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7410961 |
2,6-disubstituted piperiddines as modulators
The present invention is further directed to compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 16 , R 17 , R 18 , R 19 , R 20 , R 21 and R 22 are as...
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7390798 |
Carboxamide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where variables A 1 , A 2 , B, J, K, m, n, R 4 , R 5a , R 5b and R 5c are as defined herein) useful as antagonists of CGRP...
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7375100 |
2-amino-pyridine derivatives useful for the treatment of diseases
The invention relates to compounds of formula (1)
and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives....
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7368444 |
N-carbamoyl nitrogen-containing fused ring compounds and drugs containing these compounds as the active ingredient
The present invention relates to the compound presented by formula (I)
(wherein all symbols in formula (I) are the same mean as the description shown in the specification.), mitocondorial...
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7365196 |
Sulphonamido-substituted bridged bicycloalkyl derivatives
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of...
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7304051 |
Quinoxaline compounds
Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I)
are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
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7304050 |
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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7288651 |
Preparation of quinoxaline compounds
Certain methods are disclosed that are useful in the preparation of CCK2 active amidophenyl-sulfonylamino-quinoxaline compounds of the formula:
wherein R 1 , R 2 , R a and R b are defined.
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7262185 |
Benzazepine derivative, process for producing the same, and use
The present invention provides a novel benzazepine derivative represented by formula:
wherein, R 1 is a 5- or 6-membered aromatic ring, R 2 is lower alkyl group, etc., Y is an optionally...
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7238685 |
Benzo-fused heterocycles as endothelin antagonists
The invention relates to novel benzo-fused heterocycles and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including...
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7192950 |
Benzazepines and related heterocyclic derivatives which are useful as orexin receptor antagonists
The invention relates to novel benzazepines and related heterocyclic derivatives (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also...
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7183271 |
4,4-difluoro-1,2,3,4-tetrahydro-5h-1-benzazepine derivative or salt thereof
A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes...
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7176195 |
Fused azepine derivatives and their use as antidiuretic agents
Compounds according to general formulae (1 and 2), wherein G 1 is an azepine derivative and G 2 is a group according to general formulae (9–11) are new. Compounds according to the invention are...
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7169772 |
4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivatives or salts thereof
4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivatives, which have excellent arginine vasopressin V 2 activity and are useful for a drug for the treatment of central diabetes insipidus...
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7141562 |
Substituted benzoxazinones and uses thereof
Compound of the Formula:
and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO 2 — or —(CR a R b ) r —, n is 1 or 2, R 2 is aryl or...
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7101869 |
2,4-diaminopyrimidine compounds useful as immunosuppressants
Novel compounds according to the formula
and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein each occurrence of A is independently selected from CH or N; X is...
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7091352 |
Compounds substituted with bicyclic amino groups
Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof:
wherein A is furan, thiophene, pyrazole, imidazole, isoxazole or isothiazole; R 1...
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7091199 |
Thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives useful as d4 antagonists
The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D 4 antagonists. Said compounds are useful for the treatment of medical conditions...
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7074781 |
Condensed azepines as vasopressin agonists
This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V 1 and V 2 are both H, OMe or F, or one of V 1 and V 2 is Br,...
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7067513 |
Phenylpiperazines
The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D 2 receptor and/or the serotonin reuptake site,...
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7008938 |
Benzene-fused heteroring derivatives and pharmaceutical agents comprising the same as active ingredient
A benzene-fused heteroring derivative of formula (I)
wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an...
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6995154 |
Heterocyclic topoisomerase poisons
The invention provides compounds of formula I:
wherein R 1 to R 5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds,...
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6972286 |
Oxazolidinones having a benzannulated 6- or 7-membered heterocycle
The present invention provides oxazolidinones having a benzannelated 6- or 7-membered heterocycle as antibacterial agents.
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6953787 |
5HT2C receptor modulators
The present invention relates to novel compounds of Formula (I):
which act as 5HT 2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the...
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6936602 |
Benzazepine derivatives, process for the preparation of the same and uses thereof
Compounds of the general formula (I):
or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R 1 is a 5- to 6-membered...
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6924280 |
Dipeptide derivatives
This invention is directed to compounds of the formula
and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone...
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6919332 |
N-substituted-heteroaryloxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors
The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula
wherein X, A, Y, B, G, and R 1 are as defined in the...
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6903091 |
Biphenyl vasopressin agonists
A compound of the formulae (I) or (II):
wherein:
Y is a moiety selected from NR or —(CH 2 ) n ; wherein R is hydrogen or (C 1 -C 6 ) lower alkyl, and n is 1;
represents:
(1) a...
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6864367 |
Process for producing cyclic compound
A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates...
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6855708 |
N-arylsulfonyl aza-bicyclic derivatives as potent cell adhesion inhibitors
Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds...
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6815451 |
1,2,3,4-Tetrahydroisoquinolines derivatives as urotensin II receptor antagonists
The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions....
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6815440 |
Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids
Cyclic and heterocyclic N-substituted α-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course...
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6809092 |
Benezene-fused heteroring derivatives and pharmaceutical agents comprising the same as active ingredient
A benzene-fused heteroring derivative of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an...
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6770668 |
Pharmaceutically active compounds and methods of use
The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof,...
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6762178 |
Acetylenic aryl sulfonamide and phosphinic acid amide hydroxamic acid TACE inhibitors
Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple...
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6686351 |
Compounds and methods for modulation of estrogen receptors
Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for...
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6667302 |
Heterocyclic topoisomerase poisons
The invention provides compounds of formula I: wherein R 1 to R 5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds,...
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6642223 |
Benzoheterocyclic derivatives
A benzoheterocyclic derivative of the following formula [1]: and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and...
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6630463 |
Heterocycle-containing carboxylic acid derivative and drug containing the same
Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): wherein A represents, for example, a heteroaryl group which contains at least one...
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6608079 |
Indole derivatives and their use as 5-HT1F agonists
The present invention relates to a compound of formula (I), or a pharmaceutical acid addition salt thereof, which are useful for activating 5-HT 1F receptors and inhibiting neuronal protein...
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6602864 |
Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds
The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from...
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6596869 |
Nitrosation process
A process for preparing compounds of formula (I), by nitrosating compounds of formula (II), compounds of formula (I) having pharmaceutical activity.
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6586422 |
Pyrazine and triazine derivatives of 1,2,4,5-tetrahydro-Benzo or Thieno &lsqb d&rsqb azepine
The invention relates to compounds which are represented by the formula wherein R 1 , R 2 , R 3 , R 4 , X and Y are as defined in the specification, as well as pharmaceutically acceptable salts...
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6562828 |
Amidine compounds
A compound of the formula [I] wherein R 1 , R 2 and R 3 are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug...
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6562809 |
3-bicycloindole compounds
Described herein are compounds selective for a 5-HT1D receptor, which have the general formula:
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6534650 |
Benzisoxazole and 4-amidino-3-hydroxyphenyl chemical intermediates
This invention relates to compounds of Formula V H—Y—G—R V and Formula VI (wherein f, X, Y, G and R have the values defined in the description) which are useful as intermediates for the...
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6534496 |
Thermogenic composition and benzazepine thermogenics
The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and...
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6514964 |
Fused cycloheptane and fused azacycloheptane compounds and their methods of use
The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated...
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6498158 |
Il-5 inhibiting 6-azauracil derivatives
The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to...
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6495542 |
Benzamide derivatives as vasopressin antagonists
A compound of formula (I): wherein A is an optionally substituted heterocyclic group, R is a lower alkoxy; Z is C═O or CH 2 ; and B is benzazapinyl, which may be optionally substituted, or a...
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