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| Number | Title | Issue Date |
| 8153625 | Nitrogen-containing heterocyclic compounds and medicinal use thereof The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prev... | 04/10/2012 |
| 8063041 | Polymorphic Form D of bazedoxifene acetate and methods of preparing same The present disclosure relates to polymorphic Form D of bazedoxifene acetate, pharmaceutical compositions and methods of treatment using the same, and methods of preparing the same. ... | 11/22/2011 |
| 8034807 | Salts of bazedoxifene The invention deals with new crystalline salts of bazedoxifene, by means of which a high API quality can be achieved in a high yield. ... | 10/11/2011 |
| 8022063 | CRTH2 receptor ligands for medicinal uses Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl biois... | 09/20/2011 |
| 7989447 | 1,5 and 3,6-substituted indole compounds having NOS inhibitory activity The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other p... | 08/02/2011 |
| 7910576 | Pyrrole derivatives as P2Y12 antagonists The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated in the claims. The compounds of the formula I are valua... | 03/22/2011 |
| 7737137 | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme Methods for treating a mammal suffering from glucocorticoid-related diseases and conditions, comprising administering to the mammal an effective amount of a selective inhibitor of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme activity, wherein the inhibitor is ... | 06/15/2010 |
| 7683051 | Crystalline polymorph of bazedoxifene acetate The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof. ... | 03/23/2010 |
| 7683052 | Crystalline polymorph of bazedoxifene acetate The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof. ... | 03/23/2010 |
| 7666862 | Mitotic Kinesin Inhibitors The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which c... | 02/23/2010 |
| 7645752 | Sulfonyl substituted 1H-indoles as ligands for the 5-hydroxytryptamine receptors The present invention is directed to compounds of Formula I: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the in... | 01/12/2010 |
| 7612060 | Triazoles and methods of use Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for... | 11/03/2009 |
| 7504394 | Bazedoxifene ascorbate The present invention is directed to bazedoxifene ascorbate, compositions containing the same, dispersions thereof, preparations thereof, and uses thereof. ... | 03/17/2009 |
| 7435833 | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme A compound of formula (I): or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Methods of inhibiting 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. Methods of treating non-insul... | 10/14/2008 |
| 7407950 | -(heteroaryl)-1-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. | 08/05/2008 |
| 7405209 | Protease inhibitors The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co... | 07/29/2008 |
| 7393842 | Pyrazole analogs acting on cannabinoid receptors One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the i... | 07/01/2008 |
| 7375219 | Substituted indole compounds having NOS inhibitory activity The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other p... | 05/20/2008 |
| 7335677 | Inhibitors of dipeptidyl peptidase IV Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3 | 02/26/2008 |
| 7276518 | Substituted cyclohexane-1,4-diamine compounds Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds. ... | 10/02/2007 |
| 7235257 | Drugs for relieving hemicrania comprising 1-menthol and essential oils This invention relates to external drugs for dermal application which have a migraine-alleviating effect, in more detail ointments and patches comprising in mixing l-menthol and an essential oil into a base containing a hydrophilic high-molecular weight compound, a ... | 06/26/2007 |
| 7202237 | Pyridylether derivatives, their preparation and use The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the centra... | 04/10/2007 |
| 7179835 | 2-(3-sulfonylamino-2-oxopyrrolidin-1-yl)propanamides as factor xa inhibitors The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same. | 02/20/2007 |
| 7173024 | Compounds having prolyl oligopeptidase inhibitory activity, methods for their preparation and their use Compounds of the formula (I), wherein the symbol aa means a residue of an α-amino acid. The invention is also directed to a method for the preparation of the compounds of formula (I), as well as their use as pro... | 02/06/2007 |
| 7160877 | Aliphatic nitrogen-containing 5-membered ring compound The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, ... | 01/09/2007 |
| 7148249 | Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments The present invention relates to heterocyclically substituted indolinones of general formula wherein R1 to R5 and X are defined as in claim 1, the tautomers, the diastereomers, ... | 12/12/2006 |
| 7138392 | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: or which are useful in treat... | 11/21/2006 |
| 7105556 | Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2 | 09/12/2006 |
| 7071184 | Protease inhibitors The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel int... | 07/04/2006 |
| 7060719 | Glutaminyl based DPIV inhibitors The present invention provides compounds of the formula: wherein X=CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arth... | 06/13/2006 |
| 7034029 | 1-aryl- or 1-alkylsulfonyl-heterocyclylbenzazoles as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor ... | 04/25/2006 |
| 6982259 | N-heterocyclic derivatives as NOS inhibitors N-Heterocyclic derivatives of the following formula: where m, n, p, A1, R1, R2, R3 and R4 are described herein, as well as other N-heterocyclic derivatives, are us... | 01/03/2006 |
| 6974839 | Method of delaying ejaculation The invention provides a method of delaying ejaculation. The method comprises administering an effective amount of a tramadol material to a human male prior to sexual intercourse. The method is particularly useful for treating premature ejaculation. ... | 12/13/2005 |
| 6964973 | Bicyclic androgen and progesterone receptor modulator compounds and methods The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agon... | 11/15/2005 |
| 6887865 | N-heterocyclic derivatives as NOS inhibitors N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using the... | 05/03/2005 |
| 6887864 | Azepane derivatives This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their ... | 05/03/2005 |
| 6861432 | Piperazine derivatives that destabilize androgen receptors This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the inventio... | 03/01/2005 |
| 6849622 | Aliphatic nitrogenous five-membered ring compounds The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, | 02/01/2005 |
| 6767912 | Heterocyclylindazole and -azaindazole compounds as 5-hydroxytryptamine-6 ligands The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor. ... | 07/27/2004 |
| 6713473 | Tricyclic compounds A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and t... | 03/30/2004 |
