"What can be more palpably absurd than the prospect held out of locomotives traveling twice as fast as stagecoaches?"
The Quarterly Review ; March edition, 1825
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| Number | Title | Issue Date |
| 5952494 | Method for the preparation of pyrido benzoxazine derivatives There is disclosed a method for the preparation of pyrido benzoxazine derivative having the following formula I, that is improved in both production coat and yield. The method comprises reacting a compound of the following general formula II with tetraalk... | 09/14/1999 |
| 5847121 | Production of nitro-benzyl-dota via direct peptide cyclization Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin, as well as related compounds, are described. Articles of manufactur... | 12/08/1998 |
| 5834609 | Bicyclic aminoimidazoles The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a t... | 11/10/1998 |
| 5767272 | Method of preparing meso-haloalkylporphyrins Transition metal complexes of meso-haloalkylporphyrins, wherein the haloalkyl groups contain 2 to 8 carbon atoms have been found to be highly effective catalysts for oxidation of alkanes and for the decomposition of hydroperoxides. Also disclosed is a pro... | 06/16/1998 |
| 5723457 | Acylmercaptoalkanoylamino and mercaptoalkanoylamino benzazepines Compounds of the formula ##STR1## wherein X1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme and neutral endopeptidase and thus are useful as cardiovascular agents.... | 03/03/1998 |
| 5721231 | Thienotriazolodiazepine compound and pharmaceutical use thereof N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno 3,2-f!1,2,4!triazolo4,3-a!1,4!diazepin-6-yl )-N'- (2-methoxyphenyl)urea, optical isomers thereof and pharmaceutically acceptable salts thereof. The compounds of the present invention strongly an... | 02/24/1998 |
| 5707988 | Benzod! isoxazole derivatives, compositions containing them and their use in therapy Compounds of formula (I) ##STR1## in which X represents a group >O, >S, >C.dbd.O or >NR wherein R is hydrogen, C1-6 alkyl, phenyl or C7-12 phenalkyl, R1 and R2 each represent hydrogen or together represent ... | 01/13/1998 |
| 5708006 | Neurokinin antagonists The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing th... | 01/13/1998 |
| 5707990 | 2-substituted amino and thio alkyl benzoxazine antimicrobial agents The invention relates to benzoxazine and pyrido-oxazine antibacterial compounds of the general formula: ##STR1## wherein the moiety Q is a fused phenyl or fused pyridyl moiety and R is a substituted amine or substituted thio moiety as herein describe... | 01/13/1998 |
| 5705639 | Process to prepare herbicidal bicyclic triazoles This invention includes compounds of Formula II and IV and a process for preparing Formula I compounds by first preparing the compounds of Formula IV and then further reacting to form the compounds of Formula II and further reacting to prepare the compoun... | 01/06/1998 |
| 5703231 | Process for making antimicrobial compounds The present invention provides a process for making a compound having a structure according to Formula (I) ##STR1## wherein A1, A2 and A3 are independently carbon or nitrogen and R1, R3, R4 | 12/30/1997 |
| 5703072 | Bicyclic nonane and decane compounds having dopamine receptor affinity Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, substituted or unsubstituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings; X1 is selected from... | 12/30/1997 |
| 5700796 | Tricyclic benzazepine vasopressin antagonists Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V1 and/or V2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treatin... | 12/23/1997 |
| 5698552 | Hetrazepinoid amides The present invention relates to thienodiazepines of formula Ib: ##STR1## wherein U, V, R5, R6 and R7 are as defined herein. This invention also relates to processes for preparing these thienodiazepines and their use ... | 12/16/1997 |
| 5698563 | Bis-hydrazones! The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises bis(guanylhydrazone) of the formula ##STR1## capable of inhibiting the format... | 12/16/1997 |
| 5698586 | Angiogenesis inhibitory agent O-substituted fumagillol derivatives and its salts have an angiogenesis inhibiting activity and are useful for prophylaxis and treatment of diseases induced by abnormally stimulated neovascularization.... | 12/16/1997 |
| 5696117 | Benzoxazine antimicrobial agents The invention relates to benzoxazine and pyrido-oxazine antibacterial compounds of the general formula: ##STR1## wherein the moiety Q is a fused phenyl or fused pyridyl moiety as herein described, pharmaceutical compositions containing the compounds,... | 12/09/1997 |
| 5696258 | Process for the preparation of triphendioxazine dyestuffs amidated on both sides According to the invention, a process for the preparation of triphendioxazines symmetrically or asymmetrically amidated on both sides comprises reducing a triphendioxazine chromophore, which is optionally already amidated on one side, to give the leuco fo... | 12/09/1997 |
| 5696123 | Neurokinin antagonists The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing th... | 12/09/1997 |
| 5696112 | Fused heterocyclic azepines as vasopressin antagonists This invention relates to bicyclic non-peptide vasopressin antagonists useful in treating conditions where decreased vasopressin levels are desired, in conditions with excess renal water reabsorption and in conditions with increased vascular resistance an... | 12/09/1997 |
| 5693635 | Tricyclic benzazepine vasopressin antagonists Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V1 and/or V2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treati... | 12/02/1997 |
| 5686445 | Pyridobenzoxazepine and pyridobenzothiazepine vasopressin antagonists Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V1 and/or V2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treati... | 11/11/1997 |
| 5686614 | Preparation of chiral 5-aminocarbonyl-5H-dibenzoa,d!cyclohepten-5,10-imines by optical resolution Disclosed are processes for resolving a racemic mixture of 5-aminocarbonyl-5H-dibenzoa,d!cyclohepten-5,10-imines into component enantiomers comprising recrystallizaton of diasteriomeric tartrate salts.... | 11/11/1997 |
| 5684003 | 5-HT4 receptor agonists Compounds of formula (I) and pharmaceutically acceptable salts thereof are selective agonists for 5-HT4 receptors. ##STR1## wherein Ak is a C3 -C6 alkyl group, and R is a C2 -C6 alkyl group, a C | 11/04/1997 |
| 5684016 | Method of treating cardiac insufficiency The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R1, R2 and R3 are identical or different and each denote hydrogen or an organic... | 11/04/1997 |
| 5679673 | Aralkyl bridged diazabicycloalkane derivatives for CNS disorders Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R1, R4 | 10/21/1997 |
| 5679688 | Quinaldoyl-amine derivatives of oxo-and hydroxy-substituted hydrocarbons The present invention discloses the compounds of general formula (1) ##STR1## wherein R1, R2, R3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and ar... | 10/21/1997 |
| 5679675 | 8-amino-10-(azabicycloalkyl)-pyrido1,2,3-d,e!1,3,4!benzoxadiazine derivatives The present invention relates to new 8-amino-10-(azabicycloalkyl)-pyrido1,2,3-d,e!1,3,4!benzoxadiazine derivatives of the general formula (I) ##STR1## in which the radicals R1 to R4, Z and X1 have the meaning ... | 10/21/1997 |
| 5674877 | Muscarinic receptor ligands Described herein are D4 receptor-selective compounds of the general formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X1 is sele... | 10/07/1997 |
| 5663165 | Hypolipidaemic benzothiazepine compounds The present invention is directed to the following compounds of formula (I): ##STR1## wherein l is an integer of from 0 to 4; m is an integer of from 0 to 5; n is an integer of from 0 to 2; R and R' are atoms or groups independently selected fro... | 09/02/1997 |
| 5663203 | Agents containing prostacyclin derivatives for topical application The invention relates to a dermal application form of prostacyclin derivatives of Formula I ##STR1## wherein R1 means hydrogen or alkyl of 1-10 carbon atoms, A is a --CH2 --CH2 --, trans-CH.dbd.CH-- or --C.ident.C-group, W... | 09/02/1997 |
| 5658923 | Azepine derivatives and use thereof An azepine compound of the formula ##STR1## wherein R is (a) ##STR2## in which R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen, or optionally substituted phenyl, and n is 0 or 1, (b) cycloalkyl of C5-8 whic... | 08/19/1997 |
| 5654297 | Tricyclic thieno-azepine vasopressin antagonists This invention relates to new bicyclic non-peptide vasopressin antagonists which are useful in treating conditions where decreased vasopressin levels are desired, such as in congestive heart failure, in disease conditions with excess renal water reabsorpt... | 08/05/1997 |
| 5654308 | Bicyclic amide derivatives, compositions and methods of treatment The cyclic amide derivative is defined by the formula (I) or a salt thereof: R1 --(CH2)n-Z in which R1 is a group derived from a cyclic amide compound, substituted or unsubstituted, n is zero or an integer of 1 to 10 and Z... | 08/05/1997 |
| 5652241 | 4-(heteroaryl)-1-[(2,3-dihydro-1-indol-1-yl)alkyl]piperadines and related compounds and their therapeutic utility Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. D... | 07/29/1997 |
| 5650507 | Asymmetric dioxazine compounds and use thereof as fiber reactive dyes An asymmetric dioxazine compound of the following formula: ##STR1## wherein R is sulfo, halogeno, alkoxy, alkyl or carboxy; R1 and R2 are each hydrogen or alkyl; R3 is hydrogen, alkyl or acyl; X1 and X... | 07/22/1997 |
| 5646272 | Bile acid conjugates of proline hydroxylase inhibitors Bile acid derivatives of the formula I W--X--G in which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active... | 07/08/1997 |
| 5644056 | Method of preparing 7,8-difluoro-2,3-dihydro-3-methyl-4H-1, 4-benzoxazine A method of preparing 7,8-difluoro-2,3-dihydro-3-methyl-4H-1,4 benzoxazine. The method includes the steps of reacting 2,3,4-trifluoroaniline or trifluoronitrobenzene with hydroxyacetone or a derivative thereof under reducing conditions to yield N-(3-hydro... | 07/01/1997 |
| 5641882 | Intermediates for the preparation of 1',1'-disubstituted and 1'-spiro-nucleosides The invention relates to a novel process for stereocontrolled preparation of 1',1'-disubstituted and 1'-spiro-nucleosides of the formula I ##STR1## in which the substituents A, R8 and R9 are as defined in claim 1, and to novel i... | 06/24/1997 |
| 5637701 | Process for preparing optically active amide derivatives A novel asymmetric synthesis is provided for preparing optically active amides of formula (A) and their salts. ##STR1## In the formula, X represent --N-- or --CH--, R represents a mono or bicyclic aryl or heteroaryl group, R1 is an aryl or... | 06/10/1997 |