Abstract: This invention pertains to cyclic polypeptides having gastrointestinal motor stimulating activity which may be represented by formula (1): ##STR1## including optically active isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein groups A and D are linked to from a cyclic structure; and R.sub.1 is lower alkyl; R.sub.2 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is phenyl or substituted phenyl, wherein the phenyl group may be substituted with one or more substituents selected from the group consisting of halogen, hydroxy, and lower alkoxy; R.sub.5 is --OH or --NH.sub.2 ; A is selected from the group consisting of L-glutamic acid, L-aspartic acid, L-lysine, L-ornithine, and L-2,4-diaminobutyric acid; B is L-alanine or L-glutamine; C is L-arginine or D-arginine; D is selected from the group consisting of L-lysine, L-ornithine, L-2,4-diaminobutyric acid, L-glutamic acid, and L-aspartic acid; E is a direct bond between group D and group R.sub.

Abstract: This invention pertains to methods for preparing 5-aroyl-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1-carboxylic acids represented by formula (I): ##STR1## In a first embodiment, the method comprises the sequential steps of cyclizing, via a free radical ring closure reaction, and hydrolyzing a compound represented by formula (IV): ##STR2## wherein R.sub.1 is lower alkyl.

Abstract: Novel diquaternary polypeptides possessing skeletal muscle relaxation activity represented by the formulae: ##STR1## wherein: R is lower alkyl; R.sub.1 and R.sub.2 are lower alkyl or R.sub.1 and R.sub.2, together with the nitrogen to which they are attached form a heterocyclic ring having 5 to 7 member atoms; R.sub.3 is lower alkyl, [N,N-di(lower alkyl)-3-piperidinium].sup.(+), or [N,N-di(lower alkyl)-4-piperidinium].sup.(+) R.sub.4 is selected from the group consisting of t-butyl, benzyl or fluorenylmethyl; A.sub.1 is selected from the group consisting of trans-4-acetoxyproline, phenylalanine, glutamic acid-.gamma.-methyl ester, or proline; AA.sub.2 is selected from the group consisting of phenylalanine, leucine, 3-(2-naphthyl)alanine, 3-(1-naphthyl)alanine, and 3-cyclohexylalanine; AA.sub.3 is proline when R.sub.3 is [N,N-di(lower alkyl)-3-piperidinium].sup.(+) or [N,N-di(lower alkyl)-4-piperidinium].sup.(+), and is Orn(.delta.-N.sup.(+) --R--R.sub.1 --R.sub.2) or Lys(.epsilon.-N.sup.(+) --R--R.sub.1 --R.

Abstract: This invention pertains to novel substituted pyrazolyl compounds useful as intravenous anesthetics represented by the Formula: ##STR1## including geometric and optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein:one of Y and Z is nitrogen, and the other is CH;R.sub.1 is hydrogen or lower-alkyl;R.sub.2 and R.sub.3 are selected from the group consisting of hydrogen, --CHO, lower-alkylcarbonyl, lower-alkoxy carbonyl, lower-alkylaminocarbonyl, lower-alkyl, lower-alkenyl, lower-alkoxy-lower-alkenyl, lower-alkylcarbonyloxymethyl, substituted and unsubstituted heterocyclic rings, and substituted or unsubstituted aryl groups, wherein the symbol * represents a carbon atom which may be asymmetric and at least one of R.sub.2 and R.sub.3 is other than hydrogen.

Abstract: This invention pertains to polypeptides having gastrointestinal motor inhibitory activity represented by the formula: ##STR1## including optically active isomeric forms and the pharmaceutically acceptable acid addition salts thereof wherein A is the L-stereoisomer of a lipophilic aliphatic or alicyclic amino acid; B is selected from the group consisting of L and D aromatic, heteroaromatic, lipophilic aliphatic, and alicyclic amino acids; D is the L-stereoisomer of a lipophilic aliphatic or alicyclic amino acid; E is the L-stereoisomer of an aromatic, aliphatic, or alicyclic amino acid; F is the L-stereoisomer of an aromatic or heteroaromatic amino acid; G is glycine or D-alanine; H is L-glutamic acid or L-glutamine; I is L-glutamine, L-glutamic acid, or L-alanine; J is a direct bond between I and group --NH-- or is selected from the group consisting of Z, Z-Leu, Z-Leu-Gln, Z-Leu-Gln-Glu (SEQ ID NO:2), Z-Leu-Gln-Glu-Lys (SEQ ID NO:3), Zleu-Gln-Glu-Lys-Glu (SEQ ID NO:4), Z-Leu-Gln-Glu-Lys-Glu-Arg (SEQ ID NO:5),

Abstract: This invention pertains to polypeptides, other than motilin, having gastrointestinal motor stimulating activity and represented by the formula: ##STR1## wherein A and D are lipophilic aliphatic or alicyclic amino acids; B is L-proline or L-alanine; E is an aromatic, lipophilic aliphatic, or alicyclic amino acid; F is an aromatic or heteroaromatic amino acid; G is glycine or D-alanine; H is L-glutamic acid or L-glutamine; I is L-glutamine, L-glutamic acid, or L-alanine; J is a direct bond or is selected from, inter alia Z, Z-Leu, Z-Leu-Gln, Z-Leu-Gln-Glu (SEQ ID NO:2) or Z-Leu-Gln-Glu-Lys (SEQ ID NO:3), wherein Z is, inter alia, arginine, D-arginine, D-homoarginine, or D-lysine, and further wherein the amino acids represented by A, D, E and F are L-stereoisomers; R.sub.1 is lower-alkyl or allyl; R.sub.2 is hydrogen, lower-alkyl, propargyl, or allyl; R.sub.3 is hydrogen, lower-alkyl, and allyl; R.sub.

Abstract: An improved process for the production of isoflurane is disclosed. Isoflurane is formed by the exhaustive chlorination of 2,2,2-trifluoroethyl difluoromethyl ether with chlorine gas. The reaction mixture, preferably without purification or refining, is treated with UV light in the presence of isopropanol to reduce 1,1-dichloro-2,2,2-trifluoroethyl difluoromethyl ether, the other major component thereof, to isoflurane. Isoflurane is thereby obtained in yields of at least 80%.

Abstract: The present invention is directed to a method for replacing a carboxylic acid group with a fluorine .[.group.]. in a halogenated aliphatic carboxylic acid compound having the formula, R-COOH, to prepare a fluorinated product having the formula, R-F, wherein R is a halogenated aliphatic group including straight- and branched-chain aliphatic groups selected from the group consisting of halogenated aliphatic and .Iadd.halogenated .Iaddend.alkoxy-substituted .[.halogenated.]. aliphatic groups, wherein the method comprises the step of (a) reacting the halogenated aliphatic carboxylic acid compound with bromine trifluoride, and (b) recovering the fluorinated product.