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7592350 |
Polycyclic compounds as potent alpha2-adrenoceptor antagonists
A compound of formula I,
wherein X, Z, R 1 to R 10 , R 15 , R 16 , m, n, r and t are as defined in claim 1, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2...
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7541463 |
Sulfur-containing naphthalimide derivatives
The invention discloses novel sulfur-containing naphthalimide derivatives, and the preparation and uses thereof. The conjugated plane of naphthalimide derivatives of the invention is enlarged by...
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7511064 |
Derivatives of 4-(thio- or selenoxanthene-9-ylidene)-piperidine or acridine and its use as a selective 5-HT2B receptor antagonist
The present invention relates to derivatives of 4-(Thio- or Selenoxanthene-9-ylidene)-piperidine or acridine and pharmaceutically acceptable salts thereof, use of these compounds as a medicament...
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7510830 |
Cancer treatment by combination therapy
Methods and compositions are provided for treating cancer, the methods including the step administering, either sequentially or simultaneously, (i) a compound of the xanthenone acetic acid group of...
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7482360 |
Fused tetracyclic mGluR1 antagonists as therapeutic agents
In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate...
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7476676 |
Methods for increasing bone formation using inhibitors of glycogen synthase kinase-3β
This invention relates to the use of inhibitors of glycogen synthase kinase-3β to increase bone formation.
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7465742 |
Heterocyclic compounds having anti-HBV activity
This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to...
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7432276 |
ABCA1 elevating compounds
The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of...
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7388016 |
Dibenzonaphthyridine derivatives and methods of use thereof
The present invention relates to Dibenzonaphthyridine Derivatives, compositions comprising an effective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a...
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7354927 |
6H-[1]benzopyrano[4,3-b]quinolines and their use as estrogenic agents
This invention provides 6H-[1]benzopyrano[4,3-b]quinoline compounds having the formula I:
The invention further provides compositions including the compounds, methods for the use of the...
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7307080 |
Compounds, methods and pharmaceutical compositions for treating cellular damage, such as neural or cardiovascular tissue damage
The disclosure relates to compounds, pharmaceutical compositions and methods for inhibiting PARP by use of the disclosed compositions. The compounds of the disclosure have the following structures...
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7253179 |
Fused heterocyclic compounds
Compounds, compositions and methods are provided that are useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor. In particular, the compounds...
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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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7199130 |
Substituted 5,6,6a, 11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxylic acid compounds as NMDA-antagonists
Substituted 5,6,6a,11b-tetrahydro-7-oxa-5-aza-benzo[c]fluorene-6-carboxy
lic acid compounds, and processes for the production thereof, pharmaceutical compositions containing these compounds and the...
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7163946 |
5-substituted 7,9-difluoro-5H-chromeno[3,4-f]quinoline compounds as selective progesterone receptor modulator compounds
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by progesterone receptor. Also provided are methods of making such...
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7135478 |
Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
A compound of the formula
wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.
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7125885 |
Fused heterocyclic compounds
The present invention provides compounds having the formula:
wherein R 1 , R 2 , R, R′ and the subscript p are described herein. The compounds are useful in the treatment and/or prevention of...
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7084151 |
5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-5H-chromeno[3,4-ƒ]quinolines as selective progesterone receptor modulator compounds
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such...
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7071205 |
5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by Progesterone Receptor. Also provided are methods of making such...
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6992089 |
Nitro and amino substituted topoisomerase agents
The invention provides compounds of formula I:
wherein R 1 -R 9 , W, and X have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also...
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6989388 |
Thieno[2,3-c]iosquinolines for use as inhibitors of PARP
The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula:
wherein the constituent variables are...
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6984641 |
Carboline derivatives as PDE5 inhibitors
Selective inhibitors of cGMP-specific PDE, and use of the compounds and salts and solvates thereof as therapeutic agents, are disclosed.
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6967215 |
Tetrahydrocarbazoles, a process for the preparation of those compounds, and the use thereof
Tetrahydrocarbazoles of formula
where Q is —SO 2 —; —O—; or —(CO)—; X is —(CH)—; or —N—; m is from 1 to 3; t is 0 or 1 and the remaining substituents are as defined herein,...
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6960585 |
Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same
Compounds of formula (I), or pharmaceutically-acceptable salts thereof, are useful in treating inflammatory and immune diseases and disorders,
wherein X, Y 1 , Y 2 , and R 2- 4 are as...
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6946472 |
Polycyclic compounds exhibiting anti-tumor activities
This invention is concerned with novel polycyclic compounds of formula [I],
wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Y, R 1′ , R 2′ , R 3′ , R 4′ , R 5′ , R 6...
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6921768 |
Cytostatic cerium compounds
The invention relates to cerium compounds having general formulas (I) R n i+ Y i n− and (II) R b + Y b + and their application as medicaments in the prophylaxis and/or treatment of cancer...
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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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6893668 |
Process for isolation of anticancer agent camptothecin from Nothapodytes foetida
The present invention relates to an improved and economical process for the isolation of anticancer agent Camptothecin from the twigs and stem of Nothapodytes foetida using hot extraction 20(S)...
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6858624 |
Aryl fused azapolycyclic compounds
This invention is directed to compounds of the formula (I):
and their pharmaceutically acceptable salts, wherein R 1 , R 2 , and R 3 are as defined herein; intermediates for the synthesis of...
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6858620 |
Condensed pyridoindole derivatives
Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosed
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6858619 |
Fused heterocyclic compounds
Compounds useful in the treatment and/or prevention of a condition or disorder mediated by a G-protein coupled receptor are provided that have the formula:
wherein
A and B are CR′; V...
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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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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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6825209 |
Compounds having unique CB1 receptor binding selectivity and methods for their production and use
Compounds are provided that are amide analogs of SR141716A having unique CB1 receptor selectivity and providing WIN sparing binding characteristics, pharmaceutical compositions containing the...
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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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6696459 |
Steroid receptor modulator compounds and methods
Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds,...
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6680326 |
Polycyclic compounds
Novel polycyclic compounds of the formula [I], wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts...
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6630481 |
Viologen linked acridine based molecule and process for the preparation thereof
The present invention provides a series of novel bifunctional molecules based on viologen linked acridine, bisacridine and bisacridinium salts of the general formula 1 (1a, 1b, 1c and 1d) and or...
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6608076 |
Camptothecin derivatives and polymeric conjugates thereof
Polymeric conjugates of camptothecin derivatives having increased circulating half-lives are disclosed. In preferred aspects, the E ring lactone of the camptothecin derivative is opened and...
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6562328 |
Fatty quat based on ante-iso compounds
The invention discloses quaternary ante-iso acids useful as additives in personal care products. Various quaternary derivatives of ante-sio acids are described, and examples of their use in...
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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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6534516 |
Androgen receptor modulator compounds and methods
Non-steroidal compounds that are high affinity, high selectivity modulators for androgen receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds,...
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6506766 |
Glucocortiocoid-selective antinflammatory agents
Compounds having Formula I are useful for partially or fully antagonizing, repressing, agonizing, or modulating the glucocorticoid receptor and treating immune, autoimmune and inflammatory...
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6486167 |
Heterocyclic cytotoxic agents
The present invention provides compounds of formula I: wherein the R substituents and atoms X and Y are as defined in specification. The present invention also provides pharmaceutical...
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6469019 |
Therapeutic application of nicergoline
The invention concerns the use of nicergoline for preventing and/or treating motor neuron diseases.
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6448255 |
Imidazo-isoquinolin-5-one derivatives, pyrimido-isoquinolin-6-one derivatives and imidazo-naphthyridin-5-one derivatives
Antiatherosclerotic compounds are provided which have the following structure: wherein: R is hydrogen, lower alkyl, alkenyl, alkynyl, aryl, heteroaryl, or aryl or heteroaryl substituted with one...
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6440988 |
Use of agonists or antagonists of the 5-HT7 receptor to treat disorders of the bladder
The present invention provides a method of treating urinary incontinence in a subject which comprises administering to the subject a therapeutically effective amount of a 5-HT 7 receptor...
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6436971 |
Use of PDE 4-specific inhibitors to reduce the severity of a bacterial infection after a respiratory viral infection
This invention relates to a method for the prophylaxis of or reducing the severity of post-viral bacterial infection by administering a PDE 4-specific inhibitor prior to or during the course of a...
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6436951 |
Camptothecin tetracyclic analogues, preparation, method, applications as medicines and pharmaceutical compositions containing them
The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which...
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6420377 |
Covalent conjugates of topoisomerase I and topoisomerase II inhibitors
The present invention provides covalent conjugates of topoisomerase I and topoisomerase II inhibitors. Such compounds have a structure according to formula I: T I —L—T II (I) wherein: T I ...
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