Abstract: The present disclosure relates to indole derivatives of the formula (I) which are cannabinoid type 1 receptor modulators and which are useful in the treatment of diseases in which modulation of the receptor is beneficial; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.

Abstract: The present disclosure relates to indole derivatives of the formula (I) which are cannabinoid type 1 receptor modulators and which are useful in the treatment of diseases in which modulation of the receptor is beneficial; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.

Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain fluoro-perhexiline compounds of the following formula (also referred to herein as FPER compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, for example, those which are known to be treated with, or known to be treatable with, perhexiline, including, for example, disorders that are ameliorated by the inhibition of carnitine palmitoyltransferase (CPT); cardiovascular disorders such as: angina pectoris; heart failure (HF); ischaemic heart disease (IHD); cardiomyopathy; cardiac dysrhythmia; stenosis of a heart valve; hypertrophic cardiomyopathy (HCM); coronary heart disease; and other disorders, for example, diabetes and cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy.

Abstract: Compounds of formula (I): wherein: A, R, T, Q, L, Z, G, X and A? are as defined in the description. B and D, equal to or different from each other, are selected between heteroaryl and aryl, wherein at least one of the hydrogen atoms of said heteroaryl and aryl are substituted with groups selected from SO3?, SO3H, COO?, COOH, and one or more of the other hydrogen atoms of said heteroaryl and aryl are optionally substituted as reported in the description.

Abstract: Compounds of formula (I): wherein: A, R, T, Q, L, Z, G, X and A? are as defined in the description. B and D, equal to or different from each other, are selected between heteroaryl and aryl, wherein at least one of the hydrogen atoms of said heteroaryl and aryl are substituted with groups selected from SO3?, SO3H, COO?, COOH, and one or more of the other hydrogen atoms of said heteroaryl and aryl are optionally substituted as reported in the description.

Abstract: Tubulysine compounds of formula (A) having a high cytotoxicity wherein: B is selected from CH2, CH2—CH2 or CH2—CH2—CH2, D is an aromatic linker, X1 is alkyl or alkenyl, X2 is selected from the X2a, substituted or non substituted, selected from: aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heterocycloalkylalkyl, or heteroarylalkyl, X2b: alkylene-O-alkyl, wherein alkylene is C2-C10, X2c: CH2—O-alkyl, X3 is selected from H, or together with X4 forms the group ?O, X4 is selected from H, halogen, OH, SH, alkyl, alkenyl, (OR5)n—OR6, OC(O)R7, NR6R7, or together with X4 forms the group ?O, R5 is an alkylene, n is zero or an integer from 1 to 10, R6 and R7, equal to or different from each other, have the following meanings: z1: H, alkyl, z2 substituted or non substituted: aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, heterocycloalkyl-alkyl, X5 is z2, or has the meaning of z3-alkyl, alkenyl, X6 is selected from NR8R9, OR8, NH—NR8R9, SR8, R10, wherein R

Abstract: Synthesis natural tubulisine derivatives of formula (A) having a high cytotoxicity wherein: B is selected from CH2, CH2—CH2 or CH2—CH2—CH2, D is an aromatic linker, X1 is alkyl or alkenyl, X2 is selected from the X2a, substituted or non substituted, selected from: aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heterocycloalkylalkyl, or heteroarylalkyl, X2b: alkylene-O-alkyl, wherein alkylene is C2-C10, X2c: CH2—O-alkyl, X3 is selected from H, or together with X4 forms the group ?O, X4 is selected from H, halogen, OH, SH, alkyl, alkenyl, (OR5)n—OR6, OC(O)R7, NR6R7, or together with X4 forms the group ?O, R5 is an alkylene, n is zero or an integer from 1 to 10, R6 and R7, equal to or different from each other, have the following meanings: z1: H, alkyl, z2 substituted or non substituted: aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, heterocycloalkylalkyl, X5 is z2, or has the meaning of z3=alkyl, alkenyl, X6 is selected from NR8R9, OR8, NH—NR8R9, SR8, R10, wh

Abstract: The present invention relates to cationic lipids capable of forming complexes with nucleic acids and the use thereof for the transfection of eukaryotic cells. The cationic lipids according to the invention have general formulas (I) and (Ia): (see formulas (I) and (Ia), wherein E is a heteroaryl; R1 and R2 are selected from H, —R7—NH2, alkyl; R7 is selected from alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R3 and R4 are selected from: H, —R8—SH, R8—NH—NH2/—R8—CO—R9 or —R8—NH2; R8 is selected from: alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R9 is selected from: H, alkyl; R5 and R6 are selected from: H, alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl.

Abstract: The present invention relates to cationic lipids capable of forming complexes with nucleic acids and the use thereof for the transfection of eukaryotic cells. The cationic lipids according to the invention have general formulas (I) and (Ia): (see formulas (I) and (Ia), wherein E is a heteroaryl; R1 and R2 are selected from H, —R7-NH2, aklyl; R7 is selected from alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R3 and R4 are selected from: H, —R8-SH, R8-NH—NH2/—R8-CO—R9 or —R8-NH2; R8 is selected from: alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R9 is selected from: H, alkyl; R5 and R6 are selected from: H, alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl.

Abstract: The invention concerns quinuclidine derivatives of formula I or II wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention show high affinities for m3 and/or m2 muscarinic receptors and are particularly suited for treating urinary incontinence.