Abstract: The present invention relates to compounds of formula (I) and (II) and pharmaceutically acceptable salts thereof. The compounds of formula (I) or (II) possess utility as cytochrome P450 monooxygenase 11A1 (CYP11A1) inhibitors. The compounds are useful as medicaments in the treatment of steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer.

Abstract: Compounds of formula I, wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2, or 3 N, O, or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.

Abstract: Compounds of formula I, wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2, or 3 N, O, or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.

Abstract: Compounds of formula I, wherein Ra and Rb are as defined in the claims, exhibit alpha2C antagonistic activity and are thus useful as alpha2C antagonists.

Abstract: Compounds of formula I, wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2, or 3 N, O, or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.

Abstract: The use of specified compounds for the manufacture of a medicament for therapeutically neutralising an organoboronate drug. The specified compounds are typically hydroxy fatty acids or hydroperoxy fatty acids, for example 9(S)-HODE, 8(S)-HETRE or 8(S)-HEPE, or their salts or prodrugs. The organoboronate drug may be TRI 50c or a salt or prodrug thereof. Also disclosed are intravenous formulations containing the specified compounds.

Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.

Abstract: A thrombin inhibitor selected from boronic acids of formula (I), and salts, prodrugs and prodrug salts thereof: wherein X is H (to form NH2) or an amino-protecting group; aa1 is an amino acid residue having a side chain selected from formula (A) and (B)—(CO)a—(CH2)b-Dc-(CH2)d-E (A), —(CO)a—(CH2)b-Dc-Ce(E1)(E2)(E3) wherein E1, E2 and E3 are 5-6 membered saturated or unsaturated hydrocarbyl rings, or one of E1, E2 and E3 is hydrogen and the other two are a said hydrocarbyl ring, E, E1, E2 and E3 optionally being halogenated when saturated and mandatorily being halogenated when unsaturated, a particular halogen being fluorine; aa2 is a residue of an amino acid which binds to the thrombin S2 subsite; and R9 is a straight chain alkyl group interrupted by one or more ether linkages or R9 is —(CH2)mW and W is —OH or halogen.

Abstract: A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1–C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1–C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1–C6 alkoxy, C1–C6 alkyl, SR10 and N(R12)2; Q is C1–C6 alkylene which is unsubstituted or substituted by (i) C1–C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not ? to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1–C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attach

Abstract: The use of specified compounds for the manufacture of a medicament for therapeutically neutralising an organoboronate drug. The specified compounds are typically hydroxy fatty acids or hydroperoxy fatty acids, for example 9(S)-HODE, 8(S)-HETRE or 8(S)-HEPE, or their salts or prodrugs. The organoboronate drug may be TRI 50c or a salt or prodrug thereof. Also disclosed are intravenous formulations containing the specified compounds.

Abstract: A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1-C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1-C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R2)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, SR10 and N(R12)2; Q is C1-C6 alkylene which is unsubstituted or substituted by (i) C1-C6 alkyl which is unsubstituted or substituted, (II) hydroxy, provided that the hydroxy group is not ? to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1-C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are atta

Abstract: A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1-C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1-C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2(R11), SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, SR10 and N(R12)2; Q is C1-C6 alkylene which is unsubstituted or substituted by (i) C1-C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not, to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R1 and R9, which are the same or different, are each hydrogen or C1-C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are a

Abstract: Described are antibacterial agents of formula (I): X is O, S or N--R.sub.8 ; R.sub.1, R.sub.2, R.sub.3 and R.sub.8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, R heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, CO.sub.2 R, COR, CON(R).sub.2, CON(R").sub.2, SR, SON, SCO.sub.2 R or SCON(R).sub.2 ; R.sub.4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, NO.sub.2, N(R).sub.2, NRCOR, NRCOR", COR, CO.sub.2 R, CON(R).sub.2, CON(R").sub.2, NRCON(R).sub.

Abstract: The subject invention concerns a process for preparing a single enantiomer, either R or S, of R'--NH--(CH.sub.2).sub.3 --C(Ar)(CN)--R. The process is particularly useful for preparing verapamil, and analogues thereof, in single enantiomeric form.