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Class 514/411 - Tricyclo ring system having the five-membered hetero ring as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the polycyclo ring system consists
No. of patents: 876
Last issue date: 04/17/2012


1                      
NumberTitleIssue Date
8158670Therapeutic inhibitor of vascular smooth muscle cells
Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associa...
04/17/2012
8143304(3-amino-1,2,3,4-tetrahydro-9 -carbazol-9-yl)-acetic acid derivatives
The present invention relates to (3-amino-1,2,3,4-tetrahydro-9H-carbazol-9-yl)-acetic acid derivatives of Formula (I) wherein R1, R2, R3, R4, R5 and R6 are as described in the description and their us...
03/27/2012
8143303Carbazole derivatives as functional 5-HTligands
Carbazole derivatives of formula (I), useful in treatment of a CNS disorders related to or affected by the 5-HT6 receptor are described. The pharmacological profile of these compounds includes high affinity binding with 5-HT6 receptor along wit...
03/27/2012
8124644Carvedilol phosphate
The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical comp...
02/28/2012
8114900Amorphous carvedilol dihydrogen phosphate
The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical comp...
02/14/2012
8110596Triprenyl phenol compound, process for production of triprenyl phenol compound, and thrombolysis enhancer
The present invention provides a triprenyl phenol compound represented by the following formula (II) and (III) and having a thrombolysis-enhancing activity, and an efficient method for producing the triprenyl phenol compound. In formula (II) and (III), R1
02/07/2012
8097642Therapeutic inhibitor of vascular smooth muscle cells
Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associa...
01/17/2012
8093283Solid forms comprising (+)-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisinoline-1,3-dione, compositions thereof, and uses thereof
Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of tr...
01/10/2012
8067456Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs)
The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends...
11/29/2011
8063093Potassium channel blockers and uses thereof
The invention relates to compounds of Formula (1) for use in modulating potassium channel activity in cells. ...
11/22/2011
8026269Isoindoline compounds and methods of making and using the same
The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel...
09/27/2011
8026270Benzo [F] isoindoles as EP4 receptor agonists
The present invention relates to naphthalene derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. ...
09/27/2011
8022094Carvedilol phosphate
The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical comp...
09/20/2011
7981919Tricyclic heteroaryl piperazines, pyrrolidines and azetidines as serotonin receptor modulators
The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydroazepinoi...
07/19/2011
7968586Cytotoxic compounds and conjugates
The present disclosure provides cytoxic compounds useful as drugs or prodrugs and to drug-cleavable substrate conjugates where the drug and cleavable substrate are optionally linked through a self-immolative linker. ...
06/28/2011
7968587Tetrahydrocyclopenta[b]indole compounds as androgen receptor modulators
The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treat...
06/28/2011
7956080Deuterium-enriched SDX-101
The present application describes deuterium-enriched SDX-101, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. ...
06/07/2011
7935722Tetrahydrocarbazole derivatives useful as androgen receptor modulators
The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient...
05/03/2011
7906545Prodrugs of CC-1065 analogs
Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the pr...
03/15/2011
7906546Tetrahydrocarbazoles and derivatives
The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defin...
03/15/2011
7893101Solid forms comprising (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions thereof, and uses thereof
Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of tr...
02/22/2011
7893100Carvedilol phosphate salts and/or solvates thereof, corresponding compositions, and/or methods of treatment
The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen...
02/22/2011
7879899Injectable veterinary composition for small animals
An injectable aqueous composition for veterinary use containing a non-steroidal anti-inflammatory compound in an amount of from about 0.25 to 30% (w/v) together with a physiologically acceptable oxygenated polymeric surfactant in an amount of from about 0.5 to 20% (...
02/01/2011
78799003-aminocarbazole compounds, pharmaceutical composition containing the same and method for the preparation thereof
A compound of formula (I), in which R1, R2, R3, R4, R5, R6, X and Y have the meanings indicated in the description, and the pharmaceutically acceptable salts thereof. A pharmaceutical composition containing a compound of formula (I) or a pharmaceutically acceptable ...
02/01/2011
7868034Use of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods
This invention is directed to indolone derivatives which are antagonists or the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier...
01/11/2011
7825154Small molecule inhibitors of botulinum neurotoxins
Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain i...
11/02/2010
7786162Agents useful for reducing amyloid precursor protein and treating dementia and methods of use thereof
The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering s...
08/31/2010
7763645Carvedilol dihydrogen phosphate monohydrate
Disclosed herein is crystalline carvedilol dihydrogen phosphate monohydrate having high aqueous solubility and the process for preparation thereof. The invention further discloses methods for treating hypertension, congestive heart failure and angina in a mammal, us...
07/27/2010
7759384Carvedilol phosphate salts and/or solvates thereof, corresponding compositions, and/or methods of treatment
The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen...
07/20/2010
7750036Carvedilol salts, corresponding compositions, methods of delivery and/or treatment
The present invention relates to a salt of carvedilol and/or corresponding solvates thereof, compositions containing such carvedilol and/or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease sta...
07/06/2010
7718689Benzoisoindole derivatives and their use as EP4 receptor ligands
A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein R1 to R8, X, and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical c...
05/18/2010
7718688Nitrobenzindoles and their use in cancer therapy
The present invention relates generally to nitro-1,2-dihydro-3H-benzo[e]indoles and related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other...
05/18/2010
7714016Cytotoxic compounds and conjugates with cleavable substrates
The present disclosure provides drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-cleavable substrate conjugates, and to methods of treatment using them. ...
05/11/2010
7671079Sulfonyltetrahydro-3H-benzo(e)indole-8-amine compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a CNS disorder related to or affected by the 5-HT6 receptor. ...
03/02/2010
7655687Anti-inflammatory analgesic for external use
An objective of the present invention is to provide an anti-inflammatory analgesic for external use comprising etodolac as NSAID. The anti-inflammatory analgesic for external use is excellent not only in skin permeability but also in penetratability and diffusivity ...
02/02/2010
7655688Fused cyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds. ...
02/02/2010
7649010Carvedilol hydrobromide
The present invention relates to a salt of carvedilol, corresponding compositions containing such a carvedilol salt or corresponding solvates thereof, and/or methods of using the aforementioned compound(s) in the treatment of certain disease states in mammals, in pa...
01/19/2010
7635709Compositions and methods for bowel care in individuals with chronic intestinal pseudo-obstruction
The present disclosure provides compositions and methods for on-going bowel care for persons with chronic intestinal pseudo-obstruction. The compositions and methods can be administered in a non-clinical setting. The compositions comprise acetylcholinesterase inhibi...
12/22/2009
7622494Chemical compounds
The present invention relates to compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds. ...
11/24/2009
7618994Fluoro substituted cycloalkanoindoles, compositions containing such compounds and methods of treatment
Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases. ...
11/17/2009
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