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6719540 |
C3-cyano epothilone derivatives
The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by formula I: wherein: Q is selected from the group consisting of M is...
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6716457 |
Effects of bactericide (peracetic acid-hydrogen peroxide-water combination) to agricultural chemicals in bacteria control when they are in contact with one another
The present invention relates to a process for inhibiting or eliminating the growth of microorganisms in pesticide suspensions. More particularly, the process of the present invention includes the...
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6716843 |
Alpha-amino acid sulphonyl compounds
Compound of formula (I): wherein: represents an optionally substituted, 5-membered, nitrogen-containing heterocycle, R 1 represents hydrogen, alkyl, acyl, prolyl, alanyl, histidylprolyl or...
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6716871 |
Cyclic AMP-specific phosphodie sterase inhibitors
Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases...
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6716881 |
Carbanilides used as pesticides
The present invention provides carbanilides of formula (I), wherein A, Q, R, X, Z and m are as defined herein. A plurality of processes for preparing these compounds is provided, along with...
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6713498 |
Method for treating glaucoma VI
Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the...
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6713050 |
Method and composition for rejuvenating hairs, nails, tissues, cells and organs by ex-vivo or immersive treatment
A method and composition for the treatment of hair, nail, ex-vivo organ, ex-vivo cell or ex-vivo tissue to improve the biomechanical and diffusional characteristics comprising an effective amount...
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6710062 |
Cyanomethylene compounds, process for producing the same, and agricultural or horticultural bactericide
The cyanomethylene compound of the invention is a compound represented by the formula (1) wherein R is C 1-20 straight-chain or branched-chain alkyl, C 3-8 cycloalkyl, aryl or heterocyclic...
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6710063 |
Activators of PPAR delta
Compounds of Formula (1) are disclosed. These compounds include selective activators of human PPAR delta.
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6710056 |
Amidinophenylpyruvic acid derivatives
An amidinophenylpyruvic acid derivative of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an excellent antagonistic effect against activated blood...
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6706718 |
3-(2,4-dimethylthiazol-5-yl)indeno&lsqb 1,2-c&rsqb pyrazol-4-one derivatives and their uses
The present invention relates to 3-(2,4-dimethylthiazol-5-yl)indeno[1,2-c]pyrazol-4-ones of formula I: which are potent inhibitors of cyclin dependent kinases. This invention also provides a...
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6706743 |
β3 adrenergic receptor agonists and uses thereof
The instant invention provides β 3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds,...
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6706742 |
Alpha-amino-acid compounds
Compound selected from those of formula (I): wherein: represents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single...
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6703403 |
Method for improving pharmacokinetics
A method is disclosed for improving the pharmacokinetics of a drug which is metabolized by cytochrome P450 monooxygenase.
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6699860 |
Di-substituted aminomethyl-chroman derivative beta-3 adrenoreceptor agonists
This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.
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6699898 |
Substituted N,N-disubstituted non-fused heterocyclo amino compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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6699894 |
Methods for treatment of inflammatory bowel disease
Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of inflammatory bowel disease.
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6696437 |
Heterocyclically substituted benzimidazoles, the production and application thereof
The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
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6689794 |
Aromatic sulfone hydroxamates and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known...
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6689803 |
Compositions and methods for treating surgical adhesions
Methods and compositions for treating or preventing inflammatory diseases such as psoriasis or multiple sclerosis are provided, comprising the step of delivering to the site of inflammation an...
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6689788 |
Method and composition for treatment of inflammatory bowel disease
A composition in unit dosage form for the inhibition, prevention or treatment of inflammatory bowel disease comprising an effective amount of a compound having the formula: and a...
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6685617 |
Inhibitors of α4β1 mediated cell adhesion
The present invention relates to compound of formula (I), that are potent inhibitors of α 4 β 1 mediated adhesion to either VCAM or CS-1 and which could be useful for the treatment of...
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6686380 |
Treatment of refractory tumors using epothilone derivatives
Methods of treating tumors in a mammal, especially a human that has demonstrated resistance to other chemotherapeutic agents, is disclosed. Specifically, methods of the present invention are...
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6683100 |
Organic compounds
Pharmaceutical formulations comprising an epothilone in the form of an infusion concentrate or a lyophilised composition, and methods of administration of an epothilone in suitable form for...
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6683078 |
Use of sulfonyl aryl or heteroaryl hydroxamic acids and derivatives thereof as aggrecanase inhibitors
This invention is directed to a process for inhibiting aggrecanase activity. The process comprises administering a therapeutically effective amount of a sulfonyl aromatic or heteroaromatic...
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6680311 |
Cryptophycin compounds
The present invention provides cryptophycin compounds of Formula I that are useful in the treatment of neoplasms.
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6677353 |
Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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6677341 |
(R)-Chiral halogenated substituted heteroaryl benzyl aminoalcohol compounds useful for inhibiting cholesteryl 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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6673368 |
Colonic motor dysfunction remedies comprising aminothiazole derivatives as active ingredients
Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system....
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6673821 |
Nitrogen heterocycle inhibitors of aspartyl protease
Nitrogen heterocycles that inhibit aspartyl protease are disclosed, as are methods of treating diseases, particularly HIV, using these compounds. The compounds have the formula: A representative...
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6670384 |
Methods of administering epothilone analogs for the treatment of cancer
A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 50% by volume tertiary-butanol in water, the...
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6667328 |
Therapeutic agents for diabetes
This invention relates to therapeutic agents for diabetes comprising a 2-(N-cyanoimino)thiazolidine-4-one derivatives represented by formula I or a solvate or a pharmaceutically acceptable salt...
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6664277 |
Prenylation inhibitors containing dimethylcyclobutane and methods of their synthesis and use
The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical...
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6656711 |
Fermentative preparation process for and crystal forms of cytostatics
The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new...
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6656954 |
Sulfonyl divalent aryl or heteroaryl hydroxamic acid compounds
A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises...
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6653309 |
Inhibitors of IMPDH enzyme technical field of the invention
The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions...
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RE38330 |
Preventing and reversing advanced glycosylation endproducts
The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a...
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6653335 |
Pharmaceutical composition for inhibiting the growth of viruses and cancers
This invention is a method of treating cancer, both carcinomas and sarcomas, and viral infections, in particular HIV through the administration of a pharmaceutical composition containing a...
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6653321 |
Naphthylsulfonic acids and related compounds as glucose uptake agonists
Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or...
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6649649 |
Method of treating colonic adenomas
This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a...
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6649643 |
Imidazol-4-ylmehanols and their use as inhibitors of steroid C17-20 lyase
Imidazol-4-ylmethanols and their uses for preventing and treating primary tumors, metastasis and recurrence of tumors, various symptoms accompanying tumors, prostatic hypertrophy, virilism,...
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6642234 |
Acrylonitrile compounds
The present invention relates to acrylonitrile compounds of formula (1): [wherein, R is a C 1 -C 6 alkyl, a C 3 -C 7 cycloalkyl optionally substituted by a C 1 -C 4 alkyl, a naphthyl, etc., R...
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6635667 |
Methods of treatment using MAO-A and MAO-B inhibitors such as L-deprenyl
Effects of MAO-A or MAO-B inhibitors such as L-deprenyl on both cerebral and peripheral vasculature, on non-vascular smooth muscle, on the nervous system, and on platelets, RBC, WBC, mast cells,...
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6635666 |
Cancer treatment with epothilones
The invention relates to the treatment of a proliferative disease, especially according to certain treatment regimens, with an epothilone, especially with epothilone A and more preferably...
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6632830 |
ACE-2 inhibiting compounds and methods of use thereof
ACE-2 inhibiting compounds are disclosed. These compounds include compounds of formula (IV): wherein the variables are as described in the specification. Pharmaceutical compositions containing...
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6627624 |
Aryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 , are variables defined...
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6624182 |
Hydroxyphenylvinylthiazoles
The use of hydroxyphenylvinylthiazoles of formula wherein R 1 , R 2 , R 3 and R 4 are each independently of the others hydrogen; halogen; hydroxy, C 1 -C 16 -alkyl, C 1 -C 16 alkoxy, phenyl;...
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6610716 |
Cyanomethyl substituted thiazoliums and imidazoliums and treatments of disorders associated with protein aging
Provided, among other things, is a compound of the formula:
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6610717 |
Dihydropyridine derivatives
Dihydropyridine derivatives represented by the following formula: analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type...
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6608070 |
2,3-substituted indole compounds as anti-inflammatory and analgesic agents
This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the...
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