Abstract: In a process for urea production of the type comprising the reaction between ammonia and carbon dioxide in a high-pressure reactor followed by an autothermal stripping of the resulting reaction mixture so as to obtain a gaseous flow comprising ammonia and carbon dioxide and a liquid flow comprising urea and residual carbamate in aqueous solution and by a stripping of said gaseous flow in units operating at medium pressure, a gaseous flow coming from said units operating at medium pressure and comprising ammonia and carbon dioxide is partially condensed in a condenser to give a mixed liquid/gaseous flow. The uncondensed gases comprising ammonia and carbon dioxide are separated from the liquid phase in a separator and subjected to washing in a packed portion of a column in countercurrent with a flow of a carbonate solution obtaining a gaseous flow essentially consisting of ammonia and a liquid flow comprising a carbamate solution in which the carbon dioxide contained in said uncondensed gases has been absorbed.

Abstract: The invention concerns a method for method for preparing 1,3,5-triaminobenzene, characterized in that it comprises a step which consists in amination of a compound of formula (I), wherein: A represents a halogen atom or a NH2 group; X1 and X2, identical or different, represent each a halogen atom, the amination step being carried out in the presence of ammonia and a catalyst selected from the group consisting of copper salts, cupric and cuprous oxides or mixtures thereof at a temperature ranging between 150° C. and 250° C.

Abstract: The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

Abstract: The invention provides compounds which are PDE7 inhibitors, having the following formula (I), (II) and (III) in which X1, X2, X3, X4, X, Y, Z, A and Z1 are as defined in the description, methods for preparing them and their use for the treatment of disorders for which therapy by a PDE7 inhibitor is relevant.

Abstract: The invention relates to a novel multi step synthesis of 3-(N-methyl-N-pentyl) amino-1-hydroxypropane-1,1-diphosphonic acid, monosodium salt, monohydrate, of the formula

Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: Di- and polyamines of the diphenylmethane series are prepared by a) mixing a first portion of aniline with an acid catalyst, b) mixing a second portion of aniline with formaldehyde, and c) mixing and reacting the mixtures prepared in each of steps a) and b). The diamines produced by this process may then be phosgenated to produce the corresponding di-/polyisocyanate.

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: The invention provides 1,3,5-tris(arylamino)benzenes represented by the general formula (I) wherein A is naphthyl, anthryl, phenanthryl, biphenylyl or terphenylyl group, and R is alkyl having 1–6 carbon atoms or cycloalkyl group having five or six carbon atoms. The 1,3,5-tris(arylamino)benzenes have oxidation potentials in the range of about 0.5–0.6V, excellent reversibility in oxidation-reduction process and high glass transition temperatures and in addition, they are capable of forming stable and durable amorphous film useful as high performance organic semiconductors at normal temperatures or higher with no aid of binder resins, that is, by themselves.

Abstract: The invention provides sodium channel modulating compounds of formula I: wherein X, Y, Q, R1, w, and R2 have any of the values defined in the specification, and salts thereof, which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of formula (I) or a salt thereof, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).

Abstract: A method of thioacetate deprotection by providing a compound of the formula R1—S—CO—R2, and reacting the compound with a quaternary ammonium cyanide salt in the presence of a protic solvent in an inert atmosphere to convert the compound to a product of the formula R1—SH. R1 is an organic group in which the bonding to sulfur is through a saturated carbon, and R2 is an aliphatic group.

Abstract: Novel coordination polymers, their pharmaceutical formulations, useful for treating atheroma, tumors and other neoplastic tissue, as well as other conditions that are responsive to the induction of targeted oxidative stress, are disclosed.

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: The invention relates to a new crystalline form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of formula 1, which may be used for example for tumor therapy.

Abstract: The invention features a method for treating a patient having a cancer or other neoplasm by administering to the patient two compounds simultaneously or within 14 days of each other in amounts sufficient to treat the patient.

Abstract: This invention provides an isolated mixture of higher molecular weight primary aliphatic alcohols having 20, 22, 24, 26, 27, 28, 30, 32 and 34 carbon atoms and having enhanced purity. This invention also provides a process for obtaining the alcohol mixture by extracting a natural product with organic solvents with or without saponification of the natural product. The alcohol mixture is useful in pharmaceutical compositions, foodstuffs and dietary supplements and is effective for lowering total cholesterol and LDL-cholesterol and increasing HDL-cholesterol levels and therefore is effective in treating hypercholesterolemia. The composition may be used to reduce the risk of coronary heart disease, to inhibit the atherosclerotic process (platelet hyperaggregability, ischemia and thrombosis), and can be used as an anti-inflammatory and anti-thrombotic agent. The composition also possesses neurotrophic properties and is useful for improving male sexual activity.

Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof. In another aspect, the present invention provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. In yet another aspect, the present invention provides methods for treating cancer comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof.

Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.