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7273603 |
HFC solution formulations containing an anticholinergic
An aerosol solution formulation comprising:
(a) a salt of formula 1
wherein X − is an anion (b) an HFC propellant; (c) a cosolvent; and (d) an inorganic or an organic...
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7268144 |
Regiospecific synthesis of rapamycin 42-ester derivatives
A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described. The method involves lipase-catalyzed acetylation of 42-hydroxy of rapamycin with an acyl donor such as a...
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RE39820 |
Esters of thienyl carboxylic acids and amino alcohols and their quaternization products
Compounds of the formula
of which, in exemplary compounds, the thienyl group is attached via the 2-position and;
(a) A is 3α-(6β, 7β-epoxy)-tropanyl methobromide and R 1 is...
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7259170 |
Macrolides containing pharmaceutical compositions
A pharmaceutical compound comprising a compound of formula I and a pharmaceutically acceptable 2-amino-1,3-propanediol beside one or more pharmaceutically acceptable excipient(s).
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7250423 |
Methods for synthesizing heterocycles and therapeutic use of the heterocycles for cancers
The present invention provides methods for synthesizing novel tetrahydroquinoline derivatives that are useful for cancer chemotherapy and anti-viral applications. The present invention provides...
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7244742 |
Pharmaceutical compositions for inhalation containing an anticholinergic, corticosteroid and betamimetic
A pharmaceutical composition comprising:
(a) an anticholinergic of formula 1
wherein X − is an anion with a single negative charge;
(b) a corticosteroid; and (c) a...
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7244415 |
HFA suspension formulations of an anhydrate
The invention relates to propellant gas formulations containing suspensions of the crystalline anhydrate of...
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7241771 |
Oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin
The invention provides a purified oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin (SDZ-RAD Isomer C), a chemical process for its preparation, as well as pharmaceutical compositions and packs...
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7241745 |
Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I)
as well as methods for their production, medicaments containing these compounds...
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7220755 |
42-O-alkoxyalkyl rapamycin derivatives and compositions comprising same
42-O-alkoxyalkyl derivatives of rapamycin having biological activity are described. Compositions and delivery devices comprising the 42-O-alkoxyalkyl rapamycin derivatives are also disclosed.
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7211572 |
Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I]
wherein each symbol is as defined in the specification, or a pharmaceutically...
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7202256 |
Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779
Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of...
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7189735 |
Use of CCI-779 as an antineoplastic agent
This invention provides the use of CCI-779 in the treatment of neoplasms.
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7186729 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Chemokine receptor antagonists and methods of use thereof
Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an...
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7183289 |
39-desmethoxyrapamycin, compositions and methods of use thereof
The present invention relates to medical uses of 39-desmethoxyrapamycin.
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7166612 |
Methods for reducing platelet activation platelet aggregaton or thrombosis
The invention provides methods and compositions for reducing platelet activation, platelet aggregation and thrombosis. The invention further provides compositions and methods for treating or...
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7160867 |
Rapamycin carbohydrate derivatives
This invention provides modified rapamycins that have specific monosaccharide(s), oligosaccharide(s), pseudosugar(s) or derivatives thereof attached through a linker to create rapamycin...
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7148232 |
Oxazolo, thiazolo and selenazolo [4,5-c]-quinolin-4-amines and analogs thereof
Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators...
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7144885 |
Fused tricyclic heterocycles useful for treating hyper-proliferative disorders
This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disorders
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7135479 |
Antidepressant azaheterocyclylmethyl 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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7105529 |
Substituted oxindole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors and compositions and methods of treating chemotherapy and radiation therapy side effects
Compounds of formula (I): wherein X is N, CH, CCF 3 , or C(C 1-12 aliphatic); R 4 is sulfonic acid, C 1-12 aliphatic-sulfonyl, sulfonyl-C 1-12 aliphatic, C 1-12 aliphatic-sulfonyl-C 1-6 ...
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7101891 |
Compounds and pharmaceutical compositions for inhibiting MRP1
The present invention relates to a compound of formula (I), which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1
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7094397 |
Methods and reagents for the treatment of multiple sclerosis
The invention features methods and reagents for the diagnosis, monitoring, and treatment of multiple sclerosis. The invention is based in part on the discovery that Chlamydia is present in...
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7091213 |
Phosphorus-containing compounds and uses thereof
This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which:
A is absent or is —O—, —S— or —NR 2 —; Q is absent or (if A is —O—,...
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7090853 |
Noscapine derivatives as adjuvant compositions and methods of use thereof
An adjuvant composition comprising noscapine and its derivatives, for use in the treatment of tumors, cancer, as an adjuvant for vaccines.
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7084153 |
Medicaments comprising steroids and a novel anticholinergic
A pharmaceutical composition comprising:
(a) a salt of formula 1
wherein: X − is an anion with a single negative charge; and (b) a steroid 2,
processes for preparing...
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7084152 |
4-phenyl substituted tetrahydroisoquinolines therapeutic use thereof
Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl...
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7078054 |
Soft gelatin capsule manufacture
Soft gelatin capsules having a capsule shell comprising gelatin, plasticizers and, if desired or required, further auxiliary agents, and a capsule filling containing a solvent including a...
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7074804 |
CCI-779 Isomer C
Purified CCI-779 Isomer C is provided, as are pharmaceutical compositions and kits containing same.
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7071201 |
Quinoline derivatives
A novel compound of the formula:
wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R 1, R 2 , R 3 , R 4 , and R 5 represent each a substituent; n represents 0 or an integer...
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7067527 |
Thienopyridine derivatives, their production and use
The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical...
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7060709 |
Method of treating hepatic fibrosis
This invention provides the use of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) in the treatment or inhibition of hepatic fibrosis and hepatic cirrhosis.
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7053104 |
Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases
The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating...
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7048939 |
Methods for the inhibition of neointima formation
Restenosis is inhibited through local delivery of anti-restenotic agents including angiotensin converting enzyme inhibitors; nicotine receptor agonists, agents that increase concentrations of...
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7041674 |
Carbamic acid esters with anticholinergic activity
A compound of formula 1
wherein X − , A, R 1 , R 2 , R 3 , and R 4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in...
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7037919 |
Tetrahydroquinoline derivatives
Tetrahydroquinoline derivatives of general formula (I) or salts thereof, having a specific and strong binding affinity for AR and exhibiting AR agonism or antagonism; and pharmaceutical...
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7037920 |
Substituted tricyclic himbacine derivatives that are useful as thrombin receptor antagonists
Heterocyclic-substituted tricyclics of the formula
or a pharmaceutically acceptable salts thereof, wherein:
n 1 and n 2 are independently 0-2; Het is an optionally substituted mono-,...
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7034037 |
Compositions and medical devices utilizing bioabsorbable polymeric waxes and rapamycin
The present invention is directed to medical devices and pharmaceutical or agricultural compositions, and seeds, each containing a synthetic, bioabsorbable, biocompatible polymeric wax that is the...
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7033604 |
Composition for topical administration
The present invention provides a composition for topical administration comprising an interleukin 2 inhibitor and an antimicrobial agent as active ingredients thereof, wherein said interleukin 2...
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7030129 |
Method of reducing and treating UVB-induced immunosuppression
Methods of preventing and/or treating UV-induced immunosuppression by administration of immune response modifier compounds are disclosed herein. Suitable immune response modifier compounds include...
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7026330 |
Methods for treatment of acute lymphocytic leukemia
Methods for treating patients having an early B cell derived acute lymphoblastic leukemia with rapamycin or a derivative thereof are provided. Also provided are methods for treating patients having...
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7019014 |
Process for producing anticancer agent LL-D45042
The disclosure describes the production of anticancer agent LL-D45042, having the structure:
by fermentation, to methods for the recovery and concentration of this anticancer agent from crude...
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6989388 |
Thieno[2,3-c]iosquinolines for use as inhibitors of PARP
The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula:
wherein the constituent variables are...
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6984635 |
Dimerizing agents, their production and use
Materials and methods are disclosed for regulation of biological events such as target gene transcription and growth, proliferation or differentiation of engineered cells.
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6969721 |
Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors
The present invention relates to tricyclic 2-pyridone compounds of formula (I):
or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are...
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6967205 |
Compounds with antibacterial and antiparasitic properties
There are provided novel compounds which have both antibacterial and antiparasitic properties, thereby reducing the need for using several compounds in combined antibacterial and antiparasitic...
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6962942 |
Azacycloalkanone serine protease inhibitors
The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and...
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6956043 |
Pharmaceutical compositions comprising 33-epi-chloro-33-desoxy-ascomycin solid dispersions
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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6949510 |
Uses of diterpenoid triepoxides as an anti-proliferative agent
Combinations of diterpenoid triepoxides and anti-proliferative agents are used in a combination therapy to treat hyperproliferative disorders. Anti-proliferative agents of interest include agents...
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6939877 |
Antidepressant piperidine 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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