摘要:
The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is C1-4alkyl, C1-3fluoroalkyl, —CH2CH2OH or —CH2CH2CO2C1-2alkyl; R2 is a hydrogen atom (H), methyl or C1fluoroalkyl; R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.
摘要翻译:本发明涉及式(I)化合物或其盐:其中:R 1是C 1-4烷基,C 1-3烷基, 氟代烷基,-CH 2 CH 2 OH或-CH 2 CH 2 CO 2, C 1-12烷基; R 2是氢原子(H),甲基或C 1氟代烷基; R 3是任选取代的C 3-8环烷基或任选取代的单不饱和C 5〜5-7环烯基或任选取代的杂环基 子公式(aa),(bb)或(cc); 其中n 1和n 2独立地为1或2; 并且其中Y是O,S,SO 2或NR 10; 或R 3是双环基(dd)或(ee):其中X是NR 4 R 5或OR 5a SUP>。 这些化合物是磷酸二酯酶(PDE)抑制剂,特别是PDE4抑制剂。 还提供了式(I)化合物或其药学上可接受的盐在制备用于治疗和/或预防哺乳动物例如人的炎性和/或过敏性疾病的药物中的用途, 例如慢性阻塞性肺疾病(COPD),哮喘或过敏性鼻炎。
摘要:
The invention provides a compound of formula (I) or a salt thereof: wherein W is Ar, —CR4R5Ar or a group (y) or (y1), wherein Ar is (x) or (z): R1 is C1-4alkyl, C1-3fluoroalkyl or —CH2CH2OH. R2 is C2-6alkyl, C3-6cycloalkyl or —(CH2)n4-C3-6cycloalkyl; and R3 is optionally substituted C3-8cycloalkyl, optionally substituted mono-unsaturated-C5-7cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc) (in which Y is O, S, SO2, or NR10), or a bicyclic group (ee): These compounds are PDE4 inhibitors.
摘要:
The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is Et, n-Pr, i-Pr, C2fluoroalkyl, or —CH2CH2OH; R2 is H, Me, Et, n-Pr, i-Pr, C1-2fluoroalkyl, cyclopropyl or (cyclopropyl)methyl-; and NHR3 has the sub-formula (nhr3): wherein R3a is methyl or ethyl; R3b is H, methyl or ethyl; R3c is H, methyl or ethyl, R3d is H, methyl or ethyl, and R3e is H or methyl, provided that: (a) R3b is methyl or ethyl; and/or (b) R3c and R3d are independently methyl or ethyl; and provided that: (c) when R3c is ethyl and/or when R3d is ethyl and/or when R3e is methyl, then: R3a is methyl and/or R3b is hydrogen or methyl. These compounds are PDE4 inhibitors.
摘要:
There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20, and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
摘要:
The invention provides 4-{[1-(aminocarbonyl)-4-piperidinyl]amino}-N-[(3,4-dimethylphenyl)methyl]-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxamide, which is the compound of formula (I): or a salt thereof.
摘要:
A gravity-fed, animal feeding apparatus is equipped with a funnel, a food chute, and at least one feeding pan. The food chute of the apparatus preferably includes a transport tube configured to extend through a conventional chain-link fence gap via a diamond-shaped fitting, and terminate at the feeding pan disposed on the floor within the fenced pen area. The apparatus is configured to direct dry pet food fed into the funnel disposed on the exterior of the fenced pen area to the feeding pan on the interior of the fence. Gravity causes the food in the funnel to fall into the food chute, passing through the fence, and outputting the food to the feeding pan. The feeding pan is equipped with drainage holes to ensure that the dry food does not get wet, and that water does not collect in the feeding pan.
摘要:
The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
摘要:
A system and method for providing enhanced weight alert notification during automated patient management is presented. A plurality of weight measurements in an automated patient environment from a weight monitoring device for a patient during an observation period is remotely obtained. A raw baseline weight for the patient is determined based on a function of the weight measurements. Irregularities in the weight measurements are identified. The raw baseline weight is processed into a baseline weight by application of a correction coefficient to the irregularities. Weight remotely measured in the automated patient environment for the patient on a substantially regular basis is obtained. Changes in the weight are identified by periodic comparison to the baseline weight. An alert notification is generated in response to the change in weight.
摘要:
A method of transferring video data comprises obtaining a stream of video frames from an video capture device and identifying at least one characteristic in at least one frame of the stream of video frames. Lookup data is generated which associates the at least one characteristic with its at least one identified video frame. At least one video frame in the stream of video frames having a given characteristic is determined and notification or at least one of the determined video frames is transmitted to a client. A video transfer system, video processing device and method of image identification are also described.
摘要:
Material is incrementally deposited using material directed toward a deposition zone. The scan path of the directed material is controlled according to a path plan derived to reduce derivation from an ideal uniform temperature profile for the deposition during the deposition process. A path plan having angled scan passes that intersect (or overcross one another), for example in a mirrorbox path plan, is preferred.