"That the automobile has practically reached the limit of its development is suggested by the fact that during the past year no improvements of a radical nature have been introduced."
Scientific American ; Jan. 2 edition, 1909
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| Number | Title | Issue Date |
| 7834003 | 5-aminopyrazole derivatives as pesticidal compounds The invention relates to 5-Aminopyrazole derivatives of formula (I) or salts thereof, a process for their preparation, to compositions thereof and to their use for the control of pests, including arthropods and helminths. ... | 11/16/2010 |
| 7781426 | CETP inhibitors Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds o... | 08/24/2010 |
| 7414048 | 4,5-dihydro-isoxazole derivatives and their pharmaceutical use The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, p... | 08/19/2008 |
| 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 |
| 7319097 | Compounds The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II... | 01/15/2008 |
| 7304052 | Substituted homopiperidinyl benzimidazole analogues as fundic relaxants The present invention relates to compounds of formula (I) their prodrugs, N-oxides, addition salts, quaternary amines and stereochemically isomeric forms, wherein the bivalent radical -{circle around (A)}- repres... | 12/04/2007 |
| 7300928 | Benzimidazolidinone derivatives as muscarinic agents Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the s... | 11/27/2007 |
| 7265103 | Substituted amino isoxazoline derivatives and their use as anti-depressants The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart o... | 09/04/2007 |
| 7229987 | Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obes... | 06/12/2007 |
| 7091199 | Thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives useful as d antagonists The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These condi... | 08/15/2006 |
| 7074765 | Synthetic peptide analogs of Arg-Pro-Pro-Gly-Phe as selective inhibitors of thrombin and thrombin activation of protease activated receptors 1 and 4 The invention relates to compounds and methods for inhibiting human platelet aggregation, thrombosis and cell activation mediated by PAR1 and PAR4 using peptide analogs of Arg-Pro-Pro-Gly-Phe that contain one or more amino acid substitutions. The invention also incl... | 07/11/2006 |
| 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 |
| 7008957 | Bicyclic cyanoheterocycles, process for their preparation and their use as medicaments The invention relates to compounds of the formula I in which the radicals have the stated meanings, their stereoisomeric forms and their physiologically tolerated salts and process for their preparation. The com... | 03/07/2006 |
| 6951849 | Benzimidazolidinone derivatives as muscarinic agents Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the s... | 10/04/2005 |
| 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 |
| 6680314 | Azacyclooctane and heptane derivatives, their preparation and use in therapy Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: ##STR1## wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 ... | 01/20/2004 |
| 6667303 | Aryl substituted 1,4-diazepanes and method of use thereof Aryl substituted 1,4-diazepanes are provided such as derivatives of 6-(1,4-diazepan-1-yl)benzo[cd]indol-2(1H)-one, 6-(1,4-diazepan-1-yl)acenaphthylen-1(2H)-one and 5-(1,4-diazepan-1-yl)-2H-naphtho[1,8-cd]isothiazole-1,1-dioxide. Also provided are pha... | 12/23/2003 |
| 6544982 | Thrombin receptor antagonists A thrombin receptor antagonist having the formula ##STR1## useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non... | 04/08/2003 |
| 6521659 | Compositions containing a substituted indolealkanoic acid and an angiotensin converting enzyme inhibitor Disclosed are methods of reducing serum glucose and triglyceride levels and for inhibiting angiogenesis, the methods comprising administration of substituted indolealkanoic acids to patients in need of such treatment. Also disclosed are such compounds use... | 02/18/2003 |
| 6500817 | Thiazolyl urea derivatives and their utilization as antiviral agents The present invention relates to thiazolylurea derivatives, a process for their preparation, and their use as pharmaceuticals, in particular as antiviral pharmaceuticals.... | 12/31/2002 |
| 6436980 | Peptidomimetic efflux pump inhibitors Compounds are described which have efflux pump inhibitor activity. Also described are methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.... | 08/20/2002 |
| 6420395 | Azacyclooctane and heptane derivatives, their preparation and use in therapy The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl ... | 07/16/2002 |
| 6372736 | Heterocyclic compounds as inhibitors of rotamase enzymes Compounds of the formula (I): ##STR1## wherein A, Y, R, X, R1, R2, R3 and R4 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal r... | 04/16/2002 |
| 6335329 | Carboxylic acid substituted heterocycles, derivatives thereof and methods of use Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharm... | 01/01/2002 |
| 6335326 | Benzisoxazole derivatives having d4-antagonistic activity The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituen... | 01/01/2002 |
| 6291450 | Carboxylic acid substituted heterocycles, derivatives thereof and methods of use Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharm... | 09/18/2001 |
| 6251921 | 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... | 06/26/2001 |
| 6211214 | Biphenyl ether oxazolines and their use as pest-control agents The present invention relates to novel biphenyl ether-oxazolines of the formula (I) ##STR1## in which X, Y, Z, R1, R2, A, m and n have the meaning given in the description, to processes for their preparation and to their use for cont... | 04/03/2001 |
| 6191152 | 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives having an effect on the C.N.S. and the heart The invention refers to novel 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives of formula (I) having an influence on the heart and the central nervous system, furthermore pharmaceutical compositions containing the above derivatives, and a process for... | 02/20/2001 |
| 6166041 | 2-heteroaryl and 2-heterocyclic benzoxazoles as PDE IV inhibitors for the treatment of asthma Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen; Q is --CH2 --CH2 --, --CH2 --, a single or ... | 12/26/2000 |
| 6022868 | Substituted azacyclic or azabicyclic compounds Disclosed are compounds of formula (I) selected from the following ##STR1## wherein Y is ##STR2## and wherein A, B, C, D, R, k, m, n, o, p, s, t and u are as defined in the specification. These compounds are useful in treating diseases in the ... | 02/08/2000 |
| 6022880 | Substituted pyridylamino indoles There are disclosed various compounds of the formula below, ##STR1## where R, R1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of... | 02/08/2000 |
| 5872134 | 5-HT4 receptor antagonists The use of a compound of formula (I) or a pharmaceutically acceptable salt thereof for the treatment of artrial arrhythmia, stroke or CNS disorders X--CO--CH2 --Z (I) wherein X is a monocyclic or polycyclic aromatic... | 02/16/1999 |
| 5856360 | Pharmaceutical method for the treatment of severe blood loss and for the inhibition or treatment of hemorrhagic shock This invention is directed to a pharmacologically acceptable composition for inhibiting or treating hemorrhagic shock in a mammal. The composition includes a KATP inhibitor and a pharmacologically acceptable carrier, with the KATP in... | 01/05/1999 |
| 5705509 | Tricyclic heterocyclic compounds as 5-HT4 receptor antagonists Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X1 --(CH2)x --X2 and the aromatic carbon atoms to which they are attached form 5-7 membered ring wherein X1 is O or S; X... | 01/06/1998 |
| 5703070 | Indole, indazole and benzisoxazole compounds Compound of formula (I): ##STR1## in which: R1 represents hydrogen, halogen, alkyl, alkoxy, trihalomethyl or hydroxyl, R2 represents hydrogen, alkyl or phenyl which is optionally substituted, ##STR2## or alternatively ... | 12/30/1997 |
| 5703065 | Heteroarylamino and heteroarylsulfonamido substituted 3-benyzlaminomethyl piperidines and related compounds The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R3, Q and R1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts ... | 12/30/1997 |
| 5698573 | Imidazolone and oxazolone derivatives as dopamine antagonists A class of imidazolone and oxazolone derivatives of Structure I, ##STR1## wherein X represents oxygen or N--R1 ; Q represents a substituted five-, six- or seven-membered monocyclic heteroaliphatic ring which contains one nitrogen atom as the so... | 12/16/1997 |
| 5614535 | Adhesion receptor antagonists Compounds of the formula I ##STR1## in which R1 and X have the meanings herein defined, their physiologically unobjectionable salts and/or solvates inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the... | 03/25/1997 |
| 5574030 | N-aminoalkyl-substituted nitrogen-containing five membered heterocyclic compounds Disclosed are new alkylenediamine derivatives of the following formula which are effective for treatment of dysuria are disclosed: ##STR1## wherein R1 is hydrogen, alkyl, or a substituted or unsubstituted phenyl, naphthyl or aromatic heter... | 11/12/1996 |