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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,...
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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...
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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...
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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...
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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,...
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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...
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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,...
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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%...
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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...
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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)...
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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.
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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...
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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...
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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...
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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...
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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...
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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,...
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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...
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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—,...
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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.
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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.
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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...
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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...
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6617333 |
Antineoplastic combinations comprising
This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.
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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,...
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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).
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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,...
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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.
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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...
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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.
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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...
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