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7601838 |
2-Alkyl/aryl sulphonyl-1,2,3,4-tetrahydro-9H-pyrido (3,4-b) indole-3-carboxylic acid esters/amides useful as antithrombotic agents
The present invention relates to antithrombotic compounds 2-alkyl aryl sulphonyl-1,2,3,4-tetrahydro-9H-pyrido(3,4-b)indole-3-carbox
ylic acid esters/amides, pharmaceutically acceptable salts and...
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7601734 |
Cyclic amine compound
An object of the present invention is to provide a cyclic amine compound which has a potent inhibitory effect on the binding of α2C-adrenoceptor and is useful in preventing and treating disorders...
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7598263 |
Cyanoquinoline derivatives, their preparation, their use, and medicaments comprising them
The present invention relates to a quinoline derivative having the general formula (A):
in which R 1 , R 2 , X, Y and Z are indicated in the description and the claims, the use of the compounds...
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7598262 |
Method for treating diabetes
A method is provided for first line treatment of type 2 diabetes employing a combination of metformin and glyburide. A method for treating diabetes in drug naive human patients is also provided...
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7589100 |
Non-hygroscopic and powdery amorphous pimecrolimus
An amorphous pimecrolimus and processes for providing an amorphous pimecrolimus are provided.
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7585517 |
Transscleral delivery
Diseases associated with the tissues in the posterior segment of the eye can be effectively treated by administering therapeutic agents transsclerally to those tissues. Compositions, devices, and...
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7579358 |
Aerosol formulation for inhalation comprising an anticholinergic
A pharmaceutical composition comprising:
(a) an active substance consisting of a compound of formula 1
wherein X − is an anion;
(b) ethanol or a mixture of ethanol and...
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7576210 |
Soft anticholinergic esters
Soft anticholinergic esters of the formulas:
wherein R 1 and R 2 are both phenyl or one of R 1 and R 2 is phenyl and the other is cyclopentyl; R is C 1 -C 8 alkyl, straight or branched...
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7572804 |
Macrolides
A mixture comprising a poly-ene macrolide and an antioxidant. Preferably, the poly-ene macrolide is rapamycin and the antioxidant is 2,6-di-tert.-butyl-4-methylphenol. The presence of the...
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7560457 |
Rapamycin analogues and the uses thereof in the treatment of neurological, proliferative, and inflammatory disorders
The present invention provides compounds of the following structure, wherein R 1 , R 2 , R 4 , R 4′ , R 6 , R 7 , and R 15 are defined above:
These compounds are useful in treating...
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7553843 |
Process for the preparation of purified crystalline CCI-779
The present invention provides purified crystalline CCI-779 and processes for preparing the same.
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7553842 |
Macrocyclic analogs for the treatment of immunoregulatory disorders and respiratory diseases
Disclosed are compounds of the Formula I
and diastereomers, tautomers, solvates, metabolites, and pharmaceutically acceptable salts thereof, wherein X, A, L and Y are as defined herein. Such...
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7550479 |
Modified Pictet-Spengler reaction and products prepared therefrom
A method of introducing a second stereogenic center into a tetrahydro-β-carboline have two stereogenic centers using a modified Pictet-Spengler reaction is disclosed. The method provides a desired...
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7541365 |
Chemokine receptor antagonists and methods of use therefor
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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7538219 |
Soft anticholinergic zwitterions
Soft anticholinergic zwitterions of the formulas:
wherein R 1 and R 2 are both phenyl or one of R 1 and R 2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral...
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7538119 |
41-Methoxy isotope labeled rapamycin 42-ester
41-methoxy-labeled rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) compounds are provided, along with methods for the synthesis and use thereof.
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7528145 |
Use of an mTOR inhibitor in treatment of uterine leiomyoma
The invention provides for the use of an mTOR inhibitor in the treatment or inhibition of fibroids.
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7507745 |
Pharmaceutical compositions based on fluorenecarboxylic acid esters and soluble TNF receptor fusion proteins
The present invention relates to novel pharmaceutical compositions based on fluorene carboxylic acid ester derived anticholinergics of formula 1
and soluble TNF receptor fusion proteins,...
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7465742 |
Heterocyclic compounds having anti-HBV activity
This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to...
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7465741 |
C-substituted tricyclic isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric...
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7462367 |
Anticholinergic powder formulations for inhalation
An inhalable powder comprising:
(a) an active substance consisting essentially of a compound of formula 1
wherein X − is a pharmaceutically acceptable anion; and (b) a...
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7455853 |
Medical devices containing rapamycin analogs
A medical device comprising a supporting structure capable of containing or supporting a pharmaceutically acceptable carrier or excipient, which carrier or excipient may contain one or more...
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7446111 |
Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid and its pharmaceutical compositions
The present invention provides an amorphous form of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid. This invention also provides processes for preparing the amorphous...
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7442707 |
CCI-779 polymorph and use thereof
The present invention provides CCI-779 polymorph Form II. This invention also provides processes for preparing CCI-779 polymorph Form II and pharmaceutical compositions including CCI-779 polymorph...
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7439252 |
Ascomycin crystalline forms and preparation thereof
The present invention provides novel crystalline forms of ascomycin as well as processes for the preparation thereof and pharmaceutical compositions comprising such crystalline forms of ascomycin.
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7432277 |
Phosphorus-containing macrocycles
This invention concerns a new family of phosphorus-containing macrocycles containing various phosphonate- and phosphonate-containing moieties.
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7431916 |
Administration of medicinal dry powders
A method of administering a metered dry powder combined dose of finely divided dry medication powders is disclosed, wherein said method comprises providing a relative motion between a nozzle of a...
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7429600 |
Fluorenecarboxylic acid esters, process for the manufacture thereof, and use thereof as medicaments
Fluorenecarboxylic acid esters of general formula 1
wherein X − and the groups A, R, R 1 , R 2 , R 3 , R 3′ , R 4 , and R 4′ have the meanings given in the claims and in the...
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7419986 |
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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7419985 |
4-Phenyl substituted tetrahydroisoquinolines and 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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7417051 |
Medicaments comprising betamimetics 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 betamimetic 2,
or a solvate or hydrate thereof,...
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7405224 |
Xanthenecarboxylates, processes for preparing them, and their use as pharmaceutical compositions
Xanthenecarboxylates of formula 1
wherein:
A is a group selected from
X − is an anion with a single negative charge; R is hydroxy, methyl, hydroxymethyl, ethyl, —CF 3 , —CHF 2 , or...
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7399861 |
Soft anticholinergic esters
Soft anticholinergic esters of the formulas:
wherein R 1 and R 2 are both phenyl or one of R 1 and R 2 is phenyl and the other is cyclopentyl; R is C 1 -C 8 alkyl, straight or branched...
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RE40418 |
Treatment of neoplasms with CCI-779/EKB-569 combination
This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.
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7384953 |
Purification of rapamycin
Purified rapamycin and a chemical process for obtaining the purified rapamycin are described.
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7384947 |
Fused tricyclic heterocycles useful for treating hyper-proliferative disorders
This invention relates to a novel fused tricyclic heterocycle of the formula
and its use for the treatment of hyper-proliferative disorders.
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7378426 |
Fused heterotricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3
Disclosed are fused heterotricyclic compounds of the following formula I,
or an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of A ring or C ring...
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7378105 |
Drug delivery systems, kits, and methods for administering zotarolimus and paclitaxel to blood vessel lumens
A system and compositions including zotarolimus and paclitaxel are disclosed, as well as methods of delivery, wherein the drugs have effects that complement each other. Medical devices are...
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7368457 |
Bridged N-arylsulfonylpiperidines as gamma-secretase inhibitors
In an embodiment, this invention discloses novel gamma secretase inhibitors of Formulae I:
wherein the various moieties are described herein. Also disclosed is a method of treating Alzheimer's...
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7357942 |
Compositions, systems, and kits for administering zotarolimus and paclitaxel to blood vessel lumens
A system and compositions including zotarolimus and paclitaxel are disclosed, as well as methods of delivery, wherein the drugs have effects that complement each other. Medical devices are...
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7354949 |
Therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia
The present invention provides a therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia comprising, as an active ingredient, a tricyclic compound represented...
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7345053 |
Nitrosated and nitrosylated rapamycin compounds, compositions and methods of use
The invention describes novel nitrosated and/or nitrosylated rapamycin compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated rapamycin compound, and, optionally,...
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7332175 |
Long-acting drug combinations for the treatment of respiratory complaints
A pharmaceutical composition comprising:
(a) an anticholinergic of formula 1
wherein X − is an anion with a single negative charge; and (b) a compound of formula 2
or the...
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7320985 |
Method for stabilizing arylcarboxylic acid, stabilizer thereof and aqueous solution containing stabilized arylcarboxylic acid
A method for stabilizing an arylcarboxylic acid, which comprises adding a heterocyclic base to the arylcarboxylic acid or a pharmacologically acceptable salt thereof, a stabilizer thereof and an...
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7311894 |
HFA suspension formulations containing an anticholinergic
The invention relates to propellant gas formulations containing suspensions of the crystalline monohydrate of...
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7309707 |
Crystalline micronisate, process for the manufacture thereof and use thereof for the preparation of a medicament
The invention relates to a crystalline micronisate 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, processes for...
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7297704 |
Cycloalkyfused indole, benzothiophene, benzofuran and idene derivatives
The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central...
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7288543 |
Opioid receptor antagonists
A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3′, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate,...
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7282505 |
Rapamycin polymorphs and uses thereof
The present invention provides rapamycin polymorph Form II. This invention also provides processes for preparing rapamycin polymorph Form II and pharmaceutical compositions including rapamycin...
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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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