- GLUCOCORTICOID RECEPTOR MODULATORS
-
Described herein are glucocorticoid receptor modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.
- -
-
Paragraph 00213
(2020/05/19)
-
- GLUCOCORTICOID RECEPTOR MODULATORS
-
Described herein are glucocorticoid receptor modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.
- -
-
Paragraph 00275
(2018/11/10)
-
- Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2)
-
We report the synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamides (4) as CCR2 inhibitors for the potential treatment of inflammatory diseases. Several of the compounds display nanomolar binding affinity for CCR2. The in vitro structure-activity
- Yang, Michael G.,Xiao, Zili,Shi, Qing,Cherney, Robert J.,Tebben, Andrew J.,De Lucca, George V.,Santella III, Joseph B.,Mo, Ruowei,Cvijic, Mary Ellen,Zhao, Qihong,Barrish, Joel C.,Carter, Percy H.
-
scheme or table
p. 1384 - 1387
(2012/03/26)
-
- γ-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists
-
We describe the design, synthesis, and evaluation, of γ-lactams as glycinamide replacements within a series of di- and trisubstituted cyclohexane CCR2 antagonists. The lactam-containing trisubstituted cyclohexanes proved to be more potent than the disubst
- Cherney, Robert J.,Mo, Ruowei,Meyer, Dayton T.,Voss, Matthew E.,Yang, Michael G.,Santella III, Joseph B.,Duncia, John V.,Lo, Yvonne C.,Yang, Gengjie,Miller, Persymphonie B.,Scherle, Peggy A.,Zhao, Qihong,Mandlekar, Sandhya,Cvijic, Mary Ellen,Barrish, Joel C.,Decicco, Carl P.,Carter, Percy H.
-
scheme or table
p. 2425 - 2430
(2010/08/05)
-
- Cyclic derivatives as modulators of chemokine receptor activity
-
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.
- -
-
Page/Page column 108
(2008/06/13)
-
- Process of preparing N-ureidoalkyl-piperidines
-
The present application describes a process of preparing a compound of formula (IV), or salt or stereoisomer thereof: wherein Pg, at each occurrence, is independently selected from an amine protecting group; comprising the steps of reacting a compound of Formula with a reducing agent to give a compound of Formula III: reacting the compound of formula (III) with an amine of formula (IIa) using reductive amination to give the compound of formula (III)
- -
-
Page/Page column 4-5
(2008/06/13)
-
- Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
-
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
- -
-
Page/Page column 32
(2010/02/11)
-
- N-UREIDOALKYL-AMINO COMPOUNDS AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
-
The present application describes modulators of chemokine receptors of formula (I), or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
- -
-
Page/Page column 193-194
(2008/06/13)
-
- N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
-
The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheum
- -
-
-
- Cyclic derivatives as modulators of chemokine receptor activity
-
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis, asthma, restinosis, organ transplantation, and
- -
-
-
- Taxamycin studies: Synthesis of taxoid-calicheamicin hybrids
-
The synthesis of the bicyclic enediyne compounds 14-18 is described. The bicyclo[7.3.1]trideca-4,9-dien-2,6-diynes (21) are calicheamicin-taxoid mimics, that possess the Taxotere side chain and an enediyne core. Cyclization of the iodo-aldehyde 13 [CrCl2(THF)2] afforded the bicyclic alcohol 14 as a single diastereomer (76%) and allylic oxidation (SeO2) followed by reaction with the oxazolidine intermediate 19, resolution and hydrolysis provided the taxamycins 21.
- Py, Sandrine,Harwig, Curtis W.,Banerjee, Srabani,Brown, David L.,Fallis, Alex G.
-
p. 6139 - 6142
(2007/10/03)
-
- ENANTIOSELECTIVE SYNTHESIS OF SUBSTITUTED OCTALONES
-
The octalones (R)-(-)-1a and (S)-(-)-1b were prepared from the Michael adducts 7a and 7b respectively.These intermediates were obtained by the "deracemizing alkylation" of cyclanones 3a and 3b.
- Sequeira, Lucia C.,Costa, Paulo R. R.,Neves, Alexandre,Esteves, Pierre
-
p. 1433 - 1434
(2007/10/02)
-
- 148. Diastereo- und enantioselektive Reduktion von β-Ketoestern mit Cyclopentanon-, Cyclohexanon-, Piperidon- und Tetralon-Struktur durch nicht fermentierende Baecker-Hefe
-
Under 'nonfermenting' conditions, i.e. in tap water, in the absence of nutrients, baker's yeast (25-380 g/g of substrate, aerobic) reduces β-keto esters such as those mentioned in the title with better selectivity than under the normally employed 'ferment
- Seebach, Dieter,Roggo, Silvio,Maetzke, Thomas,Braunschweiger, Hans,Cercus, Jacques,Krieger, Manfred
-
p. 1605 - 1615
(2007/10/02)
-
- PREPARATION OF CHIRAL CYCLOHEXANOL DERIVATIVE WITH HIGH OPTICAL PURITY BY YEAST REDUCTION
-
Reduction of 2-ethoxycarbonyl-4,4-ethylenedioxycyclohexanone (6) with baker's yeast provided cis-hydroxy ester 7 in 74percent yield as a sole product.Optical purity of 7 was determined as its MTPA ester to be 98.4percent e.e. 10 g of the chiral 7 could be produced in one lot.
- Kitahara, Takeshi,Mori, Kenji
-
p. 451 - 452
(2007/10/02)
-