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6753316 |
Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each...
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6743816 |
Imidazole derivatives with anti-inflammatory activity
Novel imidazole derivatives of formula I and their salts, solvates and prodrugs, wherein the meanings of the different radicals are as shown in the description. Said compounds are useful as...
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6743793 |
Indole derivatives, process for preparation of the same and use thereof
Indole derivatives represented by formula (I): (wherein all symbols are described in the description), a process for the preparation of the same and a DP receptor antagonist comprising it as an...
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6743817 |
Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R 1 and R 2 are defined herein. These compounds are highly selective agonists,...
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6740672 |
Use of 5HT3-receptor antagonists for the treatment of chronic fatigue syndrome
5HT 3 -receptor-antagonists for the treatment of CFS (Chronic Fatigue Syndrome) are disclosed.
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6716605 |
Indole derivatives having an antiviral activity
A compound of the formula: wherein R 1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R 2 is hydrogen, lower alkyl, or optionally substituted aralkyl, or the...
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6706735 |
2-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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6699883 |
Pyrroloimidazole derivatives and their use as medicaments
The present invention relates to 3-pyrroloimidazole derivatives of the general formula (I) wherein the imidazole radical is an optionally substituted imidazole ring, X, Y, A and B are, each...
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6689787 |
Method of using an integrin antagonist and radiation therapy as combination therapy in the treatment of neoplasia
The present invention provides methods to treat neoplasia disorders in a mammal using a combination of radiation and an integrin antagonist.
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6686388 |
Regulators of the hedgehog pathway, 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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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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6664283 |
Pharmaceuticals for neurogenic pain
This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be...
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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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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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6649613 |
Diacylhydrazine derivatives
Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R 1 , 2 and R 3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin...
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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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6635630 |
Selective neurokinin antagonists
Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar 1 and Ar 2 are optionally substituted heteroaryl or optionally substituted phenyl; X 1 ...
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6632840 |
Monoacyl-substituted guanidines, a process for their preparation, their use as a medicament or diagnostic aid, and pharmaceutical compositions containing them
Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) is
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6630498 |
Eprosartan arginyl charge-neutralization-complex and a process for its preparation and formulation
This invention relates to (E)-α-[2-n-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-
yl]methylene-2-thiophenepropionic acid arginyl charge-neutralization-complex, a process for its production,...
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6630489 |
Quinoline derivatives as tyrosine kinase inhibitors
The invention concerns quinoline derivatives of formula (I) wherein n is 0-3 and each R 4 , which may be the same or different, is a substituent such as halogeno, hydroxy, amino, nitro,...
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6620826 |
Endothelin receptor antagonists
Novel N-phenyl imidazole derivatives, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
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6610664 |
Cationic lipids
The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The...
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6610687 |
Benzofuranylsulfonates
The invention relates to benzofuranylsulfonates of the general formula (I), their preparation and their use for the treatment of inflammation.
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6610722 |
Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic macrocyclic compounds that inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed...
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6610724 |
3-Aminopyrazole inhibitors of cyclin dependent kinases
The present invention describes compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds are protein kinase inhibitors and are useful in the treatment of...
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6605637 |
Lipoic acid derivatives, their preparation, and pharmaceutical compositions containing them
The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration...
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6602896 |
p38MAPK inhibitor and uses thereof
The present invention demonstrates that p38 MAPK inhibitor induces low density lipoprotein receptor expression 6-8 fold, and further provides the application of such inhibitor in the treatment of...
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6596738 |
Heterocyclic compound, composition and method for inhibiting adenosine deaminase
Heterocyclic compounds of the following formula: wherein B is [wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen or lower alkyl; and X is hydrogen or hydroxy protective group], lower...
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6596745 |
Method for treating fibrotic diseases with azolium chroman compounds
Provided is a method of treating or ameliorating hypertension in an animal comprising administering an effective amount of a compound of formula I:
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6593336 |
Methods for treating irritable bowel syndrome
This invention relates to the use of 5-HT3 receptor antagonists in the treatment of nonconstipated female IBS patients.
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6585963 |
Nail compositions and methods of administering same
Nail compositions and methods of use thereof are disclosed. Additionally, nail kits comprising a nail composition and pre-treatment compositions are disclosed. Further, supportive devices such as...
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6586445 |
β-carboline compounds
The present invention is directed to compounds of the formula wherein the variables are defined in the specification, which bind to somatostatin receptors and block Na channels.
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6586447 |
3,3-disubstituted-oxindole derivatives useful as anticancer agents
The present invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein n is 0 or 1 and R 1 , R 2 , R 3 , R 4 , and R 5 are as...
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6576656 |
Oxindole derivative
An oxindole of Formula 1 or a prodrug thereof, or a pharmaceutically acceptable salt thereof is useful for growth hormone releaser: wherein R 1 , R 2 , R 3 and R 4 are independently hydrogen,...
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6573267 |
Useful aroyl aminoacyl pyrrole compounds
This invention is directed to aroyl aminoacyl pyrroles pharmaceutically useful as agents and modulators for the treatment of central nervous system disorders and a method for the treatment of...
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6569883 |
Medicaments
The invention relates to the use of compounds of the general formula (I) wherein R 1 represents a hydrogen atom or a C 1-10 alkyl, C 3-7 cycloalkyl, C 3-7 cycloalkyl-(C 1-4 )alkyl, C 3-6 ...
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6569868 |
2-indolinone derivatives as modulators of protein kinase activity
The present invention relates to novel imidazoly 2-indolinones and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to...
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6566369 |
Medicament containing cilansetron for the treatment of non-obstipative male irritable bowel syndrome patients
The present invention relates to the use of cilansetron for the treatment of non-obstipative male IBS patients.
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6566385 |
Inhibitors of prenyl-protein transferase
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed...
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6555546 |
Use of 5HT3 antagonists for promoting intestinal lavage
The present invention is concerned with the use of 5HT 3 antagonists for promoting intestinal lavage, especially in combination with an osmotic agent.
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6552051 |
Energetic nitramine-linked azoles and related compounds as oxidizers, initiators and gas generators
Novel compounds are provided having the structural formula R[—N(NO 2 )—L—R 1 ] n wherein R, L, R 1 and n are defined herein. The compounds are useful in a variety of contexts, but are...
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6544975 |
Substituted porphyrins
The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby...
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6541505 |
Substituted (aminoiminomethyl or aminomethyl) benzoheteroaryl compounds
This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a...
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6517836 |
Nitrophenylaziridine compounds and their use as prodrugs
A range of aziridin-1-yl nitrobenzamides are provided for use as prodrugs in conjunction with nitroreductase (NR) enzymes. The amides may have 1 or 2-substituents which may be bulky and polar. For...
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6518257 |
1-substituted phenyl-1-(1h-imidazol-4-yl) alcohols, process for producing the same and use thereof
To provide a composition having a steroid C 17,20 -lyase inhibitory activity and useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer. A compound...
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6518281 |
Immunotherapeutic agents
Novel amides and imides are inhibitors of tumor necrosis factorα and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory...
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6514966 |
Compounds for the treatment of obesity
NPY antagonists, methods of using such NPY antagonists and pharmaceutical compositions containing such NPY antagonists. The NPY antagonists are useful for the treatment of NPY mediated...
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6509336 |
Imidazolyl derivatives
The present invention is directed to imidazolyl derivatives of formula (II), wherein the variables are defined in the specification, which are useful as prenyl transeferase inhibitors.
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6503938 |
2-phenylindoles as antiestrogenic pharmaceutical agents
2-phenylindoles are described, as well as a process for making them, pharmaceutical preparations that contain them, methods of using them as pharmaceutical agents.
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