Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.

Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.

Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).

Abstract: The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, R4, and R5 are defined herein. The compounds of the invention are inhibitors of lactate dehydrogenase A and can be useful in the treatment of cancer and diseases associated with tumor cell metabolism, such as cancer, and more specifically cancers of the breast, colon, prostate and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting lactate dehydrogenase A activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Abstract: Fungicidal compounds of the general formula (I), wherein the substituents are as defined in claim 1.

Abstract: Compounds of the general Formula (1) wherein the substituents are as defined in claim 1, are useful as fungicides.

Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.

Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.

Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is C(O)—O, S(O)2-O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2-NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluoromethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro, hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C

Abstract: The invention provides a compound of formula (I) as defined in the specification, a process for its preparation, pharmaceutical compositions containing it, a process for preparing the pharmaceutical composition, and its use in therapy.

Abstract: Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

Abstract: Quinoline derivatives, particularly 4-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine-2-carboxylic acid; 3-(4-(4-(quinolin-4-ylamino)benzamido)phenylthio)pyrrolidine; N-(4-(piperidin-4-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide; and N-(4-(piperidin-3-ylthio)phenyl)-4-(quinolin-4-ylamino)-benzamide, or a physiologically acceptable salt thereof, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR. Also provided are methods of making such compounds and pharmaceutical compositions.

Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lympho

Abstract: Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

Abstract: There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.

Abstract: The present invention relates to a method for the treatment, amelioration and/or prophylaxis of a neurological condition, in particular neurodegenerative disorders which comprises the administration of an effective amount of a compound of formula (I): to a subject in need thereof. The present invention also relates to a compound of formula (II) and processes for its preparation.

Abstract: Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR?. In particular, the compounds of the invention modulate the function of PPAR?. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.

Abstract: Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

Abstract: Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: Quinoline derivatives, particularly 4-anilinoquinoline derivatives, are provided. Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.

Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.

Abstract: Salts and polymorphs of a compound useful in the treatment of inflammatory and metabolic conditions and diseases are provided herein. In particular, the invention provides salts and polymorphs of a compound which modulates the expression and/or function of a peroxisome proliferator-activated receptor. The salts and polymorphs are useful for the treatment or prevention of conditions and disorders associated with energy homeostasis such as type II diabetes, lipid metabolism, adipocyte differentiation and inflammation.

Abstract: Compounds of Formula 1 [Region ?]?[Region ?]?[Region ?]?[Region ?] ??(I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.

Abstract: Compounds useful for the treatment of pain in accord with the following structural diagram, wherein A, R1, b, R3, d, R4, R5, R6 and R7 are any of a number of groups as defined in the specification, and pharmaceutical compositions and methods of treatment utilizing such compounds.

Abstract: This invention relates to novel quinoline inhibitors of hYAK1 and hYAK3 kinases and pharmaceutically acceptable salts, hydrates or solvates thereof, pharmaceutical compositions thereof, and methods of treatment of diseases in which an excessive amount of either such kinase is a factor.

Abstract: The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, which antagonize the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor and are useful for the prevention or treatment of eating disorders, weight gain and obesity.

Abstract: Compounds of general formula (I), wherein R4 and R5 stand for hydrogen atom or form together an 1,3-butadienyl group, optionally substituted by a methylenedioxy group or one or more straight or branched C1-4 alkyl group, straight or branched C1-4 alkoxy group, hydroxy group or halogen atom; are strong adenosine A3 receptor ligands preferably antagonists.

Abstract: Compounds having selective action at neuronal N-type calcium channels useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are a variety of groups as defined in the specification.

Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is (CO)—O, (SO)2—O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2—NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8, R9-aminocarbonyl(1-4C)alkyl, R8, R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifl

Abstract: The current invention provides novel 2-substituted 1,2,3,4-tetrahydroquinolin-6-ols and derivatives thereof of the formula (I) (A); pharmaceutical compositions thereof, optionally in combination with estrogen or progestin; methods for inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.

Abstract: Heteroaryl aminobenzophenones of general formula I inhibit interleukin-1&bgr; and TNF-&agr; and may therefore be useful in the therapy of inflammatory diseases and conditions.

Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.

Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).

Abstract: This invention provides compounds having the formula: ##STR1## wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted;n is 0-1;Y is --NH--, --O--, --S--, or --NR--;R is alkyl of 1-6 carbon atoms;R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino, alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, ##STR2## R.sub.

Abstract: The present invention provides novel benzimidazole derivatives or salts thereof represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom or a halogen atom; R.sup.2 is a phenyl-lower alkyl group; R.sup.3 is a heterocyclic group selected from the group consisting of an indolyl group, indolinyl group, 1H-indazolyl group, 2(1H)-quinolinonyl group, 3,4-dihydro-2(1H)-quinolinonyl group and 1,4-benzoxazinyl group; A is a lower alkylene group; n is 0 or 1.The benzimidazole derivatives or salts of the present invention are effective agents for treating various arteriosclerotic diseases.

Abstract: The present invention relates to novel quinoline derivatives of the formula ##STR1## which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.

Abstract: The invention relates to compounds of the formula I, ##STR1## to a process for their preparation and to their use as pharmaceuticals. The compounds are employed, in particular, as ester prodrugs of prolyl hydroxylase inhibitors for inhibiting collagen biosynthesis and as fibrosuppressive agents.

Abstract: The compounds of formula I are smooth muscle relaxants: ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, alkanoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; R.sub.

Abstract: Cyanoquinoline compounds Ia or Ib ##STR1## where R.sup.1 is CH.dbd.C(CN).sub.2 ; CH.dbd.N--N.dbd.CH--(5-quinolyl); methylsulfonyl; CH.dbd.NOH; halogen; hydroxyl; nitro; cyano; unsubstituted or substituted C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkylthio, pyrrolidinyl; piperidinyl; morpholinyl; thiomorpholinyl; unsubstituted or substituted phenyl, phenoxy, phenylthio, phenyldithiolyl, phenylsulfonyl or pyrrolyl;m is 0, 1, 2 or 3;R.sup.2 is hydrogen; hydroxyl; halogen; C.sub.1 -C.sub.4 -alkoxy; --NR.sup.3 R.sup.4 ; --NR.sup.5 --CXR.sup.6 or --N.dbd.CR.sup.7 R.sup.8 ;R.sup.3 is hydrogen or unsubstituted or substituted C.sub.1 -C.sub.4 -alkyl;R.sup.4 is a radical R.sup.3 ; C.sub.1 -C.sub.4 -alkylamino; di-C.sub.1 -C.sub.4 -alkylamino; substituted C.sub.1 -C.sub.4 -alkyl; CH.dbd.N--(3-cyano-2-quinolinyl); or R.sup.3 and R.sup.4 together form C.sub.4 - or C.sub.3 -alkylene which may be interrupted by a hetero atom, or unsubstituted or substituted 1,3-butadienyl;R.sup.5 and R.sup.

Abstract: This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: The present invention relates to novel quinoline derivatives of the formula ##STR1## which inhibit exogenously or endogenously stimulated gastric acid secretion and thus can be used in the prevention and treatment of gastrointestinal inflammatory diseases.

Abstract: Compounds of formula ##STR1## wherein; R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 X where X is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro;Z is NR.sub.5 or CR.sub.6 R.sub.7 ;R.sub.5 is hydrogen, aryl, arylthio, arylsulfonyl, lower-alkyl, cycloalkyl, heterocycloalkyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, dilower-alkylamino-lower-alkyl, lower-alkoxy, hydroxy or NR.sub.8 R.sub.9 ;R.sub.6 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro or lower-alkylsulfonyl;R.sub.7 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro, aryl, or lower-alkylsulfonyl;R.sub.8 is hydrogen, lower-alkyl, aryl, heterocycloalkyl, carbamyl, alkanoyl, aroyl, hydroxy-lower-alkyl; andR.sub.9 is hydrogen, lower-alkyl or lower-alkanoyl or pharmaceutically acceptable acid addition salts thereof are useful as anticancer agents.

Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.

Abstract: The present invention discloses a quinoline derivative and salt thereof of the following general formula: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n have the same meanings as defined above). Such a derivative is useful as an antiulcer agent.

Abstract: Substituted 4-aminoquinazoline derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkoxy C.sub.1-6 alkyl,C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl C.sub.1-6 alkyl, phenyl C.sub.1-6 alkyl, the phenyl group being optionally substituted;R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, amino, C.sub.1-6 alkylthio, halogen, cyano, hydroxy, C.sub.1-6 alkanoyl or trifuromethyl;m is 1 to 3;R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkanoyl, amino, C.sub.1-6 alkylamino, ci-C.sub.1-6 alkylamino, halogen, trifluoromethyl or cyano;n is 1 or 2; andR.sup.4 is hydrogen; or a salt thereof are useful as inhibitors of gastric acid secretion.

Abstract: The invention relates to a quinoline of the formula: ##STR1## wherein each of R.sup.1 and R.sup.2, which may be the same or different, is hydrogen, halogeno, hydroxy, cyano, carbamoyl, nitro or amino, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino or alkanoylamino each of up to 4 carbon atoms, or substituted alkyl or alkoxy each of up to 3 carbon atoms, provided that both R.sup.1 and R.sup.2 are not hydrogen; the quinoline ring may bear further substituents; R.sup.3 is hydrogen or alkyl of up to 4 carbon atoms; R.sup.4 is hydrogen, alkyl, alkenyl or alkynyl each of up to 4 carbon atoms or substituted alkyl of up to 3 carbon atoms; Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or which bears one or more substituents; R.sup.5 is such that R.sup.5 --NH.sub.2 is an amino acid; or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.