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7629338 |
Substituted monocyclic CGRP receptor antagonists
Compounds of formula I:
(wherein variables A 1 , A 2 , A 3 , A 4 , m, n, J, Q, R 4 , E a , E b , E c , R 6 , R 7 , R e , R f , R PG and Y are as described herein) which are antagonists of CGRP...
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7629341 |
Human ADAM-10 inhibitors
The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its...
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7582635 |
Therapeutic agents useful for treating pain
A compound of formula:
wherein Ar 1 , A, R 3 , x, and m are as disclosed herein and Ar 2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt...
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7563788 |
Substituted Imidazo[1,2-a]pyridines as Antibacterial Agents
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable...
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7354918 |
Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I)
in which R represents a radical —AR′ wherein A represents a heteroatom and R′...
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7211417 |
Antibiotic P175-A and semisynthetic derivatives thereof
This invention relates to a new antibiotic designated P175-A, to production of fermentation of Micromonospora echinospora NRRL 30633, to methods for recovery and concentration from the crude...
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7157452 |
Substituted 4,9-dihydrocyclopenta{imn}phenanthridine-5-ones derivatives thereof and their uses
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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7034036 |
Inhibitors of ABC drug transporters at the blood-brain barrier
The present invention relates to inhibitors of drug transporters of the ABC protein superfamily, particularly transporters present at the blood brain barrier. ABC transporter inhibitors identified...
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6960580 |
Nitrogenous heterocyclic substituted quinoline compounds
The present invention relates to nitrogen-containing heterocyclic quinoline compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases,...
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6936610 |
Heterocyclic derivatives
The invention relates to heterocyclic derivatives of formula (I)
A—B—X 1 —T 1 (R 2 )—L 1 —T 2 (R 3 )—X 2 —Q ...
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6800636 |
Farnesyl protein transferase inhibitors
Disclosed are compounds of the formula: wherein R 8 represents a cyclic moiety to which is bound an imodazolylalkyl group; R 9 represents a carbamate, urea, amide or sulfonamide group; and the...
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6642225 |
Diazacycloalkanedione derivatives
Compounds of formula I wherein R is carboxy, esterified carboxy or amidated carboxy; R 1 and R 3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di-lower...
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6545011 |
Substituted 4,9-dihydrocyclopenta&lsqb imn&rsqb phenanthridine-5-ones, derivatives thereof and their uses
This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
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6541483 |
Acridone-derived compounds useful as antineoplastic and antiretroviral agents
The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as...
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6444676 |
Use of PARP inhibitors in the treatment of glaucoma
The invention provides pharmaceutical compositions containing PARP inhibitors and methods of using these compositions to prevent, treat or ameliorate glaucomatous retinopathy and/or optic neuropathy.
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6358967 |
Ergoline amine derivatives with blood pressure lowering effect
The invention relates to novel derivatives of ergoline of the general formula 1 in which R 1 together with the two adjacent N atoms is the residue of a diamine and R 4 together with the two...
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6300330 |
Heterocycle derivatives which inhibit factor Xa
The invention relates to heterocyclic derivatives of the formula (I): A--B--X 1 --T 1 (R 2 )--L 1 --T 2 (R 3 )--X 2 --Q or pharmaceutically acceptable salts thereof, which possess...
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6221870 |
Ergoline derivatives and their use as somatostatin receptor antagonists
The invention provides compounds of formula I ##STR1## wherein R 1 to R 6 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as...
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6204273 |
16-substituted-4-aza-androstane 5-α-reductase isozyme 1 inhibitors
Compounds of the Formula I ##STR1## are inhibitors of the 5α-reductase 1 isozyme, and are useful alone, or in combination with a 5α-reductase 2 inhibitor, for the treatment of androgenic...
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6187775 |
Acridone-derived compounds useful as antineoplastic and antiretroviral agents
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6156754 |
Glycoconjugates of modified camptothecin derivatives (A-or B-ring linkage)
The present invention relates to glycoconjugates of camptothecin derivatives in which at least one carbohydrate component is linked via suitable spacers with the A or B ring of a camptothecin...
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6133280 |
Androgen synthesis inhibitors
This invention relates to novel inhibitors of androgen synthesis that are useful in the treatment of prostate cancer and benign prostatic hypertrophy. The present invention also provides methods of...
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6127368 |
Anellated β-carbolines
Compounds of formula I ##STR1## are described, as well as the process for their production and their use in pharmaceutical agents.
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6004962 |
Rapid opioid detoxification
Rapid opioid detoxification procedures are provided which include sedating a patient with a rapid-acting, safely reversible intravenous anesthetic agent having a very short full recovery period....
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5880125 |
4-spiroindoline piperidines promote release of growth hormone
The present invention is directed to certain novel compounds identified as 4-spiroindoline piperidines of the general structural formula: ##STR1## wherein R 1 , R 1a , R 2a , R 3a , R 3b , R 4 , R...
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5872126 |
Methods and compositions for treating preterm labor
The present invention provides for a method of treating preterm labor in a subject in need of such treatment comprising administration of a therapeutically effective amount of an inhibitor of...
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5814642 |
Tetracyclic condensed heterocyclic compounds their production, and use
A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R 1 represents H or a hydrocarbon group which may be substituted; Y...
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5756512 |
Treatment of non-small cell lung carcinoma
A method of treating non-small cell lung carcinoma in a human afflicted therewith which comprises administering to such human an effective amount of a compound of the water soluble camptothecin...
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5741795 |
16-substituted-6-aza-androsten-4-ene-3-ones as 5-α-reductase inhibitors
Compounds of the formula I ##STR1## are inhibitors of 5α-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern...
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5674872 |
Treatment of ovarian cancer
A method of treating ovarian cancer in a human afflicted therewith which comprises administering to such human an effective amount of a compound of the water soluble camptothecin analog class.
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5635506 |
1, 2-dihydro-3H-dibenzisoquinoline-1,3-dione anticancer agents
This invention relates to a compound useful for the treatment of tumors having the formula: ##STR1##
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5620986 |
17 urea, thiourea, thiocarbamyl and carbamyl4-azasteroid 5-reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
Novel substituted 4-azasteroid 5-α-reductase inhibitors of formula (I), wherein A is (a), (b) or (c), are claimed as well as pharmaceutically acceptable salts and formulations thereof. These...
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5618813 |
Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine derivatives as antibacterial and antineoplastic agents
Benzo[5.6]pyrano[2.3.4-ij]quinolizine and benzo[5.6]thiopyrano[2.3.4-ij]quinolizine compounds having the formula ##STR1## wherein A is sulfur or oxygen; R 1 is selected from the group consisting...
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5614517 |
8-Oxo-5,8-dihydro-6H-dibenzo[a,g]quinolizine-13-propanoic acid derivatives, their preparation and their therapeutic application
A compound of formula (I) ##STR1## wherein X is hydrogen, halogen, C 1 -C 3 alkyl, trifluoromethyl, or C 1 -C 3 alkoxy; Y is hydrogen, halogen, C 1 -C 3 alkyl, or C 1 -C 3 alkoxy; R...
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5604246 |
2-aminoalkyl-5-aminoalkylamino substituted-isoquinoindazole-6(2H)-ones
This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino[8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino...
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5569655 |
Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
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5543406 |
Inhibitors of 5-α-testosterone reductase
The present invention relates to certain substituted 17β-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) ##STR1## wherein R 1 and R 2 are i)...
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5516779 |
17β-substituted-6-azasteroid derivatives useful as 5α-reductase inhibitors
Compounds of the formula ##STR1## are inhibitors of 5 α-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne...
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5496830 |
Inhibition of hemoflagellates by camptothecin compounds
Camptothecin compounds are effective inhibitors of hemoflagellate growth and are useful in treating leishmaniasis and trypanosomiasis in livestock, other domestic animals and humans.
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5340817 |
Method of treating tumors with anti-tumor effective camptothecin compounds
A camptothecin analog having the structure shown below: ##STR1## where Z is H or C 1 -8 alkyl and R is NO 2 , NH 2 , N 3 , hydrogen, halogen, COOH, OH, O-C 1 -3 alkyl, SH, S-C 1 -3 alkyl, CN, CH 2 ...
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5304554 |
4-[(alkyl or dialkyl)amino]quinolines and their method of preparation
Novel 4-[(alkyl or dialkyl)amino]quinolines are disclosed that are prepared by condensin BACKGROUND OF THE INVENTION The United States government has rights in this invention as a result of a...
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5302589 |
Heterocyclic inhibitors of 5-α-testosterone reductase
The present invention relates to certain substituted 17 β-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R 1 and R 2 are i) independently hydrogen or lower...
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5229387 |
Decahydro-8H-isoquino[2,1-g][1,6]naphthyridine and decahydrobenzo[a]pyrrolo [2,3-e]quinolizine derivatives
Compounds of the formula ##STR1## wherein: m is an integer of 1-6; n is an integer of 1 or 2; X and Y are independently hydrogen; hydroxy; lower alkyl; lower alkoxy; or halo; or X and Y when...
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5227380 |
Pharmaceutical compositions and methods employing camptothecins
A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin...
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5202325 |
Use of ergoline derivatives in treating emesis
Compounds of the formula I ##STR1## wherein n is 1 or 2, R 1 represents a hydrogen atom or a C 1 -C 4 alkyl group, R 2 represents a hydrogen atom and R 3 represents a hydrogen atom or a...
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5180722 |
10,11-methylenedioxy-20(RS)-camptothecin and 10,11-methylenedioxy-20(S)-camptothecin analogs
A camptothecin analog having the structure shown below: ##STR1## where Z is H or C 1 -8 alkyl and R is NO 2 , NH 2 , N 3 , hydrogen, halogen, COOH, OH, O--C 1 -3 alkyl, SH, S--C 1 -3 alkyl, CN, CH...
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5155107 |
17β-substituted-4-aza-5α-androstan-3-one derivatives and process for their preparation
The present invention concerns steroidic 5α-reductase inhibitors having the formula: ##STR1## As a result of their 5α-reductase inhibiting activity, these compounds are useful in the treatment of...
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5122526 |
Camptothecin and analogs thereof and pharmaceutical compositions and method using them
A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin...
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5081120 |
2-,21-Dinoreburnamenines containing a 15-aminated group
A compound selected from the group consisting of a compound of the formula (I): ##STR1## in which R 1 and R 2 are individually selected from the group consisting of hydrogen, an alkyl of 1 to 5...
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5079246 |
Novel indoloquinlones
A compound for formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and Z are described in claim 1.
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