- Selective Isomerization via Transient Thermodynamic Control: Dynamic Epimerization of trans to cis Diols
-
Traditional approaches to stereoselective synthesis require high levels of enantio- and diastereocontrol in every step that forms a new stereocenter. Here, we report an alternative approach, in which the stereochemistry of organic substrates is selectivel
- Macmillan, David W. C.,Oswood, Christian J.
-
supporting information
p. 93 - 98
(2022/01/03)
-
- PEPTIDE CONJUGATES OF CYTOTOXINS AS THERAPEUTICS
-
The present invention relates to peptide conjugates of cytotoxins such as topoisomerase I inhibitors which are useful for the treatment of diseases such as cancer.
- -
-
Paragraph 0431-0432
(2021/01/25)
-
- 6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
-
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
- -
-
Paragraph 0425; 0426
(2021/11/13)
-
- ANTI-INFLAMMATORY COMPOSITIONS COMPRISING IRAK AND JAK INHIBITORS
-
The present invention discloses compositions comprising compounds according to Formula I wherein R1, R2, and Cy are as defined herein, and a second compound having a JAK inhibiting activity. The present invention relates to composition, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases, proliferative diseases, allergic diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound of the invention
- -
-
Paragraph 0245; 0246
(2018/09/21)
-
- 6-[5-AMINO-6-(2-ETHOXYETHOXY)-IMIDAZO[4,5-B]PYRIDIN-3-YL]-NICOTINONITRILE DERIVATIVES AND THEIR USE AS IRAK INHIBITORS
-
The present invention discloses compounds according to Formula (I): wherein R1, R2, and Cy are as defined herein. The present invention relates to compounds inhibiting IRAK family kinases, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of inflammatory diseases, autoimmune diseases and/or proliferative diseases by administering the compound of the invention.
- -
-
Paragraph 00186
(2017/05/10)
-
- FLOURO-NAPHTHYL DERIVATIVES
-
The present invention relates to compounds of formula wherein R1 is C4-6-cycloalkyl or C4-6-heterocycloalkyl, which are optionally substituted by one or two substituents, selected from hydroxy or lower alkyl; A is phenyl, pyridinyl or piperidinyl; R2 is hydrogen, halogen, lower alkyl, cyano, C4-6-cycloalkyl, lower alkoxy, lower alkoxy substituted by halogen, or is a five- or six-membered heteroaryl, optionally substituted by lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.
- -
-
Paragraph 0096
(2016/11/28)
-
- SUBSTITUTED PYRIDINES AND METHOD OF USE
-
The invention discloses compounds of Formula (I) wherein X, R1, R2, and R3 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
- -
-
Paragraph 00303
(2016/12/22)
-
- SELECTIVE ANDROGEN RECEPTOR MODULATORS
-
The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.
- -
-
Page/Page column 36-37
(2013/04/25)
-
- SUBSTITUTED CYCLIC COMPOUNDS AND METHODS OF USE
-
The present invention provides novel substituted cyclic compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
- -
-
Paragraph 0239
(2013/09/26)
-
- SELECTIVE KINASE INHIBITORS
-
Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
- -
-
Paragraph 0749
(2013/06/06)
-
- PYRIMIDINECARBOXAMIDE DERIVATIVES AS INHIBITORS OF SYK KINASE
-
The compound of formula (I) or a salt, preferably a pharmaceutically acceptable salt, thereof; is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate mast cell activation, for ins
- -
-
Page/Page column 33-34
(2010/09/17)
-