Abstract:
The invention relates to the use of cyclic compounds as ligands of integrin receptors, in particular as ligands of the alpha vss3 integrin receptor. The invention also relates to the novel compounds, to the use thereof and to pharmaceutical preparations which contain said compounds. Examples of said compounds include benzazepines, benzodiazepines and thieno[3,2-b]azepines, used for treating arteriosclerosis, rheumatoid arthritis, restenosis after vessel damage or stent implantation, angioplasty, acute kidney failure, microangiopathy associated with angiogenesis, diabetic angiopathy, thrombocyte-mediated vascular occlusion, arterial thrombosis, congestive heart-failure, myocardial infarct, apoplexy, cancer, osteoporosis, hypertension, psoriasis or viral, parasitic or bacterial diseases, inflammation, wound healing, hyperparathyroidism, Paget's bone disease, malignant hypercalcemia, or metastatic osteolytic lesions.
Abstract:
The present invention relates to a crystalline form of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)-pyrimidinyl]-4-fluoro-N-[[methyl-(1-methylethyl)amino]sulphonyl]benzamide. The invention also relates to a method for preparing this crystalline form and to formulations for crop protection which comprise this crystalline form of the phenyluracil.
Abstract:
The invention relates to prodrugs of pharmacologically active, five-membered heterocyclic amidines from which in vivo compounds are obtained, these compounds being competitive inhibitors of trypsin-type serin proteases, especially thrombin and kininogenases such as kallikrein. The invention also relates to the production of these prodrugs and to their use as medicaments, to pharmaceutical compositions that contain the prodrugs of the active compounds as components, and to the use of the compounds as thrombin inhibitors, anticoagulants and anti-inflammatory agents.
Abstract:
The invention relates to prodrugs of pharmacologically active, five-membered heterocyclic amidines from which in vivo compounds are obtained, these compounds being competitive inhibitors of trypsin-type serin proteases, especially thrombin and kininogenases such as kallikrein. The invention also relates to the production of these prodrugs and to their use as medicaments, to pharmaceutical compositions that contain the prodrugs of the active compounds as components, and to the use of the compounds as thrombin inhibitors, anticoagulants and anti-inflammatory agents.
Abstract:
The invention relates to peptidic substances, to the production of said substances and to their use as complement inhibitors. In particular, the invention relates to substances with a guanidine or amidine radical as the terminal group, especially inhibitors of the complement proteases C1s and C1r.
Abstract:
The invention relates to a method for producing phenyliso(thio)cyanates of general formula (I) according to which a compound of general formula (II) or the HCl adduct thereof is reacted with a phosgenating agent, wherein W represents oxygen or sulfur and Ar and A have the meanings as cited in Claim 1. The invention also relates to the use of phenyliso(thio)cyanates for producing plant protection products.
Abstract:
Bifunctional phenyl iso(thio)cyanate derivatives (I) are new. Also new are aniline and nitrobenzene derivative intermediates (II) and (V). Bifunctional phenyl iso(thio)cyanate derivatives of formula W=C=N-Ar-CO-NH-SO 2-A (I) are new. W : O or S; Ar : phenylene (optionally substituted by one or more of halo, 1-4C haloalkyl and CN), and A : NH 2 or the residue of a primary or secondary amine. Independent claims are also included for: (a) preparation of (I); (b) new aniline and nitrobenzene derivative intermediates of formulae H 2N-Ar-CO-NH-SO 2-A (II) and O 2N-Ar-CO-NH-SO 2-A (V), and (c) preparation of 4-(sulfamidocarbonyl-phenyl)-1,2,4-triazolinedione derivatives of formula (VI) by reacting an ester of diaza-ester of formula R 4>-NH-NR 3>-C(W')OR' (VII) and cyclizing the obtained urea derivative of formula R'O-C(=W')-N(R 3>)-N(R 4>)-C(=W)-NH-Ar-CO-NH-SO 2-A (VIII). [Image] W' : O or S; R 3>, R 4> : H, CN, NH 2, 1-6C alkyl, 1-6C haloalkyl, 1-6C alkoxy, 1-6C haloalkoxy, 3-7C cycloalkyl, 2-6C alkenyl, 2-6C haloalkenyl, 3-6C alkynyl, benzyl, OR 5> or (1-3C) cyanoalkyl, or R 3> + R 4> : a group completing 4-7 membered heterocyclyl optionally interrupted by S, O, NR 6> or N and optionally substituted by one or more of halo or 1-4C alkyl; R 5> : H, 1-6C alkyl, 1-6C haloalkyl, 3-7C cycloalkyl, 2-6C alkenyl, 3-6C alkynyl, optionally substituted phenyl or optionally substituted benzyl; R 6> : H, 1-6C alkyl, 3-6C alkenyl or 3-6C alkynyl, and R' : 1-4C alkyl. ACTIVITY : Herbicide. MECHANISM OF ACTION : None given.
Abstract:
Derivados del ácido benzoico substituidos por 3-heterociclilo de la fórmula general I, (Ver fórmula) en la que las variables tienen los significados siguientes: X significa oxígeno o NR9, R1 significa un resto heterocíclico de las fórmulas generales II-A hasta II-H, (Ver fórmulas) R2 significa hidrógeno o halógeno, R3 significa halógeno o ciano, R4, R5 significan, independientemente entre sí, hidrógeno, alquilo con 1 a 4 átomos de carbono o alcoxi con 1 a 4 átomos de carbono, o R4 y R5 significan conjuntamente un grupo =CH2, R6 significa hidrógeno, alquilo con 1 a 4 átomos de carbono o alcoxi con 1 a 4 átomos de carbono, R7, R8 significan, independientemente entre sí, hidrógeno, alquilo con 1 a 6 átomos de carbono, alquenilo con 3 a 6 átomos de carbono, alquinilo con 3 a 6 átomos de carbono, halógeno-alquilo con 1 a 4 átomos de carbono, alcoxi con 1 a 4 átomos de carbono-alquilo con 1 a 4 átomos de carbono, alquiltio con 1 a 4 átomos de carbono-alquilo con 1 a 4 átomos de carbono, alquilsulfinilo con 1 a 4 átomos de carbono-alquilo con 1 a 4 átomos de carbono, alquilsulfonilo con 1 a 4 átomos de carbono-alquilo con 1 a 4 átomos de carbono, ciano-alquilo con 1 a 4 átomos de carbono, alcoxicarbonilo con 1 a 4 átomos de carbono-alquilo con 1 a 4 átomos de carbono, amino-alquilo con 1 a 4 átomos de carbono, alquilamino con 1 a 4 átomos de carbono-alquilo con 1 a 4 átomos de carbono, di(alquilo con 1 a 4 átomos de carbono)amino-alquilo con 1 a 4 átomos de carbono, aminocarbonil-alquilo con 1 a 4 átomos de carbono, (alquilamino con 1 a 4 átomos de carbono)carbonil-alquilo con 1 a 4 átomos de carbono, di(alquilo con 1 a 4 átomos de carbono)aminocarbonil-alquilo con 1 a 4 átomos de carbono, fenilo o alquilfenilo con 1 a 4 átomos de carbono o R 7 y R 8 forman junto con el átomo de nitrógeno, con el que están enlazados, un heterociclo nitrogenado saturado o insaturado con 3, con 4, con 5, con 6 o con 7 miembros, que puede contener como miembros del anillo en caso dado uno o dos heteroátomos más, elegidos entre nitrógeno, azufre y oxígeno, que puede contener 1 o 2 grupos carbonilo y/o tiocarbonilo como miembros del anillo, y/o que puede estar substituido por uno, por dos o por tres substituyentes, elegidos entre alquilo con 1 a 4 átomos de carbono y halógeno.