Organic compounds -- part of the class 532-570 series inventions 08/06

20060194972 - Process for the production of imidazopyridin-8-ones: The invention relates to a process for the production of 7-(trialkyl-silanytoxy)-2,3-dimethyl-8-phenyl-8,9dihydro-7H-1,3a,9-triazacyclopenta[a]naphthalen-6-one and related compounds by using NBS as oxidizing agent....

20060189806 - Proteasome inhibitors and methods of using the same: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome...

20060189807 - Process for the manufacture of intermediates in camptothecin production: e

20060189808 - Heterocyclic inhibitors of mek and methods of use thereof: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 R10, and W are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds...

20060189809 - Method for the synthesis of quinoline derivatives: This invention relates to novel intermediates and processes for preparing pharmaceutically active quinoline compounds, including (−)-(S)—N-(α-ethylbenzyl)-3-hydroxy-2-phenylquinoline-4-carboxamide....

20060189810 - Novel sulfonamide inhibitors of aspartyl protease: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and...

20060189811 - Process for producing 1,2,4-triazole compound and intermediate therefor: (Wherein Ra, Rb and Rd represent a group, Rc represents a group which can be removed by an acid) A 1,2,4-triazole compound (5) having an optionally substituted 2-cyanopyridin-4-yl group at 3-position and an optionally substituted aromatic group at 5-position which inhibits a xanthine oxidase and is useful for treatment of...

20060189812 - Regioselective halogenation of nicotine and substituted nicotines: h

20060183904 - Acylated spiropiperidine derivatives as melanocortin-4 receptor agonists: Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction,...

20060183905 - Derivatives of 4-(thio-or selenoxanthene-9-ylidene)-piperidine or acridine and its use as a selective 5-ht2b receptor antagonist: The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament and for the manufacture of a medicament for treatment of a disease state which can be alleviated by treatment with a 5-HT2B antagonist....

20060183906 - Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-4-yl-amines as janus kinase inhibitors: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer....

20060183907 - Novel process for the manufacture of (+)-(s)-clopidogrel bisulfate form-1: The present invention relates to a novel process for the manufacture of blood-platelet aggregation inhibiting agent. In particular, the present invention is directed to a process for the manufacture of Methyl-(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-S-(4H)acetate bisulfate Form-I....

20060183908 - Heterocyclic compounds, methods of making them and their use in therapy: In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl....

20060183909 - Compositions derived from quinoline and quinoxaline, preparation and use thereof:

20060183910 - Pharmaceutical compositions of 4-amino-2-(3-methyl-2,6-dioxo-piperidin-3-yl)-isoindole-1,3-dione: Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines are disclosed. The compounds are useful, for example, in reducing the levels of TNFα in a mammal....

20060183911 - Pyridones useful as inhibitors of kinases: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and...

20060173185 - Bisphosphonate complexes: Bisphosphonate compounds are disclosed, particularly bisphosonate conjugates useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis....

20060173186 - Transition-metal-catalyzed carbon-nitrogen and carbon-carbon bond-forming reactions: One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition-metal-catalyzed reactions, including the...

20060173187 - Process for the preparation of phosphitylation agents: A process for the preparation of a compound of formula R1—Y1—P(NR2R3)2 is provided. The process comprises reacting a compound of formula PX3 with a compound of formula HNR2R3 to form a compound of formula X—P(NR2R3)2; and reacting the compound of formula X—P(NR2R3)2 with a compound of formula R1—Y1—H in the...

20060173188 - Process for producing 3-acylaminobenzofuran-2-carboxylic acid derivative: wherein X is a group of the formula: —N═ or —CH═; R1 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a cyano group or an amino group optionally substituted by a lower alkyl group; Ring A is a nitrogen-containing heterocyclic group; Ring B...

20060173189 - Synthesis of himbacine analogs: e