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7312214 |
1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors
The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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7312211 |
Pryanone compounds useful as reversible inhibitors of cysteine proteases
Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R 2 , R 3 , R 4 , R 6 , R 8 and Y are defined herein. The compounds are useful for...
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7312209 |
Acridone inhibitors of IMPDH enzyme
Compounds having the formula (I),
wherein R 3 is selected from H, OH and NH 2 ; R 30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O) 2 —; or W may be —CH 2...
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7307076 |
Beta agonists for the treatment of respiratory diseases
The present invention relates to compounds of general formula 1
wherein the groups n, A, B, R 1 , R 2 and R 3 may have the meanings given in the claims and in the specification, processes for...
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7307075 |
Tetrahydroquinoline analogues as muscarinic agonists
The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with...
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7294650 |
Benzothiophen and thiochrone containing phenethanolamine derivatives for the treatment of respiratory disorders
Compounds of formula (I):
and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective β 2...
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7265108 |
Nitrogen containing heterocyclic compounds and medicines containing the same
Compounds represented by the following general formula:
[wherein X 1 , X 2 , X 3 and X 4 each independently represent a single bond, C 1-6 alkylene, etc.; A 2 represents optionally...
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7259161 |
Compositions useful as inhibitors of JAK and other protein kinases
The present invention provides a compound of formula I:
or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the...
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7247625 |
6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators
Compounds having the structure of formula I are provided. In formula I, R 1 is H, OH, substituted or unsubstituted C 1 to C 3 alkyl, C 1 to C 3 perfluoroalkyl, or COR 6 ; R 6 is H,...
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7244728 |
Long acting betamimetics for the treatment of respiratory diseases
The present invention relates to the compounds of general formula 1
wherein the groups R, R1, R2, R3 and A may have the meanings given in the claims and specification, processes for preparing...
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7244727 |
Fused bicyclic nitrogen-containing heterocycles
Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the...
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7244726 |
Heterocyclic compounds possessing affinity at 5HT1 -type receptors and use thereof in therapy
Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:
wherein A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl,...
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7235550 |
Polycyclic azaindole compounds
The invention relates to compounds of formula (I):
wherein:
G 1 represents an alkylene chain as defined in the description, A represents
R 2 and R 3 represent...
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7220742 |
Enantiomerically pure beta agonists, process for the manufacture thereof and use thereof as medicaments
The present invention relates to enantiomerically pure compounds of general formula 1
wherein the groups R 1 , R 2 , R 3 , R 4 and X − may have the meanings given in the claims and in the...
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7217708 |
3,7-Diazabicyclo [3.3.1] formulations as anti-arrhythmic compounds
There is provided substantially crystalline forms of 4-({3-[7-(3,3-dimethyl-2-oxobutyl) -9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]propyl}amino)benzo-ni
trile; tert-butyl 2...
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7214674 |
Heterocyclymethylpiperidines and -piperazines possessing affinity at 5ht-1 type receptors
Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:
wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl,...
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7205296 |
Substituted 2H-1,3-benzoxazin-4(3H)-ones
Substituted benzoxazin-4(3H)-ones are provided which are useful for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
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7205295 |
Benzoxazin-3-ones and derivatives thereof as therapeutic agents
The present invention provides compounds of Formula I
wherein W, Q, E, D, R 6 , R 7 , R 8 , Y, K, R 9 , R 10 , R 12 , G, and the double bond denoted “*” have any of the values defined...
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7202241 |
Benzoxazine derivatives and uses thereof
Compounds of the formula (I):
or pharmaceutically acceptable salts, solvates or prodrugs thereof, where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , X, Y and m are as defined herein....
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7196108 |
Bicyclic heterocycles for the treatment of diabetes and other diseases
The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2...
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7196081 |
Compounds with hydroxycarbonyl-halogenoalkyl side chains
The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral...
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7192956 |
Methods of treating hormone-related conditions using cyclothiocarbamate derivatives
The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I or formula II, or tautomers thereof, in a...
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7189713 |
Piperidine derivatives
The present invention relates to piperidine derivatives of formula (I):
R represents halogen or C 1-4 alkyl R 1 represents C 1-4 alkyl; R 2 or R 3 independently represent hydrogen or...
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7186730 |
Bicyclic nitrogen-containing heterocyclic derivatives for use as antibacterials
Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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7176196 |
Bicyclic heterocycles as HIV integrase inhibitors
The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds...
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7169776 |
Method of preparing alkylated salicylamides via a dicarboxylate intermediate
The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention...
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7166592 |
Nonsteroidal antiinflammatory agents
Compounds of Formula 1
are useful in the treatment of inflammation.
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7166591 |
Catalytic cleavage of phosphate ester bonds by boron chelates
Novel chemical compounds are disclosed having the general formula L{YX m } n , wherein X is selected from the Group 13 elements, Y is a halide, and L is a chelating ligand containing at least one...
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7160888 |
[1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia
This invention relates to compounds of the formula 1
wherein G, D, A, Z, Q, X, Y, R 1 , and R 4 through R 7 are defined as in the specification, processes for preparing the same and...
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7160882 |
Long acting β-2-agonists and their use as medicaments
The present invention relates to compounds of formula 1
wherein the groups X, R a , R b , R 1 , R 1′ , R 2 , R 2′ , R 2″ , R 2′″ , V and n may have the meanings given in the claims...
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7160874 |
Phenylalanine derivatives
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin.
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7157447 |
Bicyclic heterocycles as HIV integrase inhibitors
The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for...
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7153852 |
Indole compounds, process for producing the same and drugs containing the same as the active ingredient
Indole derivatives represented by formula (I)
wherein all symbols represent the same as that in specification), production methods thereof, and DP receptor antagonist comprising them as active...
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7148217 |
Iminobenzoxazines, iminobenzthiazines and iminoquinazolines for controlling invertebrate pests
This invention pertains to methods for controlling invertebrate pests comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula...
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7141566 |
Benzoxazine and benzothiazine derivatives and the use thereof in medicaments
The invention relates to compounds of formula (I), the tautomeric and isomeric forms and salts thereof, in addition to a method for production and use thereof in medicaments.
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7141564 |
Nitrogen-containing bicyclic heterocycles for use as antibacterials
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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7141562 |
Substituted benzoxazinones and uses thereof
Compound of the Formula:
and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO 2 — or —(CR a R b ) r —, n is 1 or 2, R 2 is aryl or...
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7138395 |
Interleukin-1β converting enzyme inhibitors
The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula:
X is —CH 2 —, —O— or —NR 9 —; R is a...
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7129238 |
Mandelic acid derivatives
The invention is concerned with novel mandelic acid derivatives of formula (I)
wherein R 1 to R 10 , X and Y are as defined in the description and in the claims, as well as pharmaceutically...
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7122542 |
Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms...
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7122536 |
(R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity
The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma...
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7115646 |
Cyclic diamines and derivatives as factor Xa inhibitors
The present application describes cyclic diamino compounds, derivatives thereof, and pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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7112584 |
Nonsteroidal antiinflammatory agents
The invention relates to compounds of general formula I
and their use for the production of pharmaceutical agents for treatment and prophylaxis of diseases that coincide with inflammatory,...
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7101876 |
Substituted benzoxazines as integrin antagonists
The present invention relates to a class of compounds represented by the formula (I)
or a pharmaceutical acceptable salt, prodrug or ester thereof, pharmaceutical compositions comprising...
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7087626 |
Pyrrole derivatives as pharmaceutical agents
Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors. The disclosed invention relates to compounds of the...
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7081457 |
Cyclothiocarbamate derivatives as progesterone receptor modulators
Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or...
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7067513 |
Phenylpiperazines
The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D 2 receptor and/or the serotonin reuptake site,...
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7064122 |
Pancreatic lipase inhibitor compounds, their synthesis and use
The subject invention features compounds having the structure:
wherein X is O, S, CH 2 or NR 5 ; Y is O or S; R 1 is H, substituted or unsubstituted C 1 -C 15 alkyl, C 1 -C 8 alkylaryl,...
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7060705 |
Mitotic kinesin inhibitors
The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7060294 |
Compressed tablet formulation
This invention relates to a 50% drug loaded compressed tablet formulation for efavirenz. Efavirenz is a non-nucleoside reverse trancriptase inhibitor being studied clinically for use in the...
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