Abstract:
The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two carbon atoms between the hydroxy or amino group and the oxygen atom to which R25 is attached; and R4 and R5 each are hydrogen or a substituent as defined in the claims
Abstract translation:本发明提供式(II)化合物或其盐,溶剂合物,互变异构体或N-氧化物; 其中n为0或1; Y1和Y2之一是CH,另一个选自CH,CR8和N; q为0,1或2,条件是当Y1或Y2为CR8时q为0或1; R 10芳环或5至10个环成员的杂芳基; R2a和R3a各自为氢,C1-4烃基或C1-4酰基,其中烃基和酰基部分任选被氟,羟基,氨基,甲基氨基,二甲基氨基或甲氧基取代; 或NR2aR3a形成任选含有选自O和N的第二杂原子环成员的咪唑基或饱和单环4-7元杂环基; R18是氢或甲基; R 19是氢或甲基; R 24是氢或R 24,R 2a,并且插入的氮原子和碳原子一起形成氮杂环丁烷,吡咯烷或哌啶环; R 25是氢或C 1-4烷基,其中C 1-4烷基任选被羟基或氨基取代,条件是羟基或氨基与R 25所连接的氧原子之间至少有两个碳原子; 且R 4和R 5各自为氢或如权利要求中所定义的取代基
Abstract:
The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.
Abstract:
This invention provides novel crystalline acid salt forms of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine, i.e. sitagliptin, to processes for their preparation and isolation, and to pharmaceutical compositions comprising the same.
Abstract:
The present invention relates to amorphous form darifenacin hydrobromide and processes therefor. In addition, the present invention relates to compositions comprising amorphous form darifenacin hydrobromide.
Abstract:
A folding trailer may be capable of moving between a use position and a storage position. The folding trailer may include an axle that is capable of moving between a first position in which the axle is generally aligned along an axis and a second position in which the axle is disposed in a folded configuration. The folding trailer may also include a towing arm that is movable between an extended position in which a portion of the towing arm extends beyond the front portion of the frame to facilitate attached to a towing vehicle and a collapsed position in which the towing arm is at least substantially disposed underneath the frame. In addition, the trailer may include an adjustment assembly that is sized and configured to adjust the position of the axle between the first and second positions, and adjust the position of the towing arm between the extended and collapsed positions. Advantageously, the adjustment assembly may have different configurations and arrangements. In addition, the adjustment assembly may be used to secure the trailer in the use or storage positions.
Abstract:
A trailer may be purchased by a consumer from a store and the trailer may be quickly, easily and readily towed away from the store. In particular, the trailer may be essentially or completely ready to be towed away from the store and the trailer may require no or virtually no assembly. For example, a towing arm may be quickly and easily moved from the storage position to the use position. Advantageously, because the towing arm may be connected by pins to the trailer, no tools may be required to position the arm in the use position. In addition, because electrical wiring may be disposed within the arm and the arm may be simply moved forwardly when the trailer is ready to be towed, the lights for the trailer may be functional.
Abstract:
A basketball goal system may include a basketball goal, which may include a rim assembly and a backboard, and a support structure that is sized and configured to support the basketball goal above a playing surface. The backboard may include one or more openings through which one or more portions of the rim assembly may extend, which may permit the rim assembly to be connected to the support structure. The basketball goal system may also include a base that is sized and configured to support the support structure and the rim assembly in a playing position. The base and the backboard may include openings to permit the base and the backboard to be connected when the basketball goal system is in a collapsed or storage position. In addition, the base and the backboard may include receiving portions that are sized and configured to receive and/or retain at least a portion of one or more components of the basketball goal system when the system is in the collapsed position.
Abstract:
A needle valve assembly for providing fluid flow control includes a motor; an internally threaded valve body; and an externally threaded plunger threadably engaged with the internally threaded valve body and rotatably and reciprocally driven by the motor, wherein the valve body including a fluid inlet, a fluid outlet, and a flow chamber therebetween, the flow chamber including a flow chamber wall and a flow chamber outlet, the plunger including a flexible needle member reciprocating within the flow chamber outlet to provide variable flow control therethrough, the flexible needle member including a lip seal engageable with the flow chamber wall during reciprocation of the plunger and flexible needle member to provide a seal therebetween.
Abstract:
A modular enclosure, such as a shed, may include a number of components. For example, the enclosure may include roof panels, floor panels and wall panels that are connected to the roof and/or floor panels. Preferably, the wall panels span the seams disposed between the roof and/or floor panels. In addition, the wall panels are preferably offset from the roof and/or floor panels. Further, the roof panels, wall panels and floor panels desirably have a substantially similar width. The enclosure may also include one or more corner panels and the corner panels may have a living hinge that generally divides the corner panel in half. Advantageously, the offset connection of the roof panels, wall panels and floor panels may facilitate construction of an enclosure with increased strength and functionality.