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: An improved method for guanylating amines is provided. Broadly, the amines are reacted with a guanylating agent in the presence of a nickel catalyst. Preferably, the nickel catalyst comprises nickel in the zero oxidation state. Suitable nickel(0) catalysts are derived from nickel-boride alloys, nickel-phosphide alloys, aluminum-nickel alloys, nickel on kieselguhr, and nickel on silica/alumina catalysts. Preferred guanylating agents are thioureas and isothioureas. In one embodiment, protecting groups are selectively attached to the guanylating agents to yield particular substituted guanidines. The preferred protecting groups are Boc groups, Cbz groups, and arylsulfonyl groups. The reactions are particularly well suited for guanylating primary and secondary amines. The methods of the invention can be carried out under ambient conditions to provide high yields of the corresponding guanidines, with the nickel catalyst being essentially completely recoverable for reuse.

Abstract: The present invention relates to compounds, compositions, and methods which are useful for the prevention and treatment of adverse health, skin, hair, and oral conditions. The compounds, compositions, and methods are also widely applicable for use in health, skin, hair, oral, beauty, and personal care applications.In particular, the present invention relates to compounds having the structure: ##STR1## and the tautomers, acceptable salts, and biohydrolyzable amides, esters, and imides thereof, wherein A, Q, n, P, L.sub.1, L.sub.2, L.sub.3, L.sub.4, Z, X, B.sub.1, and B.sub.2 are defined herein.

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

Abstract: The present invention provides N,N'-diaryl substituted guanidines having therapeutic utility. The compounds of the present invention are represented by the formula: ##STR1## wherein R and R.sup.1 represent hydrogen or other group and Ar and Ar.sup.1 represent selected aryl groups, and at least one being acenaphthyl.

Abstract: There is disclosed compound according to the formula: ##STR1## wherein A, independently,=CH.sub.3 or CH.sub.2 CH.sub.3, P=1 or 2; and ##STR2## wherein X=NH.sub.2, CH.sub.3 or CH.sub.2 CH.sub.3 ; X'=CH.sub.3 or CH.sub.2 CH.sub.3 ; Y=NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 ; and Z=H, CH.sub.3 or CH.sub.2 CH.sub.3 ; or ##STR3## wherein Y' and Z', independently,=H, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2 or N.sup.+ (CH.sub.3).sub.3 ; Q is N or CH; and salts thereof.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: The present invention encompasses the use of the compounds of formula as given below to detect certain specific protein structures which are present in nuclear localization sequences ##STR1## wherein A is, independently CH.sub.3 or CH.sub.2 CH.sub.3 and R is ##STR2## and salts thereof.

Abstract: The present invention is the novel synthesis of sterically hindered penta-substituted guanidines by a process in which (1a) an isocyanate is reacted first with a di-substituted amine or (1b) a urea is reacted with two moles of a mono-substituted amine to form a tri-substituted urea followed by (2) treatment of the tri-substituted urea with an activating agent before reacting with a second di-substituted amine in the presence of a base.

Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: The invention provides fungicidal compounds having the general formula:X.sub.1 -A.sub.1 -B.sub.1 -C-B.sub.2 -A.sub.2 -X.sub.2 (I)wherein X.sub.1 is an amidine, a guanidine, or an imidazole group.A.sub.1 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring;B.sub.1 is either O (oxygen) or absent; C is a straight chain alkyl comprising 1-8 carbons; B.sub.2 is either O (oxygen) or absent; A.sub.2 is either a five-membered aromatic ring, a six-membered aromatic ring, a fusion of two five-membered aromatic rings, a fusion of 2 six-membered aromatic rings, or a fusion of a six-membered aromatic ring and a five-membered aromatic ring; and X.sub.2 is an amidine, a guanidine, or an imidazole.

Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: The present invention provides a no-carrier-added synthesis of radiolabeled meta-halobenzylguanidine by halodestannylation which comprises reacting a meta-trialkylstannylbenzylguanidine with a source of radionuclide of a halogen. The present invention also provides meta-trialkylstannylbenzylguanidine as intermediates in the afore-mentioned process.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

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: N,N-disubstituted-guanidines, e.g., of the formula ##STR1## wherein R and R' are substituted or unsubstituted hydrocarbon groups. Methods are provided for the treatment of psychosis and hypertension by administering an effective amount of an N,N'-disubstituted guanidine which, preferably, has a high affinity for the sigma receptor.

Abstract: A process for the preparation of a substituted guanidine by reacting a substituted cyanamide with ammonia or a substituted amine in the presence of a Lewis acid catalyst. Also disclosed is a process for the preparation of a tri-substituted guanidine by reacting a mono-substituted cyanamide with a di-substituted amine.

Abstract: The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: The invention relates to a process for the preparation of a tablet or dragee composition containing a moisture-, heat- and light-sensitive compounds having monoclinic crystalline structure as active ingredients, which comprises homogenizing the active ingredient with 0.2 to 1.5 parts by weight of an anhydrous alkaline earth metal salt and 0.5 to 2.5 parts by weight of microcrystalline cellulose calculated for the active ingredient and optionally with one or more pharmaceutically acceptable carrier(s) and/or additive(s) and compressing the homogeneous mixture obtained to tablets in a manner known per se and, if desired, coating the tablet thus obtained in a manner known per se.

Abstract: The present invention relates to bisguanidine derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkenyl; or cycloalkyl which has 5-12 carbon atoms in the ring and may be substituted, or benzyl which may be substituted, with the proviso that only one of R.sup.1 and R.sup.2 can be hydrogen; orR.sup.1 and R.sup.2 are, together with the atoms which they substitute, a heterocyclic ring which may be substituted;X is CH.sub.2, O, a single bond, NH, N-alkyl or N-benzyl whose phenyl ring may be substituted,n is 5 to 8,and their plant-compatible acid addition salts and their metal complexes and fungicides containing these compounds.

Abstract: Compounds of formula I ##STR1## and their salts in which R.sub.1 is optionally substituted phenyl, R.sub.2 is alkyl, cycloalkyl or optionally substituted amino, or R.sub.2 and R.sub.3 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring and R.sub.5 is H, halo, alkyl, alkoxy, trifluoromethyl or a group of formula S(O).sub.m R.sub.8 in which m is 0, 1 or 2 and R.sub.8 is alkyl have utility in the treatment of diabetes particularly in the treatment of hyperglycaemia.

Abstract: A process for the preparation of a substituted guanidine by reacting a substituted cyanamide with ammonia or a substituted amine in the presence of a Lewis acid catalyst. Also disclosed is a process for the preparation of a tri-substituted guanidine by reacting a mono-substituted cyanamide with a di-substituted amine.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.

Abstract: A process for the production of phenylguanidine carbonate and hydrogencarbonate by reacting aqueous cyanamide with aniline hydrochloride within a specified pH range, combining the reaction mixture with an alkali metal carbonate or hydrogencarbonate, and separating the crystalline product.

Abstract: This invention relates to new heterocyclic derivatives of guanidine and more particularly to such derivatives which have hypoglycemic activity, their methods of use for treating hyperglycemia and novel intermediate compounds for their preparation.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: A guanidine type compound has the following formula: ##STR1## wherein R.sup.1 to R.sup.8 are each a hydrogen atom, an alkyl group, an amino group, an alkoxy group, a substituted or umsubstituted aryl group, and R.sup.1 and R.sup.8 may be the same as or different from each other and together may form a ring with the adjacent substituents; X is a halogen atom, a hydroxyl group or an alkoxy group; and m and n are each an integer having a value of 1 to 8. The guanidine compound is employed in a toner for electrostatic development and the toner can be used in an electrophotographic apparatus including a facsimile apparatus for receiving image information from an electrophotographic copier.

Abstract: Disubstituted guanidines, e.g., bis-1,3-(o-isopropylphenyl)guanidine, bis-1,3-(m-isopropylphenyl)guanidine, bis-1,3-(1-naphthyl)guanidine, bis-1,3-(m-methoxyphenyl)guanidine, N-(1-naphthyl)-N'-(o-iodophenyl)-guanidine, N-(1-naphthyl)-N'-(m-ethylphenyl)guanidine, and N-(1-napthyl)-N'-(o-isoproylphenyl) guanidine, exhibit a high binding affinity to phencyclidine (PCP) receptors. These N,N'-disubstituted guanidine derivatives act as non-competitive inhibitors of glutamate-induced responses generated via the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert a neuroprotective property and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal chord ischemia, brain or spinal cord trauma, as well as being useful for the treatmnet of epilepsy, Alzheimer's disease, Amyotrophic Laterla Scherosis, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: A method of improving the adhesion of an adhesive to the surface of hard tissue. Before the adhesive is applied, the hard tissue surface is primed with a polybiguanide or an addition salt thereof, or is pretreated with an aqueous solution of a magnesium salt and then primed with a primer selected from a long chain alkyl quaternary ammonium salt, a bisbiguanide, an acid addition salt of a bisbiguanide, a polybiguanide, and an acid addition salt of polybiguanide.

Abstract: Disubstituted guanidines, e.g., N,N'-di-m-tolyl guanidine, N,N'-di-o-ethylphenyl guanidine, N,N'-di-m-ethylphenyl guanidine, and N,N'-di-o-iodophenyl-guanidine, exhibit a high binding affinity to phenylcyclidine (PCP) receptors. These guanidine derivatives act as non-competitive blockers to glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert a neuroprotective property and are useful in the therapeautic treatment of neuronal loss in ischemia, hypoxia, hypoglycemia, and brain and spinal cord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Huntington's disease, Down's Syndrome and other neurodegenerative disorders.

Abstract: Novel substituted phenyl and benzyl nitroguanidine and phenyl and benzyl cyanoguanidine compounds. Methods for increasing crop yield, inhibiting lodging of graminaceous crops, and inducing cytokinin-like responses in crop plants with said novel guanidine compounds and derivatives thereof, as well as methods for inhibiting deterioration and/or extending the shelf life of harvested fruit, vegetables, and ornamentals are disclosed.

Abstract: Diarylguanidines can be isolated from the crude melt from the reaction of arylamines and cyanogen chloride in excellent quality and yield by dissolving the hot melt in water, extracting this solution with at least one polar, water-insoluble, organic compound, and precipitating from the purified aqueous solution the diarylguanidine by adding alkali metal hydroxide.

Abstract: Diaryl guanidines can be obtained in a high degree of purity and in high yields from the crude melt obtained from the reaction of arylamines and cyanogen chloride by dissolving the hot melt in water, extracting this solution with a mixture of at least one water insoluble, apolar hydrocarbon and at least one polar organic compound and precipitating the diaryl guanidine from the purified, aqueous solution by the addition of alkali metal hydroxide.

Abstract: 1,3-Disubstituted-guanidines, e.g., of the formula ##STR1## wherein R and R' are hydrocarbon groups which preferably are the same, e.g., 1,3-dibutyl-guanidine, 1,3-diphenyl-guanidine and 1,3-di-o-tolyl-guanidine, are highly selective ligands for sigma brain receptors and are useful in the diagnosis and treatment of hallucination associated psychotic mental illness and chronic mental depression. Tritium labeled 1,3-di-(o-tolyl)-guanidine is useful as a screening tool for compounds having selective sigma receptor binding activity, as it is displaced from isolated mammalian brain membrane to which it is bound portionately to the activity of such a compound.

Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.

Abstract: Novel substituted phenyl and benzyl nitroguanidine and phenyl and benzyl cyanoguanidine compounds. Methods for increasing crop yield, inhibiting lodging of graminaceous crops, and inducing cytokinin-like responses in crop plants with said novel guanidine compounds and derivatives thereof, as well as methods for inhibiting deterioration and/or extending the shelf life of harvested fruit, vegetables, and ornamentals are disclosed.

Abstract: A new radiopharmaceutical composition for use in nuclear medicine comprises a radioiodinated meta-iodobenzylguanidine. The composition is used as an imaging agent for the heart, adrenal medulla, and tumors of the adrenal medulla and can be used for treatment of tumors of the adrenal medulla.

Abstract: Guanidines are one of the strongest organic bases and find applications where this property is needed, such as in phase transfer catalysis in the form of their substituted derivatives. Their use, however, has been hampered by their expensive nature due to the only mediocre yields in their preparation. The present invention provides a process for the preparation of substituted guanidines in high yields.

Abstract: A compound of formula (II) or a pharmaceutically acceptable acid addition salt thereof ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents C.sub.1-6 alkyl; R.sup.5 represents hydrogen or C.sub.1-6 alkyl; R.sup.6 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.5 and R.sup.6 together represent the remaining members of a 5- or 6-membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl, carboxy or C.sub.1-6 alkoxycarbonyl; and R.sup.7 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.

Abstract: The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichY and Z, which may be the same or different, each represent oxygen, sulphur, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 is hydrogen, nitro, cyano, lower alkyl, aryl, alkylsulphonyl or arylsulphonyl;p has a value from 2 to 12;R.sub.1 represents ##STR2## in which R.sub.4 and R.sub.5 which may be the same or different, each represent hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aralkyl or lower alkyl interrupted by an oxygen atom or a group >N-R.sub.6 in which R.sub.6 represents hydrogen or lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen atom to which they are attached form a 5 to 7-membered saturated heterocyclic ring which may contain an additional oxygen atom or the group >NR.sub.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent a hydrogen atom, a chlorine atom, or a methyl group, with the proviso that not both R.sub.1 and R.sub.2 are hydrogen, andR represents a radical selected from the group consisting of --(CH.sub.2).sub.2 --C(CH.sub.3).dbd.CH.sub.2, --(CH.sub.2).sub.2 --CH.dbd.CH.sub.2, --O--CH.sub.2 --CH.dbd.CH.sub.2, --O--(CH.sub.2).sub.2 --CH.dbd.CH.sub.2, --O--CH.sub.2 --C(CH.sub.3).dbd.CH.sub.2, --O--CH.sub.2 --CH.dbd.CH--CH.sub.3, ##STR2## and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.

Abstract: Novel guanylamidines and the pharmaceutically acceptable acid addition salts thereof having activity as hypoglycemic agents are disclosed.