Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T46526 Target Info
Target Name Bacterial Fimbrin D-mannose adhesin (Bact FimH)
Synonyms fimH; b4320; Type 1 fimbrin D-mannose specific adhesin; Protein FimH; JW4283
Target Type Clinical trial Target
Gene Name Bact FimH
UniProt ID
FIMH_ECOLI
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014194270
Title Compounds and Methods for Treating Bacterial Infections.
Abstract The present invention encompasses compounds and methods for treating and preventing bacterial infections specifically urinary tract infections and those caused by bacteria containing type 1 pili and FimH. The present invention also encompasses compounds and methods for treating inflammatory bowel disease specifically Crohn's Disease.
Applicant(s) Washington University
Representative Drug(s) D0R2GA Drug Info EC90 = 1 nM Click to Show More [1]
2 D0XR1C Drug Info EC90 = 1 nM [1]
3 D02AAD Drug Info EC90 = 4 nM [1]
4 D0K7TE Drug Info EC90 = 6 nM [1]
5 D0ET9M Drug Info EC90 = 8 nM [1]
6 D06PNN Drug Info EC90 = 30 nM [1]
7 D05AZE Drug Info EC90 = 31 nM [1]
8 D0L2QZ Drug Info EC90 = 250 nM [1]
9 D0UE3F Drug Info EC90 = 2000 nM [1]
10 D03WJB Drug Info EC90 = 3000 nM [1]
11 D09ZCA Drug Info EC90 = 4000 nM [1]
12 D0VG0F Drug Info EC90 = 4000 nM [1]
13 D0T6NX Drug Info EC90 = 6000 nM [1]
14 D0CR8J Drug Info EC90 = 24000 nM [1]
15 D00KKD Drug Info N.A. [1]
16 D01RHK Drug Info N.A. [1]
17 D05ZHZ Drug Info N.A. [1]
18 D09JDV Drug Info N.A. [1]
19 D09LWP Drug Info N.A. [1]
20 D0CN6Q Drug Info N.A. [1]
21 D0E1GC Drug Info N.A. [1]
22 D0N4WW Drug Info N.A. [1]
23 D0QM2O Drug Info N.A. [1]
24 D0VF5B Drug Info N.A. [1]
25 D0W1SE Drug Info N.A. [1]
Patent ID WO2014165107
Title Mannose Derivatives for Treating Bacterial Infections.
Abstract The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula (I) The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D0FS9V Drug Info IC50 = 600 nM Click to Show More [1]
2 D03HHG Drug Info IC50 = 1000 nM [1]
3 D0X4TV Drug Info IC50 = 1000 nM [1]
4 D07RAA Drug Info IC50 = 2000 nM [1]
5 D0R7YN Drug Info IC50 = 2000 nM [1]
6 D0Z1ZA Drug Info IC50 = 9000 nM [1]
7 D0XP5X Drug Info IC50 = 10000 nM [1]
8 D0X8AB Drug Info IC50 = 11000 nM [1]
9 D0D6HS Drug Info IC50 = 13000 nM [1]
10 D0H7UR Drug Info IC50 = 13000 nM [1]
11 D0OQ2R Drug Info IC50 = 13000 nM [1]
12 D0Q7QK Drug Info IC50 = 13000 nM [1]
13 D0F6TN Drug Info IC50 = 27000 nM [1]
14 D09LWZ Drug Info IC50 = 470000 nM [1]
15 D08OXD Drug Info IC50 = 750000 nM [1]
16 D0TY1Q Drug Info IC50 = 14000000 nM [1]
17 D05BUD Drug Info N.A. [1]
18 D09EXQ Drug Info N.A. [1]
19 D0B9LM Drug Info N.A. [1]
20 D0O8EX Drug Info N.A. [1]
21 D0P3SL Drug Info N.A. [1]
Patent ID WO2014100158
Title Mannose Derivatives for Treating Bacterial Infections.
Abstract The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula (I). The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D05BTL Drug Info IC50 = 0.03 nM Click to Show More [1]
2 D0UK1S Drug Info IC50 = 0.03 nM [1]
3 D0YX4L Drug Info IC50 = 0.03 nM [1]
4 D0J8HJ Drug Info IC50 = 0.07 nM [1]
5 D04PKX Drug Info IC50 = 0.11 nM [1]
6 D0SR8I Drug Info IC50 = 0.89 nM [1]
7 D05HKC Drug Info IC50 = 3.8 nM [1]
8 D0LZ1W Drug Info IC50 = 7.7 nM [1]
9 D04NXG Drug Info KD = 55 nM [1]
10 D0AY0H Drug Info N.A. [1]
11 D0GB6Y Drug Info N.A. [1]
12 D0MZ8J Drug Info N.A. [1]
13 D0O4TC Drug Info N.A. [1]
Patent ID WO2014055474
Title Mannose Derivatives for Treating Bacterial Infections.
Abstract The present invention relates to compounds useful for the treatment or prevention of bacteria infections. The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. The invention also provides processes for making the compounds of the invention. The compounds of the present invention are represented by the following structure of Formula (A); wherein the variables are as described herein.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D02XNH Drug Info KD = 19 nM Click to Show More [1]
2 D0H4CL Drug Info KD = 29 nM [1]
3 D0B3CU Drug Info KD = 48 nM [1]
4 D0US5I Drug Info KD = 51 nM [1]
5 D0XH4K Drug Info KD = 64 nM [1]
6 D03WXM Drug Info KD = 66 nM [1]
7 D02NDP Drug Info N.A. [1]
8 D0AK2Y Drug Info N.A. [1]
9 D0CN7A Drug Info N.A. [1]
10 D0Q1SX Drug Info N.A. [1]
11 D0Y3UB Drug Info N.A. [1]
Patent ID WO2013134415
Title Mannose Derivatives for Treating Bacterial Infections.
Abstract The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
Applicant(s) Vertex Pharmaceuticals Incorporated
Representative Drug(s) D02WWT Drug Info KD(Binding Assay 1) < 5 nM Click to Show More [1]
2 D07KCA Drug Info KD(Binding Assay 1) < 5 nM [1]
3 D07PVX Drug Info KD(Binding Assay 1) < 5 nM [1]
4 D08BLZ Drug Info KD(Binding Assay 1) < 5 nM [1]
5 D0AM0A Drug Info KD < 5 nM [1]
6 D0B8RU Drug Info KD < 5 nM [1]
7 D0D9MV Drug Info KD < 5 nM [1]
8 D0R1GD Drug Info KD(Binding Assay 1) < 5 nM [1]
9 D0T7VN Drug Info KD(Binding Assay 1) < 5 nM [1]
10 D0WW9B Drug Info KD(Binding Assay 1) < 5 nM [1]
11 D05XGH Drug Info N.A. [1]
12 D0DW7A Drug Info N.A. [1]
13 D0FL3H Drug Info N.A. [1]
14 D0L5OP Drug Info N.A. [1]
15 D0UZ2S Drug Info N.A. [1]
Patent ID WO2012109263
Title Mannoside Compounds and Methods of Use Thereof.
Abstract The present invention encompasses compounds and methods for treating urinary tract infections.
Applicant(s) The Washington University
Representative Drug(s) D0BS3E Drug Info EC90 = 10 nM Click to Show More [1]
2 D0QL0X Drug Info EC90 = 20 nM [1]
3 D0W7VE Drug Info EC90 = 20 nM [1]
4 D0E9GD Drug Info EC90 = 30 nM [1]
5 D0N2AI Drug Info EC90 = 30 nM [1]
6 D0RZ5E Drug Info EC90 = 30 nM [1]
7 D0HE3B Drug Info EC90 = 60 nM [1]
8 D0OW1V Drug Info EC90 = 100 nM [1]
9 D0Z1YF Drug Info EC90 = 120 nM [1]
10 D00COH Drug Info EC90 = 250 nM [1]
11 D0RE0F Drug Info EC90 = 370 nM [1]
12 D0BR9C Drug Info EC90 = 500 nM [1]
13 D0SU0E Drug Info EC90 = 1000 nM [1]
14 D0J0LC Drug Info N.A. [1]
Patent ID WO2011073112
Title Mannose Derivatives As Antagonists of Bacterial Adhesion.
Abstract Compounds of the formula (I) wherein n is 0, 1 or 2, R1 is aryl, heteroaryl or heterocyclyl, and R2 and R3 are hydrogen or a substituent as described in the specification, are useful for the prevention and treatment of bacterial infections, in particular of urinary infections caused by E. coli.
Applicant(s) University of Basel
Representative Drug(s) D09EIQ Drug Info rIC50(competitive binding assay) = 60 nM Click to Show More [1]
2 D01ZKE Drug Info rIC50(competitive binding assay) = 70 nM [1]
3 D0RG1Z Drug Info rIC50(aggreomete assay) = 80 nM; rIC50(competitive binding assay) = 90 nM [1]
4 D0WO6C Drug Info rIC50(competitive binding assay) = 100 nM [1]
5 D0QU6N Drug Info rIC50(competitive binding assay) = 200 nM [1]
6 D0B1HT Drug Info rIC50(aggreomete assay) = 210 nM; rIC50(competitive binding assay) = 220 nM [1]
7 D08WZC Drug Info rIC50(competitive binding assay) = 250 nM [1]
8 D0C8EB Drug Info rIC50(aggreomete assay) = 420 nM; rIC50(competitive binding assay) = 270 nM [1]
9 D0H1BZ Drug Info rIC50(aggreomete assay) = 650 nM; rIC50(competitive binding assay) = 300 nM [1]
10 D0KE8Q Drug Info rIC50(competitive binding assay) = 300 nM [1]
11 D0X7HN Drug Info rIC50(competitive binding assay) = 500 nM [1]
12 D02DFJ Drug Info N.A. [1]
13 D02HPF Drug Info N.A. [1]
14 D02ZYV Drug Info N.A. [1]
15 D07GAN Drug Info N.A. [1]
16 D07QAH Drug Info N.A. [1]
17 D0DI1T Drug Info N.A. [1]
18 D0EA9Y Drug Info N.A. [1]
19 D0FI3Q Drug Info N.A. [1]
20 D0K2AA Drug Info N.A. [1]
Patent ID WO2011050323
Title Compounds and Methods for Treating Bacterial Infections.
Abstract The present invention encompasses compounds and methods for treating urinary tract infections.
Applicant(s) The Washington University
Representative Drug(s) D0IB8D Drug Info EC90 = 130 nM Click to Show More [1]
2 D03KAV Drug Info EC90 = 150 nM [1]
3 D0RE0F Drug Info EC90 = 370 nM [1]
4 D01PBX Drug Info EC90 = 500 nM [1]
5 D0BR9C Drug Info EC90 = 500 nM [1]
6 D0A3PP Drug Info EC90 = 1000 nM [1]
7 D0GM6O Drug Info EC90 = 1000 nM [1]
8 D0SU0E Drug Info EC90 = 1000 nM [1]
9 D03RXE Drug Info EC90 = 2000 nM [1]
10 D05WWX Drug Info EC90 = 2000 nM [1]
11 D0D2QE Drug Info EC90 = 2000 to 4000 nM [1]
12 D0N4TO Drug Info EC90 = 2000 nM [1]
13 D0UG9S Drug Info EC90 = 2000 nM [1]
14 D0VB4T Drug Info EC90 = 2000 nM [1]
15 D03ITZ Drug Info EC90 = 4000 nM [1]
16 D0G9KS Drug Info EC90 = 4000 nM [1]
17 D0NB5P Drug Info EC90 = 4000 nM [1]
18 D0R6FO Drug Info EC90 = 6000 nM [1]
19 D0Y0SI Drug Info EC90 = 6000 nM [1]
20 D03CTH Drug Info EC90 = 8000 nM [1]
21 D05JAS Drug Info EC90 = 8000 nM [1]
22 D0FT4P Drug Info EC90 = 8000 nM [1]
23 D0L3JL Drug Info EC90 = 8000 nM [1]
24 D0SD4Q Drug Info EC90 = 23000 nM [1]
25 D09BGB Drug Info EC90 = 30000 nM [1]
26 D0DH0Y Drug Info EC90 = 30000 nM [1]
27 D06SWT Drug Info EC90 = 32000 nM [1]
28 D09SLI Drug Info EC90 = 60000 nM [1]
29 D0KX1A Drug Info EC90 = 60000 nM [1]
30 D00RQW Drug Info N.A. [1]
31 D08BNB Drug Info N.A. [1]
32 D09TKY Drug Info N.A. [1]
33 D0A8RV Drug Info N.A. [1]
34 D0GV9F Drug Info N.A. [1]
35 D0R1SQ Drug Info N.A. [1]
36 D0ZD6N Drug Info N.A. [1]
37 D0ZR2O Drug Info N.A. [1]
Patent ID WO2005089733
Title Anti-Adhesive Compounds To Prevent and Treat Bacterial Infections.
Abstract The present invention provides compounds and compositions capable of inhibiting the attachment of Gram-negative bacteria on a host epithelium. Accordingly, said compounds and compositions can for example be used for the manufacture of a medicament to treat urinary, lung and gastrointestinal infections caused by said Gram-negative bacteria.
Applicant(s) Vib Vzw Vrije Universiteit Brussel
Representative Drug(s) D07HOP Drug Info KD = 5 nM Click to Show More [1]
2 D07RQA Drug Info KD = 10 nM [1]
3 D0D6OM Drug Info KD = 25 nM [1]
4 D07POS Drug Info KD = 26 nM [1]
5 D0DI6U Drug Info KD = 86 nM [1]
6 D0E3DS Drug Info KD = 137 nM [1]
7 D0UB8U Drug Info KD = 151 nM [1]
8 D0MO0Z Drug Info KD = 300 nM [1]
9 D0L1PO Drug Info KD = 1200 nM [1]
10 D0SE7V Drug Info KD = 2200 nM [1]
11 D0VA1D Drug Info N.A. [1]
12 D0Z6PF Drug Info N.A. [1]
Patent ID WO2014016361
Title Multimeric Mannosides, A Process for Preparing The Same and Their Uses As A Drug.
Abstract The present invention relates to multimeric mannosides, a process for preparing the same and their uses in medicine for treating Escherichia Coli infections. Exemplary compounds are:.
Applicant(s) Centre National De La Recherche Scientifique
Representative Drug(s) D0GR3C Drug Info EC90 = 25000 nM Click to Show More [1]
2 D00XEM Drug Info N.A. [1]
3 D0CD7Q Drug Info N.A. [1]
4 D0M7XB Drug Info N.A. [1]
5 D0QQ5W Drug Info N.A. [1]
6 D0WV9J Drug Info N.A. [1]
Patent ID WO2015110609
Title orally Available Compounds, A Process for Preparing The Same and Their Uses As Anti-Adhesive Drugs for Treating E. Coli Induced Inflammatory Bowel Diseases Such As Crohn'S Disease.
Abstract The present invention relates to orally available compounds, a process for preparing the same and their uses as anti-adhesive drugs for treating E. coli induced inflammatory bowel diseases such as crohn's disease.
Applicant(s) Center Nat Rech Scient
Representative Drug(s) D05OMO Drug Info N.A. Click to Show More [1]
2 D0OW6O Drug Info N.A. [1]
Patent ID WO2012164074
Title Mannose Phosphate Derivatives As Antagonists of Bacterial Adhesion.
Abstract Compounds of the formula (I) (I) wherein n is 0, 1 or 2, R1 is aryl, heteroaryl or heterocyclyl, and R2 and R3 are, independent of each other, hydrogen or a substituent as described in the specification, and one of RA, RB, RC and RD is P02(OH)2 and the other ones are hydrogen; are orally available medicaments useful for the prevention and treatment of bacterial infections, in particular of urinary infections caused by E. coli.
Applicant(s) University of Basel
Representative Drug(s) D00RDO Drug Info N.A. Click to Show More [1]
2 D00XKE Drug Info N.A. [1]
3 D01CND Drug Info N.A. [1]
4 D02UDO Drug Info N.A. [1]
5 D03JFJ Drug Info N.A. [1]
6 D05CBP Drug Info N.A. [1]
7 D0A8GW Drug Info N.A. [1]
8 D0GP7L Drug Info N.A. [1]
9 D0I2MR Drug Info N.A. [1]
10 D0IF4J Drug Info N.A. [1]
11 D0K3DA Drug Info N.A. [1]
12 D0KG5U Drug Info N.A. [1]
13 D0Q0XC Drug Info N.A. [1]
14 D0TP8T Drug Info N.A. [1]
15 D0WO2I Drug Info N.A. [1]
United States Patent and Trademark Office (USPTO)
Patent ID US8937167
Title Compounds and Methods for Treating Bacterial Infections.
References  Top
REF 1 Mannose-derived FimH antagonists: a promising anti-virulence therapeutic strategy for urinary tract infections and Crohn's disease.Expert Opin Ther Pat. 2016;26(2):175-97.

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