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Datlow, Philip I.


Primary examiner statistics: 197 patents; average approval time: 695 days
Assistant examiner statistics: 189 patents; average approval time: 625 days

Patents as Primary Examiner

1          
NumberTitleIssue Date
5952494Method 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
5847121Production 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
5834609Bicyclic 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
5767272Method 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
5723457Acylmercaptoalkanoylamino 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
5721231Thienotriazolodiazepine compound and pharmaceutical use thereof
N-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno ›3,2-f!›1,2,4!triazolo›4,3-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
5707988Benzo›d! 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
5708006Neurokinin 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
57079902-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
5705639Process 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
5703231Process 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
5703072Bicyclic 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
5700796Tricyclic 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
5698552Hetrazepinoid 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
5698563Bis-›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
5698586Angiogenesis 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
5696117Benzoxazine 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
5696258Process 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
5696123Neurokinin 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
5696112Fused 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
5693635Tricyclic 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
5686445Pyridobenzoxazepine 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
5686614Preparation of chiral 5-aminocarbonyl-5H-dibenzo›a,d!cyclohepten-5,10-imines by optical resolution
Disclosed are processes for resolving a racemic mixture of 5-aminocarbonyl-5H-dibenzo›a,d!cyclohepten-5,10-imines into component enantiomers comprising recrystallizaton of diasteriomeric tartrate salts....
11/11/1997
56840035-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
5684016Method 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
5679673Aralkyl 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
5679688Quinaldoyl-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
56796758-amino-10-(azabicycloalkyl)-pyrido›1,2,3-d,e!›1,3,4!benzoxadiazine derivatives
The present invention relates to new 8-amino-10-(azabicycloalkyl)-pyrido›1,2,3-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
5674877Muscarinic 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
5663165Hypolipidaemic 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
5663203Agents 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
5658923Azepine 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
5654297Tricyclic 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
5654308Bicyclic 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
56522414-(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
5650507Asymmetric 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
5646272Bile 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
5644056Method 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
5641882Intermediates 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
5637701Process 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
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