139results about How to "Less toxicity" patented technology

The present invention has identified compounds with extended aromatic chromophores that bind the G-quadruplex formed by the folding of single-stranded human telomeric DNA. These compounds have been shown to be effective telomerase inhibitors and are contemplated to be useful in developing cancer treatments. A model of cationic porphyrin interaction with quadruplex DNA by intercalation has been established and in combination with structure activity relations has provided novel porphyrin compounds that exhibit discrimination between binding duplex and quadruplex DNA and show improved activity against telomerase.

The present invention provides a polynucleotide delivery system including a cationic polymer to which a rabies virus glycoprotein (RVG) peptide is bound, wherein the cationic polymer includes a biodegradable bond, and a method of delivering polynucleotides to a target cell by using the delivery system.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom, etc.; R3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R3 is substituted by at least one substituent selected from the group consisting of substituents α; said substituents α is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents α, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atomsThese compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

This invention provides a compound of the formula (I): wherein R<1 >and R<2 >independently represent a hydrogen atom or the like; X represents a covalent bond or the like: A represents a bicyclic, aromatic, saturated or partially unsaturated heterocyclic or carbocyclic group having from 8 to 12 ring atoms; or the like: B represents a phenyl group or a heteroaryl group having from 5 to 6 ring atoms or the like: These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

Methods of using inhibitors of the CD2 / LFA-3 interaction in treating skin conditions characterized by increased T cell activation and abnormal antigen presentation in the dermis and epidermis in mammals, including humans. Such conditions include psoriasis, UV damage, e.g., photoaging, atopic dermatitis, cutaneous T cell lymphoma such as mycosis fungoides, allergic and irritant contact dermatitis, lichen planus, alopecia areata, pyoderma gangrenosum, vitiligo, ocular cicatricial pemphigoid, and urticaria.

The present invention is directed to methods for applying bovine foot and hoof treatment compositions having two or more specific and complimentary antimicrobial components in a hoof bath just prior to use to work more effectively. These antimicrobial components may include antimicrobial inorganic salts of certain heavy metals, cationic agents, peroxides, aldehydes, fatty acids, iodines or other suitable compounds effective in the killing of microorganisms.

This invention provides a compound of formula (I): wherein R1 represents an alkyl group having from 1 to 4 carbon atoms or a halogen atom, R2 represents an alkyl group having from 1 to 4 carbon atoms, R3 represents a hydrogen atom or a hydroxy group, and A represents an oxygen atom or a group of the formula —C(R4)(R5)— (in which R4 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and R5 represents a hydroxy group or an alkoxy group having from 1 to 4 carbon atoms) or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

The present disclosure provides a fusion protein comprising IL-1 receptor antagonist fused to a hybrid Fc. Particularly the present disclosure relates to a fusion protein comprising IL-1 receptor antagonist fused to a human immunoglobulin hybrid Fc fragment. In one embodiment, the hybrid Fc fragment comprises IgD and IgG4. Also provided is a pharmaceutical composition comprising the present fusion protein, which are useful for treating autoimmune disease including rheumatoid arthritis, inflammatory bowel disease (Crohn's disease, ulcerative colitis), psoriasis and diabetes and the like. The present fusion protein with excellent efficacy and reduced side effects is qualified for clinical development as therapeutic antibodies to treat autoimmune disease.

Specific binding members, particularly antibodies and fragments thereof, which bind to transforming growth factor beta 1 (TGF-β1) are provided, particularly recognizing human and mouse TGF-β1 and not recognizing or binding TGF-β2 or TGF-β3. Particular antibodies are provided which specifically recognize and neutralize TGF-β1. These antibodies are useful in the diagnosis and treatment of conditions associated with activated or elevated TGF-β1, including cancer, and for modulating immune cells and immune response, including immune response to cancer or cancer antigens. The anti-TGF-β1 antibodies, variable regions or CDR domain sequences thereof, and fragments thereof may also be used in therapy in combination with chemotherapeutics, immune modulators, or anti-cancer agents and / or with other antibodies or fragments thereof. Antibodies of this type are exemplified by the novel antibodies hereof, including antibody 13A1, whose sequences are provided herein.

This invention provides a compound of the formula (I):or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.

A medicinal preparation is desired which has no harmful side effects such as hypersensitive reaction, heightens the water solubility of a sparingly water-soluble anticancer agent, maintains a high drug concentration in the blood, accumulates a drug in a tumor tissue at a high concentration, heightens the pharmacological effect of the sparingly water-soluble anticancer agent, and diminishes the side effects of the anticancer agent. Provided are: a novel block copolymer which can be a drug carrier having no harmful side effects such as hypersensitive reaction; a micelle preparation in which micelles are formed and which contains a sparingly water-soluble anticancer agent, especially paclitaxel, incorporated in the micelles in an amount necessary for a disease treatment without bonding it to the block copolymer and which can heighten the solubility of the drug in water; and an anticancer agent which comprises the micelle preparation as a medical ingredient, maintains a high concentration in the blood, has more potent drug activity, and is reduced in toxicity.

The invention features methods and devices for local delivery of agents that modify glutamate-mediated neurotransmission to the inner ear for treatment of inner ear disorders caused by glutamate-induced hearing loss and / or tinnitus.

The invention features methods and devices for local delivery of agents that modify glutamate-mediated neurotransmission to the inner ear for treatment of inner ear disorders caused by glutamate-induced hearing loss and / or tinnitus.