sub.3 antagonists of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.