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7618989 |
Tricyclic oxazolidone derivatives useful as PR modulators
Compounds of the following structure are described:
wherein R 1 -R 6 , R 16 , m, V, W, X, Y, and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug...
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7601846 |
Compounds having activity as inhibitors of apoptosis
The present invention provides compounds that can protect mammalian cells from the damaging effects of chemotherapy, irradiation, or in other situations in which it is desirable to protect tissue...
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7582665 |
Compounds exhibiting thrombopoietin receptor agonism
Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and...
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7538129 |
Diazonamide A analog
A specific diazonamide A analog and its salts and conjugates are effective in treating proliferative diseases.
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7517895 |
Synthetic diazonamides
The application discloses novel synthetic compounds, modeled after unique toxins extracted from the marine invertebrate Diazona angulata useful in the treatment abnormal cell mitosis. The...
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7517995 |
Thiazolyl-dihydro-cyclopentapyrazole
Disclosed are compounds of general formula (I),
wherein the groups R 1 , R 2 , R a and R b have the meanings given in the claims and specification, the tautomers, racemates, enantiomers,...
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7485655 |
2-Aminothiazole allosteric enhancers of A1 adenosine receptors
The present invention relates generally to a class of 2-aminothiazole derivatives which have recently been identified as allosteric enhancers of the A 1? adenosine receptor. These compounds, and...
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7470714 |
GM-95-containing antitumor effect potentiator, combined antitumor preparation and antitumor agent
An antitumor effect enhancer for enhancing the antitumor effects of an antitumor substance, which comprises a compound represented by the following formula (1):
wherein each R independently...
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7407977 |
Substituted N-acyl-2-aminothiazoles
There are presented compounds of the formula
or a pharmaceutically acceptable salt thereof, which are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.
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7319096 |
Thyroid hormone receptor antagonists for cardiac and metabolic disorders II
This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders,...
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7312237 |
Combination of epothilone analogs and chemotherapeutic agents for the treatment of prolilferative diseases
Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders.
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7300949 |
Thiazolopyrazoles and methods of their use
This invention concerns novel thiazolopyrazole compounds and compositions comprising them. Methods of using these compounds for the treatment, prevention and management of various diseases and...
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7294641 |
Heterocyclic compound for stimulating or inducing the growth of the hair or eyelashes and/or slowing down their loss, composition comprising it and its uses
Heterocyclic compounds useful for stimulating/inducing the growth of keratinous fibers, notably human hair/eyelashes, and/or slowing the loss of same, have the following structural formula (I) or...
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7250429 |
Aminomethyl-substituted thiazolobenzimidazole compounds
This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned...
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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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7230019 |
Imidazo [2,1-b]-1,3,4-thiadiazole sulfonamides
This invention relates to compounds of Formula (I) and the use of compounds of Formula (I) as neuroprotective agents in the treatment of neuronal disorders of the central and peripheral nervous...
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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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7132436 |
Inhibitors of 11-β-hydroxy steroid dehydrogenase type 1
The present invention relates to compounds with the formula (I) and also to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the...
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7125887 |
Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula (I), (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 and R 8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor...
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7115632 |
Sulfonyl aryl or heteroaryl hydroxamic acid compounds
A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a...
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7105529 |
Substituted oxindole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors and compositions and methods of treating chemotherapy and radiation therapy side effects
Compounds of formula (I): wherein X is N, CH, CCF 3 , or C(C 1-12 aliphatic); R 4 is sulfonic acid, C 1-12 aliphatic-sulfonyl, sulfonyl-C 1-12 aliphatic, C 1-12 aliphatic-sulfonyl-C 1-6 ...
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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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7067516 |
Serine protease inhibitors
Compounds of formula (I)
where R 5 , R 6a , each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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7022721 |
Method and composition for rejuvenating cells, tissues, organs, hair and nails
In one embodiment, the present invention relates to compounds and compositions including pharmaceutical compositions containing the compounds and associated methods that uncouple sugar-mediated...
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7022720 |
Synthetic diazonamides as novel anti-mitotic agents
The application discloses novel synthetic compounds, modeled after unique toxins extracted from the marine invertebrate Diazona angulata useful in the treatment abnormal cell mitosis. The...
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6936628 |
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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6864254 |
Inhibitor for 20-hete-yielding enzyme
An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is...
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6858607 |
7,8-fused 4H-chromene and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 4H-chromene and analogs thereof, represented by the general Formula I:
or pharmaceutically acceptable salts or prodrugs thereof, wherein:
...
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6706744 |
Glucagon antagonists/inverse agonists
Novel compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for...
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6689777 |
Anti-malarial compounds, compositions and methods
The present invention is directed to substituted naphthothiazolium, aromatic guanylhydrazones, and other compounds and compositions with anti-malarial activity useful for the treatment and...
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6669926 |
Hydrophilic light absorbing indole compounds for determination of physiological function in critically ill patients
Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function...
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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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6555540 |
Combinations of aldose reductase inhibitors and selective cyclooxygenase-2 inhibitors
This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or...
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6498176 |
3-(anilinomethylene) oxindoles as protein tyrosine kinase and protein serine/threonine kinase inhibitors
Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase...
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6489354 |
3-alkyl substituted pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4c , R 4d , and R 4f are defined herein) which are useful as modulators of chemokine...
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6476059 |
Use of polycyclic 2-aminothiazole systems for the treatment of obesity
The invention relates to the use of polycyclic 2-aminothiazole systems and their physiologically tolerated salts and physiologically functional derivatives for the treatment of obesity. The...
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6444669 |
8,8A-DIHYDROINDENO&lsqb 1,2-D&rsqb THIAZOLE DERIVATIVES WHICH CARRY IN THE 2-POSITION A SUBSTITUENT HAVING A SULFONAMIDE STRUCTURE OR SULFONE STRUCTURE; PROCESSES FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS
8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as...
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6426341 |
Treatment for diabetic complications
This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or...
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6410578 |
Benzazole compounds and their use
The present invention discloses a method for repelling insects, mites and ticks from warm-blooded animals with a benzazole compound.
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6410577 |
Substituted 8,8a-dihydro-3ah-indeno&lsqb 1,2-d&rsqb thiazoles, processes for their preparation and their use as medicaments
The invention relates to substituted 8,8a-dihydro-3aH-indeno[1,2-d]thiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in...
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6399638 |
12,13-modified epothilone derivatives
The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.
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6387935 |
Polycyclic dihydrothiazoles having substituted alkyl radicals in the two-position, process for their preparation, and their use as pharmaceuticals
The invention relates to polycyclic dihydrothiazoles, and to their physiologically acceptable salts and physiologically functional derivatives. The compounds are according to formula I: in which...
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6387919 |
Substituted oxindole derivatives as protein tyrosine kinase and as protein serine/threonine kinase inhibitors
Compounds of formula (I): wherein X is N, CH, CCF 3 , or C(C 1-12 aliphatic); R 4 is sulfonic acid, C 1-12 aliphatic-sulfonyl, sulfonyl-C 1-12 aliphatic, C 1-12 aliphatic-sulfonyl-C 1-6 ...
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6380200 |
Combination of aldose reductase inhibitors and selective serotonin reuptake inhibitors for the treatment of diabetic complications
This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or...
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6369086 |
Substituted oxidole derivatives as protein tyrosine and as protein serine/threonine kinase inhibitors
The present invention relates generally to novel substituted oxindole compounds and compositions. Such compounds and compositions have utility as pharmacological agents in treating diseases or...
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6329407 |
Use of polycyclic thiazole systems for the treatment of obesity
The invention relates to the use of polycyclic thiazole systems and their physiologically tolerated salts and physiologically functional derivatives for the treatment of obesity. The treatment...
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6329373 |
Metalloproteinase inhibitors
A compound of formula (I) ##STR1## wherein X is a --CONHOH group and the R groups are defined in the claims. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation...
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6303643 |
Substituted indoles and uses thereof
This invention is directed to indole and benzothiazole compounds which are selective for cloned human alpha 2 receptors. This invention is also related to uses of these compounds for any indication...
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6291486 |
Polycyclic Dihydrothiazoles, their preparation and use as pharmaceuticals
Polycyclic dihydrothiazoles, processes for their preparation, and their pharmaceutical uses are provided. Preferred compounds are represented by the formula I ##STR1## wherein the radicals may have...
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6291494 |
2-aminothiazol-fused 2-aminoindans and 2-aminotetralins and their use
The invention relates to 2-aminothiazol-fused 2-aminoindans and 2-aminotetralins having general formula (1): wherein R 1 and R 2 , which may be identical or different, are selected from the group...
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