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| Number | Title | Issue Date |
| 7390798 | Carboxamide spirolactam CGRP receptor antagonists The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in... | 06/24/2008 |
| 7317037 | Progesterone receptor modulators comprising pyrrole-oxindole derivatives and uses thereof Pyrrole-oxindole derivatives useful as progesterone receptor antagonists, and methods for preparing the same, are provided. Pharmaceutical compositions containing these derivatives are described, as is the use thereof in contraception and hormone-related conditions.... | 01/08/2008 |
| 7314932 | Methods for minimizing thioamide impurities Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided. ... | 01/01/2008 |
| 7309787 | Kinase inhibitors The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. ... | 12/18/2007 |
| 7205328 | Oxindoles with anti-HIV activity The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell... | 04/17/2007 |
| 7169774 | Cephalotaxane derivatives and their processes of preparation and purification The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constit... | 01/30/2007 |
| 7056910 | 1,4,5.6-tetrahydroimidazo[4,5-d]diazepine derivatives or salts thereof To provide a compound having a superior arginine vasopressin antagonism. A novel 1,4,5,6-tetrahydroimidazo[4,5-d]benzazepine derivative or a pharmaceutically acceptable salt thereof. ... | 06/06/2006 |
| 6951848 | Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor Disclosed are novel compounds having the formula or a physiologically acceptable salt, amide, ester or prodrug thereof. The compounds can be used to modulate (antagonize, agonize) chemokine receptor function. Also disc... | 10/04/2005 |
| 6911463 | 3-substituted oxindole β-3 agonists The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity. ... | 06/28/2005 |
| 6908926 | Substituted imidazoles, their preparation and use Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compoun... | 06/21/2005 |
| 6884895 | Process for the preparation of spiro[(4-cyclohexanone)-[3]indol]-2′[1′H]-one derivatives The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of the general formula I wherein R1 and R2 independently stand for hydrogen... | 04/26/2005 |
| 6825220 | 3-Substituted oxindole β 3 agonists The present invention relates to a β;3 adrenergic receptor agonist of formula I: (1); or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity. ... | 11/30/2004 |
| 6822094 | Spiro compounds and their use Spiro compounds of the formula (I), in which at least one of the radicals K1, L, M, N1, R1, R2, R3, R4 is one of the following groups ... | 11/23/2004 |
| 6806283 | Selective serotonin receptor antagonists and therapeutic applications thereof Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of 5-HT2 serotonin receptors. The compounds are useful as anti... | 10/19/2004 |
| 6638942 | Spiro-indolines as Y5 receptor antagonists Compounds of general structural formula I ##STR1## are selective NPY Y5 receptor antagonists, useful in the treatment of obesity and the complications associated therewith.... | 10/28/2003 |
| 6573386 | Process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2'[1'H]-one derivatives The invention relates to a process for the preparation of spiro [(4-cyclohexanone)-[3H]indol]-2'[1'H]-one derivatives of general formula I--wherein R1 and R2 independently stand for hydrogen, C1-4 alkyl, C1-4 al... | 06/03/2003 |
| 6562857 | Cyanopyrroles This invention provides a progesterone receptor agonist of formula 1 having the structure ##STR1## wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 | 05/13/2003 |
| 6548679 | Antitumor agents The present invention provides compounds of general formula I or II: ##STR1## wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceu... | 04/15/2003 |
| 6541643 | Process for the preparation of spiro[cis-4-(ଲ-hydroxyethyloxy)cyclohexane-[3h]indol]-2'[1'H]one derivatives The invention relates to a process for the preparation of spiro[cis-4-(ଲ-hydroxyethyloxy)cyclohexane-[3H]indol]-2'[1'H]-one derivatives of the formula (I) wherein R1 and R2 are as defined herein, by reduction of a dispiro[... | 04/01/2003 |
| 6444819 | Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic subs... | 09/03/2002 |
| 6441019 | Cyclocarbamate and cyclic amide derivatives This invention provides compounds of the formula: ##STR1## wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both ... | 08/27/2002 |
| 6358887 | 2-Phenyl-substituted heterocyclic 1,3-ketonols as herbicides and pesticides The present invention relates to new compounds of the formula (I) ##STR1## in which X, Y and Z have the meanings given in the description and Het represents one of the groups ##STR2## in which A, B, D and G have the meanings given in the description, a plurali... | 03/19/2002 |
| 6358750 | Spiro[pyrrolidine-2,3'-oxindole] compounds and method of use The invention provides spiro[pyrrolidine-2,3'-oxindole] compounds and libraries of these compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, -amino acids, and dipolarophiles (e.g., trans-chalcones, acryl... | 03/19/2002 |
| 6355648 | Thio-oxindole derivatives This invention relates to compounds which are agonists of the progesterone receptor which have the general structures: ##STR1## wherein: R1 and R2 are H, alkyl, substituted alkyl; OH; O(alkyl); O(substituted alkyl); OAc; aryl; substi... | 03/12/2002 |
| 6156783 | Spiroazabicyclic compounds, processes for their preparation, and their pharmaceutical use Novel azabicyclic derivatives, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.... | 12/05/2000 |
| 6114540 | Spiro[pyrrolidine-2,3'-oxindole] compounds and methods of use The invention provides spiro[pyrrolidine-2,3'-oxindole] compounds produced by the stereo- and regio-selective reaction of variously substituted isatins, -amino acids, and dipolarophiles (e.g., trans-chalcones, acrylate esters, or vinyl oxindoles).... | 09/05/2000 |
| 6110872 | 2,4,5-trisubstituted phenylketo-enols for use as pesticides and herbicides The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups ##STR1## wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate produc... | 08/29/2000 |
| 6090818 | Indolin-2-one derivatives, method for preparing them and pharmaceutical compositions containing them The invention relates to compounds with formula (I), a process for their preparation and pharmaceutical compositions containing them. These compounds have an excellent affinity for vasopressin and/or oxytocin ##STR1##... | 07/18/2000 |
| 6046341 | 3-spiro-indolin-2-one derivatives The subject of the invention is indolin-2-one derivatives of formula: ##STR1## in which: W represents a --CH2 -- or --SO2 -- group; Cy forms, with the carbon to which it is bonded, a non-aromatic, saturated or unsaturated C3 | 04/04/2000 |
| 5948807 | Spiroindanamines and Spiroindanimides Compounds of formula I: ##STR1## wherein R1, R2, W, X, Y and Z have any of the values defined in the specification, and their pharmaceutically acceptable salts, are inhibitors of monoamine re-uptake and are useful for treating d... | 09/07/1999 |
| 5942532 | 2-substituted phenyl-benzimidazole antibacterial agents The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhib... | 08/24/1999 |
| 5849780 | 1-benzenesulfonyl-1-1,3-dihydroindol-2-one derivatives, their preparation and pharmaceutical compositions in which they are present The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an ... | 12/15/1998 |
| 5808071 | Pictet-Spengler reaction for the synthesis of tetrahydroisoquinolines and related heterocyclic compounds A commercial scale process for the production of tetrahydroisoquinolines and related heterocyclics by reaction, in mildly acidic conditions, of aryl N-sulfonylethylamines in the presence of a suitable Lewis acid, and a compound capable of in situ generati... | 09/15/1998 |
| 5773448 | Pharmaceutical compounds A pharmaceutical compound of the formula ##STR1## and salts and esters thereof.... | 06/30/1998 |
| 5756532 | Aminomethyl-2 3 8 9-tetrahydro-7H-1 4-dioxino2 3-E!-indol-8-ones and derivatives The compounds of formula I: ##STR1## wherein R1 and R2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R1 and R2, taken together, are benzylidene optionally substituted with R3 as defin... | 05/26/1998 |
| 5723625 | Process for the production of specific isomer mixtures from oxindole alkaloids To produce defined isomer mixtures of compounds with spirocyclic beta-aminocarboxyl and/or beta-aminocarbonyl systems the invention supposes that they be dissolved in solvents which have good dissolving power for these compounds, whose relative permittivi... | 03/03/1998 |
| 5696145 | 1-benzyl-1,3-dihydroindol-2-one derivatives, their preparation and the pharmaceutical compositions in which they are present The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and ... | 12/09/1997 |
| 5618833 | 1-benzyl-1,3-dihydroindol-2-one derivatives, their preparation and the pharmaceutical compositions in which they are present The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula (I). The invention also relates to preparation of these derivatives as well as to the pharmaceutical compositions in which they are present. These derivatives have... | 04/08/1997 |
| 5616705 | N-substituted azabicycloheptane derivatives, their preparation and use Compounds of the formula I ##STR1## where the substituents have the meanings given in the description, and their preparation are described. The novel compounds are suitable for the control of diseases.... | 04/01/1997 |
| 5462913 | Substituted 1-H-3-aryl-pyrrolidine-2,4-dione derivatives The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle, X represents alkyl, halogen or alkoxy, Y repr... | 10/31/1995 |
