- THERAPEUTIC COMPOUNDS
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The present disclosure relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, and compositions and uses thereof. The compounds are useful as inhibitors of the YAP:TEAD protein:protein interaction. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various YAP:TEAD-mediated disorders, including cancer.
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Paragraph 00442-00443
(2021/06/04)
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- COMPOUNDS
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A compound of formula (I), or a pharmaceutically acceptable salt thereof.
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Page/Page column 72-73
(2020/01/24)
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- COMPOUNDS
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A compound of formula (I), or a pharmaceutical salt thereof.
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Page/Page column 103-104
(2020/01/11)
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- 2-phenylindole and arylsulphonamide: Novel scaffolds bactericidal against mycobacterium tuberculosis
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A cellular activity-based screen on Mycobacterium tuberculosis (Mtb) H37Rv using a focused library from the AstraZeneca corporate collection led to the identification of 2-phenylindoles and arylsulphonamides, novel antimycobacterial scaffolds. Both the series were bactericidal in vitro and in an intracellular macrophage infection model, active against drug sensitive and drug resistant Mtb clinical isolates, and specific to mycobacteria. The scaffolds showed promising structure-activity relationships; compounds with submicromolar cellular potency were identified during the hit to lead exploration. Furthermore, compounds from both scaffolds were tested for inhibition of known target enzymes or pathways of antimycobacterial drugs including InhA, RNA polymerase, DprE1, topoisomerases, protein synthesis, and oxidative-phosphorylation. Compounds did not inhibit any of the targets suggesting the potential of a possible novel mode of action(s). Hence, both scaffolds provide the opportunity to be developed further as leads and tool compounds to uncover novel mechanisms for tuberculosis drug discovery.
- Naik, Maruti,Ghorpade, Sandeep,Jena, Lalit Kumar,Gorai, Gopinath,Narayan, Ashwini,Guptha, Supreeth,Sharma, Sreevalli,Dinesh, Neela,Kaur, Parvinder,Nandishaiah, Radha,Bhat, Jyothi,Balakrishnan, Gayathri,Humnabadkar, Vaishali,Ramachandran, Vasanthi,Naviri, Lava Kumar,Khadtare, Pallavi,Panda, Manoranjan,Iyer, Pravin S.,Chatterji, Monalisa
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supporting information
p. 1005 - 1009
(2014/12/10)
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- NOVEL ISOPHTHALATES AS BETA-SECRETASE INHIBITORS
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There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
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Page/Page column 43-44
(2010/11/23)
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- POSITIVE ALLOSTERIC MODULATORS OF THE NICOTINIC ACETYLCHOLINE RECEPTOR
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The invention provides compounds of Formula (I). These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in wh
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Page 63; 65-66
(2010/02/08)
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- UREIDO-SUBSTITUTED ANILINE COMPOUNDS USEFUL AS SERINE PROTEASE INHIBITORS
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Compounds having formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa.
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- Adenosine receptor ligands and their use in the treatment of disease
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The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.
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- 6-HETEROCYCLIC-4-AMINO-1,2,2A,3,4,5-HEXAHYDROBENZ[CD]INDOLES
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6-Heterocyclic-4-amino-l,2,2a,3,4,5-hexahydrobenz[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
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- 6-HETEROCYCLIC-4-AMINO-1,3,4,5-TETRAHYDROBENZ[CD]INDOLES
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6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
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