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6933303 Heteroaryl-fused nitrogen heterocycles as therapeutic agents  
This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases, the compounds of the invention are useful for the management,...
6924292 Furoisoquinoline derivatives, process for producing the same and use thereof  
A compound having a partial structure represented by Formula: or a salt thereof has an excellent phosphodiesterase (PDE) IV-inhibiting effect, and is useful as a prophylactic or therapeutic...
6919325 Pharmaceutical compositions containing tiotropium salts and low-solubility salmeterol salts  
Pharmaceutical compositions and kits comprising: (a) a tiotropium salt; and (b) a salmeterol salt having a solubility in water of 0.1 mg/mL or less, processes for preparing them, and their...
6916824 Methods of treating cataracts and diabetic retinopathy with tricyclic pyrones  
Water-soluble, cell permeable aldose reductase inhibitors are presented. These compounds prevent the effects of galactosemia in patients. The compounds prevent both the accumulation of polyols and...
6911445 Antidepressant cycloalkylamine derivatives of heterocycle-fused benzodioxans  
Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
6908928 Crystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions  
Crystalline monohydrate of (1α,2β,4β,5α,7β)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9 -dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0 2,4 ]nonane bromide (tiotropium bromide monohydrate), processes for...
6903110 Antidepressant azaheterocyclylmethyl derivatives of 7,8-dihydro-6H-5-oxa-1-aza-phenanthrene  
Compounds of the formula useful for the treatment of such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
6890517 Inhalable formulation of a solution containing a tiotropium salt  
A liquid, propellant-free pharmaceutical preparation comprising: (a) a first active substance comprising a tiotropium salt, in a concentration based on tiotropium of between 0.0005% and 5%...
6884805 Polymorph forms of N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-B]quinolin-4-YL)-2-(2-oxopyrrolidin-1-YL)acetamide  
The invention relates to novel polymorph crystal forms A and B of N-(2,3-dimethyl-5,6,7,8-tetrahydrofuro[2,3-b]quinolin-4-yl)- 2-(2-oxopyrrolidin-1-yl)acetamide: The compounds and...
6881422 Powder formulations containing tiotropium suitable for inhalation  
A method of making a physically stable and homogenous powdered pharmaceutical composition comprising a tiotropium salt and a physiologically acceptable excipient, the method comprising: (a)...
6878388 Vanadium compounds for treating proliferative cell disorders  
Vanadium compounds useful to prevent and/or inhibit adhesion, migration, and invasion of proliferative cells into surrounding tissue.
6872718 Tricyclic dihydrobenzofuran derivatives, process for the preparation thereof and agents  
A compound represented by the formula: wherein Ring A is a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, Ring B is benzene ring which is...
6864253 Benzo[4,5]thieno[2,3-c]pyridine and Benzo[4,5]furo[2,3-c]pyridine Derivatives Useful as Inhibitors of Phosphodiesterase  
The present invention relates to novel β-carboline derivatives of the general formula wherein all the variables are as described within the specification, useful as phosphodiesterase...
6858621 2-(quinolonyl)-fused heterocycles as androgen receptor modulators  
The present invention is directed to novel 2-(quinolonyl)-fused heterocyclyl derivatives of the general formula (I) wherein R 1 , R 2 , R 3 , R 3a , R 4 , R 5 , R 6 and R 7 are as herein...
6852728 Anticholinergics, processes for preparing them, and pharmaceutical compositions containing them  
A compound of formula 1 wherein: A is a group selected from X − is an anion with a single negative charge; R 1 and R 2 are each independently a C 1 -C 4 -alkyl optionally substituted...
6849640 Therapeutic 1H-pyrido [4,3-b] indoles  
The present invention provides 2,3,4,4 a ,5,9 b -hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating...
6821981 Azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino&lsqb 2,3-f&rsqb -quinoline as 5-HT1A antagonists  
Compounds of the formula useful for the treatment of disorders, such as anxiety, aggression and stress, and for the control of various physiological phenomena, such as appetite,...
6821982 Preparation of a camptothecin derivative by intramolecular cyclisation  
The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention...
6815440 Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids  
Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course...
6800637 Antidepressant indolealkyl derivatives of heterocycle-fused benzodioxan methylamines  
Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
6774129 Benzothieno&lsqb 3,2-c&rsqb pyridines as α2 antagonists  
The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R 1 is...
6762191 Therapeutic compounds  
The present invention provides compounds of formula (I): wherein: R 1 , R 2 , R 3 R 4 , R 5 , R 6 , X, - - - , m, and n have any of the values defined in the specification, as well as...
6750223 4-Anilino&lsqb 2,3-b&rsqb quinoline derivatives, their preparation processes and pharmaceutical compositions comprising the same  
Disclosed herein are 4-anilino[2,3-b]quinoline derivatives of formula (I): wherein each of R 1 , R 2 , R 3 and Y is given the definition as set forth in the Specification and Claims. These...
6734189 Hydroxamic and carboxylic acid derivatives  
The invention relates to hydroxamic and carboxylic acid derivatives. Compounds of the formula: are disclosed. These compounds are useful for the treatment of diseases mediated by inhibitors of...
6726923 Apparatus and methods for preventing or treating failure of hemodialysis vascular access and other vascular grafts  
This invention is a prosthetic device generally placed on the outside surface of the vessel or graft which then elutes antiproliferative drugs or agents from a drug-eluting matrix material. Methods...
6720330 Somatostatin antagonists and agonists that act at the SST subtype 2 receptor  
Compounds according to the formula A—Z—W as herein described, wherein A is selected from the groups consisting of: A′—(CH 2 ) n —, A′—(CH 2 ) n SO 2 —, and A′—(CH 2 ) n CO—,...
6713468 Methods of using thiazolobenzoheterocycles  
Methods of using compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof.
6706727 Macrolides  
The composition of formula I wherein the substituents have various significances, whereby one of R 2 to R 4 is ethyl. They can be prepared by fermentation, or by replacement of hydroxy with...
6699877 Substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivatives  
A substituted 1,2,3,4-tetrahydroquinoline-2-carboxylic acid derivative of formula I and salts thereof with pharmaceutically acceptable acids. Also disclosed are methods for making the...
6696459 Steroid receptor modulator compounds and methods  
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds,...
6696042 Pharmaceutical compositions based on anticholinergics and NK1-receptor antagonists  
The present invention relates to novel pharmaceutical compositions based on anticholinergics and NK 1 -receptor antagonists, processes for preparing them and their use in the treatment of...
6673807 Immunosuppressive imidazole derivatives and their combination preparations with tacrolimus or cyclosporins  
Methods for increasing graft survival time comprising administering the combination of a compound that inhibits the production of nitric oxide and a compound that is a tricyclic macrolide, such as...
6673808 Medicinal compositions  
To provide a pharmaceutical composition comprising a macrolide compound, such as tricyclic compound (I) or its pharmaceutically acceptable salt, a dissolution/absorption promoter, a pharmaceutical...
6670355 Method of treating cardiovascular disease  
This invention provides a method of treating or inhibiting cardiovascular, cerebral vascular, or peripheral vascular disease in a mammal in need thereof, which comprises providing said mammal with...
6656949 4-anilinofuro &lsqb 3,2-c&rsqb quinoline derivatives, and preparation processes and uses of the same  
Disclosed herein are novel 4-anilinofuro[3,2-c]quinoline derivatives of formula (I): wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also...
6649626 N-substituted 1-(lactone) isoquinolones for treating nervous disorders  
The invention concerns compounds of general formula (I) wherein: Z represents a sulphur or oxygen atom, NH, N-alkyl or Nboc; group R′, identical or different, represent each a hydrogen atom, a...
6645983 Pharmaceutical compositions comprising 4-quinolones for treating cancers  
A non-cytotoxic pharmaceutical composition acting on the proliferation of clonogenic cells in malignant tumors and including an efficient amount of a compound selected among the compounds of...
6641800 Pressurized aerosol compositions comprising powdered medicament dispersed in hydrofluoroalkane  
Pressurized aerosol composition for administration by inhalation comprising a liquefied hydrofluoroalkane, a powdered medicament dispersed therein, and a suspending agent comprising a polymer...
6642222 Pyrano, piperidino, and thiopyrano compounds and methods of use  
The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder...
6624181 Synergistic combination  
The invention relates to the combined administration of PDE inhibitors and β 2 adrenoceptor agonists for the treatment of respiratory tract disorders.
6620818 Method for reducing the severity of side effects of chemotherapy and/or radiation therapy  
A composition and method for preventing/reducing the severity of epithelial cytoxicity side effects such as alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation...
6620785 Treatment of Mycobacterial diseases by administration of bactericidal/permeability-increasing protein products  
The present invention relates to methods for treating a subject suffering from infection with Mycobacteria, such as M. leprae or M. tuberculosis comprising administering to the subject a...
6617333 Antineoplastic combinations comprising  
This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.
6605616 Quinoline derivatives  
The invention is related to compounds of general formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is methyl, methoxy, fluoro, chloro, bromo, azido,...
6602868 Treatments for restless legs syndrome  
The invention provides methods and use of heterocyclic amines, and phenylazacycloalkane compounds, and their pharmacologically acceptable salts for the treatment of Restless Legs Syndrome (RLS).
6599915 Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-dioxinol&lsqb 2,3f&rsqb quinoline  
Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
6599914 Inhibition of cytokine generation  
Methods of inhibiting the generation of pro-inflammatory cytokines such as IL-4 and IL-13 in a human patient in need of such inhibiting are disclosed.
6599511 Pharmaceutical composition containing desoxypeganine for the treatment of drug dependence  
Desoxypeganine and its pharmaceutically acceptable acid addition salts can be used in the treatment of drug addiction or drug dependence. Said substances are administered preferably in a continuos...
6599535 Pharmaceutical compositions  
A pharmaceutical composition in the form of a solid dispersion comprising a macrolide, e.g. a rapamycin or an ascomycin, and a carrier medium.
6593335 Potassium channel openers  
Compounds having the formula I: are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method...