- ANTIBACTERIAL COMPOUNDS AND NEW USES THEREOF
-
This invention relates to a series of compounds of formula (I) for use in treating infections caused by obligate anaerobic bacteria, including Clostridium difficile, and to methods of treating said infections by administering said compounds. The compounds can be used against strains of obligate anaerobic bacteria that have developed resistance to other antibiotics. Many compounds used in the invention contain a tricyclic ring system.
- -
-
Page/Page column 97; 98
(2017/04/11)
-
- ANTIBACTERIAL COMPOUNDS
-
This invention relates to antibacterial and anti-mycobacterial drug compounds of formula (I). It also relates to pharmaceutical formulations of antibacterial drug compounds of formula (I). It also relates to uses of the derivatives in treating bacterial i
- -
-
Page/Page column 66-67
(2017/04/11)
-
- In vitro and in vivo identification of novel positive allosteric modulators of the human dopamine D2 and D3 receptor
-
Agonists at dopamine D2 and D3 receptors are important therapeutic agents in the treatment of Parkinson's disease. Compared with the use of agonists, allosteric potentiators offer potential advantages such as temporal, regional, and phasic potentiation of
- Wood, Martyn,Ates, Ali,Andre, Veronique Marie,Michel, Anne,Barnaby, Robert,Gillard, Michel
-
supporting information
p. 303 - 312
(2016/02/26)
-
- SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
-
Provided is a sulfonamide derivative represented by the following general formula (1) and having an α4 integrin inhibitory effect with high selectivity with a low effect on α4β1 and a high effect on α4β7, or a pharmaceutically acceptable salt thereof (in the general formula (1), A, B, D, E, R41, and a to h are as described in the description).
- -
-
Paragraph 0236; 0237; 0238
(2016/09/26)
-
- CARBAZOLE DERIVATIVES
-
Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein Q, R1a, R1b, R2a, R2b, R3, R4, R5a, R5b, R6a, R6c, R7a, R7b, R7c, and R7d are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
- -
-
Page/Page column 72; 73
(2016/05/24)
-
- INDOLE CARBOXAMIDE COMPOUNDS
-
Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
- -
-
Paragraph 0297-0298
(2016/05/19)
-
- TRICYCLIC ATROPISOMER COMPOUNDS
-
Disclosed are compounds of Formula (I): or a salt thereof, wherein Q is: or; and X, R1a, R1b, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bru
- -
-
Page/Page column 49-50
(2016/06/06)
-
- ANTIBACTERIAL COMPOUNDS
-
This invention relates to antibacterial and anti-mycobacterial drug compounds of formula I. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections and to methods of treating bacterial infections. The invention is also directed to antibacterial drug compounds which are capable of treating bacterial infections which are currently hard to treat with existing drug compounds, e.g. those caused by resistant bacterial or mycobacterial strains.
- -
-
Page/Page column 105; 106
(2015/11/17)
-
- SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF
-
Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent α4 integrin-inhibitory action.
- -
-
Paragraph 0673-0675
(2015/02/25)
-
- BIARYL ACYL-SULFONAMIDE COMPOUNDS AS SODIUM CHANNEL INHIBITORS
-
The present invention provides compounds of Formula (Ia), and pharmaceutically acceptable salts thereof. The compounds are useful as inhibitors of voltage-gated sodium channels, in particular Nav 1.7. (Ia); as described in the specification. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention, as well as intermediates and processes useful for making the compounds.
- -
-
Paragraph 00316
(2015/04/22)
-
- IMIDAZOPYRIDINE COMPOUNDS AND USES THEREOF
-
This invention generally relates to substituted imidazopyridine compounds, particularly substituted 4-(imidazo[1,2-a]pyridin-2-yl)benzamide compounds and salts thereof. This invention also relates to pharmaceutical compositions and kits comprising such a compound, uses of such a compound (including, for example, treatment methods and medicament preparations), processes for making such a compound, and intermediates used in such processes.
- -
-
-
- LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
-
Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
- -
-
Paragraph 1321; 1322
(2014/07/23)
-
- 4-HETEROARYL SUBSTITUTED BENZOIC ACID COMPOUNDS AS RORGAMMAT INHIBITORS AND USES THEREOF
-
Provided are compounds according to Formula I or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
- -
-
Page/Page column 57
(2014/03/22)
-
- 4-HETEROARYL SUBSTITUTED BENZOIC ACID COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
-
The present invention relates to compounds according to Formula I (Formula I), and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
- -
-
Page/Page column 59; 60
(2014/03/22)
-
- SUBSTITUTED TETRAHYDROCARBAZOLE AND CARBAZOLE CARBOXAMIDE COMPOUNDS
-
Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
- -
-
Paragraph 0430; 0431
(2015/01/07)
-
- Discovery and biological evaluation of novel 4-amino-2-phenylpyrimidine derivatives as potent and orally active GPR119 agonists
-
Novel 4-amino-2-phenylpyrimidine derivatives were synthesized and evaluated as GPR119 agonists. Optimization of the substituents on the phenyl ring at the 2-position and the amino group at the 4-position led to the identification of 3,4-dihalogenated and
- Negoro, Kenji,Yonetoku, Yasuhiro,Misawa-Mukai, Hana,Hamaguchi, Wataru,Maruyama, Tatsuya,Yoshida, Shigeru,Takeuchi, Makoto,Ohta, Mitsuaki
-
p. 5235 - 5246
(2012/11/07)
-
- RORGAMMAT INHIBITORS
-
The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
- -
-
Page/Page column 50-51
(2012/08/28)
-
- MODULATORS OF DOPAMINE NEUROTRANSMISSION
-
The present invention relates to novel1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
- -
-
Page/Page column 45
(2009/12/05)
-
- NEW ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
-
The invention provides certain compounds and salts of Formula I and Formula II:which possess antimicrobial activity. The invention also provides novel synthetic intermediatesuseful in making compounds of Formula I and Formula II. The variables A1, R2, R3, R5, R6, R7, A8, and Rg are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
- -
-
Page/Page column 47-48
(2008/06/13)
-
- ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS
-
The invention provides compounds and salts of Formula (I) and Formula (II): which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula (I) and Formula (II). The variables A1, R2, R3, R5, R6, R7, A8 and R9 are defined herein. Certain compounds of Formula (I) and Formula (II) disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula (I) or Formula (II) and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula (I) or Formula (II) as the only active agent or may contain a combination of a compound of Formula (I) or Formula (II) and one or more other active agents. The invention also provides methods for treating microbial infections in animals.
- -
-
Page/Page column 49-50
(2010/02/11)
-