Kali-chemie Pharma Gmbh

Kali-chemie Aktiengesellschaft

Kali-chemic Pharma Gmbh

Peter W Thies

Samuel David

Akiji Asai

Insa Hell

Gerd Buschmann

Ivan Ban

Ulrich G Kuehl

Hartmut Hauth

Dietmar Roemer

Klaus-Ulrich Wolf

Samuell David

Klau U Wolf

Peter Flecker

The use of valepotriate hydrins in the prevention and treatment of disorders of the gastrointestinal tract is described, together with pharmaceutical compositions containing valepotriate hydrins and certain novel valepotriate hydrins per se.

Novel valepotriate hydrin containing medicines

Valepotriate hydrin containing medicines used to treat uclers and

N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine compounds corresponding to the formula ##STR1## with blood-pressure lowering effects, a method of producing such compounds and pharmaceutical compositions incorporating such compounds, wherein R.sub.1 is hydrogen, a benzyl or lower alkyl group; R.sub.2 is a lower alkyl or lower alkanoyl group; R.sub.3 is hydrogen or a lower alkyl group; R.sub.4 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; R.sub.5 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; and A and B either are both hydrogen or together represent a bond between their respective carbons.

N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine

2,6-Dioxa-bicyclo-[2,2,2]-octane-7-yl-acetaldehydes of the general Formula I, ##STR1## wherein R.sub.1 is a benzyl or lower alkyl group, and A and B either are each hydrogen or together represent a single bond between their respective carbons, and a method for producing such compounds. The compounds are valuable intermediates in the synthesis of pharmacologically active substances having, for example, cardiovascular effects.

2,6-Dioxa-bicyclo-[2,2,2]-octane-7-yl-acetaldehydes

Novel and highly effective sleep inducing 3.beta.-hydroxy methyl-4.alpha.-hydroxy-8.beta.-alkoxy-2,9-dioxa tricyclo [4,3,1,0.sup.3,7 ] decane compounds of the following Formula: ##STR1## in which R.sub.1 indicates an alkoxy group and preferably a lower alkoxy group, such as the methoxy group, the ethoxy group, or the n-butoxy group, while

2,9-Dioxa tricyclo [4,3,1,0.sup.3,7 ] decane compounds and process of

Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes and the process for their production and the production of various intermediates are disclosed. Pharmaceutical compositions containing an effective amount of the novel compounds and a pharmaceutically acceptable carrier are also disclosed.

Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes

New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group

2,9-Dioxatricyclo [4,3,1,0.sup.3,7 ] decane derivatives and

New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group one of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygen one of R.sub.4 and R.sub.5 is hydrogen and the other represents alkyloxy or aralkyloxy y and y' each represent hydrogen or jointly form a bond and their pharmacologically acceptable salts, as well as pharmaceutical formulations thereof.

2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives and pharmaceutical

Novel cyclopentapyran esters are produced from specific plants of the genus Valeriana, i.e. from Valeriana mexicana or Valeriana toluccana. Said esters have a high tranquilizing and sedative effect which is superior to that of known cyclopentapyran esters produced from Valeriana officinales and the like Valeriana species.

Cyclopentapyrans

Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ]decanes and the process for their production and the production of various intermediates are disclosed. Pharmaceutical compositions containing an effective amount of the novel compounds and a pharmaceutically acceptable carrier are also disclosed.

Pharmaceutically active 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ]decanes

A process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives is disclosed, wherein a 10-methylen-3-iodomethyl compound of the formula ##STR1## is hydrogenated to obtain a mixture of the corresponding epimeric 10.beta.- and 10.alpha.-methyl-3-iodomethyl compounds, the pure 10.alpha.- and 10.beta.-methyl epimers are separated and recovered from this mixture and are reacted with a secondary amine. Optionally, the substituent in the 4-position of the resulting 10.alpha.- or 10.beta.-methyl-3-aminomethyl compounds are further changed.

Process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ]

New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group ONE OF R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygen

2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives and

3-Azidomethyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which exhibit analgesic, as well as antipyretic and antiphlogistic properties, and which have the formula (I) ##STR1## wherein: R.sub.1 represents alkyloxy or aralkyloxy; One of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy, acyloxy or carbamyloxy, or R.sub.2 and R.sub.3 jointly represent oxygen; and, Y and y' each represent hydrogen or jointly form a bond, As well as pharmaceutical formulations thereof. By reducing the 3-azidomethyl compounds of formula (I), the corresponding 3-aminomethyl compounds are obtained which possess sedative properties and which are valuable intermediates for preparing 3-(mono- or dialkylaminomethyl)-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes which exhibit sedative and soporific activities.

2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives, processes for

4-amino-3-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives are disclosed which exhibit analgesic properties, and which have the formula (I) ##STR1## wherein ONE OF R.sub.1 and R.sub.2 represents hydrogen and the other represents an amino group which is substituted by an arylalkyl group or an arylalkenyl group,

2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives, processes for

3-AZIDOMETHYL-2,9-DIOXATRICYCLO[4,3,1,0.sup.3,7 ] DECANE DERIVATIVES ARE DISCLOSED WHICH EXHIBIT ANALGESIC, AS WELL AS ANTIPYRETIC AND ANTIPHLOGISTIC PROPERTIES, AND WHICH HAVE THE FORMULA (I) ##STR1## wherein: R.sub.1 represents alkyloxy or aralkyloxy;

Growing community of inventors

Hanover, Germany

Peter W Thies