Patents Assigned to Gruppo Lepetit S.p.A.
  • Patent number: 4500525
    Abstract: The present invention is directed to new pyrazolo/4,3-c/pyridines, the process for their preparation, the pharmaceutical compositions containing them and their use as pharmocologically active substances. The compounds of the invention possess cardiotonic, antihypertensive, CNS depressant, neuroleptic, and analgesic activity.
    Type: Grant
    Filed: February 15, 1983
    Date of Patent: February 19, 1985
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Giorgio Winters, Alberto Sala, Domenico Barone
  • Patent number: 4496743
    Abstract: This invention relates to 1-[(2-acylthiocycloalkyl)carbonyl]-L-proline derivatives which are useful as antihypertensive agents and to a process for their preparation.
    Type: Grant
    Filed: January 26, 1983
    Date of Patent: January 29, 1985
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Romeo Ciabatti, Giovanna Padova
  • Patent number: 4487721
    Abstract: The present invention is directed to a process for producing 2-amino-2-arylacetonitriles of general formula I: ##STR1## wherein R and R.sup.1 independently represent hydrogen, hydroxy, hydroxy(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.6)alkyl, 2-furyl, 2-thienyl, 4-pyridinyl, 1-pyrrolydinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl, 4-phenylpiperazinyl, or phenyl which can optionally be substituted with from 1 to 3 substituents independently selected from (C.sub.1 -C.sub.4)alkyl and (C.sub.1 -C.sub.4)alkoxy, or R and R.sup.1 independently represent a phenyl(C.sub.1 -C.sub.4)alkyl or a phenyl(C.sub.1 -C.sub.4)alkoxy group wherein the phenyl group can be either unsubstituted or substituted as above.An arylaldehyde derivative of formula II ##STR2## is reacted with chloroform in base and in the presence of ammonia to give the 2-amino-2-arylacetonitrile derivative.
    Type: Grant
    Filed: June 7, 1983
    Date of Patent: December 11, 1984
    Assignee: Gruppo Lepetit S.p.A.
    Inventor: Romeo Ciabatti
  • Patent number: 4476111
    Abstract: A new antibiotic, designated S/433, is disclosed which is produced in a microbiological fermentation under controlled conditions using a new strain of Streptomyces. This new antibiotic is active against gram-positive and gram-negative bacteria and is also active in inhibiting the growth of transplanted tumors.
    Type: Grant
    Filed: October 19, 1981
    Date of Patent: October 9, 1984
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Carolina Coronelli, Angelo Borghi, Giorgio Pirali, Giovanni Mistrello
  • Patent number: 4461894
    Abstract: Naphth[1,2-d]imidazoles and naphth[2,1-d]oxazoles of formula ##STR1## wherein R and R.sub.1 are hydrogen, halogen, alkyl or alkoxy, R.sub.2 is hydrogen or halogen and A is one of the following moieties ##STR2## wherein R.sub.3 is alkyl, cycloalkyl, or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group in which n is 1, 2 or 3, R.sub.5 is hydrogen or alkyl, R.sub.6 is alkyl or R.sub.5 and R.sub.6 taken together with the adjacent nitrogen atom are a 4- to 7-membered saturated hetero ring which may contain a further hetero atom and optionally may be substituted, e.g., with phenyl or substituted phenyl, R.sub.4 is hydrogen, alkyl, cycloalkyl or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group, provided that one of R.sub.3 and R.sub.4 is a --(CH.sub.2).sub.n --NR.sub.5 R.sub.6 group, and R.sub.7 is --(CH.sub.2).sub.n --NR.sub.5 R.sub.6, or a pharmaceutically-acceptable acid addition salt thereof. They are made by contacting a corresponding naphth[1,2-d]imidazole or a naphth[2,1-d]oxazole wherein one of R.sub.3 and R.sub.
    Type: Grant
    Filed: April 26, 1982
    Date of Patent: July 24, 1984
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Amedeo Omodei-Sale, Emilio Toia
  • Patent number: 4459302
    Abstract: New acyl-1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy;a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.
    Type: Grant
    Filed: October 23, 1979
    Date of Patent: July 10, 1984
    Assignee: Gruppo Lepetit, S.p.A.
    Inventors: Amedeo Omodei-Sale, Pietro Consonni, Giulio Galliani
  • Patent number: 4440764
    Abstract: Water-soluble esters of steroid-oxazole derivatives of formula I ##STR1## wherein R is O or a H, (.beta.-OH) group, R.sub.1 is hydrogen, lower alkyl or phenyl, X is hydrogen, fluorine or chlorine, A stands for a direct carbon-carbon bond or a hydrocarbon chain containing from 1 to 4 carbon atoms, and M is hydrogen or a pharmaceutically acceptable cation are described as well as pharmaceutical compositions containing them particularly suitable for parenteral administration.
    Type: Grant
    Filed: April 27, 1981
    Date of Patent: April 3, 1984
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Giangiacomo Nathansohn, Giorgio Winters
  • Patent number: 4435417
    Abstract: 3H-naphtho[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for (C.sub.1-6)alkyl, (C.sub.3-6)alkenyl, (C.sub.3-6)alkynyl or (C.sub.3-7)cycloalkyl, R.sub.1 and R.sub.2, each independently may represent hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkylthio, (C.sub.1-4)alkoxy or halo(C.sub.1-4)alkoxy, R.sub.3 stands for hydrogen, hydroxy, methoxy, ethoxy, or mono- or di-methylamino, and R.sub.4 represents hydrogen or (C.sub.1-4)alkyl.Also described and claimed are their use as antiinflammatory agents and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 24, 1982
    Date of Patent: March 6, 1984
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Emilio Toja, Amedeo Omodei-Sale', Domenica Selva
  • Patent number: 4427656
    Abstract: The present invention refers to a chlorine containing antibiotic substance, named antibiotic A/16686 factor A.sub.2, in an essentially pure form. The invention also relates to the process for the production of antibiotic A/16686 factors A.sub.2 by cultivation of an Actinoplanes strain and to the co-produced antibiotic A/16686 factos A.sub.1 and A.sub.3. Antibiotic A/16686 factors A.sub.1, A.sub.2 and A.sub.3 as well as the corresponding non-toxic physiologically acceptable acid addition salts are antimicrobial agents particularly active against gram-positive bacteria.
    Type: Grant
    Filed: July 31, 1981
    Date of Patent: January 24, 1984
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Bruno Cavalleri, Enrico Selva
  • Patent number: 4412953
    Abstract: A process for preparing 16.alpha.-hydroxy-17.alpha.-aminopregnane derivatives through the opening of the corresponding 16.alpha., 17.alpha.-epoxides with amines.The use of the thus obtained compounds as intermediates in the synthesis of pharmacologically active pregnano-[17.alpha.,16.alpha.-d]oxazolines is also claimed.
    Type: Grant
    Filed: November 18, 1981
    Date of Patent: November 1, 1983
    Assignee: Gruppo Lepetit, S.p.A.
    Inventor: Giorgio Winters
  • Patent number: 4411907
    Abstract: 3H-naphth[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for hydrogen, methyl or ethyl, R.sub.1 represents hydrogen, methyl or ethyl, R.sub.2 represents hydrogen, methyl, ethyl, phenyl or substituted phenyl, the symbol R.sub.3 stands for a phenyl radical optionally substituted and R.sub.4 and R.sub.5, each independently, may represent hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkoxy or halo-(C.sub.1 -C.sub.4)alkoxy, are described. Also described is the process for preparing the novel compounds, their use as antiinflammatory agents and the pharmaceutical compositions containing them.
    Type: Grant
    Filed: May 22, 1981
    Date of Patent: October 25, 1983
    Assignee: Gruppo Lepetit, S.p.A.
    Inventor: Emilio Toia
  • Patent number: 4409388
    Abstract: Novel 1,2,4-triazole derivatives are described having the following formula ##STR1## wherein R represents hydrogen or methyl, R.sub.1 stands for hydrogen or (C.sub.1 -C.sub.4)alkyl, or R and R.sub.1 taken together may represent a further bond between the carbon atom and the oxygen atom, R.sub.2 and R.sub.4, each independently, represent hydrogen, chloro, fluoro, bromo, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, R.sub.3 stands for (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, chloro, fluoro, bromo or dimethylamino or R.sub.3 and R.sub.4 taken together may represent a methylenedioxy group.Also described is a process for their manufacture.Use of the novel compounds as antireproductive agents and pharmaceutical compositions containing them as active ingredients are also claimed.
    Type: Grant
    Filed: October 23, 1979
    Date of Patent: October 11, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Amedeo Omodei-Sale', Pietro Consonni, Giulio Galliani
  • Patent number: 4402970
    Abstract: 1,7-Dihydro-pyrrolo[3,4-e][1,4]diazepin-2(1H)-ones of the formula ##STR1## wherein R is lower alkyl, R.sub.1 stands for hydrogen, methyl, ethyl or phenyl, R.sub.2 is hydrogen or lower alkyl and R.sub.3 is hydrogen, chloro, fluoro, bromo, trifluoromethyl or methoxy are described with anticonvulsant and anti-anxiety activity.Also described is the process for preparing the above compounds and pharmaceutical preparations containing them.
    Type: Grant
    Filed: May 24, 1982
    Date of Patent: September 6, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Luigi Mariani, Giorgio Tarzia
  • Patent number: 4391817
    Abstract: A new class of pyrrolo-diazepines with anticonvulsant and anti-anxiety activity of the general formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl, R.sub.1 is chloro, bromo or nitro, R.sub.2 is hydrogen or (C.sub.1 -C.sub.4)alkyl and R.sub.3 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or methoxy. The new compounds are prepared starting from the corresponding compounds wherein R.sub.1 is hydrogen through halogenation or nitration. Pharmaceutical preparations containing the new compounds of formula I are also described.
    Type: Grant
    Filed: May 24, 1982
    Date of Patent: July 5, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Luigi Mariani, Giorgio Tarzia
  • Patent number: 4385179
    Abstract: The present invention refers to a new process for preparing N-2,3,4,5-substituted-1H-pyrrol-1-yl)-6-substituted amino-3-pyridazineamine, known as antihypertensive agents. The process is characterized in that a suitable 3,6-dihalogenopyridazine is reacted with hydrazine hydrate or other hydrazine derivatives of formula NH.sub.2 NHR, the obtained compound is reacted with a suitable dicarbonyl compound yielding first an alcandione-bis-[6-halogen-3-pyridazininyl]hydrazone, and then a 6-halogen-3-pyrrolylpyridazineamine derivative which is in turn reacted with an amine to yield the desired compounds.
    Type: Grant
    Filed: December 18, 1981
    Date of Patent: May 24, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventor: Elvio Bellasio
  • Patent number: 4385062
    Abstract: 1-[(2-Mercaptocycloalkyl)carbonyl]-L-proline derivatives of the formula ##STR1## wherein R, R.sup.1, and R.sup.2, each independently, represent hydrogen or a (C.sub.1 -C.sub.4)alkyl radical, n represents the integer 1, 2, 3, 4, or 5, and, in each of the n (CR'.sub.2) groups, R' represents hydrogen or (C.sub.1 -C.sub.4)alkyl, are described as well as the process for their manufacture, the intermediates for their synthesis and their use as antihypertensive agents.
    Type: Grant
    Filed: March 3, 1981
    Date of Patent: May 24, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Romeo Ciabatti, Giovanna Padova
  • Patent number: 4379155
    Abstract: New 3,5-disubstituted 1H-1,2,4-triazoles of formula I ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, fluoro, chloro and dimethylamino;R.sub.1 represents a (C.sub.1-4)alkyl group;R.sub.2 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl, methoxy and ethoxy;R.sub.3 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R and R.sub.3 taken together represent a methylenedioxy group; with the proviso that, when R, R.sub.2 and R.sub.3 simultaneously represent hydrogen, R.sub.1 cannot be methyl;with the further proviso that, when R.sub.2 and one of R and R.sub.3 simultaneously represent hydrogen, R.sub.1 and the other of R and R.sub.3 cannot simultaneously represent methyl; and with the still further proviso that compounds of formula I are excluded wherein R.sub.2 is hydrogen and one of R and R.sub.3 is simultaneously a 2-positioned alkyl group and the other of R and R.sub.
    Type: Grant
    Filed: July 17, 1981
    Date of Patent: April 5, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Amedeo Omodei-Sale, Pietro Consonni, Giulio Galliani, Leonard J. Lerner
  • Patent number: 4370336
    Abstract: New 3,5-disubstituted-1H-1,2,4-triazoles of formula ##STR1## wherein: R is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, fluoro, chloro and dimethylamino;R.sub.1 represents a (C.sub.1-4)alkyl group;R.sub.2 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl, methoxy and ethoxy;R.sub.3 is selected from hydrogen, fluoro, chloro, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R and R.sub.3 taken together represent a methylenedioxy group; with the proviso that, when simultaneously R, R.sub.2 and R.sub.3 represent hydrogen,cannot be methyl;with the further proviso that, when simultaneously R.sub.2 and one of R and R.sub.3 represent hydrogen, R.sub.1 and the other of R and R.sub.3 cannot simultaneously represent methyl;and salts therewith of pharmaceutically acceptable acids.The compounds possess anti-reproductive utility.
    Type: Grant
    Filed: April 16, 1981
    Date of Patent: January 25, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Amedeo Omodei-Sale, Pietro Consonni, Giulio Galliani, Leonard Lerner
  • Patent number: 4370337
    Abstract: Novel 1,2,4-triazole derivatives are described having the following formula ##STR1## wherein R represents hydrogen or methyl, R.sub.1 stands for hydrogen or (C.sub.1 -C.sub.4)alkyl, or R and R.sub.1 taken together may represent a further bond between the carbon atom and the oxygen atom, R.sub.2 and R.sub.4, each independently, represent hydrogen, chloro, fluoro, bromo, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, R.sub.3 stands for (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, chloro, fluoro, bromo or dimethylamino or R.sub.3 and R.sub.4 taken together may represent a methylenedioxy group.Also described is a process for their manufacture. Use of the novel compounds as antireproductive agents and pharmaceutical compositions containing them as active ingredient are also claimed.
    Type: Grant
    Filed: July 16, 1980
    Date of Patent: January 25, 1983
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Amedeo Omodei-Sale', Pietro Consonni, Giulio Galliani
  • Patent number: 4360674
    Abstract: Naphth[1,2-d]imidazoles and naphth[2,1-d]oxazoles of formula ##STR1## wherein R and R.sub.1 are hydrogen, halogen, alkyl or alkoxy, R.sub.2 is hydrogen or halogen and A is one of the following moieties ##STR2## wherein R.sub.3 is alkyl, cycloalkyl, or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group in which n is 1,2 or 3, R.sub.5 is hydrogen or alkyl, R.sub.6 is alkyl or R.sub.5 and R.sub.6 taken together with the adjacent nitrogen atom are a 4- to 7-membered saturated hetero ring which may contain a further hetero atom and optionally may be substituted, e.g., with phenyl or substituted phenyl, R.sub.4 is hydrogen, alkyl, cycloalkyl or a --(CH.sub.2).sub.n NR.sub.5 R.sub.6 group, provided that one of R.sub.3 and R.sub.4 is a --(CH.sub.2).sub.n --NR.sub.5 R.sub.6 group, and R.sub.7 is --(CH.sub.2).sub.n --NR.sub.5 R.sub.6, or a pharmaceutically-acceptable acid addition salt thereof. They are made by contacting a corresponding naphth[1,2-d]imidazole or a naphth[2,1-d]oxazole wherein one of R.sub.3 and R.sub.4 or R.
    Type: Grant
    Filed: January 30, 1981
    Date of Patent: November 23, 1982
    Assignee: Gruppo Lepetit S.p.A.
    Inventors: Amedeo Omodei-Sale, Emilio Toia