- METHODS FOR INHIBITING CASEIN KINASES
-
The present disclosure provides methods for inhibiting CK1 delta or CK1 epsilon activity, comprising administering an effective amount of the compound of Formula (I) to (IV), or a pharmaceutically acceptable salt thereof.
- -
-
Paragraph 00349-00352
(2021/10/02)
-
- COMPOUNDS AS CASEIN KINASE INHIBITORS
-
Provided are novel casein kinase inhibitors, or pharmaceutically acceptable salts thereof. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also provided.
- -
-
Paragraph 00494-00497
(2021/10/02)
-
- HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF CYSTIC FIBROSIS
-
The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular to modulate CFTR protein or ABC protein activities.
- -
-
Page/Page column 62-63
(2018/10/19)
-
- PROCESS FOR PREPARING TEMOZOLOMIDE AND AN INTERMEDIARY
-
The present invention relates to an efficient and industrially advantageous process for preparing temozolomide and the carbamoyl-AICA intermediate through the use of N-methyl carbamoylimidazole in a good overall yield and high purity.
- -
-
Paragraph 054
(2018/07/29)
-
- Noncanonical RNA Nucleosides as Molecular Fossils of an Early Earth—Generation by Prebiotic Methylations and Carbamoylations
-
The RNA-world hypothesis assumes that life on Earth started with small RNA molecules that catalyzed their own formation. Vital to this hypothesis is the need for prebiotic routes towards RNA. Contemporary RNA, however, is not only constructed from the four canonical nucleobases (A, C, G, and U), it also contains many chemically modified (noncanonical) bases. A still open question is whether these noncanonical bases were formed in parallel to the canonical bases (chemical origin) or later, when life demanded higher functional diversity (biological origin). Here we show that isocyanates in combination with sodium nitrite establish methylating and carbamoylating reactivity compatible with early Earth conditions. These reactions lead to the formation of methylated and amino acid modified nucleosides that are still extant. Our data provide a plausible scenario for the chemical origin of certain noncanonical bases, which suggests that they are fossils of an early Earth.
- Schneider, Christina,Becker, Sidney,Okamura, Hidenori,Crisp, Antony,Amatov, Tynchtyk,Stadlmeier, Michael,Carell, Thomas
-
supporting information
p. 5943 - 5946
(2018/04/30)
-
- THERAPEUTIC INHIBITORY COMPOUNDS
-
Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds which are complement factor D inhibitors. Such compounds are useful for treating complement related disorders including, but are not limited to, autoimmune, inflammatory, and neurodegenerative diseases.
- -
-
Paragraph 00361; 00415; 00435; 00452; 00478; 00507; 00519
(2019/01/08)
-
- HEMI-SYNTHETIC TRILOBINE ANALOGS FOR USE AS A DRUG
-
The invention concerns a compound of the following formula (I) or a pharmaceutically acceptable salt or solvate thereof as well as a pharmaceutical composition containing such a compound, and the use of such a compound as a drug, notably as a DNMT inhibit
- -
-
Page/Page column 56
(2017/08/01)
-
- STABILITY-MODULATING LINKERS FOR USE WITH ANTIBODY DRUG CONJUGATES
-
The present invention provides stability-modulated antibody-drug conjugates, stability-modulating linker components used to make these stability-modulated antibody-drug conjugates, therapeutic methods using stability-modulated antibody-drug conjugates, and methods of making stability modulating linkers and stability-modulated antibody-drug conjugates.
- -
-
Page/Page column 85
(2016/03/22)
-
- THERAPEUTIC COMPOUNDS
-
Compounds of formula (I): or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) an
- -
-
Page/Page column 49; 50
(2015/05/05)
-
- PYRROLOPYRROLONE DERIVATIVES AND THEIR USE AS BET INHIBITORS
-
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
- -
-
Page/Page column 70
(2015/06/08)
-
- CERTAIN DIPEPTIDYL PEPTIDASE INHIBITORS
-
Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
- -
-
Paragraph 0231
(2014/06/11)
-
- CERTAIN DIPEPTIDYL PEPTIDASE INHIBITORS
-
Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
- -
-
Paragraph 0231
(2014/06/11)
-
- Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1h- pyrazol-1-yl)ethoxy]-6-methylphenyl}-n-(2,2-difluoropropyl)-5, 7-dihydro-6h-pyrrolo[3,4-d]pyrimidine-6-carboxamide
-
Figure Presented. A novel class of heat shock protein 90 (Hsp90) inhibitors was discovered by high-throughput screening and was subsequently optimized using a combination of structure-based design, parallel synthesis, and the application of medicinal chemistry principles. Through this process, the biochemical and cell-based potency of the original HTS lead were substantially improved along with the corresponding metabolic stability properties. These efforts culminated with the identification of a development candidate (compound 42) which displayed desired PK/PD relationships, significant efficacy in a melanoma A2058 xenograft tumor model, and attractive DMPK profiles.
- Zehnder, Luke,Bennett, Michael,Meng, Jerry,Huang, Buwen,Ninkovic, Sacha,Wang, Fen,Braganza, John,Tatlock, John,Jewell, Tanya,Zhou, Joe Zhongxiang,Burke, Ben,Wang, Jeff,Maegley, Karen,Mehta, Pramod P.,Yin, Min-Jean,Gajiwala, Ketan S.,Hickey, Michael J.,Yamazaki, Shinji,Smith, Evan,Kang, Ping,Sistla, Anand,Dovalsantos, Elena,Gehring, Michael R.,Kania, Robert,Wythes, Martin,Kung, Pei-Pei
-
experimental part
p. 3368 - 3385
(2011/06/27)
-