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7622497 |
Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis
The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are...
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7612219 |
11—[ (Z) -3- (dimethylamino) propylidene]—6, 11-dihydro-dibenz [B,E] oxepin-2-YI ]—acetic acid
Process for the preparation of olopatadine (I), which comprises reacting a compound of formula (V) in the presence of a palladium catalyst to provide a compound of formula (VI), wherein the acid...
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7605134 |
4″-Deoxy-4″-(s)-amino avermectin derivatives
A description is given of compounds of the formula which in the 4″-position has the (S)-configuration and wherein R 1 is C 1 -C 12 alkyl, C 3 -C 8 cycloalkyl; or C 2 -C 12 alkenyl; R 2 is...
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7569576 |
Cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, compositions and uses thereof
The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl...
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7553979 |
HSP90-inhibiting zearalanol compounds and methods of producing and using same
Zearalanol compounds are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various disorders. Methods of...
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7553859 |
Macrocycles for the treatment of cancer
The present invention relates to new Macro-cycles of Formula (I), and their use for the treatment of cancer.
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7550503 |
Physiologically active substances
The present invention relates to a compound represented by the formula (I):
(wherein, R 3 , R 6 , R 7 and R 21 are the same as or different from one another and each represents a hydroxyl...
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7521474 |
Biologically active lasonolide compounds
The subject invention provides novel compositions of biologically active macrolide compounds which can advantageously be used in blocking cellular proliferation, treatment of cancer, treatment of...
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7470720 |
Methods and compositions for use in treating cancer
The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as cancer.
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7470719 |
Metastable benzoxepne derivatives which can be used in the treatment of dyslipidaemia a therosclerosis and diabetes, pharmaceutical compositions comprising them and processes for the preparation thereof
The present invention relates to novel metastable derivatives of benzoxepines of the formula (I) in which n represents 0, 1 or 2; and the radicals R, which may be identical or different, are alkyl...
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7465753 |
Glycoside-containing liposome
A drug product which can maximize the effect of a cholestanol glycoside useful as an anticancer agent. The present invention provides a liposomal composition containing a glycoside exhibiting...
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7459480 |
Benzodioxepine derivatives
This invention relates to compounds of the formula
wherein B, X, Y, Z, R 1 and R 2 are as defined in the description, and pharmaceutically acceptable salts thereof. The invention further...
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7456212 |
Storage stable cyclic ketone peroxide compositions
The present invention relates to peroxide compositions comprising one or more cyclic ketone peroxides, one or more dialkyl peroxides, and, optionally, one or more conventional phlegmatisers. These...
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7452915 |
Antiparasitic artemisinin derivatives (endoperoxides)
This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite,...
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7439264 |
Therapeutic compounds
This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding...
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7435754 |
Laulimalide microtubule stabilizing agents
A method of inhibiting the proliferation of a hyperproliferative mammalian cell having a multiple drug resistant phenotype utilizing an amount of a laulimalide compound effective to disrupt the...
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7417155 |
Artemisinine derivatives, and uses thereof for treating malaria
A new artemisinin derivatives, of following general formula (I):
In which: a and b represent a single or a double bond, n1 and n2 represent 0 or 1, R 1 represents a fluoroalkyl group or a...
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7410997 |
Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
Compounds represented by formula (1),
wherein X is, for example, CH, CH 2 , CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the...
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7407984 |
Tetraoxaspriro anti-malarials
The present invention is to provide an antimalarial agent having excellent antimalarial activity with little side effects, in particular, having remarkable antimalarial activity against...
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7402609 |
Olopatadine formulations for topical administration
Topical formulations of olopatadine for treatment of allergic or inflammatory disorders of the eye and nose are disclosed. The aqueous formulations contain approximately 0.17-0.62% (w/v) of...
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7399782 |
Polyether brevetoxin derivatives as a treatment for cystic fibrosis, mucociliary dysfunction, and pulmonary diseases
Disclosed are compounds that are derivatives of brevetoxin, or PbTx, pharmaceutical formulations comprising the compounds, and methods of regulating mucus transport in a cell, treating mucociliary...
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7390831 |
Tetracyclic steroid derivatives useful as progesterone receptor modulators
The present invention is directed to tetracyclic steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a...
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RE40387 |
Pharmaceutical compositions, dosage forms and methods for oral administration of epothilones
The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have...
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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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7381744 |
Method of treating osteoporosis comprising vacuolar-type (H+)-ATPase-inhibiting compounds
The present invention provides vacuolar-type (H+)-ATPase-inhibiting compounds, compositions thereof, and methods of using them to treat or prevent a condition treatable by the inhibition of a...
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7381743 |
Macrocycles for the treatment of cancer
The present invention relates to new macrocycles of the general formula (I) as well as their use for the treatment of cancer diseases
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7378399 |
Avermectins substituted in the 4″ and 4′-positions having pesticidal properties
What is described are a compound of the formula (I) Wherein A-B is —CH═CH— or —CH 2 —CH 2 —; n is 0 or 1; R 1 , is C 1 -C 12 alkyl, C 3 -C 8 cycloalkyl or C 2 -C 12 alkenyl; R 2 and R...
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7375099 |
Malonamide derivatives
The invention relates to malonamide derivatives of formula
wherein each of the variables are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The...
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7365095 |
Chromane and chromene derivatives and uses thereof
Compounds of formula I or pharmaceutically acceptable salts thereof are provided:
wherein each of R 1 , R 2 , R 3 , R 4 , y, m, n, and Ar are as defined, and described in classes and subclasses...
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7358275 |
Internal 1,15-lactones of fluprostenol and related prostaglandin F2a analogs and their use in the treatment of glaucoma and intraocular hypertension
Novel derivatives of prostaglandin compounds of the F-series (PGF), specifically macrocyclic internal 1,15-lactones of fluprostenol and related PGF analogs, such as cloprostenol or latanoprost. The...
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7351736 |
Therapeutic compositions (II)
Method of producing a physiologically acceptable ketosis such as to treat a patient in need of therapy for one or more of Amylotrophic lateral sclerosis, Free Radical disease, Heart failure and...
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7329654 |
Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders...
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7320974 |
Cytoskeletal active compounds, compositions and use
The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical...
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RE39991 |
Fungicidal heterocyclic aromatic amides and their compositions, methods of use and preparation
A compound having the following formula:
wherein R 3 and M are defined herein, and processes therewith.
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7312203 |
1-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof
The present invention relates to 1-aza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to...
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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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7244594 |
Microbial transformation method for the preparation of an epothilone
A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or...
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7241804 |
Compositions and methods for modulating apoptosis in cells over-expressing Bcl-2 family member proteins
The present invention provides agents and compositions for modulating the apoptotic state of a cell. The agents comprise derivatives of antimycins which bind to an anti-apoptotic Bcl-2 family...
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7241755 |
Epothilone derivatives
The present invention relates to compounds of the formula
in which the variables G, W, Q, X, Y, B 1 , B 2 , Z 1 , Z 2 , and R 1 –R 7 are as defined herein, methods for the preparation of the...
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7214705 |
Bafilomycin-like metabolite from a novel micromonospora species
The invention provides a compound of formula (I) and pharmaceutically acceptable salts thereof. Processes for the isolating of this bafilomycin metabolite from a novel Micromonospora species,...
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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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RE39592 |
Extended release growth promoting two component composition
An extended release composition comprising a first composition comprising growth promoters and a second composition comprising growth promoters and a biodegradable polymer is described. A method of...
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7205332 |
Deoxoartemisinin analogs, process for their preparation, and anticancer agent comprising them
The present invention relates to a new deoxoartemisinin dimer and trimer, which have excellent anticancer activity and lower toxicity and are stable to acids, to a new deoxoartemisinin monomer of...
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7202271 |
Fused pentacyclic polyethers
Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds.
wherein R, OR 1 , and R 2 are as defined herein.
Also...
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7189757 |
Treatment of sleep disorders using CNS target modulators
The invention is directed to compositions used for treating Central Nervous System (CNS) disorders. In addition, the invention provides convenient methods of treatment of a CNS disorder....
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7176235 |
Epothilone derivatives and methods for making and using the same
This invention relates to compounds of formula (I)
and to pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , W, X, Y, and Ar are as defined herein....
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7176234 |
Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis
The present invention is directed to derivatives of gambogic acid and analogs thereof. Exemplary gambogic acid derivatives of the present invention include, among others, derivatives substituted in...
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7166583 |
1,3-diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof
The present invention relates to 1,3-diaza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well...
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7160898 |
Pharmacological treatment for sleep apnea
The present invention relates to pharmacological methods for the amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess...
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7151116 |
Apoptolidin analogs and derivatives for inducing apoptosis in transformed cells
The invention provides novel apoptosis-inducing compounds that include isolated, purified isoapoptolidin, and selectively functionalized isoapoptolidin derivatives and stereoisomers thereof;...
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