"What, sir, would you make a ship sail against the wind and currents by lighting a bonfire under her deck? I pray you, excuse me, I have not the time to listen to such nonsense."
Napoleon Bonaparte ; When told of the Robert Fulton steamboat
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| Number | Title | Issue Date |
| 7351721 | Amino acid derivatives and pharmaceutical composition comprising, as active ingredients, them The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-... | 04/01/2008 |
| 7265145 | Substituted piperidines and pyrrolidines as calcium sensing receptor modulators and method Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula wherein m is 0, 1, 2, 3 or 4; each X is indepe... | 09/04/2007 |
| 7166590 | Amino acid derivatives A compound of the formula (I): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO,... | 01/23/2007 |
| 7160732 | Fluorescein-based metal sensors, and methods of making and using the same The present invention is directed, in part, to fluorescein-based ligands for detection of metal ions, and methods of making and using the same. ... | 01/09/2007 |
| 7101874 | Antimicrobial dihydrothiazine and dihydrothiopyran oxazolidinones The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof wherein Y is —S(═O)n—, —S(═NR8)—, or —S(═NR8)(═O)—; Z is ... | 09/05/2006 |
| 7053212 | Acyclic amide and sulfonamide ligands for the estrogen receptor The present invention provides estrogen receptor (ER) ligands of structural formula (I) the pharmaceutically acceptable salts, stereoisomers, and prodrugs thereof, and the pharmaceutically acceptable salts of the... | 05/30/2006 |
| 6756370 | Piperidine alcohols The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, imp... | 06/29/2004 |
| 6689909 | Substituted N-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity A compound of formula (I) wherein: n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is as defined within; R3 is as defined within; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable sa... | 02/10/2004 |
| 6579982 | Pyrimidine-2,4,6-trione metalloproteinase inhibitors The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula ##STR1## wherein X, Y, Ar1, Z, R1, R2 and R3 are as defined in the specification, and to pharmaceutical compos... | 06/17/2003 |
| 6569888 | Anti-inflammatory indole derivatives Compounds of formula (I) or a pharmaceutically acceptable salt, in vivo hydrolysable ester, or an N--C1-6 alkyl or N,N-di-(C1-6 alkyl)amide thereof, where X is CH2 or SO2 ; R1 is an aryl optionally su... | 05/27/2003 |
| 6355634 | Aromatic compounds The invention relates to novel compounds of the formula ##STR1## in which R1 is C1-4 alkyl and (Y--X) is CH2, C1-2 alkylthio-CH.dbd. or C1-2 alkyl-ON.dbd. and Z is an aldimino or ketimino group, and t... | 03/12/2002 |
| 6335334 | Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them The present invention relates to compounds of the formula I ##STR1## wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the ther... | 01/01/2002 |
| 6265575 | Antithrombotic diamines This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparat... | 07/24/2001 |
| 6225311 | Acetylenic -amino acid-based sulfonamide hydroxamic acid tace inhibitors Compounds of the formula: ##STR1## are useful in treating disease conditions mediated by TNF-, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.... | 05/01/2001 |
| 6183726 | Versatile hydrophilic dyes The sensitivity and specificity of the optical modality can be enhanced by the use of highly absorbing dyes as contrast agents. Novel cyanine dyes that absorb and emit light in the near infrared region of electromagnetic spectrum are disclosed. These dyes... | 02/06/2001 |
| 6172058 | Compounds with pharmaceutical properties A pharmaceutical compound of the formula ##STR1## in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cyclo... | 01/09/2001 |
| 6124332 | Metalloproteinase inhibitors Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.... | 09/26/2000 |
| 6124333 | Metalloproteinase inhibitors Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.... | 09/26/2000 |
| 6117869 | Compounds for and methods of inhibiting matrix metalloproteinases The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds ##STR1## More particularly, the present invention relates to a method of treati... | 09/12/2000 |
| 6107508 | Convergent synthesis of -aryl-ଲ-ketonitriles The present invention relates to processes for the production of -aryl-ଲ-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) rece... | 08/22/2000 |
| 6017902 | Boron containing amino acid compounds and methods for their use The present invention provides new boron containing amino acid compounds and methods for making these compounds by contacting melphalan or another nitrogen mustard derivative and sodium borocaptate. The present invention also provides a method of treating... | 01/25/2000 |
| 6008223 | Therapeutic compounds Compounds of formula I ##STR1## wherein Q1, Q2, Q3, and Q4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP a... | 12/28/1999 |
| 5929077 | Thioproline-containing inhibitors of farnesyl protein transferase Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected b ##STR1## its enantiomers, diastereomers, and pharmaceutically acceptable salts and solvates thereof.... | 07/27/1999 |
| 5922706 | Morpholine and thiomorpholine tachykinin receptor antagonists Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of ca... | 07/13/1999 |
| 5780625 | 4-aminophenol derivatives A description is given of novel O-phenol-substituted aminophenol derivatives of the formula ##STR1## in which the symbols are as defined in claim 1, which can be used in particular as stabilizers for magenta couplers in color-photographic record... | 07/14/1998 |
| 5763438 | 2-acylaminopropanol compound and medical composition This invention relates to a 2-acylaminopropanol compound represented by the formula (I): ##STR1## (wherein R1 represents a phenyl group which may be substituted by 1 to 3 same or different substituents selected from alkyl, alkoxy, hydroxyl... | 06/09/1998 |
| 5731309 | Substituted heteroalkyleneamine neurokinin antagonists Compounds of formula I ##STR1## wherein Q1, Q2, Q3, and Q4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP a... | 03/24/1998 |
| 5719147 | Morpholine and thiomorpholine tachykinin receptor antagonists Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of ca... | 02/17/1998 |
| 5674864 | N-substituted derivatives of -mercapto alkylamines, their preparation process and the intermediates obtained, their use as medicaments and the compositions containing them Novel -mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein the substituents are as defined in the specification.... | 10/07/1997 |
| 5672615 | Arylsulfonamido-substituted hydrodxamic acids Disclosed are the compounds of formula I ##STR1## wherein R and R1 together with the chain to which they are attached or R1 and R2 together with the carbon atom to which they are attached form a ring; pharmaceutically... | 09/30/1997 |
| 5641778 | Aromatically substituted ω-amino-alkanoic acid amides and alkanoic acid diamides Compounds of formula I ##STR1## wherein R1 is a 2-RA -3-RB -phenyl radical, a 2-RA -4-RC -phenyl radical, a 2-RA -pyridin-3-yl radical, a 3-RA -pyridin-2-yl radical or a 1-R... | 06/24/1997 |
| 5552543 | Six-membered hetero "N" compounds Novel six-membered hetero "N" compounds having antibiotic activity, represented by the formula: ##STR1## where X.dbd.S, O, CH2, or Se Y.dbd.OH, NH2, NHCOR9, or SH R1,R2,R3,R4,R | 09/03/1996 |
| 5552419 | Arylsulfonamido-substituted hydroxamic acids The invention relates to the compounds of formula I ##STR1## pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and a ... | 09/03/1996 |
| 5543433 | Azine-substituted phenylacetic acid derivatives and fungicides containing these Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro, Y is an amino, methylamino or dimethylamino group, Z is a group CHCH3, CHOCH3 or NOCH3, R is hydrogen or alk... | 08/06/1996 |
| 5516789 | Lipoxygenase and cyclooxygenase inhibiting compounds Compounds having the structure ##STR1## or a pharmaceutically acceptable salt thereof have activity as inhibitors of cylooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B4, C4, D4, and E4 | 05/14/1996 |
| 5476850 | Amino-substituted benzenesulfonylureas and -thioureas and their use as pharmaceuticals There are described amino-substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## The compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmias and can ther... | 12/19/1995 |
| 5472974 | Benzimidazole derivatives, agricultural and horticultural fungicides containing the same as an active ingredient and intermediate compounds thereof A benzimidazole derivative having the formula, ##STR1## wherein R is cyano or thiocarbamoyl; Q is lower alkyl or a group represented by the formula NQ1 Q2, in which Q1 and Q2 are independently lower alkyl, ... | 12/05/1995 |
| 5451394 | Quaternary salts of para-dialkylamino benzamide derivatives This invention relates to non-hydrolyzable, non-irritating, hair, skin and textile substantive quaternary ammonium salts of a para-dialkylamino benzamide having the formula ##STR1## wherein R' and R" are each selected from the group of C1 ... | 09/19/1995 |
| 5411959 | 1,4-Thiomorpholino-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension Compounds characterized generally as 1,4-thiomorpholinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## ... | 05/02/1995 |
| 5354862 | Preparation and the use of halopropargylated cyclic quaternary ammonium compounds as antimicrobial agents Antimicrobial compounds of the formula ##STR1## wherein R is selected from (A)(C1 to C20) straight or branched alkyl, optionally substituted with hydroxy, halogen, alkoxy, phenoxy, or --C(.dbd.O)R' wherein R' is selected from C | 10/11/1994 |