- THERAPEUTIC INHIBITORY COMPOUNDS
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Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. Said heterocyclic derivative compounds are complement factor D inhibitors. Such compounds are useful for treating complement related disorders including, but are not limited to, autoimmune, inflammatory, and neurodegenerative diseases.
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Paragraph 00174
(2018/02/22)
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- THERAPEUTIC INHIBITORY COMPOUNDS
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Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds which are complement factor D inhibitors. Such compounds are useful for treating complement related disorders including, but are not limited to, autoimmune, inflammatory, and neurodegenerative diseases.
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Paragraph 00175
(2019/01/08)
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- THERAPEUTIC INHIBITORY COMPOUNDS
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Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds which are complement factor D inhibitors. Such compounds are useful for treating complement related disorders including, but are not limited to, autoimmune, inflammatory, and neurodegenerative diseases.
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Paragraph 00205
(2017/07/04)
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- 1 - (3 - benzoyl-aminobenzyl) - 1H - indazole - 3 - carboxamides and its preparation method and anti-viral uses (by machine translation)
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The invention relates to a anti-viral inhibitors, in particular, relates to a class of non-nucleoside anti-virus can be used as an inhibitor of the general formula 1 indicated by the 1 - (3 - benzoyl-aminobenzyl) - 1H - indazole - 3 - carboxamides of the organic small molecule compound, and its pharmaceutically acceptable salt or hydrate, its preparation method and its in preparation for treating hepatitis c, hepatitis b, influenza, herpes, viral diseases such as aids in the application of the pharmaceutical, in particular for the preparation of a medicament in the treatment of hepatitis c of the application. Said compound of the invention has the advantages of simple synthesis, easy availability of raw materials, the advantages of low toxicity. (by machine translation)
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Paragraph 0041; 0042; 0043; 0044
(2017/01/17)
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- INDAZOLE DERIVATIVES AS ADENOSINE MONOPHOSPHATE DEAMINASE (AMPD) INHIBITORS FOR USE IN DIABETES AND RELATED DISEASES OF METABOLIC SYNDROME
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Herein, we describe a method for treatment of diabetes and other disorders classified as Metabolic Syndrome. The invention provides novel AMP Deaminase (AMPD) inhibitors comprising novel indazole and benzotriazole derivatives including a phosphorous containing derivative, a carboxylic acid, or an amino acid ester prodrug. The invention also provides support for a novel mechanism of action for the existing drug metformin: direct inhibition of the enzyme AMPD. The inhibition of AMPD in turn activates AMP Kinase, known to be linked to the action of metformin. The invention also makes novel use of a double inhibitor assay allowing identification of selective AMPD inhibitors over ADA inhibitors. The new inhibitors, structurally distinct from metformin, offer selectivity that may obviate side effects known for metformin itself, providing new benefits for diabetes and Metabolic Syndrome.
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Page/Page column 2-3
(2012/06/01)
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- Design and Synthesis of N-Substituted Indazole-3-Carboxamides as Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors
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A group of novel N-1-substituted indazole-3-carboxamide derivatives were synthesized and evaluated as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). A structure-based design strategy was applied to a weakly active unsubstituted 1H-indazole-3-carboxamide 2, by introducing a three carbon linker between 1H-indazole-3-carboxamide and different heterocycles, and led to compounds 4 [1-(3-(piperidine-1-yl)propyl)-1H-indazole-3-carboxamide, IC50=36μm] and 5 [1-(3-(2,3-dioxoindolin-1-yl)propyl)-1H-indazole-3-carboxamide, IC50= 6.8μm]. Compound 5 was evaluated in rats for its protective action against diabetes induced by a treatment with streptozotocin, a known diabetogenic agent. In addition to preserving the ability of the pancreas to secrete insulin, compound 5 was also able to attenuate the ensuing hyperglycemic response to a significant extent.
- Patel, Maulik R.,Pandya, Kashyap G.,Lau-Cam, Cesar A.,Singh, Satyakam,Pino, Maria A.,Billack, Blase,Degenhardt, Kurt,Talele, Tanaji T.
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experimental part
p. 488 - 496
(2012/06/18)
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- NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
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Compounds of Formula (I) are HIV reverse transcriptase inhibitors, wherein X, R1, R2, R3, R4 and R5 are defined herein. The compounds of Formula (I) and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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Page/Page column 63
(2008/12/05)
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- Diazabicyclo derivatives
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Diazabicyclo derivatives of formula (I) and pharmaceutically acceptable salts thereof: STR1 wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, oxoalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyl, dialkylaminoalkyl, hydroxyalkyl, haloalkyl, cyanoalkyl, heterocycloalkyl, aryl, heteroarylalkyl or arylalkyl, the aryl group and the aryl moiety being optionally substituted by alkoxy, nitro, alkyl, amino or halo;R 2 is hydrogen or alkyl;R 3 and R 4 may be the same or different and each is hydrogen, alkyl, alkenyl, acyl, alkoxyalkyl or arylalkyl wherein the aryl moiety is optionally substituted by alkoxy, nitro, alkyl, amino or halo;with the proviso that when R 2 is hydrogen and both R 3 and R 4 are methyl, R 1 does not represent hydrogen, alkyl, unsubstituted benzyl or dimethylaminoethyl; having 5-HT 3 receptor antagonist activity.
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