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Pyrimido[5,4]-dipyrimidines, pharmaceuticals containing them, their use and processes for the preparation thereof

Pyrimido[5,4-d]pyrimidines of the general formula [Figure] which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are: 4-[(3-Chloro-4-fluorophenyl)amino]-6-[1-methyl-4-piperidinylamino]pyrimido[5,4-d]pyrimidine, and 4-[(3-Chloro-4-fluorophenyl)amino]-6-[trans-4-dimethyl-aminocycohexylamino]pyrimido[5,4-d]pyrimidine.

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Quinuclidine – Wikipedia,
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2 SUBSTITUTED CEPHEM COMPOUNDS

The compounds of formula (I) of the subject invention are related to 2-substituted cephem compounds, which have a wide antimicrobial spectrum, in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical compositions comprising the same.

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Quinazolinone derivatives possessing calcium uptake inhibiting activity

This invention is to provide quinazolinone derivatives, and their acid salts and quaternary ammonium salts, having an effect of preventing or treating diseases caused by calcium ion overload in cells, such as ischemic heart disease, ischemic cerebral disease and ischemic renal disease, and their usage. The quinazolinone derivatives are represented by the formula: STR1 typically, T represents an oxygen atom; Y represents a phenyl or cyclohexyl group; R1 represents a hydrogen or chlorine atom; R2 represents a hydrogen atom; ring W represents a benzene or pyridine ring; Z represents a group of the formula: STR2

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Quinuclidine – Wikipedia,
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CEPHALOSPORIN HAVING CATECHOL GROUP

The present invention provides Cephem compounds which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria as follows: A compound of the formula: wherein, X is N, CH or C-Cl; T is S or the like; A and G are lower alkylene or the like; B is a single bond or the like; D is a single bond, -NR7-, -CO-, -CO-NR7-, -NR7-CO-, -NR7-CO-NR7-, or the like; E is optionally substituted lower alkylene; F is a single bond or optionally substituted phenylene; R3, R4, R5 and R6 each is independently hydrogen, halogene, nitrile, or the like; or an ester, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.

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2? Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR

Biaryl amides were discovered as novel and subtype selective M1 muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M1 agonist potency and intrinsic activity, and subtype selectivity for M1 over M2-5, are described.

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Discovery of highly potent and selective type I B-Raf kinase inhibitors

A series of pyrazolo[1,5-alpha]pyrimidine analogs has been prepared and found to be potent and selective B-Raf inhibitors. Molecular modeling suggests they bind to the active conformation of the enzyme.

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CEPHEM DERIVATIVE HAVING CATECHOL GROUP

A compound represented by formula (I) or a pharmaceutically acceptable salt thereof wherein A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom.

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CEPHEM COMPOUND HAVING PSEUDO-CATECHOL GROUP

A compound of the formula: wherein X is ?N?, ?CH?, or the like; W is ?CH2? or the like; U is ?S? or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; Q is a single bond or the like; R3 is hydrogen or the like; Ring A is a 6-membered aromatic heterocyclic group having 1-3 nitrogen atoms; each R4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; G is ?C(?O)? or the like; D is a single bond, ?NH?, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.

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BRIDGED, BICYCLIC HETEROCYCLIC OR SPIRO BICYCLIC HETEROCYCLIC DERIVATIVES OF PYRAZOLO[1,5-A]PYRIMIDINES, METHODS FOR PREPARATION AND USES THEREOF

Compounds of formula A: Formula (1) pharmaceutically acceptable salts thereof are described, which selectively inhibit Raf kinase activity and are useful for treating disorders mediated by Raf kinases.

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Quinuclidine – Wikipedia,
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Discovery of highly potent and selective type I B-Raf kinase inhibitors

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Quinuclidine – Wikipedia,
Quinuclidine | C7H29N | ChemSpider