The present invention features compounds having the Formula (Ia) and (Ib) (e.g., a compound of any of Formulas ((Ia-2)-(Ia-21)), including other tautomers, stereoisomers, E/Z stereoisomers, prodrugs, pharmaceutically acceptable salts, and compositions thereof. The invention also features methods for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient by administering an effective amount of a compound of Formula (Ia) or (Ib). The invention also features a method for treating or preventing pain (e.g., neuropathic pain), inflammation, or epilepsy in a patient that includes administering to a patient in need thereof an effective amount of a compound of Formula (IIa) or (IIb) (e.g., a compound of any of Formulas ((IIa-2)-(IIa-6)). The compounds described herein (e.g., a compound of Formulas (Ia), (Ib), (IIa), or (IIb)) can also be used as anticonvulsants.

The present invention generally relates to use of compounds and compositions as a chemosensitizers and/or radiosensitizers and/or inhibitors of PNKP phosphatase activity. The present invention provides pharmaceutical combinations and/or a pharmaceutically acceptable salt thereof, kits containing such compounds and/composition and methods of using such compounds and/or compositions.

The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which relates to mophinan compounds useful as μ, δ and/or κ receptor opioid compounds and pharmaceuticals containing same that may be useful for mediating analgesia, combating drug addiction, alcohol addiction, drug overdose, mental illness, bladder dysfunctions, neurogenic bladder, interstitial cystitis, urinary incontinence, premature ejaculation, inflammatory pain, peripherally mediated and neuropathic pain, cough, lung edema, diarrhea, cardiac disorders, cardioprotection, depression, and cognitive, respiratory, diarrhea, irritable bowel syndrome and gastro-intestinal disorders, immunomodulation, and anti-tumor agents.

The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Disclosed are solid forms of 8-chloro-N-[(2-chloro-5-methoxyphenyl)sulfonyl]-6-(trifluoromethyl)-imidazo[1,2-a]pyridine-2-carboxamide (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are nematocidal compositions comprising a nematocidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other nematicide, insecticide and/or fungicide are also disclosed.Also disclosed are methods for protecting a plant from nematodes comprising applying to the plant, or portion, or seed thereof, or to the growing medium of the plant, a nematocidally effective amount of Compound 1 comprising the polymorph Form A.

The present invention provides compounds having the general structural formula (I), and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving abnormal or excessive fibrosis.

The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.

The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Cyanine dye compounds having a substituted methine moiety that are nucleic acid stains, particularly for fluorescent staining of RNA, including compounds having the formula where R1 is a C1-C6 alkyl, sulfoalkyl, carboxyalkyl or C1-C6 alkoxy; each R2 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, fused benzo, trifluoromethyl, amino, sulfo, carboxy and halogen, that is optionally further substituted; at least one of R3, R4, and R5 is an alkyl, aryl, heteroaryl, cyclic, or heterocyclic moiety that is optionally substituted by alkyl, amino, aminoalkyl, carboxy, nitro, or halogen; and the remaining R3, R4 or R5 are hydrogen; X is S, O, or Se; and D is a substituted or unsubstituted pyridinium, quinolinium or benzazolium moiety.

There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.

The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension.

The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.

The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

A platinum complex of a formula (I): whereR1 and R2 are each fluoroalkyl,X is C—H or nitrogen, andL1 is a bidentate, nitrogen-containing heteroaromatic ligand.

Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.

Herein are disclosed fluorescent dyes based around a framework for a ligand comprising a pyridyl group linked to a diaryl anilido unit. A variety of ligands based on this framework are disclosed. The ligands chelate to a BF2 center to produce the fluorescent dye. The disclosed dyes combine longer Stokes shifts (approximately 100 nm) with increased quantum yields. They are also photostable in aqueous and organic solutions for several hours. These dyes may be used in the labeling of biomolecules for bioimaging and assays. Also disclosed are methods for the synthesis of these dyes.

The present invention provides processes for the preparation of saturated ketone morphinan compounds. In particular, the invention provides processes for the conversion of a morphinan comprising an allyl alcohol ring moiety into a morphinan comprising a saturated ketone ring moiety by an isomerization reaction catalyzed by an inorganic salt of a late transition metal.

The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved.

A compound of formula (I) wherein R1 to R4 are, for example, each hydrogen, R5 is pyridyl, which has two or more substituents selected, for example, from halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, and cyano; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.

The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.

The present invention is concerned with a process for preparing 5-(2{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(R)-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one or a pharmaceutically acceptable salt thereof.

An objective of the present invention is to provide a process for producing 4-carbonyl oxyquinoline derivatives useful as agricultural and horticultural pesticides and fungicides. The objective can be attained by a process for producing 4-carbonyl oxyquinoline derivatives represented by general formula (1), the process including reacting a quinolone derivative with a halogenated compound or an acid anhydride in the presence of a phase transfer catalyst and a base.

The present invention relates to electronic devices, in particular organic electroluminescent devices, comprising compounds of the formula (1), and the corresponding compounds.

The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.

An electronic device includes, a circuit board including a through hole, a member including a screw hole, a screw including a screw body having an outer diameter smaller than an inner diameter of the through hole and a screw head having an outer diameter larger than the inner diameter of the through hole, wherein the screw body penetrates through the through hole to engage with the screw hole and the screw head is disposed on an opposite side of the circuit board to the member, and a first washer provided between the screw head and the circuit board, the first washer including a first washer body and a plurality of first washer legs extending from the first washer body toward the circuit board, the first washer legs being in contact with the circuit board and having a characteristic of reducing stress on the circuit board upon being heated.

Cage nut having a cylindrical nut body (14) provided with a coaxial bore having an interior thread, wherein the nut body is ending in an rectangular plate (16) and, wherein the nut body (14) by means of the rectangular plate (16) is floatingly supported within a cage (12) and, wherein the entire cage nut (10), i.e. the nut body (14), and the cage (12) merely is manufactured from a single strip (100) of metal sheet by tube-forming, thread-cutting, bending and punching as well as a method for producing such a cage nut.

A method of manufacturing fastenings or fasteners with radial outer contours, especially screws or threaded bolts, made of solid metal is performed by a device. The method manufactures the fastenings or fasteners preferably on a multi-stage press. Several recesses running in an axial direction at a fixed radial distance are formed in the shank-shaped section of a blank. The prefabricated blank with the recesses is inserted into a multi-part split mold within a multi-stage press, whose die stocks have an inner profiling forming the outer contour, and are opened in the starting position, that at the places where the die stocks are opened, there are the recesses. During the closing movement of the die stocks, at least one radial outer contour is pressed on the shank-shaped section of the blank by radial action of forces, with the recesses preventing material from getting between the die stocks during the pressing process.

The theft-protected screw part in the form of a nut or a screw has a free end region and a ring-shaped depression formed at the end region for the engagement of a wrench for rotation the screw part. Viewed from radially outside to radially inside, the depression is delimited by an outer edge, a bottom and an inner edge. The outer edge forms outer abutment surfaces and the inner edge forms inner abutment surfaces for the wrench. The screw part is composed of a main part and an insert. The main part has a protrusion, which is located within the inner edge. The insert is designed in a ring shape, has a hole for accommodating the protrusion and forms the inner abutment surfaces.

The present invention is premised upon method of manufacturing rolled pierce nuts having a predetermined profile from a metal rod, more particularly to a method and apparatus delivering greater manufacturing flexibility through the use of multiple stations with flexible inputs and outputs.

The present invention provides a method for manufacturing a fitting that has a configuration where a fitting plate and a blind nut are integrally formed and also provides a tap tool for use in this method. According to the present invention, performing tap processing to an internal diameter portion to integrally form a portion corresponding to the blind nut, when a tap tool having a protrusion at an end thereof is utilized to be inserted into the bag-like blind hole at a planned part of the blind nut and the tap processing is carried out, the protrusion provided at the end of the tap tool comes into contact with an inner wall at the end of the bag-like blind hole, and a pressed material thereby forms a convex shape on an outer side of the bag-like blind hole.

A magnetized nut for fastening a compressor wheel of an exhaust turbocharger to a turbo shaft. The nut has a base body made of a non-magnetic material forming a hollow space for accommodating a magnetic material, and a method for the production of the magnetized nut. In order to provide a magnetized nut that is produced in a simple and cost-effective manner and ensures as equal a distribution of mass as possible with regard to the rotational axis of the nut, the magnetic material is introduced into the hollow space using injection molding.

There is provided a nut having a thread portion having a female thread, a metallic plate portion having a base segment, and a hardness gradient portion provided between the thread portion and the metallic plate portion. The thread portion, metallic plate portion and the hardness gradient portion are monolithic each other, a metallographic structure of the metallic plate portion differs from a metallographic structure of the thread portion and a hardness of the hardness gradient portion is lower than a hardness of the thread portion and lowers from the thread portion toward the metallic plate portion.

The invention relates to a profile-rolling machine for rolling a profile in a blank, wherein the profile-rolling machine has a first and a second profile-rolling jaw. The second profile-rolling jaw (126) is guided—held by a carriage (124)—in a guide track (130) relative to the first profile-rolling jaw (110) for the purpose of rolling the profile into the blank. The carriage (124) has a carriage slide plate (122) and the guide track (130) has a guide slide plate (132). The two slide plates together form a sliding pairing and slide on each other. In order to render said sliding pairing less susceptible to dirty lubricant and less susceptible to wear, it is proposed according to the invention to manufacture the guide slide plate (132) and/or the carriage slide plate (122) at least partially from ceramic or from a non-metallic material or to coat the same with such materials.

A rolling machine comprises parallel guides delimiting a workpiece conveying channel extending from a plurality of per se known rolling tools to a machined workpiece unloading arrangement, wherein, upstream of the workpiece unloading arrangement, one of the channel delimiting guides is operatively coupled to a structural element swingably supported by a pivot pin, the structural element being integral with the piston rod of a cylinder-piston unit slidably driving the structural element together with the channel delimiting guide, thereby providing a side unloading opening for the workpiece.

Provided is a method for manufacturing an FRP member with insert which enables to reduce a machining time to improve productivity. First, a threaded hole 11 is formed in an insert 3. An FRP member 2 where at least the threaded hole 11 of the insert 3 is covered with a coating 4 made of FRP is molded. A counter-bored hole 31 that penetrates the coating 4 of the FRP member 2 to communicate with the threaded hole 11 of the insert 3 is formed, to thereby obtain an FRP component 1 with insert. Accordingly, a machining step after molding the FRP member 2 in which dry machining is required includes only the boring step of forming the counter-bored hole 31 in the FRP member 2. Thus, the machining time can be reduced, and the productivity can be improved.

In FIG. 2, a diameter Dd of drilling edges of a drill is selected smaller than a valley diameter d1 of a male thread of a tap portion, and an inner diameter D1 of a female thread is defined by the valley diameter d1 of the male thread. Therefore, a predetermined radial gap is formed between the male thread 30 formed by the tap portion and the drill. When a tap with the drill is reversely rotated to be pulled out from the female thread after cutting the female thread, the tap released from the restriction may deflectively displace in the diameter direction upon pulling out the male thread of the tap portion from the female thread. However, the drill hardly contacts with the female thread, so that the occurrence of the defective product due to the contact is suppressed.

Techniques for reinforcing concrete using rebar are disclosed. Some example embodiments may include prestressed concrete structures reinforced by twisted, threaded reinforcing bars. An example reinforcing bar for a prestressed concrete structure may include an elongated, generally cylindrical rod; an external thread disposed on the generally cylindrical rod, the external thread formed from an elongated, generally nonlinear channel wrapped about a radial surface of the generally cylindrical rod in a generally helical fashion. A base portion of the nonlinear channel may be disposed substantially against the radial surface of the generally cylindrical rod and/or an upstanding portion of the nonlinear channel may extend generally orthogonally from the radial surface of the generally cylindrical rod.

Disclosed is a tap driver and tap driver system for rigid tapping, which includes a unique flexure system. In some embodiments, an integrated flexure component and housing configuration provides and may provide both a more economical and a universal configuration of the tap driver flexure component that allows the central body to be integrated with and into different types of tap drivers.

A clinch-type fastener is formed by simultaneously creating an undercut during the same forging that creates the head and displacer of the fastener. A fastener blank is compressed end-to-end between top and bottom dies whereby the axial compression of a blank causes the outward bulging of the shank at its midline. Simultaneously, a tapered end point and a tangential interference band are formed provided by a curvilinear-shaped bulge in the shank. As the bulge is formed an undercut is created between the bulge and a shoulder which extends downwardly from a head of the fastener. This method of formation and the fastener produced thereby are particularly suited to the manufacture of small clinch pins having a diameter in the range of 1.0 mm.

An anchor bolt locator is provided that is inexpensively manufactured on automatic die-press machines from sheet steel and a structural nut that does not require any welding, while also being easy to use and install with current, commonly-used building practices and anchor designs. The anchor bolt locator is made from a galvanized sheet metal chair and a structural nut attached to the chair by way of a friction fit.

A process for producing hollow bolts including a longitudinal bore with the hollow bolts being provided with circumferential notches. The hollow bolts are provided with longitudinal grooves extending between elevations determining the bolt diameter, wherein circumferential notches are rolled onto the hollow bolts provided with the longitudinal grooves and the elevations, the longitudinal grooves being of such cross-section that some of the material displaced during rolling-on of the notches flows into the longitudinal grooves.

A testing method for the bolt to be used under the conditions of excessive wind force by which bolts made of Cr—Mo steel can be separated into a group of bolts usable in cold areas and a group of bolts unusable in cold areas without conducting Charpy impact test involving complicated operation, specifically, a testing method for determining whether bolts made of heat-treated Cr—Mo steel are usable or unusable in cold areas, wherein the determination is conducted on the basis of both J parameter calculated by formula: J=(Si %+Mn %) (P %+Sn %) 104 (wherein P %, Si %, Mn % and Sn % are contents (mass %) of phosphorus (P), silicon (Si), manganese (Mn) and tin (Sn) respectively as disclosed in the inspection certificate of the Cr—Mo steel) and bolt diameter.

A radial tapping attachment for a motor-driven tool includes an enclosed, box-shaped housing, a main shaft assembly adapted to retain a tap, a drive mechanism rotatably driven by the tool and a guide member assembly for supporting an object to be tapped. The main shaft assembly includes a main shaft rotatably coupled to the housing by a pair of bearings, a pair of spaced apart discs fixedly mounted on the main shaft, and a pair of axially mounted compression springs that allow for slight, bi-directional, axial displacement of the main shaft relative to the housing. The drive mechanism includes a drive shaft rotatably coupled to the housing at an approximate right angle relative to the main shaft and a drive wheel mounted on the drive shaft that selectively engages the pair of discs to rotate the main shaft in either direction when an axial force is applied to the tap.

The invention relates to a method for producing hollow body elements (200), for example, nut elements which are applied to components which are normally made of steel (280), in particular, for producing hollow body elements having an essentially quadratic or rectangular external profile (202). Said method consists of cutting individual elements of a profile in the form of a profile rod (1) or a winding after holes (204) have previously been stamped in the profile, a threaded cylinder (206) is subsequently, optionally, formed using a follow-on composite tool (10) which consists of several working stations. The invention is characterized in that a penetrating process and a punching process are carried out in the working station. The invention also relates to hollow body elements (200), components, follow-on composite tools (10) and rolling mills (600, 602).

A method for manufacturing a thread-forming screw having a shank and a thread formed in one piece with the shank and region-wise circumferentially arranged on the shank, is disclosed. After the formation of the thread on the shank, a plurality of recesses is subsequently stamped into the thread. Then, a plurality of compact cutting elements is welded into the recesses in the thread, where the cutting elements are made of a hard material and have a hardness greater than the hardness of the thread. Additionally, a stamping device for carrying out the method is also disclosed.

A spiral fluted tap is provided which includes a threaded portion having an external thread corresponding to an internal thread to be cut and a cutting edge formed along a spiral flute formed to divide the external thread, and being screwed into a prepared hole that is provided on a workpiece to cut an internal thread by the cutting edge on an inner circumferential surface of the prepared hole with discharging chips toward a shank via the spiral flute, the spiral flute having a stepped portion at a rear end of a chamfer portion or in a portion on a shank side from the rear end of the chamfer portion in the threaded portion, and a flute bottom diameter on a distal end side of the spiral fluted tap from the stepped portion being smaller than a flute bottom diameter on a shank side from the stepped portion.

A threading cutting insert achieves high shape accuracy of a screw to be processed, and saves on manufacturing cost. Therefore in the threading cutting insert, a plurality of tooth-shaped cutting edges are formed in a cross ridge line portion between a rake face and flanks formed in a cutting side face, wherein the plurality of mountain-shaped cutting edges provides at least one finishing cutting edge for transferring a shape of a screw, and at least one roughing cutting edge formed in a tooth shape smaller than that of the finishing cutting edge. A flank of the finishing cutting edge includes a first flank, and a second flank having a clearance angle larger than that of the first flank, wherein the finishing cutting edge, the first flank, and the second flank are sequentially provided in that order from the rake surface in a direction of a lower surface of the insert.

A pivoting split thread chasing die with fastener is disclosed. In one example, the fastener can include a retainer that captures the fastener within one half of the thread chasing die. The thread chasing die may make it easier for a user to refurbish threads of large bolts and studs.

A slotted inverse tap, compressible for insertion past damaged entry threads in blind holes. (FIG. 1 thru FIG. 5) The tool can be made to smaller sizes than that of prior art. An elongate slot (23) proceeds through a first threaded end (21), then well into a reduced diameter cylindrical body (25). After insertion to the hole bottom, a tabbed shim (28) is inserted to the slot from its side, then pressed down until stopped. The shim (28) enforces mating engagement with undamaged internal threads. A second end of hex and/or squared or other configuration facilitates use of a tap wrench or other tool for rotational extraction. Damaged threads are reformed/re-cut upon rotational withdrawal.