- NOVEL CYTOTOXIC AGENTS FOR CONJUGATION OF DRUGS TO CELL BINDING MOLECULE
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Provided are cytotoxic agents, pyrrolo[2,1-c][1,4]benzodiazepine (PBD) derivatives, their conjugates with a cell-binding agent, the preparation and the therapeutic uses in the targeted treatment of cancers, autoimmune disorders, and infectious diseases.
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Page/Page column 88
(2015/03/16)
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- Bridged Ring compounds As Hepatitis C Virus (HCV) Inhibitors And Pharmaceutical Applications Thereof
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Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
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Paragraph 1638; 1654; 1655; 1656; 1657
(2015/03/28)
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- BRIDGED RING COMPOUNDS AS HEPATITIS C VIRUS (HCV) INHIBITORS AND PHARMACEUTICAL APPLICATIONS THEREOF
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Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
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Paragraph 00601
(2014/02/16)
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- SPIRO RING COMPOUND AS HEPATITIS C VIRUS (HCV) INHIBITOR AND USES THEREOF FIELD OF THE INVENTION
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A compound of formula (I) or a stereoisomer, a geometric isomer. a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof is provided, which can be used for treating HCV infection or a HCV disorder. Also a pharmaceutical composition comprising the compound and the use of the compound and the pharmaceutical composition thereof are provided, which can also be used for treating HCV infection or a HCV disorder.
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Page/Page column 170; 171
(2014/06/23)
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- Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists
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This Letter describes a chemical lead optimization campaign directed at a weak mGlu5 NAM discovered while developing SAR for the mGlu 5 PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu5 NAMs, mGlu5 PAMs as well as mGlu5 partial antagonists.
- Lamb, Jeffrey P.,Engers, Darren W.,Niswender, Colleen M.,Rodriguez, Alice L.,Venable, Daryl F.,Conn, Jeffrey P.,Lindsley, Craig W.
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scheme or table
p. 2711 - 2714
(2011/06/20)
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- A new highly versatile handle for chemistry on a solid support: The pipecolic linker
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The design, synthesis, and potential application of the pipecolic linker is presented. This new versatile handle can immobilize primary, secondary, and aromatic amines, as well as alcohols, phenols, and hydrazides, on a solid support. Compared with other linkers, the anchoring step is easy and efficient. The release of final products from the resin proceeds upon acidic treatment with high purities. The pipecolic linker offers the promise of being using in peptide chemistry to produce peptides modified at the N and C terminus, peptidomimetics, as well as small organic molecules.
- Zajdel, Pawel,Nomezine, Gael,Masurier, Nicolas,Amblard, Muriel,Pawlowski, Maciej,Martinez, Jean,Subra, Gilles
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supporting information; experimental part
p. 7547 - 7553
(2010/08/20)
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- Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors
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The cholecystokinin-8 (CCK-8)-inactivating peptidase is a serine peptidase that has been shown to be a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4.14.10). It cleaves the neurotransmitter CCK-8 sulfate at the Met-Gly bond to give Asp-Tyr(SO
- Ganellin, C. Robin,Bishop, Paul B.,Bambal, Ramesh B.,Chan, Suzanne M. T.,Leblond, Bertrand,Moore, Andrew N. J.,Zhao, Lihua,Bourgeat, Pierre,Rose, Christiane,Vargas, Froylan,Schwartz, Jean-Charles
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p. 7333 - 7342
(2007/10/03)
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- Heterocyclic compounds as inhibitors of rotomase enzymes
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Compounds of the formula: wherein R1, Y, W, A and R2are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.
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- Benzhydryl derivatives
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A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the
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- Heterocyclic compounds as inhibitors of rotamase enzymes
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Compounds of the formula (I): wherein A, Y, R, X, R1, R2, R3and R4are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases or other disorders involving nerve damage.
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- FKBP inhibitors
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Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors.
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- Synthesis of (D)- And (L)-forms of differentially protected 2-piperidinemethanamine
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(D)- and (L)-isomers of pipecolic acid were converted into (D)- and (L)-2-piperidinemethanamine using an efficient sequence. The amino groups were selectively protected for further functionalization.
- Perumattam, John,Shearer, Barry G.,Confer, William L.,Mathew, Rose M.
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p. 7183 - 7186
(2007/10/02)
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- ENANTIOSELECTIVE REDUCTIONS OF KETONES WITH OXAZABOROLIDINES DERIVED FROM (R) AND (S)-α,α-DIPHENYL-2-PIPERIDINE METHANOL
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Oxazaborolidnes obtained from (R) and (S)-α,α-diphenyl-2-piperidine methanol have been used as catalysts in the enantioselective reductions of ketones with borane.
- Rao, A. V. Rama,Gurjar, M. K.,Sharma, P. A.,Kaiwar, Vijay
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p. 2341 - 2344
(2007/10/02)
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