Abstract: Substituted phenoxy-aminopropanols of the formula ##STR1## wherein R is a branched-chain alkyl of 3 or 4 carbon atoms, R.sup.1 is hydrogen, halogen or lower alkyl and R.sup.2 and R.sup.3, independently, are hydrogen, halogen, lower alkyl, lower alkoxy or lower alkylthio, and pharmaceutically acceptable acid addition salts thereof, are described. A process for their preparation, as well as pharmaceutical preparations containing them are also described. The compounds of formula I and their salts possess cardioselective .beta.-adrenergic blocking activity and antihypertensive activity.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 lower alkoxy groups, or 1 to 3 halogens; R.sub.2 is hydroxy or lower alkanoyloxy; R.sub.3 and R.sub.4 are each independently lower alkyl or together form a pyrrolidine or piperidine ring; and n is 2 to 4, and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I are active as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.

Abstract: A process for the manufacture of intermediates in the synthesis of biotin as well as of biotin itself is described. In this process the side chain is attached to the ring system by means of a Grignard reaction, the resulting compound is then dehydrated and subsequently reduced.

Abstract: Tricyclic imidazole derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is lower alkyl and the other is hydrogen or lower alkyl, R.sup.2 is lower alkyl, n is the number 0 or 1, A is ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each is lower alkyl and R.sup.8 is hydrogen or lower alkyl, and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increased gastric acid secretion.

Abstract: 1.alpha.,25-Dihydroxy-24R-fluorocholecalciferol and 1.alpha.,25-dihydroxy-24S-fluorocholecalciferol, analogs of 1.alpha.,25-dihydroxy-cholecalciferol which is physiologically the most active metabolite of vitamin D.sub.3, are synthesized in a multistep process from the known substance 1.alpha.,3.beta.-dihydroxyandrost-5-en-17-one. The new analogs are characterized by the ability to increase intestinal calcium transport, increase serum calcium and phosphate concentrations and to increase the deposition of these minerals in bones. These compounds will find a ready application as substitutes for natural 1.alpha.,25-dihydroxycholecalciferol in the treatment of disease states characterized by metabolic calcium and phosphate deficiencies.

Abstract: The present invention relates to the method of treating disease states characterized by higher than normal levels of endogenously produced 1.alpha.,25 dihydroxy-cholecalciferol or conditions where there is an increased sensitivity to 1.alpha., 25 dihydroxy-cholecalciferol by administering to an organism suffering from such a disease state a pharmaceutically effective amount of the R or S epimer of 1.alpha.,25,26 trihydroxy-cholecalciferol.

Abstract: Naphthalenyloxy carboxylic acids of the formula ##STR1## wherein X, R, m and n are as hereinafter set forth, are described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.

Abstract: Novel hexafluoro-cholecalciferol compounds and processes for preparing such compounds are disclosed. Intermediates utilized in the preparation of such compounds and pharmaceutical preparations containing these compounds are also disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each individually is hydrogen, or lower alkyl and R.sup.4 is hydroxy, lower alkoxy, aryl-(lower alkoxy), amino, mono(lower alkyl)amino or di(lower alkyl) amino,and pharmaceutically acceptable salts thereof which are useful in the treatment of degenerative joint diseases and of Wilson's disease are described.

Abstract: The syntheses of 25,26-dehydro-1.alpha.,23S-dihydroxycholecalciferol, 25,26-dehydro-1.alpha.,23R-dihydroxycholecalciferol, and the epimeric mixture thereof which are useful as differentiation inducing agents and anti-proliferation agents are described, 25,26-dehydro-1.alpha.,23S-dihydroxycholecalciferol 25,26-dehydro-1.alpha.,23R-dihydroxycholecalciferol and the epimeric mixture thereof are useful for treating tumors and leukemia, and osteoporosis.

Abstract: The present invention relates to a method of preventing milk fever which comprises administering to a preparturient female ruminant an effective amount of 24,24-difluoro-1.alpha.,25-dihydroxycholecalciferol.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, hydroxy, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, di-(C.sub.1 -C.sub.7) alkyl-N(CH.sub.2).sub.n O-- or 2-hydroxyethoxy; n is 2 to 7; R.sub.2 is hydrogen, lower alkyl or lower alkoxy; R.sub.3 is hydrogen or methyl; R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen or lower alkyl provided however if R.sub.2 is other than hydrogen R.sub.5 is hydrogen; m is 1 to 7; Y is ##STR2## --O-- or --S--; w is zero or one; and A is an unsubstituted or substituted aromatic 5- or 6-membered heterocyclic radical;or pharmaceutically acceptable addition salts thereof are described. The compounds of formula I are useful for treating allergic conditions and vascular disorders.

Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 to 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.

Abstract: A method of treating inflammation which comprises topically administering to the affected area a compound of the formula ##STR1## or a pharmaceutically acceptable addition salt thereof, is described.

Abstract: The syntheses of 25,26-dehydro-1.alpha.,24R-dihydroxycholecalciferol and 25,26-dehydro-1.alpha.,24S-dihydroxycholecalciferol and the epimeric mixture which are useful as differentiation inducing agent and anti-proliferation agents are described. 25,26-dehydro-1.alpha.,24R-dihydroxycholecalciferol, 25,26-dehydro-1.alpha.,24S-dihydroxycholecalciferol, and the epimeric mixture are useful in treating osteoporosis, tumors and leukemia.

Abstract: The pyrimidine derivatives of formula I ##STR1## wherein R.sup.1 is naphthyl, substituted naphthyl or substituted phenyl; R.sup.2 is hydrogen or lower alkoxy; and A is an optionally present ethylene or 1,3-propylene, and wherein the diaminopyridine group has the exo-configuration when A is present,are described. These compounds are useful as antibacterial agents, antimalarial agents and antitumor agents, and can be used in combination with sulfonamides in the control of bacterial infections.

Abstract: Imidazole derivatives of the formula ##STR1## wherein X is hydrogen or C.sub.1-4 -n-alkyl and Y is thienyl, optionally substituted by methyl or fluorine, or a group of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen, methyl, fluorine, hydroxy or methoxy, or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy, or one of R.sup.1, R.sup.2 and R.sup.3 is mono- or di-(C.sub.1-4 -n-alkyl)-amino and the other two are hydrogen, and physiologically compatible or pharmaceutically acceptable acid addition salts thereof, are described. These compounds of formula I inhibit the aggregation of the blood platelets.

Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.

Abstract: Pyrido[2,1-b]quinazoline derivatives of the formulas ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as hereinafter set forth, are described. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions as well as for the treatment of vascular disorders involving thrombosis.

Abstract: Naphthalenyloxy carboxylic acids of the formula ##STR1## wherein X, R, m and n are as hereinafter set forth, are described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.