摘要:
α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; R1, R2 and R3 are each independently selected from H, halogen and OH; or R1 and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or I2; R6 is selected from —CO2—C1-4alkyl, —O—C1-4alkyl, —O—C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl-1,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-1,2,4-oxadiazol-3-yl, 3-halomethyl-1,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-1,2,3-triazolyl, and 5-methyl-1,2,3-triazolyl; R7 and R8 are each independently Cl or I2; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译:式(I)的α-羟基环烷甲酰胺衍生物或其药学上可接受的盐,其中式(a)是单键或双键; R 1,R 2和R 3各自独立地选自H,卤素和OH; 或连接在同一碳原子上的R1和R2一起代表氧代; R4是H或甲基; R5是Cl或I2; R 6选自-CO 2 -C 1-4烷基,-O-C 1-4烷基,-O-C 1-4卤代烷基,2-甲基四唑-5-基,5-甲基-1,2,4-恶二唑-3-基,3 - 甲基-1,2,4-恶二唑-5-基,5-卤代甲基-1,2,4-恶二唑-3-基,3-卤代甲基-1,2,4-恶二唑-5-基,四唑-5 - 5-氯甲基-1,2,3-三唑基和5-甲基-1,2,3-三唑基; R 7和R 8各自独立地为Cl或I 2; 和n为0或1是缓激肽B1拮抗剂或反激动剂,其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。
摘要:
A compact, portable electrical tester to test the functionality of the lights of a lighting system of vehicle-towed commercial and utility trailers. By virtue of the presently-disclosed lighting tester, the lights of a trailer can be remotely tested by a single test taker without the presence of a tow vehicle or tow vehicle operator. Housed within the chassis of the lighting tester are a 120-volt AC/12-volt DC power supply and a set of DC test circuits. The DC test circuits are connected between the power supply and different ones of the lights of the trailer to be tested. In the preferred embodiment, each DC test circuit includes a light selection toggle switch that is connected in electrical series with a DC circuit breaker toggle switch. A particular light selection toggle switch is selectively actuated to a closed switch position so that DC power will be supplied from the power supply to illuminate a particular light or group of lights under test. A particular series connected circuit breaker toggle switch is selectively actuated to a closed circuit position to close the DC test circuit in which it is connected. Each of the light selection and circuit breaker toggle switches is accessible to be manually actuated at the front of the chassis.
摘要:
α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; R1, R2 and R3 are each independently selected from H, halogen and OH; or R1 and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or I2; R6 is selected from —CO2—C3-4alkyl, —O—C1-4alkyl, —O—C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl-1,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-1,2,4-oxadiazol-3-yl, 3-halomethyl-1,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-1,2,3-triazolyl, and 5-methyl-1,2,3-triazolyl; R7 and R8 are each independently Cl or I2; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要:
In one aspect, the invention relates to compounds which are useful as allosteric or bitopic agonists of the M1 muscarinic receptor; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurodegenerative diseases, including Alzheimer's Disease. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要:
Compounds of formula I: (wherein variables A, m, n, J, Re, Rf, R4, Ea, Eb, Ec, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要:
α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3) (CH2)nNRbSO2Rd. (4) (CH2)nNRbCO2Ra. (5) (CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6) (CH2)kCO2Ra. and (7) (CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl.
摘要翻译:通式(I)的α-羟基酰胺衍生物是可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状的缓激肽B1拮抗剂或反向激动剂。 R2a选自(1)选自Ra的基团。 (2)(CH2)nNRbC(O)Ra。 (3)(CH2)nNRbSO2Rd。 (4)(CH2)nNRbCO2Ra。 (5)(CH2)k-杂环,其任选被1至3个独立地选自卤素,硝基,氰基,硫代C 1-4烷基和C 1-3卤代烷基的基团取代,其中所述杂环是(a)5元杂芳族 环,其具有选自NO和S的环杂原子,并且任选地具有至多3个另外的环氮原子,其中所述环任选地被苯并稠合; 或(b)含有1至3个环氮原子的6-元杂环和其N-氧化物。 其中所述环任选地被苯并稠合。 (6)(CH2)kCO2Ra。 和(7)(CH 2)C(O)NR b R c。 R2b是OH或选自R2a的基团; 或R 2a和R 2b与它们所连接的碳原子一起形成任选被1至4个独立地选自卤素的基团取代的3至7元碳环。 ORa。 C 1-4烷基和C 1-4卤代烷基。
摘要:
An apparatus for orienting open-toe sock blanks includes a tube for receiving a sock blank sleeved thereover such that the open toe end of the blank extends beyond the end of the tube, a clamping mechanism for engaging the blank against the tube and for rotating the blank about the tube, a sensor system for detecting one or more predetermined features on the toe end of the blank so that the blank can be rotated to a proper orientation for sewing the toe end closed, and a spreader device that moves into the open toe end of the blank and spreads the toe end into a flattened orientation so that overlying edge portions of the open toe end are generally aligned with each other, and then moves away from the tube to remove the blank from the tube and transport the flattened toe end into an automatic sewing machine for sewing the overlying edge portions of the toe end together.
摘要:
N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要:
N-Biphenyl(substituted methyl) aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要:
An apparatus for orienting sock blanks or the like so that the open toes of the blanks can be sewn closed includes a device for turning the sock inside out, a sock rotation device for grasping the sock and rotating it until sensors detect that the sock is in the proper orientation, a sock transfer device for taking the sock from the sock rotation device toward a sewing machine, and sock guiding and positioning mechanisms for feeding the sock into the in-feed nip of the sewing machine.