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7612082 |
Prostaglandin EP4 antagonists
Disclosed herein are methods and compositions related to compound 1 or compound 2
or pharmaceutically acceptable salts, or prodrugs thereof, which are antagonists of a prostaglandin EP 4 ...
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7531550 |
Pseudobase benzo[c]phenanthridines with improved efficacy, stability, and safety
Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I
are provided herein. The variables R, R 1 , R 2 , R 3 , and R 4 are defined herein. Certain...
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7446110 |
17-Heterocyclic-4-azasteroid derivatives as androgen receptor modulators
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment...
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7410977 |
Fluorinated 4-azasteroids as androgen receptor modulators
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment...
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7381722 |
Tetracyclic amino and carboxamido compounds and methods of use thereof
The present invention relates to Tetracyclic Amino Compounds and Tetracyclic Carboxamido Compounds, compositions comprising an effective amount of a Tetracyclic Amino Compound or a Tetracyclic...
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7354926 |
Molecules derived from noraporphine
The invention concerns novel molecules derived from noraporphine, as well as cosmetic and dermopharmaceutical compositions containing one or several of said derivatives, alone or combined with a...
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7351698 |
Androgen receptor modulators and methods of use thereof
Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation,...
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7332503 |
Aporphine esters and their use in therapy
New aporphine derivatives are disclosed which have formula (I) and the physiologically acceptable salts thereof. Said derivatives may be used for the treatment of Parkinson's disease, hemicrania,...
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7312229 |
21-Heterocyclic-4-azasteroid derivatives as androgen receptor modulators
Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue...
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7312228 |
Cytotoxic indeno and isoindoloisoquinolones
The synthesis and biological activity of benzoisoindoloisoquinolone compounds are described. The synthesis and biological activity of C-11-substituted indenoisoquinolones are also described....
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7276513 |
Steroidal compounds for inhibiting steroid sulphatase
There is provided a compound of formula XII, wherein G is H or a substituent, and wherein R 1 is a sulphamate group.
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7220754 |
Mono-ester and asymmetrically substatuted di-ester pro-drugs of dopamide D1 receptor agonists
Mono-ester and asymmetrically substituted diesters of dihydrexidine, dinapsoline and A-86929 and substituted derivatives thereof are described. The novel ester/diester derivatives exhibit improved...
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7217720 |
17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while...
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7217709 |
Tetracyclic benzamide derivatives and methods of use thereof
The invention relates to Tetracyclic Benzamide Derivatives; compositions comprising a Tetracyclic Benzamide Derivative; and methods for treating or preventing an inflammatory disease, a reperfusion...
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7186728 |
Methylene-4-azasteroids
17-methylene-4-azasteroid compounds of formula I:
wherein R 20 denotes fluoro, chloro or bromo R 20a denotes hydrogen, R 10 and R 4 each denote a hydrogen atom or a methyl group, and R 1 ...
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7138389 |
Oral androgen therapy using modulators of testosterone bioavailability
This invention provides methods of treating a mammalian subject in need of androgen therapy by orally administering to the subject testosterone, a testosterone ester, or a testosterone precursor in...
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7122534 |
Aryl fused azapolycyclic compounds
The present invention relates to compounds of formula (I)
and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 and Z are as defined herein, intermediates in the synthesis of...
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7098218 |
Steroidal compounds for inhibiting steroid sulphatase
There is provided a compound having Formula (I) wherein G is H or a substituent, and wherein R 1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group...
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7091212 |
Chiral dinapsoline
The present invention relates to the preparation of the optical isomer (R)-(+)-8,9-dihydroxy-2,3,7,11b-tetrahydro-1H-napth[1,2,3-de
]isoquinoline. This invention also relates to the use of...
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7071158 |
Antioxidant enhancement of therapy for hyperproliferative conditions
A method to enhance the cytotoxic activity of an antineoplastic drug comprising administering an effective amount of the antineoplastic drug to a host exhibiting abnormal cell proliferation in...
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RE39056 |
4-Azasteroids for treatment of hyperandrogenic conditions
Compounds of structural Formula (I)
and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type...
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6992088 |
Nitro and amino substituted heterocycles as topoisomerase I targeting agents
The invention provides compounds of formula I:
wherein: R 1 -R 5 , “a” and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The...
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6949561 |
Steroid 3-O-sulphamate derivatives as inhibitors of oestrone sulphatase
A sulphamate compound suitable for use as an inhibitor of oestrone sulphatese (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the...
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6916823 |
Method of treatment of dopamine-related dysfunction
The present invention relates to the treatment of dopamine-related dysfunction using full D 1 dopamine receptor agonists in an intermittent dosing protocol with a short, but essential,...
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6897222 |
Pyrido[2,1-a]isoquinoline derivatives
The present invention provides compounds of formula (I):
wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification, and pharmaceutically acceptable salts thereof. The...
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6844353 |
Fungicidal properties of sampangine and its analogs to agriculturally important fungal plant pathogens
It has been found that sampangine and related analogs such as benzo[4,5]sampangine, 4-bromosampangine and 4-methoxysampangine may be used as effective fungicidal agents for plants. Fungicidal plant...
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6844320 |
Treatment of preeclampsia, toxemia and preterm labor with combination of progestational agent and a nitric oxide synthase substrate and/or donor
Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both,...
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6828319 |
Substituted indeno&lsqb 1,2-c&rsqb isoquinoline derivatives and methods of use thereof
The invention provides novel classes of substituted Indeno[1,2-c]isoquinoline Compounds. Pharmaceutical compositions and methods of making and using the compounds, are also described.
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6825208 |
Tetrahydroquinoline derivatives as antithrombotic agents
This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine...
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6818635 |
7-substituted tetracycline compounds
The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states,...
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6756407 |
Method and compositions for the treatment or amelioration of female sexual dysfunction
The present invention provide a method of treating sexual dysfunction in a female, including the vasculogenic symptoms of delayed vaginal engorgement, diminished vaginal lubrication, pain or...
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6747038 |
Phenanthridine derivatives and antitumoral medicaments containing phenanthridine
The invention relates to novel phenanthridine derivatives and to medicaments, which are for use in antitumoral therapy and prophylaxis and which contain these phenanthridine derivatives. It could...
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6740660 |
Nasal delivery of apomorphine
Intranasal delivery methods and compositions for the delivery of dopamine receptor agonists are provided which are effective for the amelioration of erectile dysfunction in a mammal without causing...
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6723730 |
Capsaicin receptor ligands
Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin...
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6706704 |
Method of inducing opioid analgesia and anesthesia without respiratory suppression
The invention is directed to a pharmaceutical composition and a corresponding method for inhibiting respiratory depression in a mammalian subject during treatment with opiates. The composition...
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6699676 |
Uses of ouabain and ouabain-like molecules in apoptosis related pathologies
Longterm elevation of the intracellular Na + /K + ratio inhibits macromolecule synthesis and proliferation in the majority of cell types studied so far, including vascular smooth muscle cells...
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6686371 |
Non-steroidal, tetracylic compounds for estrogen-related treatments
The invention provides non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having...
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6667056 |
Pharmaceutical compositions containing an effervescent acid-base couple
A pharmaceutical formulation in the form of a fast dissolving tablet comprising an active ingredient, sodium glycine carbonate and an acid capable of reacting rapidly with sodium glycine carbonate...
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6645975 |
Process for the preparation of dinaposoline
The present invention relates to a novel process for the preparation of compounds of the formula wherein R 1 , R 2 , R 4 , R 5 , R 6 and A are as defined herein, and to certain derivations of...
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6645974 |
Androgen receptor modulators and methods for use thereof
Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation,...
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6632419 |
Increasing libido in humans via acute testosterone administration
The libido of adult human female patients is increased by the bolus delivery of a testosterone which is preferably dihydrotestosterone. The formulation is preferably aerosolized and inhaled into a...
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6630482 |
CFTR channel activator compounds and pharmaceutical compositions containing same
CFTR channel activator compounds from the benzo[c]quinolizinium family or families of compounds derived therefrom, as well as pharmaceutical compositions containing said compounds, and the uses...
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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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6583152 |
Composition for reducing the risk or progression of cardiovascular diseases
Elevated levels of homocysteine have been implicated as an important risk factor for cardiovascular and other diseases. A composition for decreasing levels of plasma homocysteine and a method for...
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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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6566368 |
Apomorphine-containing dosage form for ameliorating male erectile dysfunction
Impotence can be ameliorated without substantial undesirable side effects by nasal administration of apomorphine, optionally with an antiemetic agent present in an amount sufficient to...
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6548515 |
Dihydrofuro&lsqb 3,4-b&rsqb quinolin-1-one compounds
The invention relates to compound of formula (I): wherein: represents a single or double bond, R 0 represents hydrogen or hydroxy or alkoxy, R 1 and R 2 , which are identical or different,...
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6545011 |
Substituted 4,9-dihydrocyclopenta&lsqb imn&rsqb phenanthridine-5-ones, derivatives thereof and their uses
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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6541483 |
Acridone-derived compounds useful as antineoplastic and antiretroviral agents
The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as...
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6528521 |
Treatment of anti-depression drug-induced sexual dysfunction with apomorphine
A method for treating sexual dysfunction that is caused by anti-depressant medication in a patient in need of such treatment, comprising administering a therapeutically effective amount of...
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