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7414071 |
Methods of treatment with selective EP4 receptor agonists
The present invention provides a method of treating hypertension, liver failure, loss of patency of ductus arteriosus, glaucoma or ocular hypertension in a patient, comprising administering to the...
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7402606 |
Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The...
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7402605 |
8-azaprostaglandin derivative compounds and drugs containing the compounds as the active ingredient
An 8-azaprostaglandin represented by formula (I)
(wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin...
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7396846 |
Growth hormone secretagogues
This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the...
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7345087 |
Aminocyclohexyl ether compounds and uses thereof
Aminocyclohexyl ether compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses uses for the compounds and...
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7345086 |
Uses of ion channel modulating compounds
Methods, formulations, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias, including the treatment or prevention of atrial fibrillation. In these methods,...
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7345082 |
Phosphinic acids
The present invention relates to phosphinic acid derivatives of formula I
wherein R 1 , R 2 , R 3 and R 4 are described hereinabove. These compounds can be used in the treatment or prevention...
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7338975 |
Lactams as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis,...
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7329685 |
1-Phenyl-2-oxo-3-sulfonylamino-pyrrolidine derivatives and related compounds as factor Xa inhibitors for the treatment of acute vascular diseases
The invention relates to compounds of formula (I):
wherein substituents are as defined.
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7326696 |
Amino-methyl substituted tetracycline compounds
Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.
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7312218 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7304088 |
Protease inhibitors
This invention relates to treating an infection with a virus using protease inhibitors. Examples of the protease inhibitors include compounds of formula (I). Each variable is defined in the...
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7300929 |
Mediators of hedgehog signaling pathways, compositions and uses related thereto
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function...
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7297712 |
Cationic amphiphiles for intracellular delivery of therapeutic molecules and its composition, process and method of treatment
The present invention provides novel cationic amphiphiles capable of facilitating transport of biologically active molecules into cells wherein the said amphiphiles contain cyclic head group having...
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7294647 |
Kappa agonist compounds and pharmaceutical formulations thereof
Compounds having kappa opioid agonist activity, compositions containing them and 5 method of using them as analgesics and pruritic agents are provided. The compounds of formulae I, II, III and IV...
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7291620 |
N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme...
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7288565 |
Azasugar compound
The present invention provides a compound represented by the formula (I) or a salt thereof:
wherein R 1 represents a hydrogen atom, a C 1-10 alkyl group optionally having a substituent, or a...
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7276531 |
G-lactam derivatives as prostaglandin agonists
A gamma-lactam diene of Formula I:
which is particularly useful as a medicament for the treatment of various disorders such as asthma, hypertension, osteoporosis, sexual dysfunction and...
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7259184 |
Ion channel modulating compounds and uses thereof
Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and...
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7256211 |
8-azaprostaglandin derivatives and medical use thereof
The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I)
(wherein, all the symbols have the same meanings as that of...
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7253205 |
Gem-disubstituted cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 represent a variety of substituents, ring A is a phenyl or pyridyl...
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7253198 |
Hydroxyethylamine derivatives for the treatment of Alzheimer's disease
The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing...
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7244753 |
Cyclooxygenase-2 selective inhibitors, compositions and methods of use
The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least...
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7235581 |
4-pyrrolidino-phenyl-benzyl ether derivatives
The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the...
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7232821 |
(2-((2-alkoxy)-phenyl) -cyclopent-1enyl) aromatic carbo and heterocyclic acid and derivatives
Compounds of formula (I) or a pharmaceutically acceptable derivative thereof:
wherein A, R 1 , R 2 , R x , R 8 , R 9 and n are as defined in the specification, a process for the preparation of...
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7208488 |
N-substituted benzene sulfonamides
Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease.
In Formula (I), R 1 , R 2 , R 3 , R 4 , R 3′ , R 10 and R...
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7196113 |
Lactam tachykinin receptor antagonists
The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention...
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7192979 |
EP4 receptor selective agonist in the treatment of osteoporosis
This invention is directed to EP4 receptor selective prostaglandin agonists of the Formula I,
wherein R 2 , X, Z and Q are as defined in the specification. This invention is also directed to...
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7192978 |
Pyrrolidinium derivatives
New pyrrolidinium derivatives having the chemical structure of general formula (I)
are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and...
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7189756 |
Pyrrolidine derivatives
The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with...
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7189755 |
Pyrrolidine melanocortin-specific compounds
Melanocortin receptor-specific pyrrolidine compounds having the structure:
and stereoisomer and pharmaceutically acceptable salts thereof, where R 1 , R 2 , and R 3 are as described in the...
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7183277 |
Carboxylic acid amides
Novel compounds of the formula I
in which
D, W, X, Y, T and R 1 are as defined in Patent Claim 1,
are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or...
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7173055 |
Pyrazolecarboxamide and pyrazolethioamide as fungicide
Novel pyraole derivatives of formula (I), wherein: X is oxygen or sufu, R 1 is C 1 –C 3 alkyl, C 1 –C 3 haloalkyl, C 1 –C 3 alkoxy-C 1 –C 3 alkyl or C 1 –C 3 haloalkoxy-C 1 –C 3 alkyl;...
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7160905 |
Hydroxyethylene compounds with Asp2 inhibitory activity
The present invention relates to novel hydroxyethylene compounds having Asp2 (β-secretase. BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them...
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7160902 |
Amide derivatives and methods of their use
Amide derivatives of the general formulae Ia and Ib:
are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing...
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7151111 |
4-pyrrolidino-phenyl-benzyl ether derivatives
The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the...
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RE39419 |
Estrogen agonist/antagonist metabolites
This invention relates to compounds that are mammalian metabolites of (−)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5
,6,7,8-tetrahydro-naphthalene-2-ol. The compounds of the invention...
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7132444 |
Process for the preparation of trans-3-ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl cyclohexyl) amino]carbonyl]amino]sulfonyl] phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide
The present invention provides a novel process for preparation of trans-3-ethyl 2,5-dihydro-4-methyl-N-[2-[4-[[[[(4-methyl...
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7129266 |
Antibiotic Cyan426-A
The invention relates to a new antibiotic designated Cyan426-A, to its production by fermentation, to methods for its recovery and concentration from the crude solutions, and to a process for its...
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7112605 |
Sulfonyl-containing 3,4-diaryl-3-pyrrolin-2-ones, preparation method, and medical use thereof
The invention relates to sulfonyl-containing 3,4-diaryl-3-pyrrolin-2-ones compounds having formula (I)
wherein R 1 is selected from the group consisting of 4-methylsulfonyl, 4-aminosulfonyl,...
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7105564 |
Pharmaceutical composition comprising a dual antagonist against PGD2/TXA2 receptors having a [2.2.1] or [3.1.1] bicyclic skeleton
The present invention provides novel compounds having a dual antagonistic activity against thromboxane A2 receptor and prostaglandin D 2 receptor and pharmaceutical compositions comprising them. ...
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7101897 |
Farnesyl transferase inhibitors
This invention relates to compounds of formula (I) that inhibit farnesylation of gene products through inhibition of the enzyme farnesyl-protein transferase (FPTase). The invention also relates to...
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7101895 |
Cyclohexyl sulphone derivatives as gamma-secretase inhibitors
Compounds of formula I:
wherein Ar 1 and Ar 2 are optionally substituted aryl or heteroaryl, L is a bond, ═CH— or —(CHR a ) n —, and X is SCN, SR 1 , S(O)R 1 , (CR a R b ) m SO 2 R 1...
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7098238 |
Degradation fragments
A pharmaceutical composition comprising a compound of formula (I) wherein X is an electron withdrawing group, Y 1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO 2 R 4 , —CO 2 R...
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7091236 |
Method for increasing the bioavailability of glycopyrrolate
The invention relates to a method of increasing the bioavailability of glycopyrrolate by administration of a therapeutically effective amount of glycopyrrolate without food.
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7084139 |
Pyrrolidin-2-one derivatives as inhibitors of factor Xa
The invention relates to compounds of formula (Ic)
processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the...
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7078400 |
20-HETE synthase inhibitor
The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or...
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7064145 |
Inhibition of beta cell degeneration
Methods for preventing beta cell degeneration, such as necrosis or apoptosis of beta cells in a subject, comprising administering a DPP-IV inhibitor to a subject in need thereof. The invention...
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7060289 |
Topical glycopyrrolate product
This invention relates to a convenient and safe product and method of applying glycopyrrolate topically in order to reduce excessive sweating in localized areas for those who suffer from this...
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