The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.

Brigham &amp; Women's Hospital

S-nitroso derivatives of hydrazinoacetic acids, 1-[(acylthio and (mercapto)-1-oxoalkyl]-1,2,34-Tetrahydroquinoline-2-carboxylic acids and alanyl prolines and isoquinolines

A compound represented by formula (1) (in the formula: ring-D represents a three- to eight-membered hydrocarbon ring; R.sup.a represents an optionally substituted amino C.sub.1-6 alkyl group or the like; R.sup.b1 and R.sup.b2 each independently represent a hydrogen atom, a halogen atom, or the like; R.sup.c represents an optionally substituted C.sub.6-10 aryl group or the like; R.sup.d represents a hydrogen atom or the like; and ring-Q represents a (hetero)aryl group or the like which may be substituted with a carboxyl group or the like) or a pharmaceutically acceptable salt thereof exhibits an excellent FXIa inhibitory activity, and is useful as a therapeutic agent against thrombosis or the like. ##STR00001##

SUMITOMO DAINIPPON PHARMA CO., LTD.

1-(cycloalkyl-carbonyl)proline derivative

A hexapeptide represented by formula (II):where A represents an L- or D- form of arginine or lysine whose N-terminal amino group is alkylated or acylated, B represents an L- or D- form of argine, lysine, or histidine, Pro represents an L- or D- form of proline, C represents an L- or D- form of tyrosine, tryptophan, or phenylalanine, D represents an L- or D- form of valine, isolencine, or leucine, and E represents an L-or D- form of valine, isolencine, or lencine, one of the hydrogen atoms of the amino group of which may be substituted a C.sub.1 to C.sub.4 alkyl group, and C-terminal carboxyl group of which is substituted with --COOR*, --CH.sub.2 OR, or --CONHR wherein R* represents a C.sub.1 to C.sub.4 alkyl group, and R represents a hydrogen atom or an C.sub.1 to C.sub.4 alkyl group. The hexapeptide or a pharmaceutically acceptable salt of the hexapeptide is useful as medical agent such as an anti-edematous agent, an anti-shock agent, an anti-thrombus agent, an anti-arteriosclerotic agent, an anti-allergic agent, a hypotensive agent, a wound healing agent, and an anti-inflammatory agent.

Tsumura &amp; Co.

Neurotensin Hexapeptides

A human prourokinase-like polypeptide having the following amino acid sequence:wherein Met is an occasionally present methionine, Ser is the first N-terminal serine, X is the 156th arginine or other amino acid, Y is the 157th proline, glycine, alanine or valine, Z is the 158th lysine or arginine, and the solid lines represent the same amino acid sequences as corresponding parts of an amino acid sequence of a natural type human prourokinase or a human prourokinase-like polypeptide wherein the 135th lysine is changed to an amino acid other than a basic amino acid, or substantially the same amino acid sequence as the above-mentioned amino acid sequence, is provided.Moreover, a DNA segment coding for the above-mentioned polypeptide; a plasmid containing the DNA segment; E. coli transformed with the plasmid; a process for production of the polypeptide characterized by culturing the E. coli; a pharmaceutical preparation containing the polypeptide; use of the polypeptide for prophylaxis or treatment of thrombus formation; and use of the polypeptide for the production of pharmaceutical preparation used for that purpose.

thrombosis/proline

S-nitroso derivatives of hydrazinoacetic acids, 1-[(acylthio and (mercapto)-1-oxoalkyl]-1,2,34-Tetrahydroquinoline-2-carboxylic acids and alanyl prolines and isoquinolines

1-(cycloalkyl-carbonyl)proline derivative

Neurotensin Hexapeptides

Rapidly acting prourokinase

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