Abstract:
Compounds represented by formula (I): wherein R 1 is H, halogen, (C 1-4 ) alkyl, O(C 1-4 ) alkyl, and haloalkyl; R 2 is H or (C 1-4 )alkyl; R 3 is H or (C 1 - 4 ) alkyl; R 4 is (C 1 . 4 )alkyl, (C 1 - 4 )alkyl(C 3 . 7 ) cycloalkyl, or (C 3 _ 7 ) cycloalkyl; and Q is a fused phenyl-5 or 6-membered saturated heterocycle having one to two heteroatoms selected from O and N, said Q being optionally substituted with hydroxy, or (C 1 . 4 ) alkyl which in turn maybe optionally substituted with pyridinyl-Noxide or C(O) OR wherein R is H or (C 1-4 ) alkyl; or a salt thereof. The compounds have inhibitory activity against Wild Type, and single and double mutants strains, of HIV.
Abstract translation:由式(I)表示的化合物:其中R 1是H,卤素,(C 1-4)烷基,O(C 1-4)烷基和卤代烷基; R 2是H或(C 1-4)烷基; R 3是H或(C 1-4)烷基; R 4是(C 1-4)烷基,(C 1-4)烷基(C 3-7)环烷基或(C 3-7)环烷基; 且Q为具有一至二个选自O和N的杂原子的稠合苯基-5或6元饱和杂环,所述Q任选被羟基取代,或(C 1-4)烷基,其又可任选被吡啶基 - 或C(O)OR,其中R是H或(C 1-4)烷基; 或其盐。 该化合物对野生型具有抑制活性,并具有HIV和HIV的单和双突变株。
Abstract:
An endplate for an intervertebral prosthesis prosthesis endplate of the invention includes: a generally- planar base plate, a first elevated region, or dome, within the base plate periphery, and a second elevated region, or dome, within the boundary of the first elevated region. The antero-posterior and side-to-side (medial-lateral) dimensions of the first elevated region are made to be unequal in order to provide resistance to torsional stresses, and the laterally opposite sidewalls of the first elevated region are defined by arcs that terminate in sagittal planes of the endplate, and are symmetrical with respect to a coronal plane of the endplate. A bone rasp for preparing a surgical site for implantation of the prosthesis has a rasp head having a pivot point and rasp teeth arranged to produce a recess or seat of predetermined shape. A groove-cutter for preparing a medial antero- posterior groove in a vertebral body without damaging the anterior rim of the vertebral body has a guide head that is seated ina prepared recess in the vertebral body and a reciprocable tooth that can be stowed in a recess while the cutter is initially positioned within the intervertebral space.
Abstract:
A method of manufacturing a patterned electric circuit. The method comprises the steps of providing a cold gas-dynamic spraying (CGDS) device, providing a substrate, and depositing a pattern of electrically conductive material with the CGDS device on the substrate by relative movement between the CGDS device to the substrate.
Abstract:
An interpositional biarticular disk implant (11) having a circular peripheral rim, a generally toroidal axial center opening (13) and convex upper and lower surfaces (15, 17) is implanted between resected concave surfaces of the metacarpal base and the trapezium or other carpal bone in a CMC joint replacement. The disk (11) is anchored in operative position through the use of a flexible cord, such as a harvested tendon, that passes through the center opening (13) and through osseous passageways created in the two facing bones.
Abstract:
Disclosed are compounds of formula I:whereinR2 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, NH(C1-4alkyl) or N(C1-4alkyl)2;R4 is H or CH3;R5 is H or CH3;R12 is H, halogen, (C1-4)alkyl, CF3, or NO2; R13 is H, (C1-4)alkyl, halogen, OH, or NH2, with the proviso that R12 and R13 are not both H; andR14 is COOR14a wherein R14a is H or (C1-6)alkyl; or R14 is (C2-4)alkenyl-COOR14a wherein R14a is as defined herein; or R14 is (C1-4)alkyl-COOR14a wherein R14a is as defined above;or a salt or a prodrug thereof, useful as inhibitors of HIV reverse transcriptase.
Abstract:
A compound of formula (I), wherein X is CF3, C2F5, 2-benzothiazole, CF2CONHR6, CONHR6, wherein R6 is CH2C6H5, CH2(4-iodophenyl), CH3, (CH2)2OCH2C6H5, CH2-2-benzimidazole, CH2-(3,4-methylenedioxybenzene), CH(CH3)C6H5 or CH(CH2CH3)C6H5; or X is 2-benzoxazole-R7 wherein R7 is H, 4-CH3, 5-CH3, 6-CH3 or 7-CH3; R1 is H, CH3 or CH2CH3; R2 is CH2CONH2, CH2CH2CONH2, CH2-thiazole, CH2CON(CH3)2, CH2CO-(pyrrolidino), CH2CH(CH3)2 or CH2C6H5; R3 is Et, CH(CH3)2, C(CH3)3, adamantyl, CH2C(CH3)3 or C(CH3)2CO2H; and R20 is COCH2C(CH3)3, COCH2CH2C6H4OH, COCH2CH(CH3)2, CO2C(CH3)3, CONHC(CH3)3, COCH2N(CH3)2, CO(CH2)3CO2H, CO-(S)-CH(NH2)C(CH3)3, CO-(S)-CH{NHC(O)O-C(CH3)3}C(CH3)3, CO-(S)-CH{NHCO(CH2)5NHC(O)OC(CH3)3}C(CH3)3 or CO-(S)-CH{NHCO(CH2)5NH2}C(CH3)3. These compounds are useful for the treatment of human cytomegalovirus infection.
Abstract translation:式(I)化合物,其中X为CF 3,C 2 F 5,2-苯并噻唑,CF 2 CONHR 6,CONHR 6,其中R 6为CH 2 C 6 H 5,CH 2(4-碘苯基),CH 3,(CH 2)2 OCH 2 C 6 H 5,CH 2 -2-苯并咪唑, (3,4-亚甲二氧基苯),CH(CH3)C6H5或CH(CH2CH3)C6H5; 或X是2-苯并恶唑-R 7,其中R 7是H,4-CH 3,5-CH 3,6-CH 3或7-CH 3; R1是H,CH3或CH2CH3; R2是CH2CONH2,CH2CH2CONH2,CH2-噻唑,CH2CON(CH3)2,CH2CO-(吡咯烷子基),CH2CH(CH3)2或CH2C6H5; R3是Et,CH(CH3)2,C(CH3)3,金刚烷基,CH2C(CH3)3或C(CH3)2CO2H; 和R 20是COCH 2 C(CH 3)3,COCH 2 CH 2 C 6 H 4 OH,COCH 2 CH(CH 3)2,CO 2 C(CH 3)3,CONHC(CH 3)3,COCH 2 N(CH 3)2,CO(CH 2)3 CO 2 H,CO-(S) )C(CH 3)3,CO-(S)-CH(NHC(O)OC(CH 3)3} C(CH 3)3,CO-(S)-CH(NHCO(CH 2)5 NHC(O) )3} C(CH 3)3或CO-(S)-CH(NHCO(CH 2)5 NH 2)C(CH 3)3。 这些化合物可用于治疗人巨细胞病毒感染。
Abstract:
An endplate for an intervertebral disc prosthesis includes: a plate member having a generally planar rim for contacting the peripheral cortical rim of a vertebral body, and an elevated region within the rim having an anterior region and a posterior region, wherein the anterior region of the elevated region is preferably recessed with respect to the posterior region and is treated to promote bone ingrowth. The endplate may be provided with a medial fin extending partway from the anterior edge of the endplate toward the posterior edge of the endplate.
Abstract:
The present invention provides an orthopedic device assembly comprising a first assembly element (200), a second assembly element (300), and a retaining mechanism (400). The first assembly element has a recess (214) that receives the second assembly element, and the retaining mechanism holds the second element in an assembled state with the first assembly element. The retaining mechanism includes a retaining member with an angular cross-section defined by a base portion and a lateral flange portion projecting from the base portion. The retaining member is inserted through an aperture (226) of the first assembly element into a groove in a wall of the recess of the first assembly element, with the flange portion projecting laterally of the groove and overhanging a shoulder portion of the second assembly element so as to retain the second assembly element in the assembled state with the first assembly element.
Abstract:
An endplate for an intervertebral prosthesis includes : a generally- planar base plate (162 ), a f irst elevated region ( 152 ), or dome, within the base plate periphery, and a second elevated region ( 153 ), or dome, within the boundary (164 ) of the f irst elevated region. The antero-posterior and side-to-side (medial-lateral ) dimensions of the f irst elevated region are made to be unequal in order to provide resistance to torsional stresses, and the laterally opposite sidewalls of the f irst elevated region are def ined by arcs that terminate in sagittal planes of the endplate, and are symmetrical with respect to a coronal plane of the endplate. A bone rasp (201 ) for preparing a surgical site for implantation of the prosthesis has a rasp head (202 ) having a pivot point and rasp teeth (224 ) arranged to produce a recess or seat of predetermined shape. A groove-cutter (300 ) for preparing a medial antero- posterior groove in a vertebral body without damaging the anterior rim of the vertebral body has a guide head that is seated in a prepared recess in the vertebral body and a reciprocable tooth ( 301 ) that can be stowed in a recess while the cutter is initially positioned within the intervertebral space.
Abstract:
A method of creating a fuse. The method comprises the steps of creating a fusible link electrically connecting a first terminal portion to a second terminal portion, the fusible link, the first terminal portion and the second terminal portion being made of a first electrically conductive material; and spraying a coating of a second electrically conductive material onto the fusible link. The second electrically conductive material has a lower melting point than the first electrically conductive material and is absorbable in the first electrically conductive material.