- Pd-Catalysed direct C(sp2)-H fluorination of aromatic ketones: Concise access to anacetrapib
-
The Pd-cataylsed direct ortho-C(sp2)-H fluorination of aromatic ketones has been developed for the first time. The reaction features good regioselectivity and simple operations, constituting an alternative shortcut to access fluorinated ketones. A concise synthesis of anacetrapib has also been achieved by using late-stage C-H fluorination as a key step.
- Wu, Qiuzi,Mao, Yang-Jie,Zhou, Kun,Wang, Shuang,Chen, Lei,Xu, Zhen-Yuan,Lou, Shao-Jie,Xu, Dan-Qian
-
supporting information
p. 4544 - 4547
(2021/05/17)
-
- Dual-Metal N-Heterocyclic Carbene Complex (M = Au and Pd)-Functionalized UiO-67 MOF for Alkyne Hydration-Suzuki Coupling Tandem Reaction
-
Metal N-heterocyclic carbene complexes (NHC-M) have been recognized as an important class of organometallic catalysts. Herein, we demonstrate that different NHC-M (M = Au and Pd) species can be simultaneously introduced into a single metal organic framework (MOF) by direct assembly of NHC-M-decorated ligands and metal ions under solvothermal conditions. The obtained UiO-67-Au/Pd-NHBC MOF with different organometallic NHC-M species can be a highly reusable dual catalyst to sequentially promote alkyne hydration-Suzuki coupling reaction. The potential utility of this strategy is highlighted by the preparation of many more new multicatalysts of this type for various organic transformations in a sequential way.
- Dong, Ying,Li, Wen-Han,Dong, Yu-Bin
-
p. 1818 - 1826
(2021/01/13)
-
- Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mG
-
This work describes the discovery and characterization of novel 6-(1H-pyrazolo[4,3-b]pyridin-3-yl)amino-benzo[d]isothiazole-3-carboxamides as mGlu4 PAMs. This scaffold provides improved metabolic clearance and CYP1A2 profiles compared to previo
- Bollinger, Sean R.,Engers, Darren W.,Panarese, Joseph D.,West, Mary,Engers, Julie L.,Loch, Matthew T.,Rodriguez, Alice L.,Blobaum, Anna L.,Jones, Carrie K.,Thompson Gray, Analisa,Conn, P. Jeffrey,Lindsley, Craig W.,Niswender, Colleen M.,Hopkins, Corey R.
-
supporting information
p. 342 - 358
(2018/10/20)
-
- HEPARAN SULFATE BIOSYNTHESIS INHIBITORS FOR THE TREATMENT OF DISEASES
-
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions in need of inhibition of heparan sulfate biosynthesis.
- -
-
Paragraph 000463; 000672
(2016/05/02)
-
- HETEROCYCLIC COMPOUNDS AS CALCIUM SENSING RECEPTOR MODULATORS FOR THE TREATMENT OF HYPERPARATHYROIDISM, CHRONIC RENAL FAILURE AND CHRONIC KIDNEY DISEASE
-
The invention relates to heterocyclic compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their pharmaceutical compositions for use in medicine for the treatment of diseases or disorders associated with the modulation of calcium sensing receptor modulators (CaSR), like e.g. hyperparathyroidism, chronic renal failure and chronic kidney disease and their complications.
- -
-
Page/Page column 50; 51
(2015/11/16)
-
- HETEROCYCLIC COMPOUND AND USE THEREOF
-
The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and use thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
- -
-
Page/Page column 69; 70
(2012/06/01)
-
- PHTALAZINE DERIVATIVES AS JAK1 INHIBITORS
-
JAK1 inhibitors of structural formula (I), wherein Ar1, Ar2, Q, W, X, Y, and Z are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
- -
-
Page/Page column 42; 43
(2012/04/04)
-
- HETEROCYCLIC COMPOUND AND USE THEREOF
-
The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
- -
-
Page/Page column 41
(2012/03/26)
-
- INDAZOLE COMPOUNDS USEFUL AS KETOHEXOKINASE INHIBITORS
-
The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
- -
-
Page/Page column 37
(2011/11/06)
-
- NOVEL KINASE MODULATORS
-
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
- -
-
Page/Page column 97-98
(2011/06/10)
-
- NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5- DISUBSTITUTED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN KINASES
-
The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
- -
-
Page/Page column 85-86
(2011/11/30)
-
- NOVEL 3,5-DISUBSTITUED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5- DISUBSTITUED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN KINASES
-
The present invention provides, inter alia, compounds of formula ΙΑ,ΙΙΑ and III as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
- -
-
Page/Page column 114-115
(2011/12/04)
-
- COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
-
This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
- -
-
Page/Page column 119
(2010/06/11)
-
- PYRAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH
-
The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and t
- -
-
-
- Oxazolidone derivatives as PR modulators
-
Compounds of the following structure are described: wherein R1, R2, R5, R6, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
- -
-
Page/Page column 32
(2008/06/13)
-
- 7-Fluoroindazoles as potent and selective inhibitors of factor Xa
-
We have developed a novel series of potent and selective factor Xa inhibitors that employ a key 7-fluoroindazolyl moiety. The 7-fluoro group on the indazole scaffold replaces the carbonyl group of an amide that is found in previously reported factor Xa inhibitors. The structure of a factor Xa cocrystal containing 7-fluoroindazole 51a showed the 7-fluoro atom hydrogen-bonding with the N-H of Gly216 (2.9 ?) in the peptide backbone. Thus, the 7-fluoroindazolyl moiety not only occupied the same space as the carbonyl group of an amide found in prior factor Xa inhibitors but also maintained a hydrogen bond interaction with the protein's β-sheet domain. The structure-activity relationship for this series was consistent with this finding, as the factor Xa inhibitory potencies were about 60-fold greater (ΔΔG ≈ 2.4 kcal/mol) for the 7-fluoroindazoles 25a and 25c versus the corresponding indazoles 25b and 25d. Highly convergent synthesis of these factor Xa inhibitors is also described.
- Lee, Yu-Kai,Parks, Daniel J.,Lu, Tianbao,Thieu, Tho V.,Markotan, Thomas,Pan, Wenxi,McComsey, David F.,Milkiewicz, Karen L.,Crysler, Carl S.,Ninan, Nisha,Abad, Marta C.,Giardino, Edward C.,Maryanoff, Bruce E.,Damiano, Bruce P.,Player, Mark R.
-
p. 282 - 297
(2008/09/17)
-
- Therapeutic Piperazines
-
The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administra
- -
-
Page/Page column 13-14
(2010/11/28)
-
- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
-
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
- -
-
Page/Page column 67
(2010/11/27)
-
- CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
-
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
- -
-
Page/Page column 260-262
(2008/06/13)
-
- INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
-
Compounds of formula (I) are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus.
- -
-
Page/Page column 78-79
(2010/02/07)
-
