SUBSTITUTED 5-AMINOTHIENO[2,3-C]PYRIDAZINE-6-CARBOXAMIDE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4

In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Substituted 5-aminothieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4

In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

SUBSTITUTED 2-(4-HETEROCYCLYLBENZYL)ISOINDOLIN-1-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1

In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein L is —(C═O)—.9. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any of - claim 1 , or pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or polymorph thereof claim 1 , and a pharmaceutically acceptable carrier.11. The method of claim 10 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.12. The method of claim 10 , further comprising the step of identifying a mammal in need of treatment of the disorder.13. The method of or claim 10 , wherein the disorder is associated with a mAChR Mdysfunction.14. The method of claim 10 , wherein the disorder is a neurological and/or psychiatric disorder associated with mAChR Mdysfunction.15. The method of claim 10 , wherein the disorder is selected from Alzheimer's disease claim 10 , schizophrenia claim 10 , a sleep disorder claim 10 , a pain disorder and a cognitive disorder.16. The method of claim 15 , wherein the disorder is Alzheimer's disease.17. The method of claim 10 , wherein the disorder is selected from psychosis claim 10 , schizophrenia claim 10 , conduct disorder claim 10 , disruptive behavior disorder claim 10 , bipolar disorder claim 10 , psychotic episodes of anxiety claim 10 , anxiety ...

Substituted thieno[2,3-C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4

In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Substituted 5-aminothieno[2,3—C]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4

In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6 -carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1

In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

CGRP RECEPTOR ANTAGONISTS

Compounds of Formula (I) (wherein variables A, A, A, ring-B, m, n, J, E, E, E, R, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved. 2. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Eand Eare ═C(R)—.3. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Aand Aare each a bond claim 1 , and Ais selected from the group consisting of{'sup': 1', '2, '(1) —CRR—,'}{'sup': 'b', '(2) —NR—,'}{'sup': 1', '2', 'b, '(3) —CRR—NR—,'}{'sup': 1', '2, 'sub': '2', '(4) —CRR—CH—,'}{'sup': 1', '2, '(5) —O—CRR—,'}{'sup': 1', '2, '(6) —CRR—O—, and'}(7) —C(═O)—.4. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ais —C(═O)—.7. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m and n are each 1.8. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein J is ═C(R)— and Y is ═C(R)— claim 1 , and Rand Rand the atom(s) to which they are attached join to form a ring selected from cyclopentenyl claim 1 , cyclohexenyl claim 1 , phenyl and pyridyl claim 1 , wherein the ring is optionally substituted as described above.9. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein J is —N(Rb)— and Y is ═C(═O)— claim 1 , and Rb is selected from hydrogen or —C1-6alkyl claim 1 , which is unsubstituted or substituted with 1-3 halo. Typically claim 1 , Rb is methyl.12. A compound of claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , wherein m and n are each ...

SUBSTITUTED BENZYLSPIROINDOLIN-2-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1

In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein Qis CR; wherein Qis CR; wherein Qis CR; and wherein Qis CR.3. The compound of claim 1 , wherein Qis CR; wherein Qis CR; wherein Qis CR; and wherein Qis CR.4. The compound of claim 1 , wherein Qis NR.5. The compound of claim 4 , wherein Qis NR claim 4 , and wherein Ris selected from cyclopentyl and cyclohexyl.6. The compound of claim 1 , wherein Ris 1H-pyrazol-4-yl; and wherein Ris monosubstituted with methyl.7. The compound of claim 1 , wherein m is 0 claim 1 , n is 2 claim 1 , and q is 2.8. The compound of claim 1 , wherein m is 0 claim 1 , n is 2 claim 1 , and q is 1.14. The method of claim 13 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.15. The method of claim 13 , further comprising the step of identifying a mammal in need of treatment of the disorder.16. The method of claim 15 , wherein the disorder is associated with a mAChR Mdysfunction.17. The method of claim 13 , wherein the disorder is a neurological and/or psychiatric disorder associated with mAChR Mdysfunction.18. The method of claim 13 , wherein the disorder is selected from Alzheimer's disease claim 13 , schizophrenia claim 13 , a sleep disorder claim 13 , a pain disorder and a cognitive disorder.19. The method of claim 18 , wherein the disorder is ...

SUBSTITUTED (1-(METHYLSULFONYL)AZETIDIN-3-YL)(HETEROCYCLOALKYL)METHANONE ANALOGS AS ANTAGONISTS OF MUSCARINIC ACETYLCHOLINE M1 RECEPTORS

In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein L is N.5. The compound of claim 1 , wherein Ris selected from aryl and heteroaryl; and wherein Ris substituted with 0-3 groups selected from halogen claim 1 , hydroxyl claim 1 , cyano claim 1 , —NH claim 1 , C1-C6 alkyl claim 1 , C1-C6 alkoxy claim 1 , C1-C6 haloalkyl claim 1 , C1-C6 polyhaloalkyl claim 1 , C1-C6 alkylamino claim 1 , and C1-C6 dialkylamino.10. The method of claim 9 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.11. The method of claim 9 , further comprising the step of identifying a mammal in need of treatment of the disorder.12. The method of claim 9 , wherein the disorder is a movement disorder.13. The method of claim 9 , wherein the disorder is a pain disorder.14. The method of claim 13 , wherein the pain disorder is selected from neuropathic pain claim 13 , central pain syndrome claim 13 , postsurgical pain syndrome claim 13 , bone and joint pain claim 13 , repetitive motion pain claim 13 , dental pain claim 13 , cancer pain claim 13 , myofascial pain claim 13 , perioperative pain claim 13 , chronic pain claim 13 , dysmennorhea claim 13 , inflammatory pain claim 13 , headache claim 13 , migraine headache claim 13 , cluster headache claim 13 , headache claim 13 , primary hyperalgesia claim ...

PRECISION-FASTENING HANDHELD CORDLESS POWER TOOLS

Cordless power tools include a pistol housing having an upper portion that merges into a downwardly extending handle, a DC motor residing in the upper portion of the housing, the DC motor having a rotor that drives an output shaft; a torque transducer on board the tool in communication with the output shaft; and a dynamic motor control circuit residing in the housing in communication with the motor and torque transducer. The dynamic motor control circuit includes a Kelvin resistor in communication with the motor for measuring motor current and digital hall switches in communication with the motor for measuring motor speed. The motor current can vary by at least 100 A during operation. 1. A hand-held cordless fastening power tool , comprising:a housing;a motor residing in the housing, the motor having a rotor that drives an output shaft;a torque transducer in the housing in communication with the output shaft; anda dynamic motor control circuit residing in the housing in communication with the motor and torque transducer, the dynamic motor control circuit comprising a Kelvin resistor in communication with the motor for measuring motor current and digital hall switches in communication with the motor for measuring motor speed, wherein the motor current can vary by at least 100 A during operation.2. The cordless power tool of claim 1 , further comprising:a rechargeable battery pack releasably attached to the lower portion of the power tool, wherein the battery pack is a low voltage battery pack of about 36V or less; anda plurality of hall sensors held internal to the motor in communication with the motor control circuit to allow for at least one of angle monitoring or angle positioning.3. The cordless power tool of claim 1 , wherein the Kelvin resistor comprises four terminals claim 1 , two used for current sensing and two used as a current path claim 1 , and wherein the dynamic motor control circuit is configured to run the motor using current that is between about ...

HETEROCYCLYL-AZABICYCLO[3.2.1]OCTANE ANALOGS AS SELECTIVE M1 AGONISTS AND METHODS OF MAKING AND USING SAME

In one aspect, the invention relates to compounds which are useful as allosteric or bitopic agonists of the Mmuscarinic 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. 3. The compound of claim 1 , wherein n is 1.4. The compound of claim 1 , wherein Y claim 1 , Y claim 1 , and Yare each O.5. The compound of claim 1 , wherein R claim 1 , each R claim 1 , and each Ris hydrogen.6. The compound of claim 1 , wherein Ris selected from optionally substituted methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl claim 1 , and hexyl.8. The compound of claim 7 , wherein Ris selected from optionally substituted C1-C6 alkyl and optionally substituted phenyl.9. The compound of claim 7 , wherein each Ris hydrogen.10. The compound of claim 7 , wherein each Ris hydrogen.11. The compound of claim 7 , wherein Ris selected from optionally substituted methyl claim 7 , ethyl claim 7 , propyl claim 7 , butyl claim 7 , and hexyl.13. The compound of claim 12 , wherein Ris selected from optionally substituted C1-C6 alkyl and optionally substituted phenyl.14. The compound of claim 1 , which activates Mreceptor response in M-transfected CHO-K1 cells.19. The method of claim 18 , wherein the disorder is selected from psychosis claim 18 , schizophrenia claim 18 , conduct disorder claim 18 , disruptive behavior disorder claim 18 , bipolar disorder claim 18 , psychotic episodes of anxiety claim 18 , anxiety associated with psychosis claim 18 , psychotic mood disorders such as severe major depressive disorder; mood disorders associated with psychotic disorders claim 18 , acute mania claim 18 , depression associated with bipolar disorder claim 18 , mood ...

Substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4

In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Stillage solids concentration

Stillage solids concentration methods are disclosed wherein a solids concentration aid is added to a process stream mixture in a corn to ethanol process. The solids concentration aid may comprise a cationic polymer coagulant or flocculant or both, a starch based coagulant or flocculant or a biologically derived (i.e., plant or animal origin) coagulant or flocculant. Acrylamide/quaternary ammonium copolymers and homopolymeric polydiallyldimethyl ammonium chloride polymers are noteworthy examples of suitable solids concentration aids.

SUBSTITUTED 1-BENZYLINDOLIN-2-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF MUSCARINIC ACETYLCHOLINE M1 RECEPTORS

In one aspect, the invention relates to substituted 1-benzylindolin-2-one analog compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein each of Q claim 1 , Q claim 1 , Q claim 1 , and Qis not N.3. The compound of claim 1 , wherein each of Q claim 1 , Q claim 1 , Q claim 1 , and Qis not N.4. The compound of claim 1 , wherein Ris —CF.5. The compound of claim 1 , wherein Ris selected from hydrogen and —CH.6. The compound of claim 1 , wherein Ris hydrogen.7. The compound of claim 1 , wherein Ris selected from 1H-pyrazol-3-yl claim 1 , 1H-pyrazol-4-yl claim 1 , 1H-pyrazol-5-yl; and wherein Ris monosubstituted with a group selected from methyl claim 1 , ethyl claim 1 , propyl claim 1 , and isopropyl.8. The compound of claim 1 , wherein n is 1; L is O; wherein Ris selected from hydrogen claim 1 , —CH claim 1 , —CHCH claim 1 , —CHF claim 1 , —CHF claim 1 , —CF claim 1 , —CHCl claim 1 , —CHCl claim 1 , —CCl claim 1 , —CHCHF claim 1 , —CHCHF claim 1 , —CHCF claim 1 , —CHCHCl claim 1 , —CHCHCl claim 1 , and —CHCCl; Ris hydrogen; wherein each of Rand Ris hydrogen; wherein Ris selected from 1-methyl-1H-pyrazol-4-yl claim 1 , 1-ethyl-1H-pyrazol-4-yl claim 1 , and 1-propyl-1H-pyrazol-4-yl; wherein each of Q claim 1 , Q claim 1 , Q claim 1 , and Qis not N; and wherein each of Q claim 1 , Q claim 1 , Q claim 1 , and Qis not N.11. The method of claim 10 , wherein the mammal has been diagnosed with a need for treatment of the disorder ...

Substituted 4-(1h-pyrazol-4-yl)benzyl analogues as positive allosteric modulators of machr m1 receptors

In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

SUBSTITUTED 2-(4-HETEROCYCLYLBENZYL)ISOINDOLIN-1-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1

In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein L is —(C═O)—.9. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any of - claim 1 , or pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or polymorph thereof claim 1 , and a pharmaceutically acceptable carrier.11. The method of claim 10 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.12. The method of claim 10 , further comprising the step of identifying a mammal in need of treatment of the disorder.13. The method of or claim 10 , wherein the disorder is associated with a mAChR Mdysfunction.14. The method of claim 10 , wherein the disorder is a neurological and/or psychiatric disorder associated with mAChR Mdysfunction.15. The method of claim 10 , wherein the disorder is selected from Alzheimer's disease claim 10 , schizophrenia claim 10 , a sleep disorder claim 10 , a pain disorder and a cognitive disorder.16. The method of claim 15 , wherein the disorder is Alzheimer's disease.17. The method of claim 10 , wherein the disorder is selected from psychosis claim 10 , schizophrenia claim 10 , conduct disorder claim 10 , disruptive behavior disorder claim 10 , bipolar disorder claim 10 , psychotic episodes of anxiety claim 10 , anxiety ...

CGRP RECEPTOR ANTAGONISTS

Compounds of Formula I: 117-. (canceled)21. A pharmaceutical composition which comprises an inert carrier and the compound of claim 19 , or a pharmaceutically acceptable salt thereof.221. A method of treating headache in a mammalian patient in need of such treatment claim 19 , which comprises administering to the patient a therapeutically effective amount of the compound of claim claim 19 , or a pharmaceutically acceptable salt thereof.23. The method of claim 22 , wherein the headache is migraine headache or cluster headache.2425-. (canceled) CGRP (Calcitonin Gene-Related Peptide) is a naturally occurring 37-amino acid peptide that is generated by tissue-specific alternate processing of calcitonin messenger RNA and is widely distributed in the central and peripheral nervous system. CGRP is localized predominantly in sensory afferent and central neurons and mediates several biological actions, including vasodilation. CGRP is expressed in alpha- and beta-forms that vary by one and three amino acids in the rat and human, respectively. CGRP-alpha and CGRP-beta display similar biological properties. When released from the cell, CGRP initiates its biological responses by binding to specific cell surface receptors that are predominantly coupled to the activation of adenylyl cyclase. CGRP receptors have been identified and pharmacologically evaluated in several tissues and cells, including those of brain, cardiovascular, endothelial, and smooth muscle origin.Based on pharmacological properties, these receptors are divided into at least two subtypes, denoted CGRPand CGRP. Human α-CGRP-(8-37), a fragment of CGRP that lacks seven N-terminal amino acid residues, is a selective antagonist of CGRP, whereas the linear analogue of CGRP, diacetoamido methyl cysteine CGRP ([Cys(ACM)2,7]CGRP), is a selective agonist of CGRP. CGRP is a potent neuromodulator that has been implicated in the pathology of cerebrovascular disorders such as migraine and cluster headache. In clinical studies, ...

Substituted thieno[2,3-b]pyridine-2-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4

In one aspect, the invention relates to substituted thieno[2,3-b]pyridine-2-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

SUBSTITUTED 2-(4-HETEROCYCLYLBENZYL)ISOINDOLIN-1-ONE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1

In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein L is —(C═O)—.9. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 , or pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or polymorph thereof claim 1 , and a pharmaceutically acceptable carrier.11. The method of claim 10 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.12. The method of claim 10 , further comprising the step of identifying a mammal in need of treatment of the disorder.13. The method of claim 10 , wherein the disorder is associated with a mAChR Mdysfunction.14. The method of claim 10 , wherein the disorder is a neurological and/or psychiatric disorder associated with mAChR Mdysfunction.15. The method of claim 10 , wherein the disorder is selected from Alzheimer's disease claim 10 , schizophrenia claim 10 , a sleep disorder claim 10 , a pain disorder and a cognitive disorder.16. The method of claim 15 , wherein the disorder is Alzheimer's disease.17. The method of claim 10 , wherein the disorder is selected from psychosis claim 10 , schizophrenia claim 10 , conduct disorder claim 10 , disruptive behavior disorder claim 10 , bipolar disorder claim 10 , psychotic episodes of anxiety claim 10 , anxiety associated ...

SUBSTITUTED THIENO[2,3-C]PYRIDAZINE-6-CARBOXAMIDE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4

In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein each of Rand Ris methyl.3. The compound of claim 1 , wherein each of Rand Ris methyl; and wherein each of Rand Ris hydrogen.4. The compound of any of - claim 1 , wherein Ris hydrogen and Ris —(CH)—Arsubstituted with 0-2 groups independently selected from —F claim 1 , —Cl claim 1 , —NH claim 1 , —OH claim 1 , —CN claim 1 , methyl claim 1 , —CHF claim 1 , —CHCl claim 1 , —CHF claim 1 , —CF claim 1 , —CHCl claim 1 , —CCl claim 1 , —OCH claim 1 , —NHCH claim 1 , —N(CH) claim 1 , and —S(O)R.5. The compound of any of - claim 1 , wherein Aris phenyl; and wherein each Aris independently substituted with 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3 groups independently selected from halogen claim 1 , —NH claim 1 , —OH claim 1 , —CN claim 1 , C1-C8 alkyl claim 1 , C1-C8 haloalkyl claim 1 , C1-C8 polyhaloalkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 alkylamino claim 1 , C1-C8 dialkylamino claim 1 , and —S(O)R.13. The compound of any of - claim 1 , wherein the compound exhibits positive allosteric modulation of the mAChR Mresponse to acetylcholine with an ECof less than about 10 claim 1 ,000 nM.14. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any of - claim 1 , or pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , ...

Substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m1

In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

SUBSTITUTED 1H-PYRAZOLO[3',4',4,5]THIENO[2,3-B]PYRIDIN-3-AMINE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYCHOLINE RECEPTOR M4

In one aspect, the invention relates to substituted 1H-pyrazolo[3′,4′:4,5]thieno[2,3-b]pyridin-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein Ris hydrogen.3. The compound of claim 1 , wherein each of Rand Rare methyl.4. The compound of claim 1 , wherein Ris hydrogen; and each of Rand Rare methyl.5. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , —(CH)OH claim 1 , and —(CH)OH.9. The compound of claim 1 , wherein the compound exhibits positive allosteric modulation of the mAChR Mresponse to acetylcholine with an ECof less than about 10 claim 1 ,000 nM.10. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 , or pharmaceutically acceptable salt claim 1 , solvate claim 1 , or polymorph thereof claim 1 , and a pharmaceutically acceptable carrier.12. The method of claim 11 , wherein an effective amount is a therapeutically effective amount.13. The method of claim 11 , wherein treatment is symptom amelioration or prevention claim 11 , and wherein an effective amount is a prophylactically effective amount.14. The method of claim 11 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.15. The method of claim 11 , wherein the disorder is a neurological and/or psychiatric disorder associated with mAChR Mdysfunction.16. The method of claim ...

SUBSTITUTED PYRAZOLO[3',4':4,5]THIENO[2,3-C]PYRIDAZIN-3-AMINE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4

In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M(mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. 2. The compound of claim 1 , wherein each of Rand Ris independently selected from hydrogen claim 1 , C1-C8 alkyl claim 1 , C1-C8 monohaloalkyl claim 1 , C1-C8 polyhaloalkyl claim 1 , Cy claim 1 , Cy-(C1-C6 alkyl)- claim 1 , Ar claim 1 , and Ar—(C1-C6 alkyl)-;{'sup': 1', '1', '5', '5', '5', '5', '5', '5', '6', '2, 'sub': 2', '5', 'm', 'm, 'claim-text': wherein each m is an integer independently selected from 0, 1 and 2;', {'sup': 2', '2', '5, 'sub': 2', 'm, 'wherein each Ar, when present, is independently selected from phenyl and heteroaryl, and wherein each Aris independently substituted with 0, 1, 2, or 3 groups independently selected from halogen, —NH, —OH, —CN, C1-C8 alkyl, C1-C8 monohaloalkyl, C1-C8 polyhaloalkyl, C1-C8 alkoxy, C1-C8 alkylamino, C1-C8 dialkylamino, and —S(O)R;'}, {'sup': 5', '2', '2, 'wherein each R, when present, is independently selected from hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C1-C8 monohaloalkyl, C1-C8 polyhaloalkyl, —(C1-C3)-Ar, and Ar; and'}, {'sup': '6', 'sub': '2', 'wherein each R, when present, is selected from C1-C4 alkyl, C1-C4 alkoxy, C1-C4 monoalkylamino, or C1-C4 dialkylamino substituted with 1 or 2 groups selected from fluoro, trifluoromethyl, methyl, —OH, —NH, and —CN;'}], 'wherein each Ar, when present, is independently selected from phenyl and heteroaryl, and ...

Substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m1

In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin- 1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Indole compounds as positive allosteric modulators of the muscarinic receptor

In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Spirohydantoin aryl cgrp receptor antagonists

Compounds of formula (I); (wherein variables A1, A2. A3, A4, A5, A6, A7, B3 E1, E2, E3, E4, E5, G1, G2 and R.6 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. The invention is also directed to 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.

Cationic polymer for water clarification and sludge dewatering

ABSTRACT Methods of clarifying wastewater and of dewatering sludge are disclosed. The methods comprise adding to the wastewater or the sludge an effective amount for the purpose of a polymer comprising repeat unit moieties of methacryloyloxyethyl trimethyl ammonium chloride, said polymer having an intrinsic viscosity from about 1.0 to about 4.5 dl/g.

Apparatus for tightening threaded fasteners

A portable torque power tool is disclosed herein and includes: a motor to generate a turning force; a drive to transfer the turning force; a turning force multiplication mechanism assembly to multiply the turning force; a shifter assembly to shift the tool between a lower speed / higher torque (LSHT) mode and a higher speed / lower torque (HSLT) mode; a torque transducer to measure torque output; wherein torque output is controlled by the torque transducer in LSHT mode; and wherein torque output is controlled by motor current in HSLT mode. In one embodiment of the present application, the torque transducer is a wireless torque transducer assembly formed at or near an output of a housing of the turning force multiplication assembly to improve measurement accuracy of torque output. Advantageously, simplified tool and system design and operation; reduced tool and system size; expanded functionality, greater durability and intuitive usability; and increased tool and system portability, efficiency, reliability and repeatability, all at low cost, are achieved. Further disclosed herein is an operation parameter regulation unit for use with a bolting system having a plurality of networked electrically powered torque tools and/or drive portions of torque tools described above for simultaneous tightening of industrial threaded fasteners. The operation parameter regulation unit includes: a processing unit; an output unit connected and/or integrated with the processing unit; an input unit connected and/or integrated with the processing unit; an activation unit connected and/or integrated with the processing unit for activating operation units of the plurality of networked electrically powered torque tools and/or drive portions of torque tools; and a control unit for controlling operation parameters of each of the plurality of networked electrically powered torque tools and/or drive portions of torque tools to maintain a difference between the operation parameters within a ...

Alpha-hydroxy amides as bradykinin antagonists or inverse agonists

.alpha.-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;

Alkyl 3-((2-amidoethyl)amino)-8-azabicyclo[3.2.1]octane-8-carboxylate analogs as selective m1 agonists and methods of making and using same

In one aspect, the invention relates to compounds having a general structure: which are useful as selective allosteric or bitopic agonists of the M 1 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.

Substituted 1-benzylindolin-2-one analogs as positive allosteric modulators of muscarinic acetylcholine m1 receptors

In one aspect, the invention relates to substituted l-benzylindolin-2-one analog compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor Mi (mAChR Mi); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

"method for the recovery of tallow from animal or food processing wastewater and method for the recovery of fats, oils and greases in a solid phase from animal or food processing wastewater"

Spirohydantoin Aryl Cgrp Receptor Antagonists

Compounds of formula I: (wherein variables A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , B, E 1 , E 2 , E 3 , E 4 , E 5 , G 1 , G 2 and R 6 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. The invention is also directed to 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.

Substituted spirocyclic cgrp receptor antagonists

Compounds of formula I: I (wherein variables A1, A2, A3, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, 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. The invention is also directed to 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.

Apparatus for tightening threaded fasteners

A portable torque power tool is disclosed herein and includes: a motor to generate a turning force; a drive to transfer the turning force; a turning force multiplication mechanism assembly to multiply the turning force; a shifter assembly to shift the tool between a lower speed/higher torque (LSHT) mode and a higher speed/lower torque (HSLT) mode; a torque transducer to measure torque output; wherein torque output is controlled by the torque transducer in LSHT mode; and wherein torque output is controlled by motor current in HSLT mode. In one embodiment of the present application, the torque transducer is a wireless torque transducer assembly formed at or near an output of a housing of the turning force multiplication assembly to improve measurement accuracy of torque output. Advantageously, simplified tool and system design and operation; reduced tool and system size; expanded functionality, greater durability and intuitive usability; and increased tool and system portability, efficiency, reliability and repeatability, all at low cost, are achieved. Further disclosed herein is an operation parameter regulation unit for use with a bolting system having a plurality of networked electrically powered torque tools and/or drive portions of torque tools described above for simultaneous tightening of industrial threaded fasteners. The operation parameter regulation unit includes: a processing unit; an output unit connected and/or integrated with the processing unit; an input unit connected and/or integrated with the processing unit; an activation unit connected and/or integrated with the processing unit for activating operation units of the plurality of networked electrically powered torque tools and/or drive portions of torque tools; and a control unit for controlling operation parameters of each of the plurality of networked electrically powered torque tools and/or drive portions of torque tools to maintain a difference between the operation parameters within a ...

Methods for removing fats, oil and grease and recovering tallow from wastewater

A method for recovering tallow from food or animal processing wastewater includes adding a flocculant to the wastewater to agglomerate suspended fats, oil and grease particles in the wastewater, separating solid waste materials from the wastewater and processing the solid waste materials to recover tallow. The flocculant includes polyacrylamide or an acrylamide copolymer. A process for separating fats, oil and grease from food or animal processing wastewater is also provided.

Substituted monocyclic CGRP receptor antagonists

Branched 3- and 6-substituted quinolines as cgrp receptor antagonists

The present invention is directed to novel branched 3- and 6-substituted quinoline derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to 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.

Branched 3- and 6-substituted quinolines as CGRP receptors antagonists

The present invention is directed to novel branched 3- and 6-substituted quinoline derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to 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.

1-hydroxycycloalkanecarboxamide derivatives as bradykinin antagonists

.alpha.-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; Rl, R2 and R3 are each independently selected from H, halogen and OH; or Rl and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or F; R6 is selected from -CO2-C1-4alkyl, -O-C1-4alkyl, -O- C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl l,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-l,2,4-oxadiazol-3-yl, 3-halomethyl- l,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-l,2,3-triazolyl, and 5-methyl-l ,2,3-triazolyl; R7 and R8 are each independently Cl or F; 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.

Cationic polymers for sludge dewatering

A method of dewatering sludge is disclosed. This method comprises adding to the sludge an effective amount for the purpose of a polymer comprising repeat unit moieties of the compound methacryloxyethyl trimethyl ammonium chloride, said polymer having an intrinsic viscosity of about 1.0 to about 4.5 dl/g.

Spirohydantoin aryl cgrp receptor antagonists

Compounds of formula (I); (wherein variables A1, A2. A3, A4, A5, A6, A7, B3 E1, E2, E3, E4, E5, G1, G2 and R.6 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. The invention is also directed to 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.

Substituted monocyclic CGRP receptor antagonists

Compounds of formula I: (wherein variables A 1 , A 2 , A 3 , A 4 , m, n, J, Q, R 4 , E a , E b , E c , R 6 , R 7 , R e , R f , R PG 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. The invention is also directed to 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.

Modified polymeric flocculants with improved performance characteristics

Methods for the preparation of high molecular weight cationic poly(meth) acrylamide/quaternary ammonium salt copolymers are disclosed wherein after a t least about 50% of the monomers have been polymerized, a cross-linking agent is then added to the reaction mixture on a continuous basis and in the absen ce of any feed of chain transfer agent. Cationic copolymers so produced exhibit improved floc formation properties and are useful as flocculants and dewatering aids in aqueous systems that include an oily sludge or the like.< /SDOAB>

Substituted 3-aminothieno[2,3-c]pyridine-2-carboxamide analogs as positive allosteric modulators

In one aspect, the invention relates to substituted 3-aminothieno[2,3-c]pyridine-2- carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Non-amidic linkers with branched termini as cgrp receptor antagonists

The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to 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.

Spirolactam aryl cgrp receptor antagonists

Compounds of formula (I): (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, J and K 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. The invention is also directed to 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.

DERIVATIVES OF DIBENZOTIAZEPINA AND ITS USES

LOS COMPUESTOS DE LA SIGUIENTE FÓRMULA: (VER FORMULA); DONDE Z SE DESCRIBE EN LA DESCRIPCIÓN, SALES FARMACÉUTICAMENTE ACEPTABLES DE ESTOS, COMPOSICIONES QUE LOS COMPRENDEN Y MÉTODOS PARA TRATAR EL TRASTORNO BIPOLAR, UN TRASTORNO DE ANSIEDAD, UN TRASTORNO DEL ESTADO DE ÁNIMO O LA ESQUIZOFRENIA, U OTRO TRASTORNO PSICÓTICO CON DICHOS COMPUESTOS

Branched 3- and 6-substituted quinolines as cgrp receptor antagonists

Substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1

In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Methods for sludge dewatering.

Substituted 4-(1H-pyrazol-4-yl)benzyl analogues as positive allosteric modulators of mAChR M1 receptors

In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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.

Spirolactam aryl CGRP receptor antagonists

N-biphenylmethyl aminocycloalkanecarboxamide derivatives with a substituent on the methyl useful as bradykinin antagonists

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.

3- and 6-quinolines with n-attached heterocyclic cgrp receptor antagonists

N-biphenylmethyl aminocycloalkanecarboxamide derivatives with a substiituent on the methyl useful as bradykinin antagonists

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.

Cgrp receptor antagonists with tertiary amide, sulfonamide, carbamate and urea end groups

Compounds of formula I: (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.

Heterocyclyl-azabicyclo[3.2.1]octane analogs as selective m1 agonists and methods of making and using same

In one aspect, the invention relates to compounds which are useful as allosteric or bitopic agonists of the M 1 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.

1-Hydroxycycloalkanecarboxamide derivatives

α-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; R 1 , R 2 and R 3 are each independently selected from H, halogen and OH; or R 1 and R 2 attached to the same carbon atom together represent oxo; R 4 is H or methyl; R 5 is Cl or I 2 ; R 6 is selected from —CO 2 —C 3-4 alkyl, —O—C 1-4 alkyl, —O—C 1-4 haloalkyl, 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; R 7 and R 8 are each independently Cl or I 2 ; 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.

Substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1

In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin 1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor Mi (mAChR M); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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. -313-

N-biarylmethyl aminocycloalkanecarboxamide derivatives

Stillage solids concentration

Stillage solids concentration methods are disclosed wherein a solids concentration aid is added to a process stream mixture in a com to ethanol process. The solids concentration aid may comprise a cationic polymer coagulant or flocculant or both, a starch based coagulant or flocculant or a biologically derived (i.e., plant or animal origin) coagulant or flocculant. Acrylamide / quaternary ammonium copolymers and homopolymeric polydiallyldimethyl ammonium chloride polymers are noteworthy examples of suitable solids concentration aids.

Methods for sludge dewatering

Substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4

N-biphenylmethylaminocycloalkancarboxamid- derivative

Arylsulfonamide derivatives

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.

Apparatus and method for automatically orienting hosiery articles for closing toe ends thereof

Heterocyclyl-azabicyclo[3.2.1]octane analogs as selective m1 agonists and methods of making and using same

In one aspect, the invention relates to compounds which are useful as allosteric or bitopic agonists of the M 1 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.

Derivati N-bifenil metil amino cikloalkan karboksamida s substituentom na metilni skupini, primerni kot antagonisti bradikinina

Als bradykininantagonisten geeignete n-biphenyl methyl amino cyclo alkan carbonsäure amid derivate mit einem substituenten an der methylgruppe

N-biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin b1 antagonists

Precision-fastening handheld cordless power tools

Cordless power tools include a pistol housing having an upper portion that merges into a downwardly extending handle, a DC motor residing in the upper portion of the housing, the DC motor having a rotor that drives an output shaft; a torque transducer on board the tool in communication with the output shaft; and a dynamic motor control circuit residing in the housing in communication with the motor and torque transducer. The dynamic motor control circuit includes a Kelvin resistor in communication with the motor for measuring motor current and digital hall switches in communication with the motor for measuring motor speed. The motor current can vary by at least 100A during operation.

Precision-fastening handheld cordless power tools

N-biphenylmethyl aminocycloalkanecarboxamide derivatives with a substituent on the methyl useful as bradykininantagonists

Monocyclic cgrp receptor antagonists

The present invention is directed to compounds of the formula (I): (wherein variables A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , G 1 , G 2 , G 3 , G 4 , J, Q, E a , E b , E c , R 6 , R 7 , R PG 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 CGRP is involved, such as migraine. The invention is also directed to 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.