Patent classifications
C07D279/12
Bumetanide analogs, compositions and methods of use
The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na.sup.+K.sup.+Cl.sup. co-transporter or GABA.sub.A receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma. Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.
Onium salt compound, resist composition, and pattern forming process
Sulfonium and iodonium salts of a carboxylate having an aromatic ring to which a nitrogen-containing alkyl or cyclic structure is attached are novel. The onium salt functions as an acid diffusion controlling agent in a resist composition, enabling to form a pattern of good profile with high resolution, improved MEF, LWR and DOF.
Onium salt compound, resist composition, and pattern forming process
Sulfonium and iodonium salts of a carboxylate having an aromatic ring to which a nitrogen-containing alkyl or cyclic structure is attached are novel. The onium salt functions as an acid diffusion controlling agent in a resist composition, enabling to form a pattern of good profile with high resolution, improved MEF, LWR and DOF.
NON-ATP/CATALYTIC SITE p38 MITOGEN ACTIVATED PROTEIN KINASE INHIBITORS
Compounds that inhibit p38 MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
METHOD OF INHIBITING TAU PHOSPHORYLATION
A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.
METHOD OF INHIBITING TAU PHOSPHORYLATION
A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.
Compositions of dual thyrointegrin antagonists and use in vascular-associated disorders
A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and v3 integrin antagonist in the same molecule.
Compositions of dual thyrointegrin antagonists and use in vascular-associated disorders
A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and v3 integrin antagonist in the same molecule.
Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
- Richard T. Lewis ,
- Jennifer R. Allen ,
- Yuan Cheng ,
- Deborah Choquette ,
- Oleg Epstein ,
- Angel Guzman-Perez ,
- Paul E. HARRINGTON ,
- Zihao Hua ,
- Randall W. Hungate ,
- Jason Brooks Human ,
- Ted Judd ,
- Qingyian Liu ,
- Patricia Lopez ,
- Ana Elena MINATTI ,
- Philip Olivieri ,
- Karina Romero ,
- Shannon Rumfelt ,
- Robert M. Rzasa ,
- Laurie Schenkel ,
- JOHN STELLWAGEN ,
- Ryan White ,
- Qiufen Xue ,
- Xiao Mei Zheng ,
- Wenge Zhong
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A.sup.4, A.sup.5, A.sup.6, A.sup.8, R.sup.1, R.sup.2, R.sup.3, R.sup.7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II. ##STR00001##
Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
- Richard T. Lewis ,
- Jennifer R. Allen ,
- Yuan Cheng ,
- Deborah Choquette ,
- Oleg Epstein ,
- Angel Guzman-Perez ,
- Paul E. HARRINGTON ,
- Zihao Hua ,
- Randall W. Hungate ,
- Jason Brooks Human ,
- Ted Judd ,
- Qingyian Liu ,
- Patricia Lopez ,
- Ana Elena MINATTI ,
- Philip Olivieri ,
- Karina Romero ,
- Shannon Rumfelt ,
- Robert M. Rzasa ,
- Laurie Schenkel ,
- JOHN STELLWAGEN ,
- Ryan White ,
- Qiufen Xue ,
- Xiao Mei Zheng ,
- Wenge Zhong
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A.sup.4, A.sup.5, A.sup.6, A.sup.8, R.sup.1, R.sup.2, R.sup.3, R.sup.7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II. ##STR00001##