摘要:
Compounds of the formula I: ##STR1## wherein X, Y, Z, a, b, c, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined in the specification are provided. The compounds are useful as inhibitors of retroviral protease enzymes.
摘要:
This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3) alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which are taken together to form a 4- to 7- membered ring;(C) R.sub.3 is selected from the group consisting of H, --CH.sub.3, --CH.sub.2 CH.sub.3, and --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) Y is a heterocyclic radical having 5-14 atoms, located at the 2- or 3- position of the pyridoquinazolinone nucleus, in which 1-3 of the heterocyclic ring atoms are independently nitrogen, oxygen, or sulfur; wherein Y may be optionally mono-, di-, or tri- substituted with --OR.sub.4, --NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, or phenyl;R.sub.4 is H or (C.sub.1 -C.sub. 4) straight-chain alkyl;R.sub.5 and R.sub.6 are the same or different and are selected from the group consisting of H, (C.sub.1 -C.sub.4) straight-chain alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.5 and R.sub.6 are alkyl moieties which are taken together to form a 4-7 membered ring;or a pharmaceutically acceptable salt thereof which is useful as an antineoplastic agent.
摘要:
This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3)alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which may taken together to form a 4- to 7-membered ring;(C) R.sub.3 is selected from H, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) X is located at the 2-, or 3-position and is selected from the group consisting of 2-naphthyl, 1-naphthyl, 1-phenanthrenyl, 2-phenanthrenyl, 3-phenanthrenyl, 4-phenanthrenyl, 9-phenanthrenyl, phenyl, and mono- or polysubstituted phenyl wherein the substituents are selected from the group consisting of --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3) alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.3 H, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, and phenyl;R.sub.4 is H or (C.sub.1 -C.sub.4)alkyl;R.sub.5 and R.sub.6 are the same or different and are selected from H, or (C.sub.1 -C.sub.4)alkyl, or R.sub.5 and R.sub.6 are alkyl groups which may be taken together to form a 4-7 membered ring;(E) W is selected from H, --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3)alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 R.sub.4 ; or a pharmacologically acceptable salt thereof which is useful as an antineoplastic agent.
摘要:
An automated blood sampling system for PET imaging applications that can be operated in or very near to the field of view (FOV) of an MR scanner, such as in a combined MR/PET imaging system. A radiation detector uses APDs (avalanche photo-diodes) to collect scintillation light from crystals in which the positron-electron annihilation photons are absorbed. The necessary gamma shielding is made from a suitable shielding material, preferably tungsten polymer composite. Because the APDs are quite small and are magnetically insensitive, they can be operated in the strong magnetic field of an MR apparatus without disturbance.
摘要:
A representative positron emission tomography (PET) system includes a positron emission tomography detector having one or more silicon photomultipliers that output silicon photomultipliers signals. The PET system further includes a calibration system that is electrically coupled to the silicon photomultipliers. The calibration system determines a single photoelectron response of the silicon photomultipliers signals and adjusts a gain of the silicon photomultipliers based on the single photoelectron response.
摘要:
As file systems reach the petabytes scale, users and administrators are increasingly interested in acquiring high-level analytical information for file management and analysis. Two particularly important tasks are the processing of aggregate and top-k queries which, unfortunately, cannot be quickly answered by hierarchical file systems such as ext3 and NTFS. Existing pre-processing based solutions, e.g., file system crawling and index building, consume a significant amount of time and space (for generating and maintaining the indexes) which in many cases cannot be justified by the infrequent usage of such solutions. User interests can often be sufficiently satisfied by approximate (i.e., statistically accurate) answers. A just-in-time sampling-based system can, after consuming a small number of disk accesses, produce extremely accurate answers for a broad class of aggregate and top-k queries over a file system without the requirement of any prior knowledge. The system is efficient, accurate and scalable.
摘要:
A scintillation detector including one or more photomultiplier tubes, a scintillation block optically attached to the photomultiplier tubes, and a DC-coupled bleeder circuit combining outputs of dynodes of the photomultipliers to provide a DC-coupled dynode output together with a DC-coupled anode output of the photomultiplier tubes. The DC-coupled bleeder circuit includes a RF transformer. A positive high voltage supply also can be used together with a DC-coupled bleeder circuit for the anode outputs.
摘要:
Systems and methods for correcting output signals from non-linear photosensors, specifically silicon photomultipliers (SiPMs). SiPMs are used in a PET detector to readout light emissions from LSO scintillator crystals. The non-linear output of the SiPM can distort and compress the energy spectrum which is crucial in PET imaging. The non-linearity effect for inter-crystal scattered events can place an energy event outside of the PET detector energy window, resulting in a rejected event. Systems and methods to correct the SiPM non-linearity for inter-crystal scattered events, so as to be able to obtain the proper energy event and produce an accurate medical image, are disclosed.
摘要:
The present invention discloses a compound of formula (I) and citrate thereof as type 5 phosphodiesterase inhibitor, a preparation method thereof, and a pharmaceutical composition including the compound of formula (I) and citrate thereof. The experimental results of the present invention prove that the compound of formula (I) and citrate thereof can inhibit activity of type 5 phosphodiesterase, and can be used for treating erectile dysfunction, inhibiting platelet aggregation and treating thrombosis, decreasing pulmonary hypertension and treating cardiovascular diseases, treating asthma and treating diabetes gastroparesis.
摘要:
Using standard or “off the shelf” cable to interconnect between the PET block detector and the detector circuit may save substantial costs given the number of PMTs in a PET system. Given space constraints, simple maintenance with reduced risk of disturbing cabling is desired, making ongoing use of standard cabling without adding further cabling desired. To implement digital gain control, a further communication is provided between the PET detector block and the detector circuit. Since the standard cable may not have additional wires for such communications and to reduce timing degradation, the PMT signals are combined, such as generating position and energy signals at the PET detector block. The four PMT signals are reduced to three signals without reduction in function, allowing a fourth twisted pair of wires in a CAT5 cable to be used for digital gain control.