C07C281/16

Inhibitors of creatine transport and uses thereof
10308597 · 2019-06-04 · ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Inhibitors of creatine transport and uses thereof
10308597 · 2019-06-04 · ·

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.

Therapeutic compounds

The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia, Ib, Ic, and Id: ##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables A, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.x, L, X, Y, and Z have the meaning as described herein.

Therapeutic compounds

The invention provides methods for producing analgesia in an animal comprising administering to the animal a compound of the formula Ia, Ib, Ic, and Id: ##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables A, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.x, L, X, Y, and Z have the meaning as described herein.

Antiviral agent

The invention relates to antiviral agents and specifically to synthetic biologically-active derivatives, and can be used in the pharmaceutical industry, in medicine, in plant husbandry and in biotechnology. The antiviral agent is based on poly-N1-hydrazino(imino)methyl-1,6-hexanediamine-poly-N1-amino(imino)methyl-1,6-hexane diamine of general formula (1), ##STR00001##
where: HX is an acid, n=3-20, and m=4-20, and which is active against viruses of humans, animals, plants, bacteria and fungi, said viruses being non-enveloped and enveloped and containing RNA or DNA. The antiviral agent exhibits a broad range of effectiveness, and is active against viruses both in intracellular and extracellular locations.

Antiviral agent

The invention relates to antiviral agents and specifically to synthetic biologically-active derivatives, and can be used in the pharmaceutical industry, in medicine, in plant husbandry and in biotechnology. The antiviral agent is based on poly-N1-hydrazino(imino)methyl-1,6-hexanediamine-poly-N1-amino(imino)methyl-1,6-hexane diamine of general formula (1), ##STR00001##
where: HX is an acid, n=3-20, and m=4-20, and which is active against viruses of humans, animals, plants, bacteria and fungi, said viruses being non-enveloped and enveloped and containing RNA or DNA. The antiviral agent exhibits a broad range of effectiveness, and is active against viruses both in intracellular and extracellular locations.

COMPOUNDS AND METHODS OF TREATING INFECTIONS

The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

COMPOUNDS AND METHODS OF TREATING INFECTIONS

The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases
20180354914 · 2018-12-13 ·

The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, Cl, F or Br, R.sub.2 is H or F; R.sub.3 is selected from H and alkyl; R.sub.4 is selected from H and C(O)R.sub.6; R.sub.5 is H or R.sub.4 and R.sub.5 are linked to form a heterocyclic group which is optionally substituted with one or more R.sub.10 groups R.sub.6 is selected from R.sub.7, OR.sub.7 and NR.sub.8R.sub.6; R.sub.7R.sub.8 and R.sub.9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocycyl and aryl, each of which is optionally substituted with one or more R.sub.10 groups; each R.sub.10 is independently selected from halogen. OH, CN NO.sub.2, COO-alkyl, aralkyl, SO.sub.2-alkyl, SO.sub.2-aryl, COOH, CO-alkyl, CO-aryl, NH.sub.2, NH-alkyl, N(alkyl).sub.2, CF.sub.3, alkyl and alkoxy, X and Z are each independently CR.sub.11 and Y is selected from CR.sub.11 and N and R.sub.11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.

##STR00001##

Benzylideneguanidine Derivatives and Therapeutic Use for the Treatment of Protein Misfolding Diseases
20180354914 · 2018-12-13 ·

The present invention relates to a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, Cl, F or Br, R.sub.2 is H or F; R.sub.3 is selected from H and alkyl; R.sub.4 is selected from H and C(O)R.sub.6; R.sub.5 is H or R.sub.4 and R.sub.5 are linked to form a heterocyclic group which is optionally substituted with one or more R.sub.10 groups R.sub.6 is selected from R.sub.7, OR.sub.7 and NR.sub.8R.sub.6; R.sub.7R.sub.8 and R.sub.9 are each independently selected from alkyl, cycloalkyl, aralkyl, cycloalkenyl, heterocycyl and aryl, each of which is optionally substituted with one or more R.sub.10 groups; each R.sub.10 is independently selected from halogen. OH, CN NO.sub.2, COO-alkyl, aralkyl, SO.sub.2-alkyl, SO.sub.2-aryl, COOH, CO-alkyl, CO-aryl, NH.sub.2, NH-alkyl, N(alkyl).sub.2, CF.sub.3, alkyl and alkoxy, X and Z are each independently CR.sub.11 and Y is selected from CR.sub.11 and N and R.sub.11 is H or F; for use in treating a disorder associated with protein misfolding stress and in particular associated with accumulation of misfolded proteins.

##STR00001##