74901-69-2Relevant academic research and scientific papers
Development of a Practical Process for the Synthesis of PDE4 Inhibitors
Frutos, Rogelio P.,Tampone, Thomas G.,Mulder, Jason A.,Rodriguez, Sonia,Yee, Nathan K.,Yang, Bing-Shiou,Senanayake, Chris H.
, p. 982 - 988 (2016/06/09)
A practical, safe, and efficient process for the synthesis of PDE4 (phosphodiesterase type 4) inhibitors represented by 1 and 2 was developed and demonstrated on a multi-kilogram scale. Key aspects of the process include the regioselective synthesis of dihydrothieno[3,2-d]pyrimidine-2,4-diol 9 and the asymmetric sulfur oxidation of intermediate 11.
NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA
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, (2015/02/25)
Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein: Ring A is a 6-membered aromatic ring optionally comprising one or two nitrogen atoms andR is Cl and is located in the para-, meta-, or ortho-position of Ring A,S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
SPECIFIC PDE4B-INHIBITORS FOR THE TREATMENT OF DIABETES MELLITUS
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, (2014/08/19)
A method of treating diabetes mellitus or a microvascular or macrovascular complication of diabetes mellitus in a patient in need thereof, the method comprising administering to the patient a compound of formula 1 wherein R1, R2, R3, and R4 are as defined in claim 1.
SPECIFIC PDE4B-INHIBITORS FOR THE TREATMENT OF DIABETES MELLITUS
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, (2014/09/03)
The invention relates to compounds of formula 1 for their use for the treatment of diabetes mellitus or for the treatment of a microvascular or macrovascular complication of diabetes mellitus wherein R1, R2, R3 and R4 are defined as summarized in claim 1. Further the invention relates to the use of compounds of the above formula 1 for the manufacture of a medicament for the treatment of diabetes mellitus or for the treatment of a microvascular or macrovascular complication of diabetes mellitus.
MORPHOLINO SUBSTITUTED BICYCLIC PYRIMIDINE UREA OR CARBAMATE DERIVATIVES AS MTOR INHIBITORS
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Page/Page column 44; 63; 64, (2013/04/24)
The invention relates to compounds of formula (I) wherein m, o, Ra, Rb, R1 and T1 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments
NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA
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, (2013/03/26)
The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is CI and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
NOVEL COMPOUNDS
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Paragraph 0364; 0365; 0366; 0367, (2013/06/27)
This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
1,2,4 -TRIAZOLES AS ALLOSTERIC MODULATORS OF MGLU5 RECEPTOR ACTIVITY FOR THE TREATMENT OF SCHIZOPHRENIA OF DEMENTIA
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Page/Page column 90, (2013/06/27)
This invention relates to compounds of formula (I) their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
Compounds for the treatment of inflammatory diseases
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Page/Page column 30; 31, (2008/06/13)
Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
DIHYDROTHIENOPYRIMIDINES FOR THE TREATMENT OF INFLAMMATORY DISEASES
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, (2008/06/13)
The invention relates to novel dihydrothienopyrimidines of formula (1) as well as pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of ailments or diseases of the respiratory tract, gastrointestinal ailments or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system, or cancer diseases. Also disclosed are pharmaceutical compositions containing the inventive compounds.
