Dihydropyridines substituted by heterocycles, process for their preparation and their use in medicaments

Bicyclic pyran derivatives and their use as inhibitors of 5-lipoxygenase

Preparation of 2-(2'-thienyl) alkylamines and derivatives thereof and synthesis of 4,5,6,7- thieno [3,2-c] pyridine derivatives therefrom

N-Aryl nitrogen heterocycles having fluorine-containing substituents

Azafluorene derivative and organic light-emitting device using the derivative

A novel azafluorene derivative and an organic light-emitting device having the derivative are provided. The organic light-emitting device includes a pair of electrodes composed of an anode and a cathode one of which is a transparent or semi-transparent electrode, and an organic compound layer interposed between the pair of electrodes. The organic compound layer contains the azafluorene derivative represented by the following general formula (I):

Manufacture of 4-((1r,3s)-6-chloro-3-phenyl-indan-1-yl)-1,2,2-trimethyl-piperazine and 1-((1r,3s)-6-chloro-3-phenyl-indan-1-yl)-3,3-dimethyl-piperazine

The present invention relates to a process for the manufacture of 4-((1R,3S)-6-Chloro-3-phenyl-indan-1-yl)-1,2,2-trimethyl-piperazine or a pharmaceutically acceptable salt thereof and a process for the manufacture of 1-((1R,3S)-6-Chloro-3-phenyl-indan-1-yl)-3,3-dimethyl-piperazine or a pharmaceutically acceptable salt thereof.

DIHYDROETHIDINE ANALOGUES AND USES THEREOF

Tracers for imaging distribution of reactive oxygen species (ROS) are disclosed. The tracers include radiolabeled dihydroethidine (DHE) analogues. Further disclosed are uses of the compounds, including methods of imaging tissue distribution of ROS in vivo by positron emission tomography (PET). Methods of synthesizing the compounds are also disclosed. 2. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein the radioisotope is a positron-emitting radioisotope.3. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein Ris H.4. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein the compound or salt thereof comprises an CH.5. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein Ris (CH)—CHand q is 0.6. A radiolabeled compound or salt thereof in accordance with claim 5 , wherein Ris CH.8. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein Ris O—R claim 1 , Ris CH.9. A radiolabeled compound or salt thereof in accordance with claim 8 , wherein Ris O—R claim 8 , wherein Ris CH.11. A radiolabeled compound or salt thereof in accordance with claim 10 , wherein n is 1.12. A radiolabeled compound or salt thereof in accordance with claim 10 , wherein m is 2.13. A radiolabeled compound or salt thereof in accordance with claim 10 , wherein n is 1 and m is 2.15. A radiolabeled compound or salt thereof in accordance with claim 13 , wherein p is 2. The disclosed subject matter was developed in part with Government support under grant RC1AG036045 from the National Institutes of Health. The Government has certain rights in the invention.This application claims priority to U.S. Provisional Application Ser. No. 61/287,115 filed on Dec. 16, 2009, which is incorporated herein by reference in its entirety.The present teachings relate to the field of free radicals in biology and medicine.Free radicals play key roles in the pathogenesis of a large number of diseases and ...

MATERIALS AND METHODS FOR THE PREPARATION OF ANISOTROPICALLY-ORDERED SOLIDS

The invention provides materials and methods for making anisotropic solids which may be in the form of films, layers, shaped elements, and other shaped articles. The methods provide anisotropic solids without the need for rolling, rubbing, or stretching to impart orientational alignment of the molecules of the solid. The methods employ organic or organometallic compounds which are soluble orienting molecules. The solvent or solvent system must be sufficiently volatile to be removed without disruption of the molecular orientation. The soluble orienting molecules include those containing one or more hydrophilic and/or ionic groups and the solvent or solvent system can be a polar organic solvent or solvent system or an aqueous solvent or solvent system. The invention also provides novel compounds having quaterrylene, perylene and naphthalene ring systems carrying one or more hydrophilic and/or ionic groups. These novel compounds can exhibit useful absorption and fluorescence properties in solution and in the solid phase and can exhibit useful liquid crystalline properties. 127-. (canceled)28. A compound of formula III herein.2933-. (canceled) This invention takes priority under 35 U.S.C.119(e) from U.S. provisional application U.S. Ser. No. 60/524,272, filed Nov. 21, 2003, which is incorporated by reference herein in its entirety.This invention was funded in part by the United States government through the National Science Foundation grants NSF DMR 9876027 and NSF DMR0405532, NSF EPSCoR Infrastructure Enhancement Grant UCCSN-02-124. The United States government has certain rights in this invention.The construction of devices and materials through molecular self-assembly and self-organization processes is of considerable interest. This invention relates to methods for controlling the self-organization of organic compounds, particularly into a lyotropic (solvent- and concentration-dependent) liquid-crystalline phase, in order to prepare micro-patterned organic solids in ...

INDENOQUINOLONE COMPOUND, PREPARATION METHOD AND USE THEREOF

An indenoquinolone compounds of Formula (A) is disclosed, wherein the definition of each group is described in the description. These compounds may specifically inhibit topoisomerase I, and they have good activities against many kinds of human tumor cells, such as lung cancer, colon cancer, breast cancer, liver cancer and the like. They can be used in the manufacture of antitumor drugs. The method for preparing the compound of formula (A), and pharmaceutical compositions containing such compounds and the use in the manufacture of antitumor drugs are also disclosed. 3. The compound according to claim 1 , wherein claim 1 , Rmay be located at one or two positions of 2- and 3-position; and/or Rmay be located at one or two positions of 8- and 9-position.4. The compound according to claim 1 , wherein claim 1 , Ris any one of the following groups: a) a hydrogen; b) a C1-8 straight-chain or branched alkyloxy; c) a halogen; and/or{'sub': '2', 'Ris any one of the following groups: a) a hydrogen; b) a C1-8 straight-chain or branched alkyloxy; c) a halogen; and/or'}{'sub': 3', '2', '4', '4', '5', '6', '5', '6, 'Ris —(CH)mR, wherein m is 1-4, and Rmay be a saturated or unsaturated 4-7 membered nitrogen-containing heterocycle, halogen, or NRR, wherein Ror Ris any one of the following groups: a) a hydrogen; b) a substituted or unsubstituted C1-8 straight-chain or branched alkyl.'}5. The compound according to claim 1 , wherein claim 1 , m in Ris 2-3 claim 1 , and Rmay be a saturated or unsaturated 5-6 membered nitrogen-containing heterocycle claim 1 , halogen claim 1 , or NRR claim 1 , wherein Ror Ris any one of the following groups: a) a hydrogen; b) a substituted or unsubstituted C1-8 straight-chain or branched alkyl.6. The compound according to claim 1 , wherein claim 1 , Ris halo-ethyl claim 1 , dimethylamino-ethyl claim 1 , diethylamino-ethyl claim 1 , piperidyl-ethyl claim 1 , morpholinyl-ethyl claim 1 , pyrrolidinyl-ethyl claim 1 , imidazolyl-ethyl claim 1 , dimethylamino- ...

TARGETED NITROXIDE AGENTS

Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation. 45-. (canceled)6. The compound of claim 1 , in which R is Ac claim 1 , Boc claim 1 , Cbz claim 1 , or —P(O)-Ph.7. The compound of claim 1 , in which R claim 1 , R claim 1 , Rand Rare independently chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , 2-propyl claim 1 , butyl claim 1 , t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , benzyl claim 1 , hydroxybenzyl claim 1 , phenyl and hydroxyphenyl.8. The compound of claim 1 , wherein when X is —CH═CR— claim 1 , Ris hydrogen claim 1 , methyl or ethyl.912-. (canceled)13. The compound of in which R1 claim 1 , R2 and R3 independently are methyl claim 1 , ethyl claim 1 , propyl claim 1 , 2-propyl claim 1 , butyl claim 1 , t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , benzyl claim 1 , hydroxybenzyl claim 1 , phenyl and hydroxyphenyl.1421-. (canceled)27. A method of making a targeted antioxidant compound claim 1 , comprising:{'sub': 1', '1', '1', '6', '6', '5, 'a. reacting an aldehyde of structure R—C(O)— with (R)-2-methylpropane-2-sulfinamide to form an imine, in which Ris C-Cstraight or branched-chain alkyl, optionally including a phenyl (CH) group, that optionally is methyl-, hydroxyl- or fluoro-substituted;'}{'sub': 2', '2', '2, 'b. reacting a terminal alkyne-1-ol (HCC—R—CH—OH), in which Ris not present or is branched or straight-chained alkylene, with a tert-butyl)diphenylsilane salt to produce an alkyne;'}c. ...

CATIONIC LIPID

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 2. The cationic lipid according to claim 1 , wherein Xand Xare combined together to form a single bond or alkylene.3. The cationic lipid according to claim 1 , wherein Lis a single bond claim 1 , Ris a hydrogen atom claim 1 , methyl claim 1 , pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4-yl claim 1 , or alkyl having 1 to 6 carbon atoms or alkenyl having 3 to 6 carbon atoms substituted with 1 to 3 substituent(s) claim 1 , which is(are) claim 1 , the same or different claim 1 , amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , hydroxy claim 1 , alkoxy claim 1 , carbamoyl claim 1 , monoalkylcarbamoyl claim 1 , dialkylcarbamoyl claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , and Land Lare —O—.4. The cationic lipid according to claim 1 , wherein Lis —CO— or —CO—O— claim 1 , Ris pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4-yl claim 1 , or alkyl having 1 to 6 carbon atoms or alkenyl having 3 to 6 carbon atoms substituted with 1 to 3 substituent(s) claim 1 , which is(are) claim 1 , the same or different claim 1 , amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , hydroxy claim 1 , alkoxy claim 1 , carbamoyl claim 1 , monoalkylcarbamoyl claim 1 , dialkylcarbamoyl claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , wherein at least one of the substituents is amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , and Land Lare identically —CO—O— or —O—CO—.5. The cationic lipid according to any one of to claim 1 , wherein Xis absent claim 1 , or is methyl.64. The cationic lipid according to any one of to claims 1 , wherein Land Lare —O— or —O—CO— claims 1 , and Rand Rare (Z)-hexadec-6-enyl or (Z)-hexadec ...

PIPERIDINE DERIVATIVES

The present invention relates to a compound of formula I 2. A compound of claim 1 , wherein Ris lower alkyl.3. A compound of claim 2 , wherein the phenyl group for Ar is substituted by at least two CFgroups.4. A compound of claim 3 , selected from the group consisting ofrac-2-fluoro-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-2-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-2-ethyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide;rac-N-[3-(4-fluoro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-4,6-bis-trifluoromethyl-benzamide; and2-methoxy-N—((R)-1-methyl-3-phenyl-piperidin-3-yl)-4,6-bis-trifluoromethyl-benzamide.5. A compound of claim 1 , wherein the phenyl group for Ar is substituted by at least one CFgroup.6. A compound of claim 5 , selected from the group consisting ofrac-2-ethyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-2-bromo-6-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-N-(1,2-dimethyl-3-phenyl-piperidin-3-yl)-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-2-cyclopropyl-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide;rac-2-methoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-(1-methyl-3-phenyl-piperidin-3-yl)-2-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-[3-(4-fluoro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;rac-N-[3-(4-chloro-phenyl)-1-methyl-piperidin-3-yl]-2-methoxy-6-methylsulfanyl-4-trifluoromethyl-benzamide;2-methoxy-N-((S)-1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide;2-methoxy-N—((R)-1-methyl-3-phenyl-piperidin-3-yl)-6-methylsulfanyl-4-trifluoromethyl-benzamide; andrac-2-difluoromethoxy-N-(1-methyl-3-phenyl-piperidin-3-yl)-4-trifluoromethyl-benzamide.7. A compound of claim 5 , selected from the group consisting ofrac-N-[3-(3-chloro-phenyl)-1-methyl- ...

TRICYCLIC COMPOUNDS AND PBK INHIBITORS CONTAINING THE SAME

Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer. 3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris hydrogen claim 2 , cyano claim 2 , C-Calkyl optionally substituted with hydroxyl or halogen claim 2 , C-Ccycloalkyl claim 2 , C-Calkenyl claim 2 , C-Calkynyl claim 2 , or halogen.4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris hydrogen claim 2 , hydroxyl claim 2 , halogen claim 2 , C-Calkoxy claim 2 , or C-Caryl optionally substituted with hydroxyl.5. The compound of or a pharmaceutically acceptable salt claim 2 , wherein Ris hydrogen claim 2 , hydroxyl claim 2 , halogen claim 2 , C-Calkoxy claim 2 , or dihydroxyphenyl.6. The compound of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris selected from the group consisting of: hydrogen; hydroxyl; C-Calkyl optionally substituted with hydroxyl claim 2 , halogen claim 2 , or hydroxyethylamino; halogen; C-Calkoxy optionally substituted with dimethylamino or morpholinyl; C-Calkylphenyl claim 2 , wherein the aliphatic carbons are optionally substituted with —NRR; cyano; nitro; amino; 3- to 8-membered heterocycloalkyl optionally substituted with amino; heteroaryl; —OSOCH; —OSOCF; —OCOR claim 2 , wherein Rrepresents C-Calkyl; —OCOORwherein Rrepresents C-Calkyl; —OCONRRwherein Rand Reach independently represent hydrogen or C-Calkyl claim 2 , or Rand Rtaken together form morpholinyl; and —CONH.7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein when Ris a 3- to 8-membered heterocycloalkyl claim 6 , the 3- to 8-membered heterocycloalkyl is selected from the group consisting of piperidyl claim 6 , pyrrolidinyl claim 6 , morpholinyl claim 6 , or piperazinyl and optionally substituted with amino; and when Ris heteroaryl claim 6 , the heteroaryl is pyridyl.8. The compound of ...

CHIRAL AUXILIARIES

Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries. 2. The compound or a salt thereof according to claim 1 , wherein Rand Rare hydrogen atom or an alkyl group claim 1 , Ris phenyl group claim 1 , Rand Rare hydrogen atom or an alkyl group claim 1 , and Y is —C(R)(R)— (Rand Rare independently hydrogen atom or an alkyl group claim 1 , and when Rrepresents an alkyl group claim 1 , Rmay bind with the phenyl group represented by Rto form a ring) claim 1 , o-phenylene group claim 1 , or naphthalene-1 claim 1 ,2-diyl group.8. The method according to claim 7 , wherein 3% dichloroacetic acid (DCA) in dichloromethane is used for the acidic condition in the step (c).9. The method according to claim 7 , wherein claim 7 , as the modification of phosphorus atom claim 7 , a group represented by X (X represents an alkylthio group which may have a substituent claim 7 , an alkenylthio group which may have a substituent claim 7 , an alkynylthio group which may have a substituent claim 7 , an arylthio group which may have a substituent claim 7 , thiol group claim 7 , an alkoxy group which may have a substituent claim 7 , —BH claim 7 , —Se claim 7 , an alkyl group which may have a substituent claim 7 , an alkenyl group which may have a substituent claim 7 , an alkynyl group which may have a substituent claim 7 , an aryl group which may have a substituent claim 7 , an acyl group which may have a substituent claim 7 , or —N(R)(R) (Rand Rindependently represent hydrogen atom claim 7 , an alkyl group which may have a substituent claim 7 , an alkenyl group which may have a substituent claim 7 , an alkynyl group which may have a substituent claim 7 , or an aryl group which may have a substituent) is introduced on the phosphorus atom.11. The compound or a salt thereof according to ...

2-ALKOXY-11-HYDROXYAPORPHINE DERIVATIVES AND USES THEREOF

The invention features 2-alkoxy-11-hydroxyaporphine derivatives that selectively bind Dreceptors. The compounds are useful for imaging Dreceptors and for the treatment of diseases, such as Parkinson's disease, sexual dysfunction, and depressive disorders. 2. The compound of claim 1 , wherein Ris H claim 1 , CH claim 1 , CHCH claim 1 , CHCHCH claim 1 , CHCH═CH claim 1 , or cyclopropylmethyl.4. The compound of claim 1 , wherein Ris CH claim 1 , CHCH claim 1 , or CHCHCH; and Xis fluoromethyl claim 1 , difluoromethyl claim 1 , trifluoromethyl claim 1 , 2-fluoroethyl claim 1 , 1-fluoroethyl claim 1 , 1 claim 1 ,2-difluoroethyl claim 1 , 2 claim 1 ,2-difluoroethyl claim 1 , 2 claim 1 ,2 claim 1 ,2 claim 1 ,-trifluoroethyl claim 1 , 1 claim 1 ,2-difluoroethylene claim 1 , 2 claim 1 ,2-difluoroethylene claim 1 , pentafluoroethyl claim 1 , 3-fluoro-n-propyl claim 1 , 3 claim 1 ,3-difluoro-n-propyl claim 1 , 3 claim 1 ,3 claim 1 ,3-trifluoro-n-propyl claim 1 , 3 claim 1 ,3 claim 1 ,3 claim 1 ,2 claim 1 ,2-pentafluoro-n-propyl claim 1 , heptafluoro-n-propyl claim 1 , 3 claim 1 ,3 claim 1 ,3-trifluoro-1-propene claim 1 , 3 claim 1 ,3 claim 1 ,3-trifluoro-1-propyne claim 1 , iodomethyl claim 1 , iodoethyl claim 1 , or iodopropyl.5. The compound of claim 1 , wherein said Cfluoroalkyl comprises a radioactive fluorine atom.7. The compound of claim 6 , wherein Rt is H claim 6 , CH claim 6 , CHCH claim 6 , CHCHCH claim 6 , CHCH═CH claim 6 , or cyclopropylmethyl.8. The compound of claim 6 , wherein Zis a radioactive fluorine atom.9. The compound of claim 1 , wherein said compound is selected from R(−2-(trifluoromethoxy)-11-hydroxy-N-methyl-noraporphine claim 1 , R(−)-2-(fluoromethoxy)-11-hydroxy-N-methyl-noraporphine claim 1 , R(−)-2-(2-fluoroethoxy)-11-hydroxy-N-methyl-noraporphine claim 1 , R(−)-2-(3-fluoro-n-propanoxy)-11-hydroxy-N-methyl-noraporphirte claim 1 , R(−)-2-(trifluoromethoxy)-11-hydroxy-N-ethyl-noraporphirte claim 1 , R(−)-2-(fluoromethoxy)-11-hydroxy-N-ethyl- ...

INDENOPYRIDINE DERIVATIVES

Disclosed is a compound of formula (I) 2. The compound of formula (I) of in free-base form.3. The compound of formula (I) of in the form of a salt.4. The compound of formula (I) of claim 3 , wherein the salt is selected from chloride claim 3 , bromide claim 3 , iodide claim 3 , sulfonate claim 3 , triflate claim 3 , and methanesulfonate.5. The compound of formula (I) of in the form of a hydrogen chloride salt.7. The method of claim 7 , wherein the compound of formula (I) is in the form of a hydrogen chloride salt claim 7 , and the salt-forming acid is hydrochloric acid.9. The method claim 8 , wherein the compound of formula (I) is in the form of a hydrogen chloride salt claim 8 , and the salt-forming acid is hydrochloric acid. This application relates to indenopyridine derivatives. The indenopyridine derivatives of the invention are useful as intermediates for the preparation of pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridines are reportedly useful as inhibitors of 11-β-hydroxysteroid hydrogenase type 1 (“11-β-HSD1”) and for treatment of disorders associated with 11β-HSD1 activity including, for example, diabetes mellitus (e.g., type II diabetes), obesity, symptoms of metabolic syndrome, glucose intolerance, hyperglycemica (see, e.g., WO 2011/057054).The aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridines can be prepared, for example, from nitrile-substituted hexahydroindenopyridines as described in WO 2011/057054. In one method described in WO 2011/057054, the intermediate (4aR,9aS)-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine-6-carbonitrile (A) is allowed to react with 1H-benzoimidazole-5-carboxylic acid (B) followed by reaction with hydrogen chloride to provide the 11-β-HSD1 inhibitor (4a-R,9a-S)-1-(1H-benzoimidazole-5-carbonyl)-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine-6-carbonitrile (C) as depicted below:Methods ...

CARBOXAMIDE BIOISOSTERES OF OPIATES

A compound of formula I is disclosed. 111-. (canceled)13. A method according to wherein said disease or condition is chosen from the group consisting of pain claim 12 , pruritis claim 12 , diarrhea claim 12 , irritable bowel syndrome claim 12 , gastrointestinal motility disorder claim 12 , obesity claim 12 , respiratory depression claim 12 , convulsions claim 12 , coughing claim 12 , hyperalgesia claim 12 , inflammation claim 12 , osteoarthritis and drug addiction.14. A method according to wherein said drug addiction is selected from heroin claim 13 , cocaine claim 13 , nicotine claim 13 , amphetamine and alcohol addiction.15. A method according to claim 13 , wherein the condition is pain and the composition further comprises an effective amount of an opioid.16. A method according to claim 13 , wherein the condition is osteoarthritis and the composition further comprises an effective amount of an opioid.1732-. (canceled)33. A method according to claim 12 , wherein Rand Rare hydrogen.34. A method according to claim 12 , wherein Ris —OH claim 12 , —CHO claim 12 , —CONH claim 12 , —CON(H)CHCONH claim 12 , —CON(H)CHCHCONH claim 12 , —CON(H)CHCOOH claim 12 , or —CON(H)CHCHCOOH; or Rand Rtogether with the atoms to which they are attached forms a —OCHO— fused ring.35. A method according to claim 12 , wherein Ris H.39. A method according to wherein Ris in the para position relative to B and Ris hydrogen or methyl; or Rand Rtogether with the atoms to which they are attached claim 38 , and a fragment selected from —OCHO— or —OCHCHO— claim 38 , form a ring.44. A method according to wherein Ris in the para position relative to B and Ris hydrogen.45. A method according to claim 12 , wherein Aris phenyl and one of Ror Ris in the para position relative to B. This application is a divisional application of U.S. patent application Ser. No. 13/069,104, filed Mar. 22, 2011, now allowed. U.S. patent application Ser. No. 13/069,104 claims priority of U.S. provisional applications 61/316 ...

4-HYDROXYBENZOMORPHANS

4-Hydroxybenzomorphans containing carboxamide or thiocarboxamide at the 3-position are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. A compound of formula This application is a continuation application of U.S. application Ser. No. 11/760,039, filed Jun. 8, 2007, which was a divisional application of U.S. application Ser. No. 11/266,651, filed Nov. 3, 2005, and issued as U.S. Pat. No. 7,262,298 on Aug. 28, 2007. U.S. application Ser. No. 11/266,651 claims priority from U.S. Provisional Application 60/625,348 filed Nov. 5, 2004. The entire disclosures of each of the prior applications are hereby incorporated herein by reference.The invention relates to 4-hydroxybenzomorphans substituted at the 3-position with carboxamide or thiocarboxamide. The compounds are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives, anti-cocaine, and anti-addiction medications.Opiates have been the subject of intense research since the isolation of morphine in 1805, and thousands of compounds having opiate or opiate-like activity have been identified. Many opioid receptor-interactive compounds including those used for producing analgesia (e.g., morphine) and those used for treating drug addiction (e.g., naltrexone and cyclazocine) have been employed in human therapy. Almost all therapeutically useful opioids in the benzazocine and morphinane classes have a phenolic hydroxyl group (OH) at a position which is numbered “8” in the numbering system used for 2,6-methano-3-benzazocines [e.g., cyclazocine and EKC (ethylketocyclazocine)] and which is numbered “3” in the numbering system used for morphinanes (e.g., morphine).Although the compounds of the present invention do not possess the furan ring of the morphinans, the morphinan numbering system will be used:2,6-Methano-3-benzazocines are also known as benzomorphans, and this terminology will be used interchangeably herein.Until the publications of Wentland et al ...

Novel Antiviral Compounds

The present invention relates to compounds of formula (A), as further defined herein, having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. The invention further relates to the use of such compounds, optionally combined with one or more other drugs having antiviral activity, for the treatment of animals suffering from viral infections, in particular HIV infection. 13. A compound according to wherein Ris COOR claim 1 , wherein Ris selected from hydrogen and alkyl.14. A compound according to wherein Ris COOH.15. A compound according to wherein Ris selected from alkyl claim 1 , aryl; heterocycle or arylalkyl; wherein in the alkyl moiety of said arylalkyl one —CH— is optionally replaced by —NH— claim 1 , —O— claim 1 , or —S—; and wherein said aryl claim 1 , heterocycle claim 1 , or arylalkyl can be unsubstituted or substituted with one or more halogen claim 1 , OH or alkyl.16. A compound according to wherein Ris selected from C-Calkyl claim 1 , phenyl; phenylalkyl claim 1 , heteroaryl claim 1 , O-phenyl; S-phenyl or NH-phenyl and wherein said phenyl; phenylalkyl claim 1 , heteroaryl claim 1 , O-phenyl; S-phenyl or NH-phenyl can be unsubstituted or substituted with one or more halogen claim 1 , OH or C-Calkyl.17. A compound according to wherein one of Rand Ris hydrogen and the other one of Rand Ris selected from the group consisting of C-Calkyl and C-C-alkoxy claim 1 , said C-Calkyl and C-Calkoxy being optionally substituted with up to three F atoms.18. A compound according to wherein the dotted line “a” forms a double bond claim 1 , the dotted line “b” does not form a double bond claim 1 , Ris not present and Ris selected from hydrogen claim 1 , hydroxyl claim 1 , alkyl or aryl claim 1 , wherein said alkyl and aryl can be unsubstituted or substituted with one or more halogens.19. A ...

NITRIC OXIDE AND ITS BIOMEDICAL SIGNIFICANCE

A pharmaceutical composition for stimulating nitric oxide production in mammalian cells, the pharmaceutical composition including at least one compound selected from a group consisting of: 2,3-dihydroxypropyl oleate; bis(m-phenoxyphenyl) ether; 6-acetyl-5,6,6a,7-tetrahydro-4H-dibezo(de,g)quinoline; and (+)-N-(p-(2-methylbutoxy)benzylidene)-4-(2-methylbutyl)aniline. 1. A pharmaceutical composition for stimulating nitric oxide production in mammalian cells , the pharmaceutical composition comprising:at least one compound selected from a group consisting of: 2,3-dihydroxypropyl oleate; bis(m-phenoxyphenyl)ether; 6-acetyl-5,6,6a,7-tetrahydro-4H-dibezo(de,g)quinoline; and (+)-N-(p-(2-methylbutoxy)benzylidene)-4-(2-methylbutyl)aniline.2. The pharmaceutical composition of claim 1 , wherein the at least one compound includes 2 claim 1 ,3-dihydroxypropyl oleate.3. The pharmaceutical composition of claim 1 , wherein the at least one compound includes bis(m-phenoxyphenyl)ether.4. The pharmaceutical composition of claim 1 , wherein the at least one compound includes 6-acetyl-5 claim 1 ,6 claim 1 ,6a claim 1 ,7-tetrahydro-4H-dibezo(de claim 1 ,g)quinoline.5. The pharmaceutical composition of claim 1 , wherein the at least one compound includes (+)-N-(p-(2-methylbutoxy)benzylidene)-4-(2-methylbutyl)aniline.6Allium vineale, Salix alba, AgropyrumPetroselinium crispum, Taraxacum officinale, Sesamum indicum, MedicagoPiper methysticum, AnthemisTurnera diffusa, Verbascum densiflorum, OcimumMaranta arundinaceae, Coriandrum sativum, Artemesia dracunculus, Lavendula augustifolia, Mentha pulegium, Centella asiatica, Ginko bilobaVitis vinifera.. The pharmaceutical composition of claim 1 , wherein the at least one compound is derived/extracted from at least one plant species selected from the group consisting of spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , and7. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition has the ability to stimulate ...

PREMATURE-TERMINATION-CODONS READTHROUGH COMPOUNDS

Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided. 1. A system for high throughput assay for readthrough compound having the ability to read through premature termination codons (PTCs) in RNA , comprising high throughput reading trays and wells containing a plasmid ,wherein the plasmid comprises a fragment of ATM gene that contains a PTC mutation, which fragment being flanked by a sequence that initiates transcription of:a) a myc epitope,b) the ATM fragment, andc) a V5 epitope;wherein the assay is based on a coupled protein transcription/translation (PTT) reaction that is driven by the plasmid;wherein the reading trays are coated with an antibody to the myc epitope; andwherein an antibody to V5 is provided for attaching to readthrough proteins expressing the V5 epitope.2. The system of claim 1 , wherein the V5 epitope is conjugated to horseradish peroxidase.3. The system of claim 1 , further comprising a robot.4. A method of screening for readthrough compounds having the ability to read through premature termination codons (PTCs) in RNA claim 1 , comprising: a) a myc epitope,', 'b) the ATM fragment, and', 'c) a V5 epitope;, 'providing a plasmid template to a reaction well having a test compound to cause a coupled protein transcription/translation (PTT) reaction to occur to generate a PTT reaction product, the plasmid template comprising a fragment of ATM gene that contains a PTC mutation, which fragment being flanked by a sequence that initiates transcription ofadding the PTT reaction product to high throughput reading trays, which are coated with an antibody to the myc epitope to capture a protein fragment of the fragment of ATM gene,adding an antibody to the V5 epitope (V5 antibody) to wells in the reading trays,detecting the attachment of the V5 antibody to proteins in the PTT product, andidentifying the test compound as a readthrough compound if the attachment of the V5 antibody to ...

PHENYL-TETRAHYDROISOQUINOLINE DERIVATIVES

The invention provides novel compounds having the general formula (I) 3. A compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare independently selected from H claim 1 , halogen claim 1 , cyano claim 1 , alkyl and haloalkyl.4. A compound according to claim 1 , wherein Ris H or halogen.5. A compound according to claim 1 , wherein Ris H claim 1 , alkyl or halogen.6. A compound according to claim 1 , wherein Ris H or halogen.7. A compound according to claim 1 , wherein Ris halogen claim 1 , cyano or haloalkyl.8. A compound according to claim 1 , wherein Ris cyano or haloalkyl.9. A compound according to claim 1 , wherein Ris haloalkyl.10. A compound according to claim 1 , wherein Ris H or halogen.11. A compound according to claim 1 , wherein Ris H.12. A compound according to claim 1 , wherein Ris H.13. A compound according to claim 1 , wherein Ris H or aryl substituted with R claim 1 , Rand R.14. A compound according to claim 1 , wherein Ris H.15. A compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently selected from H and alkyl.16. A compound according to claim 1 , wherein Ris H or alkyl.17. A compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , Rand Rare H.18. A compound according to claim 1 , wherein A is —(CRR)—NRR.19. A compound according to claim 1 , wherein A is —(CRR) claim 1 , —OR.20. A compound according to claim 1 , wherein Ris H.21. A compound according to claim 1 , wherein Ris H claim 1 , alky claim 1 , —S(O)R claim 1 , —S(O)NRR claim 1 , —C(O)R claim 1 , —C(O)ORor —C(O)NRR.22. A compound according to claim 1 , wherein in case A is{'sup': 13', '14', '15', '16', '16', '17', '17', '18', '17', '17', '17', '18, 'sub': p', '2', '2, '—(CRR)—NRR, then Ris H, —S(O)R, —S(O)NRR, —C(O)R, —C(O)ORor —C(O)NRR.'}23. A compound according to claim 1 , wherein in case A is{'sup': 13', '14', '16', '16', '17', '18, 'sub': 'p', '—(CRR)—OR, then Ris H, alkyl or —C(O)NRR.'}24. A ...

Carbonyl propyl sulfuryl anthrapyridone sulfonic acid compounds and their preparation methods and applications

The present invention relates to compounds shown in the general formula (I) or (III), the salts thereof or their mixtures, as well as their preparation method and application. In the general formula (I), X 1 is H or CO 2 H; X 2 is OH or phenyl group with 0-2 sulfonic acid substituents, and the sulfonic acid substituents are located at random positions of a benzene ring; when X 2 is OH, X 1 is H; when X 2 is phenyl group with 0-2 sulfonic acid substituents, X 1 is H or CO 2 H; n is an integer of 0-2; and in the general formula (III), n and m are respectively an integer of 0-2. The compounds and the mixtures not only have improved light resistance, ozone resistance and water resistance, but also have excellent water solubility and long-term stability in ink-jet ink.

Modulators of Muscarinic Receptors

The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases. 171-. (canceled)73. The method according to claim 72 , wherein G is an optionally substituted bicyclic group of formula (III) in which ring B is absent.74. The method according to claim 73 , wherein Xis —(CH)—.75. The method according to claim 74 , wherein G is optionally substituted bicyclo[2.2.1]heptyl claim 74 , bicyclo[3.2.1]octyl claim 74 , bicyclo[3.3.1]nonyl claim 74 , bicyclo[2.2.2]octyl claim 74 , or bicyclo[2.2.1]heptanyl.76. The method according to claim 75 , wherein G is substituted with 1 to 2 substituents independently selected from Q claim 75 , and —C(O)—X-aliphatic claim 75 , where Xis absent claim 75 , —O— claim 75 , —NH— claim 75 , or —NQ- claim 75 , and the aliphatic group is optionally substituted with 1-3 substituents independently selected from Q.77. The method according to claim 73 , wherein Xis —N(Q)— or —N(C(O)—X-aliphatic) claim 73 , where Xis absent claim 73 , —O— claim 73 , —NH— claim 73 , or —NQ- claim 73 , and the aliphatic group is optionally substituted with 1-3 substituents independently selected from Q.78. The method according to claim 77 , wherein G is an optionally substituted tropane.79. The method according to claim 78 , wherein the tropane is substituted with Q claim 78 , or —C(O)—X-aliphatic claim 78 , where Xis absent claim 78 , —O— claim 78 , —NH— claim 78 , or —NQ- claim 78 , and the aliphatic group is optionally substituted with 1-3 substituents independently selected from Q.80. The method according to claim 78 , wherein the tropane is substituted at the tropane ring nitrogen atom with alkoxycarbonyl claim 78 , alkoxyalkoxycarbonyl claim 78 , heterocycloalkoxy carbonyl claim 78 , cycloalkoxycarbonyl claim 78 , alkoxyaryloxycarbonyl claim 78 , alkylaminocarbonyl claim 78 , haloalkoxy carbonyl claim 78 , ...

PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF

The present invention provides a compound of formula I: 118-. (canceled)20. The composition of claim 19 , wherein X is selected from the group consisting of the anion of a suitable BrØnsted acid claim 19 , a hydrogen halide claim 19 , a carboxylic acid claim 19 , a sulfonic acid claim 19 , a sulfuric acid claim 19 , a phosphoric acid claim 19 , chloride claim 19 , bromide claim 19 , iodide claim 19 , fluoride claim 19 , bisulfate claim 19 , tartrate claim 19 , nitrate claim 19 , citrate claim 19 , bitartrate claim 19 , carbonate claim 19 , phosphate claim 19 , malate claim 19 , maleate claim 19 , fumarate sulfonate claim 19 , methylsulfonate claim 19 , formate claim 19 , carboxylate claim 19 , sulfate claim 19 , methylsulfate and succinate.21. The composition of claim 19 , wherein Ris Caliphatic and Ris lower alkyl;{'sup': '1', 'optionally wherein Ris a (cycloalkyl)alkyl group or alkenyl group, or'}{'sup': 1', '2, 'optionally wherein Ris cyclopropyl methyl or allyl and Ris methyl.'}24. The composition of claim 23 , wherein X is selected from the group consisting of the anion of a suitable BrØnsted acid claim 23 , a hydrogen halide claim 23 , a carboxylic acid claim 23 , a sulfonic acid claim 23 , a sulfuric acid claim 23 , a phosphoric acid claim 23 , chloride claim 23 , bromide claim 23 , iodide claim 23 , fluoride claim 23 , bisulfate claim 23 , tartrate claim 23 , nitrate claim 23 , citrate claim 23 , bitartrate claim 23 , carbonate claim 23 , phosphate claim 23 , malate claim 23 , maleate claim 23 , fumarate sulfonate claim 23 , methylsulfonate claim 23 , formate claim 23 , carboxylate claim 23 , sulfate claim 23 , methylsulfate and succinate.25. The composition of claim 23 , wherein Ris Caliphatic and Ris lower alkyl;{'sup': '1', 'optionally wherein Ris a (cycloalkyl)alkyl group or alkenyl group, or'}{'sup': 1', '2, 'optionally wherein Ris cyclopropyl methyl or allyl and Ris methyl.'}28. The compound of claim 27 , wherein X is selected from the group consisting ...

QUINOLINE DERIVATIVE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention relates to a novel quinoline derivative compound, an optical isomer thereof, a pharmaceutically acceptable salt thereof, and a hydrate or a solvate thereof. The novel quinoline derivative compound, the optical isomer thereof, the pharmaceutically acceptable salt thereof, and the hydrate or the solvate thereof accelerates gastrointestinal movement, and thus can effectively prevent or treat gastrointestinal motility disorders.

Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions

Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

TETRAHYDROISOQUINOLINE DERIVATIVE

To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HTreceptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HTreceptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed. 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '1', '2', '3', '4, 'wherein Rrepresents phenyl, pyridyl, or cycloalkyl which may be respectively substituted with group(s) selected from G, Rrepresents halogen, m represent 1, n represents 1, and both Rand Rrepresent H.'}3. The compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '2', '3', '4, 'wherein Rrepresents phenyl which may be substituted with halogen or —O-(lower alkyl), Rrepresents H, F, Cl, or methyl, m represents 1, n represents 1, and both Rand Rrepresent H.'}4. The compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '2', '3', '4, 'wherein Rrepresents pyridyl which may be substituted with halogen or —O-(lower alkyl), Rrepresents H, F, Cl, or methyl, m represents 1, n represents 1, and both Rand Rrepresent H.'}5. The compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '2', '3', '4, 'wherein Rrepresents phenyl which may be substituted with halogen or —O-(lower alkyl), Rrepresents H, F, Cl, or methyl, m represents 1, n represents 1, and Rand Rform cyclopropane-1,1-diyl or cyclobutane-1,1-diyl together with the carbon atom binding thereto, as ethylene or trimethylene.'}6. A compound selected ...

CROSS-LINKED CYCLIC AMINE COMPOUNDS AND AGENTS FOR PEST CONTROL

Cyclic amine compounds represented by formula (1) 116-. (canceled)19. Cyclic amine compounds according to claim 17 , wherein Cyrepresents a pyridazyl group substituted by halogen claim 17 , nitro claim 17 , or haloalkyl.20. Agents for pest control comprising at least one of the cyclic amine compounds of . The present invention relates to novel cyclic amine compounds and agents for pest control which contain these cyclic amine compounds or the like as active ingredients.Priority is claimed on Japanese Patent Application No. 2005-294126, filed Oct. 6, 2005, Japanese Patent Application No. 2005-294127, filed Oct. 6, 2005, Japanese Patent Application No. 2005-297803, filed Oct. 12, 2005, Japanese Patent Application No. 2005-297804, filed Oct. 12, 2005, Japanese Patent Application No. 2006-016877, filed Jan. 25, 2006, and Japanese Patent Application No. 2006-182314, filed Jun. 30, 2006, the contents of which are incorporated herein by reference.Although many compounds which have insecticidal/acaricidal activities are conventionally known, there are problems such as insufficient effect thereof, limitation of use thereof because of drug resistance problems, occurrence of phytotoxicity or contamination in plant bodies, or strong toxicity against mammalians, fish, or the like.As compounds with backbones similar to those of the compounds of the present invention, compounds represented by the formula below are known.In the formula, X represents —O—, —N(R)—, —S—, or the like and Rrepresents a substituted saturated heterocyclic group or the like. As a representative of such compounds, the compound represented by the formula below is known (refer to Patent document 1).Moreover, the compounds represented by the formula below are known.In the formula, X represents —CH— or the like; Z represents a bonding or the like; Rrepresents an optionally substituted aryl or an optionally substituted heteroaryl; and Rand Rrepresent —(CH)— or the like together. However, when Rand Rrepresent —(CH ...

NOVEL MORPHINANS USEFUL AS ANALGESICS

Compounds of Formula (I) are disclosed. 2. A compound or salt of claim 1 , wherein{'sub': 1', '2', '3', '4', '5', '6', '6a', '7', '8', '9', '11, 'R, R, R, R, R, R, R, R, R, R, and Rare independently selected from'}(i) hydrogen, hydroxyl, cyano, and halogen; and{'sub': 11', '12', '2', '11', '12', '11', '12', '11', '12', '1', '6, '(ii) hydrocarbyl and heteroatom-containing hydrocarbyl, each of which (ii) is unsubstituted or substituted with one or more substituents independently chosen from hydroxyl, amino, cyano, halogen, oxo, —COOH, —CONRR, —SONRR, and —NRCOR, where Rand Rare independently hydrogen and C-Calkyl; and'}{'sub': 10', '10', '11', '12', '2', '11', '12', '11', '12', '11', '12', '1', '6, 'Ris hydrocarbyl or carbon-linked, heteroatom-containing hydrocarbyl, which Ris unsubstituted or substituted with one or more substituents independently chosen from hydroxyl, amino, cyano, halogen, oxo, —COOH, —CONRR, —SONRR, and —NRCOR, where Rand Rare independently chosen from hydrogen and C-Calkyl.'}7. A compound or salt of claim 1 , where{'sub': 1', '2', '4', '5', '6', '6a', '7', '8', '9', '11, 'R, R, R, R, R, R, R, R, R, and Rare independently selected from'}(i) hydrogen, hydroxyl, cyano, and halogen; and{'sub': 1', '8', '2', '8', '3', '7', '0', '4', '11', '12', '2', '11', '12', '11', '12', '11', '12', '1', '6, '(ii) C-Calkyl, C-Calkenyl, and (C-Ccycloalkyl)C-Calkyl, each containing zero or one or two heteroatoms independently chosen from N, O, and S, each of which (ii) is unsubstituted or substituted with one or more substituents independently chosen from hydroxyl, amino, cyano, halogen, oxo, —COOH, —CONRR, —SONRR, and —NRCOR, where Rand Rare independently chosen from hydrogen and C-Calkyl;'}{'sub': '3', 'Ris'}(i) hydroxyl, halogen, or{'sub': 1', '8', '2', '8', '3', '7', '0', '4', '11', '12', '2', '11', '12', '11', '12', '11', '12', '1', '6, '(ii) C-Calkoxy, C-Calkenyloxy, and (C-Ccycloalkyl)C-Calkoxy, each containing zero or one or two heteroatoms independently ...

LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF

8-Substituted-2,6-methano-3-benzazocines of general structure This application is a divisional of allowed U.S. application Ser. No. 13/215,392, filed Aug. 23, 2011; which is a continuation of U.S. application Ser. No. 12/477,223, filed Jun. 3, 2009, and issued as 8,026,252 on Sep. 27, 2011; which is a continuation of U.S. application Ser. No. 11/459,203, filed Jul. 21, 2006, and issued as 7,557,119 on Jul. 7, 2009; and claims priority of U.S. provisional application 60/701,407, filed Jul. 21, 2005. The entire disclosures of each of the prior applications are hereby incorporated herein by reference.The following invention was made with Government support under contract number 5 R01 DA12180 awarded by U.S. Dept of Health and Human Services. The Government has certain rights in this invention.The invention relates to opioid receptor binding compounds containing carboxamides that have large substitutents on the nitrogen of the carboxamide. The compounds are useful as analgesics, anti-diarrheal agents, anticonvulsants, anti-obesity agents, antitussives, anti-cocaine, and anti-addiction medications.Opiates have been the subject of intense research since the isolation of morphine in 1805, and thousands of compounds having opiate or opiate-like activity have been identified. Many opioid receptor-interactive compounds including those used for producing analgesia (e.g., morphine) and those used for treating drug addiction (e.g., naltrexone and cyclazocine) in humans have limited utility due to poor oral bioavailability and a very rapid clearance rate from the body. This has been shown in many instances to be due to the presence of the 8-hydroxyl group (OH) of 2,6-methano-3-benzazocines, also known as benzomorphans [(e.g., cyclazocine and EKC (ethylketocyclazocine)] and the corresponding 3-OH group in morphinanes (e.g., morphine).The high polarity of these hydroxyl groups retards oral absorption of the parent molecules. Furthermore, the 8-(or 3-)OH group is prone to ...

Synthesis and use of dual tyrosyl-dna phosphodiesterase i (tdp1)- topoisomerase i (top1) inhibitors

The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds.

Papaver bracteatum with modified alkaloid content

The present invention relates to genetically modified plants of the species Papaver bracteatum wherein the type or amount of one or more alkaloids produced by the plants has been modified. Specifically, the genetically modified plants have an increased expression of one or more of thebaine 6-O-demethylase, codeine O-demethylase and/or codeinone reductase relative to wild type P. bracteatum such that the genetically modified poppy plants produce an increased quantity of an alkaloid selected from codeine, oripavine and/or morphine relative to a wild type P. bracteatum . Also provided are progeny plants having the genetically modified poppy plants described above as a parent; mutant or derivative plants of the aforementioned plants; reproductive material derived from, straw produced from, straw concentrate produced from, latex derived from, or one or more isolated cells derived from, the aforementioned plants. Methods for producing an alkaloid from the aforementioned plants are also provided, together with nucleic acid and amino acid sequence variants of the 6-O-demethylase and codeine O-demethylase genes.

Patch preparation

A patch preparation containing a support and an adhesive layer formed on one surface of the support, wherein the adhesive layer contains 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine or a physiologically acceptable acid addition salt thereof, an acrylic polymer, lactic acid, sesame oil and one or more kinds of stabilizers selected from 2-mercaptobenzimidazole, 2,6-di-tert-butyl-4-methylphenol and propyl gallate. A patch preparation containing a support and an adhesive layer containing lactic acid and magnesium aluminometasilicate and formed on at least one surface of the support, which preparation is superior in both skin permeability and adhesiveness in the presence of water.

INSECTICIDAL SPIRONINDANE DERIVATIVES

An insecticidal compound of formula I 2. A compound according to claim 1 , wherein X is NH and Y is a single bond or C═O.3. A compound according to claim 1 , wherein each Ra is hydrogen and Rand Rare each independently hydrogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy or cyano.4. A compound according to claim 1 , wherein{'sup': 1', '13', '14, 'sub': 1-6', '1-6', '1-6', '3-7', '1-4', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-4', '1-4', '1-4', '1-4', '2', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '2-6', '2-6', '3-6', '5-7', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6, 'Ris hydrogen; Calkyl; Ccyanoalkyl; Chaloalkyl; Ccycloalkyl(C)alkyl; Calkoxy(C)alkyl; heteroaryl(C)alkyl wherein the heteroaryl group may be optionally substituted by halo, nitro, cyano, Calkyl, Chaloalkyl, Calkoxy, Chaloalkoxy, Calkylsulfonyl, Calkylsulfinyl, Calkylthio, Calkoxycarbonyl, Calkylcarbonylamino, or arylcarbonyl, or two adjacent positions on the heteroaryl ring may be cyclised to form a 5, 6 or 7 membered carbocyclic or heterocyclic ring, itself optionally substituted with halogen; aryl(C)alkyl wherein the aryl group may be optionally substituted by halo, nitro, cyano, Calkyl, Chaloalkyl, Calkoxy, Chaloalkoxy, Calkylsulfonyl, Calkylsulfinyl, Calkylthio, Calkoxycarbonyl, Calkylcarbonylamino, or arylcarbonyl, or two adjacent positions on the aryl ring may be cyclised to form a 5, 6 or 7 membered carbocyclic or heterocyclic ring, itself optionally substituted with halogen; Calkylcarbonylamino(C)alkyl; aryl which may be optionally substituted by halo, nitro, cyano, Calkyl, Chaloalkyl, Calkoxy, Chaloalkoxy, Calkylsulfonyl, Calkylsulfinyl, Calkylthio, Calkoxycarbonyl, Calkylcarbonylamino, or arylcarbonyl, or ...

Boron containing perylene monoimides, a process for their production, their use as building blocks for the production of perylene monoimide derivatives, monoimide derivatives and their use in dye-sensitized solar cells

Boron-comprising perylene monoimides and a process for producing the boron-comprising perylene monoimides are provided. The boron-comprising perylene monoimides are useful as building blocks for producing perylene monoimide derivatives and monoimide derivatives. The boron-comprising perylene monoimides are also useful for preparing dye-sensitized solar cells.

ANTIDIABETIC TRICYCLIC COMPOUNDS

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. 2. The compound according to wherein n is 1; or a pharmaceutically acceptable salt thereof.3. The compound according to wherein X is oxygen; or a pharmaceutically acceptable salt thereof.4. The compound according to wherein T is CH claim 3 , U is N or N-oxide claim 3 , and V is CH; or a pharmaceutically acceptable salt thereof.5. The compound according to wherein T is CH claim 3 , U is N claim 3 , and V is CH; or a pharmaceutically acceptable salt thereof.6. The compound according to wherein A is selected from the group consisting of: phenyl and pyridine claim 5 , wherein A is unsubstituted or substituted with one to five substituents selected from R; or a pharmaceutically acceptable salt thereof.7. The compound according to wherein A is phenyl claim 5 , wherein phenyl is unsubstituted or substituted with one to five substituents selected from R; or a pharmaceutically acceptable salt thereof.8. The compound according to wherein B is selected from the group consisting of: aryl and heteroaryl claim 7 , wherein B is unsubstituted or substituted with one to five substituents selected from R; or a pharmaceutically acceptable salt thereof.9. The compound according to wherein B is selected from the group consisting of: phenyl claim 7 , pyridine claim 7 , pyrimidine claim 7 , thiazole claim 7 , benzimidazole claim 7 , benzthiazole claim 7 , benzoxazole claim 7 , and benzisoxazole claim 7 , wherein B is ...

Fused and Spirocycle Compounds and the Use Thereof

The invention relates to fused and spirocycle compounds of Formula (I), or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R, R, Q-Q, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain. 2. (canceled)4. The compound of claim 3 ,{'sup': 1', '2', '3', '4', '5, 'wherein Z is Z, Z, Z, Zor Z.'}5. The compound of claim 3 ,{'sup': '26', 'wherein Rare both hydrogen.'}6. The compound of claim 3 , wherein Ris hydrogen or unsubstituted benzyl.7. The compound of claim 1 , wherein{'sup': 3', '4', '1, 'a) Rand Rtogether form ═O and Z is Z; or'}{'sup': 3', '4', '2, 'b) Rand Rare both hydrogen, Z is Zand n is 0.'}9. The compound of claim 4 , wherein{'sup': 1', '5', '6', '7', '8, 'a) Z is Zand R, R, Rand Rare each independently selected from the group consisting of hydrogen, alkyl, alkoxy, halogen, haloalkyl, hydroxy, cyano, amino, alkylamino, and dialkylamino; or'}{'sup': '2', 'claim-text': [{'sup': '9', 'i. Ris phenyl optionally substituted with one or two substituents independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, cyano, amino, aminoalkyl, alkylamino, and dialkylamino; or'}, {'sup': '9', 'ii. Ris pyridyl optionally substituted with one or two substituents independently selected from the group consisting of alkyl, haloalkyl, halogen, haloalkoxy, and alkoxy; or'}], 'b) Z is Zand'}{'sup': '3', 'claim-text': [{'sup': '10', 'i. Ris phenyl optionally substituted with one or two substituents independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, amino, alkylamino, dialkylamino, and alkylcarbonylamino; or'}, {'sup': '10', 'ii. Ris 1,2,3,4-tetrahydroquinolinyl or 1,2,3,4- ...

LPA2 Receptor-Specific Benzoic Acid Derivatives

Disclosed are compounds effective for inhibiting cellular apoptosis and for protecting cells and tissues from the apoptotic effects of chemotherapeutic agents and/or ionizing radiation. Compounds of the invention act as agonists of the LPAreceptor. Compounds of the invention comprise non-lipid benzoic acid derivatives. This application claims the benefit of priority of U.S. Provisional Patent Application No. 61/693,731, filed Aug. 27, 2012, the contents of which are incorporated herein by reference.The invention relates to compositions comprising new benzoic acid derivatives. More specifically, the invention relates to compounds comprising new sulfamoyl benzoic acid derivatives, these compounds acting as LPAreceptor agonists.The growth factor-like lysophospholipids lysophosphatidic acid (LPA) and sphingosine-1-phosphate (S1P) regulate many fundamental cellular responses, including cell survival, cell proliferation, cellular motility and migration. LPA has been shown to have profound activity in preventing apoptosis and rescuing cells from the progression of the apoptotic cascade. An LPA mimic, octadecenyl thiophosphate (OTP) (Durgam et al., Synthesis and pharmacological evaluation of second-generation phosphatidic acid derivatives as lysophosphatidic acid receptor ligands. (2006) 16(3): 633-640), has demonstrated superior efficacy in vitro and in vivo, as compared to LPA, in rescuing cells and animals from radiation-induced apoptosis (Deng et al., The lysophosphatidic acid type 2 receptor is required for protection against radiation-induced intestinal injury. (2007) 132(5): 1834-1851).The G protein-coupled lysophosphatidic acid 2 (LPA) receptor elicits prosurvival responses to prevent and rescue cells from apoptosis. LPAstimulation provides protection from chemotherapeutic agent-induced apoptosis and radiation-induced apoptosis. Highly effective LPA-specific agonists may therefore have significant therapeutic value.Development of LPA-based drug candidates has thus ...

Azide Substituted Naphthylene or Rylene Imide Derivatives and their Use as Reagents in Click-Reactions

Novel mono-azide substituted rylene-imide derivatives, their use in methods for the detection of analytes and reagents kits for the detection of analytes comprising said novel mono-azide substituted rylene-imide derivatives. 6. A reagent kit for detecting an analyte in a sample , comprising:(a) a functionalized compound comprising at least one functional group which is a first reaction partner for a click reaction,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) a second reaction partner for a click reaction, wherein the second reaction partner further comprises a marker group said second reaction partner being selected from the mono-azide substituted naphthylene or rylene-imide derivative in accordance with .'}7. A method for detecting an analyte comprising the steps of(i) providing a sample;(ii) contacting the sample with a functionalized compound comprising at least one functional group which is a first reaction partner for a click reaction under conditions wherein said compound forms an association product with the analyte to be detected,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(iii) contacting the association product with a second reaction partner for a click reaction under conditions wherein a click reaction between the first and second reaction partner occurs, wherein the second reaction partner is a monoazide substituted naphthylene or rylene-imide derivative in accordance with , and'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(iv) detecting the marker groups in the compounds in the mono-azide substituted naphthylene or rylene-imide derivative in accordance with .'} This application is a divisional of application Ser. No. 13/006,572, filed on Jan. 14, 2011, which is incorporated by reference herein in its entirety. Application Ser. No. 13/006,572 is a continuation-in-part of application Ser. No. 12/180,071 filed on Jul. 25, 2008 which is incorporated by reference in its entirety.The present invention relates to new mono-azide ...

Spirocyclic nitriles as protease inhibitors

The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments. 2. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or a physiologically tolerated salt thereof and a pharmaceutically acceptable carrier.4. The method of claim 3 , wherein the condition or disorder is osteoarthritis.5. The method of claim 3 , wherein the condition or disorder is bone loss. This application is a continuation of U.S. application Ser. No. 13/248,366, filed Sep. 29, 2011, which is a divisional of U.S. application Ser. No. 12/277,880, filed Nov. 25, 2008, which is a continuation of International Application No. PCT/EP2007/004550, filed May 23, 2007, which are incorporated herein by reference in their entirety; and claims the benefit of priority of German Patent Application No. 102006025630.1, filed Jun. 1, 2006.The invention relates to substituted carbo- and heterocyclic spiro compounds of the formula Ia which inhibit thiol proteases, to processes for their preparation and to the use thereof as medicaments.Proteolytic enzymes, known as proteases and peptidases, are very important enzymes which make up about 2% of the genes in the human organism, pathogenic microorganisms and also other life forms. Their particular significance is that they influence many physiological processes by playing an important role in the activation, synthesis or degradation of other proteins. This inevitably gives rise to a crucial regulatory function starting at conception, birth, growth, maturation, aging, diseases up to death.The balance of the different processes is of crucial significance for the life and survival of the organism. When there is an imbalance of protease-catalyzed processes as a result of endogenous or exogenous factors such as genetic predisposition or environmental factors, massive disruption can occur in the normal ...

Azide Substituted Naphthylene or Rylene Imide Derivatives and their Use as Reagents in Click-Reactions

Novel mono-azide substituted rylene-imide derivatives, their use in methods for the detection of analytes and reagents kits for the detection of analytes comprising said novel mono-azide substituted rylene-imide derivatives. 6. A reagent kit for detecting an analyte in a sample , comprising:(a) a functionalized compound comprising at least one functional group which is a first reaction partner for a click reaction,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) a second reaction partner for a click reaction, wherein the second reaction partner further comprises a marker group said second reaction partner being selected from the mono-azide substituted naphthylene or rylene-imide derivative in accordance with .'}7. A method for detecting an analyte comprising the steps of(i) providing a sample;(ii) contacting the sample with a functionalized compound comprising at least one functional group which is a first reaction partner for a click reaction under conditions wherein said compound forms an association product with the analyte to be detected,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(iii) contacting the association product with a second reaction partner for a click reaction under conditions wherein a click reaction between the first and second reaction partner occurs, wherein the second reaction partner is a mono-azide substituted naphthylene or rylene-imide derivative in accordance with , and'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(iv) detecting the marker groups in the compounds in the mono-azide substituted naphthylene or rylene-imide derivative in accordance with .'} This application is a divisional of application Ser. No. 13/006,572, filed on Jan. 14, 2011, which is incorporated by reference herein in its entirety. Application Ser. No. 13/006,572 is a continuation-in-part of application Ser. No. 12/180,071 filed on Jul. 25, 2008 which is incorporated by reference in its entirety.The present invention relates to new mono-azide ...

Anti-fibrotic pyridinones

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

FACTOR XIa INHIBITORS

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. 3. The compound of wherein Ris phenyl claim 1 , which optionally is substituted with two or three substituents independently selected from the group consisting of halo and heteroaryl; or a pharmaceutically acceptable salt thereof.4. The compound of wherein Ris phenyl claim 1 , which optionally is substituted with halo and tetrazolyl; or a pharmaceutically acceptable salt thereof.5. The compound of where in Ris phenyl claim 1 , which optionally is substituted with three halo; or a pharmaceutically acceptable salt thereof.6. The compound of wherein Ris hydroxy; or a pharmaceutically acceptable salt thereof.7. The compound of wherein Ris phenyl claim 1 , which is optionally substituted with one to three substituents independently selected from the group consisting of (C═O)ORand NH(C═O)R; or a pharmaceutically acceptable salt thereof.8. The compound of wherein Ris phenyl claim 1 , which is substituted with (C═O)OR; or a pharmaceutically acceptable salt thereof.10. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.11. A method for inhibiting thrombus formation in blood or treating thrombus formation in blood comprising administering a composition of to a mammal in need of thereof.12. A method for preventing thrombus formation in blood comprising administering a composition of to a mammal in need thereof.13. A method of treating venous thromboembolism and pulmonary embolism in a mammal comprising administering a composition of to a mammal in need thereof.14. A method of treating deep vein thrombosis in a mammal comprising ...

MATERIALS FOR ELECTRONIC DEVICES

The present invention relates to compounds according to formula (I), which are suitable for use in electronic devices, preferably organic electroluminescent devices. 118-. (canceled)20. The compound of claim 19 , wherein the compound of formula claim 19 , (1) contains exactly one Y wherein a group of formula (N) is bonded thereto instead of R.21. The compound of claim 19 , wherein in the group of formula (N) claim 19 , Aris the same or different in each instance and is selected from the group consisting of phenyl claim 19 , naphthyl claim 19 , phenanthrenyl claim 19 , biphenyl claim 19 , terphenyl claim 19 , quaterphenyl claim 19 , fluorenyl claim 19 , indenofluorenyl claim 19 , carbazolyl claim 19 , dibenzothiophenyl claim 19 , dibenzofusanyl claim 19 , benzofuranyl claim 19 , benzothiophenyl claim 19 , indolyl claim 19 , triazinyl claim 19 , pyrimidinyl claim 19 , pyridyl claim 19 , and pyridazinyl claim 19 , each of which is optionally substituted by one or more radicals R.22. The compound of claim 19 , wherein Aris the same in each instance.25. The compound of claim 19 , wherein all Y are CR.26. The compound of claim 19 , wherein X is C(R).27. The compound of claim 19 , wherein the radicals Rof X are the same or different in each instance and are selected from the group consisting of straight-chain alkyl groups having 1 to 12 carbon atoms claim 19 , branched or cyclic alkyl groups having 3 to 12 carbon atoms claim 19 , and aromatic ring systems having 6 to 20 aromatic ring atoms; wherein the alkyl groups and aromatic ring systems are each optionally substituted by one of more radicals R.28. The compound of claim 19 , Therein the radicals Rin Y are the same or different each instance and are selected from the group consisting of H claim 19 , D claim 19 , F claim 19 , CN claim 19 , straight-chain alkyl groups having 1 to 20 carbon atoms claim 19 , branched or cyclic alkyl groups having 3 to 20 carbon atoms claim 19 , aromatic ring systems having 6 to 40 aromatic ...

SULFONIC ACID DERIVATIVE COMPOUNDS AS PHOTOACID GENERATORS IN RESIST APPLICATIONS

Novel photoacid generator compounds are provided. Photoresist compositions that include the novel photoacid generator compounds are also provided. The invention further provides methods of making and using the photoacid generator compounds and photoresist compositions disclosed herein. The compounds and compositions are useful as photoactive components in chemically amplified resist compositions for various microfabrication applications. 2. A photoresist composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) at least one sulfonic acid derivative compound according to ;'}(ii) at least one polymer or copolymer which is capable of being imparted with an altered solubility in an aqueous solution in the presence of an acid;(iii) an organic solvent; and, optionally,(iv) an additive.3. The composition according to claim 2 , wherein the organic solvent is propylene glycol monomethyl ether acetate (PGMEA).4. The composition according to comprising:0.05 to 15 wt. % of the sulfonic acid derivative compound;5 to 50 wt. % of the at least one polymer or copolymer;0 to 10 wt. % of the additive; andreminder is propylene glycol monomethyl ether acetate.5. A process of producing a patterned structure on the surface of a substrate claim 3 , the process comprising the steps of{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, '(a) applying a layer of the composition according to onto the surface of the substrate and at least partial removal of the organic solvent (iv);'}(b) exposing the layer to electromagnetic radiation, thereby releasing an acid from the sulfonic acid derivative compound (i) in the areas exposed to the electromagnetic radiation;(c) optionally heating the layer to impart compound (ii) in the areas in which the acid has been released with an increased solubility in an aqueous solution; and(d) at least partial removal of the layer with an aqueous solution in these areas.6. The composition according to wherein claim 2 , during the exposure step ...

N AND P ACTIVE MATERIALS FOR ORGANIC PHOTOELECTRIC CONVERSION LAYERS IN ORGANIC PHOTODIODES

The field of the DISCLOSURE lies in active materials for organic image sensors. The present disclosure relates to transparent N materials and/or to transparent P materials and their use in absorption layer(s), photoelectric conversion layer(s) and/or an organic image sensor and methods for their synthesis. The present disclosure also relates to photoelectric conversion layer(s) including an active material according to the present disclosure, to a device, including active material(s) according to the present disclosure or photoelectric conversion layer(s) according to the present disclosure. Moreover, the present disclosure relates to an organic image sensor including photoelectric conversion layer(s) according to the present disclosure. 2. The organic image sensor according to claim 1 , wherein the naphthalene dimide based material dissociates excitons created on colored N or a mixture of colored N materials (N1:N2) or of another colored P or mixture of colored P and N materials (P2:N or P2:N1:N2) via a process of HOMO dissociation in a P:N heterojunction or P:N bilayer or multilayer junction claim 1 , where transparent refers to an absorption coefficient of less than about 60 claim 1 ,000 cmin the visible wavelength range in the region from about 400 to about 700 nm claim 1 , or to an extinction coefficient of less than about 60 claim 1 ,000 Mcmin toluene claim 1 , and colored refers to an absorption coefficient of more than about 60 claim 1 ,000 cmin the visible wavelength range in the region from about 400 nm to about 700 nm.3. The organic image sensor according to claim 1 , wherein the naphthalene dimide based material has an absorption coefficient of less than about 60 claim 1 ,000 cmin the visible wavelength range in the region from about 400 to about 700 nm claim 1 , or an extinction coefficient of less than about 60 claim 1 ,000 Mcmin toluene claim 1 , and is forming homogenous films formed by a deposition method.5. The organic image sensor according to ...

GLUCOCEREBROSIDASE MODULATORS AND USES THEREOF

The invention provides compounds for modulating glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. 2. The method of wherein the compound is one or more of the compounds described in Table 1.4. The method of wherein the condition is Parkinson's disease claim 3 , Dementia with Lewy bodies claim 3 , Multiple system atrophy claim 3 , Pick's disease claim 3 , Corticobasal degeneration claim 3 , Alzheimer's disease claim 3 , Amyotrophic lateral sclerosis claim 3 , Amyotrophic lateral sclerosis with cognitive impairment claim 3 , Argyrophilic grain dementia claim 3 , Bluit disease claim 3 , Dementia pugilistica claim 3 , Diffuse neurofibrillary tangles with calcification claim 3 , Down's syndrome claim 3 , Familial British dementia claim 3 , Familial Danish dementia claim 3 , Frontotemporal dementia with parkinsonism linked to chromosome 17 claim 3 , Gerstmann-Straussler-Scheinker disease claim 3 , Guadeloupean parkinsonism claim 3 , Hallevorden-Spatz disease claim 3 , neurodegeneration with brain iron accumulation type 1 claim 3 , Myotonic dystrophy claim 3 , Multi-infarct dementia claim 3 , Niemann-Pick disease type C claim 3 , Pallido-ponto-nigral degeneration claim 3 , Parkinsonism-dementia complex of Guam claim 3 , Post-encephalitic parkinsonism claim 3 , Prion diseases claim 3 , Creutzfeldt-Jakob Disease claim 3 , Variant Creutzfeldt-Jakob Disease claim 3 , Fatal Familial Insomnia claim 3 , Kuru claim 3 , Progressive supercortical gliosis claim 3 , Progressive supranuclear palsy claim 3 , Richardson's syndrome claim 3 , Subacute sclerosing panencephalitis claim 3 , Tangle-only dementia claim 3 , Huntington's disease claim 3 , Schizophrenia claim 3 , Mild Cognitive Impairment claim 3 , Neuropathy claim 3 , or Glaucoma.5. The method of wherein the condition is Parkinson's disease.6. The method of wherein the condition is Gaucher's disease.7. The method of wherein the compound is one or more of ...

Photoelectric conversion element and method of using same, optical sensor and image sensor

A photoelectric conversion element exhibiting excellent responsiveness and high photoelectric conversion efficiency, a method of using the photoelectric conversion element, and an optical sensor and an image sensor including the photoelectric conversion element are provided. The photoelectric conversion element includes a conductive film, a photoelectric conversion film containing a photoelectric conversion material and a transparent conductive film. The conductive film, the photoelectric conversion film and the transparent conductive film are formed in this order. The photoelectric conversion material contains a compound (A) represented by formula (1):

Morphan And Morphinan Analogues, And Methods Of Use

The present application relates to analogues of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof. 19-. (canceled)11. The compound of claim 10 , wherein Ris C-Calkenyl or cycloalkyl.12. The compound of claim 10 , wherein Rand R claim 10 , together with the carbon atoms to which they are attached claim 10 , form a 6-membered unsubstituted carbocyclic ring or a 6-membered carbocyclic ring substituted with a hydroxyl or a ketone.13. The compound of claim 10 , wherein Rand R claim 10 , taken together with the carbon atom to which they are attach to claim 10 , form a C═O group.14. The compound of claim 10 , wherein Ris substituted heteroaryl comprising one or two 5- or 6-membered rings and 1-4 heteroatoms selected from N claim 10 , O and S.16. The compound of claim 15 , wherein Ris cyclopropyl.17. The compound of claim 15 , wherein X is H or hydroxyl.18. The compound of claim 15 , wherein Y and Z are each claim 15 , independently claim 15 , H or hydroxyl claim 15 , or alternatively claim 15 , Y and Z claim 15 , together with the carbon atom to which they are attached claim 15 , form C═O.19. The compound of claim 15 , wherein Ris —C(O)NH.2128-. (canceled)29. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and the compound of .30. A method of treating a depressive symptom in a subject in need thereof claim 10 , the method comprising administering to the subject an effective amount of a compound of claim 10 , wherein the compound is a μ opioid receptor agonist having an Emax of 5% to 45% in a GTPγS binding assay.31. (canceled)32. The method of claim 30 , wherein said agonist has a low risk of opioid dependence claim 30 , opioid addiction claim 30 , and/or symptoms of opioid withdrawal.33. A method of treating a depressive symptom in a subject in need thereof claim 10 , the method comprising ...

CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE

The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): 130-. (canceled)321. The composition of claim , wherein the additional therapeutic agent is an acetylcholinesterase inhibitor.331. The composition of claim , wherein the acetylcholinesterase inhibitor is donepezil.35. The composition of claim 34 , wherein the additional therapeutic agent is an acetylcholinesterase inhibitor.365. The composition of claim claim 34 , wherein the acetylcholinesterase inhibitor is donepezil.38. The method of claim 37 , wherein the treating is for Alzheimer's Disease.39. The method of claim 38 , wherein the treating is for mood disorder.40. The method of claim 39 , wherein the mood disorder is depression.41. The method of claim 38 , further comprising administration of an acetylcholinesterase inhibitor.42. The method of claim 41 , wherein the acetylcholinesterase inhibitor is donepezil.44. The method of claim 43 , wherein the treating is for Alzheimer's Disease.45. The method of claim 43 , wherein the treating is for mood disorder.46. The method of claim 45 , wherein the mood disorder is depression.47. The method of claim 44 , further comprising administration of an acetylcholinesterase inhibitor.48. The method of claim 47 , wherein the acetylcholinesterase inhibitor is donepezil. The invention is directed to certain chromane, isochromane, and dihydroisobenzofuran derivatives, their salts, pharmaceutical compositions comprising them and their use in therapy of the human body. The compounds of the invention have been found to modulate the metabotropic glutamate receptor 2 (mGluR2), and hence are expected to be useful in the treatment of Alzheimer's Disease and other diseases mediated by the mGuR2 receptor.The metabotropic glutamate receptors are known to contain one or more allosteric sites, which may alter the affinity with which glutamate and other metabotropic glutamate (mGuR) ligands bind to the primary binding ...

Polycyclic aromatic compounds and methods for making and using the same

Disclosed herein are embodiments of polycyclic aromatic compounds and methods of making and using the same. Various different types of polycyclic ring systems are disclosed, including, but not limited to, polymeric aromatic compounds (e.g., nanographene compounds), pentacene-like compounds, chiral aromatic compounds, asymmetric arene compounds formed from naphthalene-, anthracene-, phenanthrene-, and pyrene-based starting compounds, and dimerized aromatic compounds. Also disclosed herein are novel benzannulation-based methods for making the disclosed polycyclic aromatic compounds.

SUBSTITUTED 2-PYRIDONE TRICYCLIC COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME

The present invention includes in one aspect substituted 2-oxo-1,2,5,6-tetrahydrobenzo[h]quinoline-3-carboxylic acids, analogues thereof, and compositions comprising the same, which can be used to treat and/or prevent hepatitis B virus (HBV) infection and/or hepatitis D virus (HDV) in a patient. In certain embodiments, the invention provides a compound of formula (I), or a salt, solvate, geometric isomer, stereoisomer, tautomer, and any mixtures thereof: 3. (canceled)5. (canceled)7. The compound of claim 1 , wherein at least one applies:{'sup': 1', '2', '3', '4, '(a) at least one of X, X, X, and Xis N;'}{'sup': 3a', '3b, 'sub': 1', '6', '3', '8, '(b) at least one of Ror Ris independently selected from the group consisting of optionally substituted C-Calkyl and optionally substituted C-Ccycloalkyl;'}{'sup': 6I', '6II', '6III', '6IV, '(c) none of R, R, Rand R, if present, are N-linked;'}{'sup': 6I', '6II', '6III', '6IV, '(d) none of R, R, Rand R, if present, comprise a basic nitrogen group;'}{'sup': 6II', '6III, '(e) at least one of Rand R, if present, is O-linked;'}{'sup': 6II', '6III, '(f) both of Rand R, if present, are O-linked.'}8. The compound of claim 1 , wherein each occurrence of alkyl claim 1 , alkenyl claim 1 , or cycloalkyl is independently optionally substituted with at least one substituent selected from the group consisting of C-Calkyl claim 1 , halo claim 1 , —OR″ claim 1 , phenyl claim 1 , and —N(R″)(R″) claim 1 , wherein each occurrence of R″ is independently H claim 1 , C-Calkyl claim 1 , or C-Ccycloalkyl.9. The compound of claim 1 , wherein each occurrence of aryl or heteroaryl is independently optionally substituted with at least one substituent selected from the group consisting of C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Chaloalkoxy claim 1 , halo claim 1 , —CN claim 1 , —OR″ claim 1 , —N(R″)(R″) claim 1 , —NO claim 1 , —S(═O)N(R″)(R″) claim 1 , acyl claim 1 , and C-Calkoxycarbonyl claim 1 , wherein each occurrence of R″ is independently H ...

Heterocyclic compound and organic light-emitting device including the same

A heterocyclic compound and an organic light-emitting device including the same are provided, the heterocyclic compound being represented by <Formula 1>

Dyes and Labeled Molecules

Dimeric and trimeric nucleic acid dyes, and associated systems and methods are provided. Such a dye may form a hairpin-like structure that enables it to stain nucleic acids via a release-on-demand mechanism, for example. Such a dye may have low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, for example. A dye provided herein may be useful in a variety of applications, such as in DNA quantitation in real-time PCR, for example.

Inhibitors of Protein Phosphatase-1 and Uses Thereof

Inhibitors of protein phosphatase-1 (PP-1) and their use in a method for the treatment or prevention of viral infections caused by HIV or ebola virus are disclosed. Inhibitors of protein phosphatase-1 in effective amounts have been shown to slow down viral replication upon contacting ebola virus or cells containing the ebola virus. 2. The method of claim 1 , comprising a pharmaceutically acceptable salt of a compound of formula I.3. The method of claim 1 , wherein Z is O.4. The method of claim 1 , wherein n is 1.5. The method of claim 1 , wherein n is 2.6. The method of claim 1 , wherein Ris H or C1-C4 alkyl.7. The method of claim 1 , wherein Ar is optionally substituted phenyl.8. The method of claim 1 , wherein Ar is optionally substituted 2-thienyl.9. The method of claim 1 , wherein Ar is optionally substituted 3-thienyl.10. A method to inhibit replication of Ebola virus claim 1 , comprising contacting the Ebola virus or a cell containing the Ebola virus with a compound of formula (I). This application claims the benefit of U.S. Provisional Application Ser. No. 61/682,952, filed Aug. 14, 2012 which is incorporated herein as if fully rewritten.The present application relates to inhibitors of Protein Phosphatase-1 and medical uses of such inhibitors. More specifically, a class of compounds is provided that inhibit PP-1. Further, methods to use PP-1 inhibitors for treating Ebola viral infection are described.The family Filoviridae, which includes Marburg virus and five species of Ebola virus (EBOV), four of which are Zaire, Sudan, Ivory Coast and Bundibugyo (Towner, J. S., et al., . PLoS Pathog, 2008. 4(11): p. e1000212), causes severe hemorrhagic fever in humans, with a lethality of up to 90%. Outbreaks of Ebola (EBOV) and Marburg (MARV) infections occur in Central Africa on a regular basis (Groseth, A., H. Feldmann, and J. E. Strong, . Trends Microbiol, 2007. 15(9): p. 408-16). Sequences of EBOV Zaire identified in wild apes during the 2003-2005 outbreaks in Gabon ...

OPIOID AGONISTS AND USES THEREOF

Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry. 2. The compound of claim 1 , wherein Ris hydrogen.3. The compound of any one of the preceding claims claim 1 , wherein Ris alkyl.4. The compound of any one of the preceding claims claim 1 , wherein Ris cyclopropylmethyl.5. The compound of any one of the preceding claims claim 1 , wherein G is O and represents a double bond.6. The compound of any one of the preceding claims claim 1 , wherein Ris hydrogen.7. The compound of any one of the preceding claims claim 1 , wherein Ris selected from optionally substituted alkyl claim 1 , optionally substituted amino claim 1 , and —X-POLY.8. The compound of any one of the preceding claims claim 1 , wherein Ris optionally substituted amino.9. The compound of any one of the preceding claims claim 1 , wherein Ris amino substituted with an optionally substituted aryl or optionally substituted alkyl.10. The compound of any one of the preceding claims claim 1 , wherein Ris amino substituted with an optionally substituted phenyl.12. The compound of claim 11 , wherein q is 1.13. The compound of any one or claim 11 , wherein X is —NH—.14. The compound of any one of or claim 11 , wherein X is —O—.15. The compound of any one of to claim 11 , wherein POLY is a poly(alkylene oxide) oligomer.16. The compound of any one of to claim 11 , wherein POLY is a poly(ethylene oxide) oligomer.17. The compound of any one of to claim 11 , wherein POLY is capped with an optionally substituted alkyl.18. The compound of any one of to claim 11 , wherein POLY is capped with a methyl claim 11 , trifluoromethyl claim 11 , or methyl substituted with a carboxy group.20. The compound of claim 19 , wherein X is —O—.21. The compound of claim 19 , wherein X is —NH—.22. ...

ANTI-FIBROTIC PYRIDINONES

Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders. 2. The compound of claim 1 , wherein{'sup': 2', '5', '6', '7', '8, 'Ris selected from the group consisting of halogen, —OR, —NRR, and —C(O)R;'}{'sup': 3', '9, 'sub': 2', 'n', '6-10', '2', 'n', '2', 'n', '3-10', '2', 'n, 'Ris selected from the group consisting of —(CH)—(Caryl), —(CH)-(5-10 membered heteroaryl), —(CH)—(Ccarbocyclyl), and —(CH)-(3-10 membered heterocyclyl), each optionally substituted with one or more R;'}{'sup': 9', '5', '14', '15', '8', '16, 'sub': 1-6', '2-6', '2-6', '1-6', '2-8', '3-10', '6-10', '2', '2, 'each Ris independently selected from the group consisting of halogen, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, optionally substituted Calkylthio, optionally substituted Calkoxyalkyl, optionally substituted Ccarbocyclyl, optionally substituted Caryl, —OR, —NRR, —C(O)R, —SOR, and —NO; and'}{'sup': '11', 'sub': 1-6', '2-6', '2-6', '1-6, 'each Ris independently selected from the group consisting of halogen, —CN, optionally substituted Calkyl, optionally substituted Calkenyl, optionally substituted Calkynyl, and optionally substituted Calkoxy.'}3. The compound of claim 1 , wherein Ris a Caryl optionally substituted with one or more R.4. The compound of claim 3 , wherein Ris a phenyl optionally substituted with one or more R.5. The compound of claim 1 , wherein Ris a 5-10 membered heteroaryl optionally substituted with one or more R.6. The compound of claim 5 , wherein Ris a pyrazolyl or 1-methylpyrazolyl optionally substituted with one or more R.7. The compound of claim 1 , wherein each Ris independently selected from halogen claim 1 , or optionally substituted Calkyl.8. (canceled)9. The compound of claim 7 , wherein Ris methyl.10. (canceled)11. (canceled)12. The compound of claim 1 , wherein Ris —CN.13. The compound of claim 1 , wherein Ris −OR.14. The compound of claim 13 , ...

INDENOPYRIDINE DERIVATIVES

Disclosed is a compound of formula (I) 19-. (canceled)14. The method of claim 13 , wherein the palladium catalyst is Pd(dba)or Pd(OAc).16. The compound of formula (V) of claim 15 , wherein X is iodo.17. The compound of formula (V) of claim 15 , wherein X is bromo.19. The method of claim 18 , wherein X is iodo. This application relates to indenopyridine derivatives. The indenopyridine derivatives of the invention are useful as intermediates for the preparation of pharmaceutically active compounds such as 11-β-hydroxysteroid hydrogenase type 1 (11-β-HSD1) inhibitors.Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridines are reportedly useful as inhibitors of 11-β-hydroxysteroid hydrogenase type 1 (“11-β-HSD1”) and for treatment of disorders associated with 11β-HSD1 activity including, for example, diabetes mellitus (e.g., type II diabetes), obesity, symptoms of metabolic syndrome, glucose intolerance, hyperglycemica (see, e.g., WO 2011/057054).The aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridines can be prepared, for example, from nitrile-substituted hexahydroindenopyridines as described in WO 2011/057054. In one method described in WO 2011/057054, the intermediate (4aR,9aS)-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine-6-carbonitrile (A) is allowed to react with 1H-benzoimidazole-5-carboxylic acid (B) followed by reaction with hydrogen chloride to provide the 11-β-HSD1 inhibitor (4a-R,9a-S)-1-(1H-benzoimidazole-5-carbonyl)-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-b]pyridine-6-carbonitrile (C) as depicted below:Methods of preparing the compound of formula (A) described in WO 2011/057054 include a 13-step synthesis and a low overall yield (˜2.9%). In addition, some of the described methods utilize corrosive and/or toxic reagents (e.g., trifluoromethanesulfonic acid anhydride (TfO), boron tribromide (BBr) and Zinc cyanide (Zn(CN)), which produce a problematic by-product stream. Thus, there is a need, for improved processes for making ...

METAL OXIDE NANOPARTICLE ELECTRON TRANSPORT LAYERS IN PEROVSKITE SEMICONDUCTOR DEVICES

A nanoparticle that includes a metal oxide core having the formula MOwherein M is either tantalum (V) or niobium (V) and alkylsiloxane ligands surrounding the metal oxide core. 1. A metal oxide nanoparticle comprising:{'sub': 2', '5, 'a metal oxide core of formula MO, wherein M is tantalum (V) or niobium (V); and'}alkylsiloxane ligands bonded to the metal oxide core.2. The metal oxide nanoparticle of claim 1 , wherein the alkylsiloxane ligands are selected from the group consisting of: isobutylsiloxane claim 1 , allylsiloxane claim 1 , vinylsiloxane claim 1 , n-propylsiloxane claim 1 , n-butylsiloxane claim 1 , sec-butylsiloxane claim 1 , tert-butylsiloxane claim 1 , phenylsiloxane claim 1 , n-octylsiloxane claim 1 , isooctylsiloxane n-dodecylsiloxane claim 1 , 4-(trimethylsilyl)phenylsiloxane claim 1 , para-tolylsiloxane claim 1 , 4-fluorophenylsiloxane claim 1 , 4-chlorophenylsiloxane claim 1 , 4-bromophenylsiloxane claim 1 , 4-iodophenylsiloxane claim 1 , 4-cyanophenylsiloxane claim 1 , benzylsiloxane claim 1 , methylsiloxane claim 1 , ethylsiloxane claim 1 , 4-(trifluoromethyl)phenylsiloxane claim 1 , 4-ammoniumbutylsiloxane claim 1 , and any combination thereof.3. The metal oxide nanoparticle of claim 1 , wherein the alkylsiloxane ligands are crosslinked to alkylsiloxane ligands of at least one other nanoparticle.4. The metal oxide nanoparticle of claim 1 , wherein the metal oxide core is doped with a metal selected from the group consisting of: Ti claim 1 , Zr claim 1 , Hf claim 1 , Cr claim 1 , Mo claim 1 , W claim 1 , V claim 1 , or any combination thereof.5. The metal oxide nanoparticle of claim 1 , wherein the metal core comprises TaO.6. The metal oxide nanoparticle of claim 1 , wherein the metal core comprises NbO. This application is a divisional application of U.S. patent application Ser. No. 17/106,002 filed Nov. 27, 2020, which claims priority to U.S. Provisional Patent Application No. 62/941,066 filed Nov. 27, 2019, the contents of which are ...

FLUORESCENT MARKERS AND METHODS FOR IMAGING DISEASES

Methods and fluorescent probes that detect the presence of diseased cells such as cancer. The fluorescent probes are cloaked, turn-on probes having the fluorescence reporter released only in the presence of enzymes typically over-expressed in diseased and cancerous tissue. Probes include a fluorescent napthalimide reporter with a quinoidal moiety cloak. 3. A cloaked fluorophore , comprising:a fluorescent napthalimide reporter;a quinoidal moiety; anda linker;wherein the linker links the quinoidal moiety to the reporter.5. The method of claim 4 , wherein the diseased cells are cancerous.6. The method of claim 4 , wherein the diseased cells express NAD(P)H:quinone oxidoreductase isozyme I.7. The method of claim 4 , further comprising:analyzing the cells under a fluorescent microscope.8. The method of claim 4 , further comprising:analyzing the cells with multiphoton microscopy imaging.9. The method of claim 4 , where the diseased cells are circulating tumor cells.10. The method of claim 9 , further comprising:analyzing the cells with a flow cytometer. This application claims benefit of U.S. Provisional Application 61/804,961 filed Mar. 25, 2013, which is incorporated herein by reference.The invention was made with U.S. Government support under grant R21 CA135585 awarded by the National Institutes of Health and grant CHE 0910845 awarded by the National Science Foundation. The U.S. Government has certain rights in the invention.The present invention relates to fluorescent markers and methods for imaging diseases, and in particular though non-limiting embodiments, to cloaked fluorophores which activate in the presence of enzymes present in tumor tissues and inflammatory diseases.Molecular probes whose fluorescent reporter signal is generated by enzyme activation (turn-on probes) hold great potential for identification, enumeration and study of living cancer cells and/or diseased tissues. Such probes may be invaluable for accurate and early diagnoses and optimization of ...

COMPOSITIONS AND METHODS FOR THE TREATMENT OF PARKINSON'S DISEASE

The invention relates to the compounds of formula I, formula II and formula III or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II and formula III, and methods for treating or preventing Parkinson's disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment or management of Parkinson's disease such as Parkinson's disease, scleroderma, restless leg syndrome, hypertension and gestational hypertension. 4. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.5. The pharmaceutical composition of claim 4 , which is formulated to treat the underlying etiology with an effective amount of the composition for administering to a patient in need by oral administration claim 4 , delayed release or sustained release claim 4 , transmucosal claim 4 , syrup claim 4 , topical claim 4 , parenteral administration claim 4 , injection claim 4 , depot claim 4 , spray claim 4 , subdermal claim 4 , oral solution claim 4 , rectal administration claim 4 , buccal administration claim 4 , or transdermal administration.6. The compounds and compositions of claim 5 , formulated for the treatment of Parkinson's disease claim 5 , scleroderma claim 5 , restless leg syndrome claim 5 , hypertension claim 5 , and gestational hypertension.7. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.8. The pharmaceutical composition of claim 7 , which is formulated to treat the underlying etiology with an effective amount claim 7 , for administering the composition to a patient in need by oral administration claim 7 , delayed release or sustained release claim 7 , transmucosal claim 7 , syrup claim 7 , topical claim 7 , ...

INHIBITING FATTY ACID SYNTHASE (FASN)

The present disclosure is directed to inhibitors of FASN. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of FASN. For instance, the disclosure is concerned with compounds and compositions for inhibition of FASN, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of FASN, and methods of synthesis of these compounds. 2. The method of claim 1 , wherein said treating the compound of formula (A) with the compound of formula (B) is performed in the presence of a palladium catalyst and a base.14. The method of claim 12 , wherein said converting the compound of formula (C) to the compound of formula (VII-A) comprises:coupling the compound of formula (C) with 1-hydroxycyclopropane-1-carboxylic acid to afford the compound of formula (VII-A). This application is a continuation of U.S. patent application Ser. No. 16/598,481, filed Oct. 10, 2020, which claims the benefit of U.S. Provisional Application No. 62/744,071, filed on Oct. 10, 2018, both of which are incorporated by reference in their entirety.The present disclosure relates to novel chemical compositions for inhibiting fatty acid synthase (FASN).Non-alcoholic steatohepatitis (NASH) is a chronic liver disease with varying degrees of inflammation and fibrosis that can progress to cirrhosis and end-stage liver complications. The disease affects greater than 16 million people in the US and is the second leading cause of liver transplants in the US. Moreover, NASH is a strong predictor for type 2 diabetes, cardiovascular disease and end-stage kidney disease. There are no pharmacological agents currently approved for the treatment of NASH, which represents a substantial healthcare burden. The pathogenesis of NASH has been associated with obesity or aberrant metabolic syndrome. Consistent with a proposed role for increased de novo lipogenesis (DNL) as a mediator of steatosis and liver injury, FASN expression is significantly ...

Morphinan Compounds

This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σreceptor agonist that also has NMDA antagonist activity. 111-. (canceled)13. The method of claim 12 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.14. The method according to or claim 12 , further comprising administering a second therapeutic agent useful in the treatment or prevention of autism.15. The method of claim 14 , wherein the second therapeutic agent is selected from quinidine claim 14 , quinidine sulfate claim 14 , oxycodone claim 14 , and gabapentin.17. The separate dosage forms of claim 16 , wherein any atom not designated as deuterium is present at its natural isotopic abundance in the compound or pharmaceutically acceptable salt thereof. This application is a continuation of U.S. patent application Ser. No. 12/112,936, filed Apr. 30, 2008, which claims the benefit of priority under 35 U.S.C. §119 to U.S. Provisional Application Ser. Nos. 60/915,130, filed May 1, 2007, 60/916,662, filed May 8, 2007, and 60/976,044, filed Sep. 28, 2007, the entire contents of which are incorporated by reference in their entirety herein.This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σreceptor agonist that also has NMDA antagonist activity.Dextromethorphan is currently one of the most widely used antitussives. Also known by the chemical name (+)-3-methoxy-17-methyl-(9α,13α, ...

Fluorophore and fluorescent sensor compound containing same

The invention provides fluorophores of formulae (I) and (II) and also fluorescent sensor compounds comprising fluorophore moieties based on such fluorophores in combination with a receptor moiety: There is further provided a method of sensing the presence of a target analyte using the fluorescent sensor compound, as well as the use of the fluorescent sensor compounds to sense a target analyte.

Condensed cyclic compound and organic light-emitting device including the same

A condensed cyclic compound and an organic light-emitting device including the same are disclosed. According to an embodiment of the present disclosure, a condensed cyclic compound is represented by Formula 1:

Compounds having valerolactam structures

The present invention describes compounds comprising at least one structural element having at least three fused aromatic or heteroaromatic rings (AR) and at least one structural element having an aromatic or heteroaromatic valerolactam (AV), especially for use in electronic devices. The invention further relates to a process for preparing the compounds of the invention and to electronic devices comprising these.

PHOTOACID GENERATOR AND CHEMICALLY AMPLIFIED POSITIVE-TYPE PHOTORESIST COMPOSITION FOR THICK FILM COMPRISING THE SAME

A non-ionic photoacid generator and a chemically amplified positive-type photoresist composition for a thick film including the non-ionic photoacid generator. The non-ionic photoacid generator may not only exhibit high solubility in a solvent of the photoresist composition, but may also exhibit chemical and thermal stability and high sensitivity. In particular, the non-ionic photoacid generator is decomposed by light to generate an acid, and at the same time, can exhibit a corrosion preventing effect on a metal substrate. 5. A chemically amplified positive-type photoresist composition for a thick film comprising the non-ionic photoacid generator of .6. The non-ionic photoacid generator of claim 1 , comprising one claim 1 , two claim 1 , three or four functional groups represented by Chemical Formula 1 as defined in .7. The non-ionic photoacid generator of claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl claim 1 , sec-butyl claim 1 , tert-butyl claim 1 , isobutyl claim 1 , amyl claim 1 , isoamyl claim 1 , tert-amyl claim 1 , hexyl claim 1 , 2-hexyl claim 1 , 3-hexyl claim 1 , heptyl claim 1 , 2-heptyl claim 1 , 3-heptyl claim 1 , isoheptyl claim 1 , tert-heptyl claim 1 , octyl claim 1 , isooctyl claim 1 , tert-octyl claim 1 , 2-ethylhexyl claim 1 , nonyl claim 1 , isononyl claim 1 , decyl claim 1 , dodecyl claim 1 , tridecyl claim 1 , tetradecyl claim 1 , pentadecyl claim 1 , hexadecyl claim 1 , heptadecyl claim 1 , octadecyl claim 1 , trifluoromethyl claim 1 , pentafluoroethyl claim 1 , heptafluoropropyl claim 1 , nonafluorobutyl claim 1 , tridecylfluorohexyl claim 1 , heptafluorooctyl claim 1 , 2 claim 1 ,2 claim 1 ,2-trifluoroethyl claim 1 , 1 claim 1 ,1-difluoroethyl claim 1 , 1 claim 1 ,1-difluoropropyl claim 1 , 1 claim 1 ,1 claim 1 ,2 claim 1 ,2-tetrafluoropropyl claim 1 , 3 claim 1 ,3 claim 1 ,3-trifluoropropyl claim 1 , 2 claim 1 ,2 claim 1 ,3 claim 1 ,3 claim 1 ,3-pentafluoropropyl claim 1 , 1 claim 1 ,1 ...

Multi function photoacid generator and chemically amplified photoresist composition for thick layer comprising the same

In Chemical Formula 1, the definition of each substituents is the same as the detail description of the specification.

ANTIBACTERIAL COMPOUNDS AND METHODS FOR USE

The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens. 2. The compound of claim 1 , wherein Ris{'sub': '3-14', 'Ccycloalkyl selected in each instance, when present, from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl;'}aryl selected in each instance, when present, from phenyl;heteroaryl selected in each instance, when present, from pyrrolyl, thiazolyl, 1H-1,2,3-triazolyl, 1H-tetrazolyl, 2H-tetrazolyl, imidazolyl or pyridinyl;heterocyclyl selected in each instance, when present, from azetidinyl, pyrrolidinyl,tetrahydrofuranyl, piperidinyl, piperazinyl, morpholinyl, 1,4-diazepanyl, 1,3-dioxolanyl, 2,5-dihydro-1H-pyrrolyl, dihydro-1H-imidazolyl, 1,4,5,6-tetrahydropyrimidinyl, 1,2,3,6-tetrahydropyridinyl; tetrahydro-2H-pyranyl, indolinyl, 2,3-dihydrobenzo[d]oxazolyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, 3,4-dihydroisoquinolin-(1H)-yl, 1,2,3,4-tetrahydroisoquinolinyl, 1,2,3,4-tetrahydroquinoxalinyl, hexahydropyrrolo[3,4-b][1,4]oxazin-(2H)-yl, (4aR,7aS)-hexahydropyrrolo[3,4-b][1,4]oxazin-(4aH)-yl, 3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazinyl, (cis)-octahydrocyclopenta[c]pyrrolyl, hexahydropyrrolo[3,4-b]pyrrol-(1H)-yl, (3aR,6aR)-hexahydropyrrolo[3,4-b]pyrrol-(1H)-yl, (3aR,6aS)-hexahydropyrrolo[3,4-c]pyrrol-(1H)-yl, 5H-pyrrolo[3,4-b]pyridin-(7H)-yl, 5,7-dihydro-6H-pyrrolo[3,4-b]pyridinyl, tetrahydro-1H-pyrrolo[3,4-b]pyridin-(2H,7H,7aH)-yl, hexahydro-1H-pyrrolo[3,4-b]pyridin-(2H)-yl, (4aR,7aR)-hexahydro-1H-pyrrolo[3,4-b]pyridin-(2H)-yl, octahydro-6H-pyrrolo[3,4-b]pyridinyl, 2,3,4,9-tetrahydro-1H-carbazolyl, 1,2,3,4-tetrahydropyrazino[1,2-a]indol-8-yl, 2,3-dihydro-1H-pyrrolo[1,2-a]indolyl, (3aR,6aR)-hexahydrocyclopenta[c]pyrrol-(1H)-yl, (3aR,4R,6aS)-hexahydrocyclopenta[c]pyrrol-(1H)-yl, (3aR,4S,6aS)-hexahydrocyclopenta[c]pyrrol-(1H)-yl, (3aR,5r,6aS)- ...

TETRAHYDROPHENANTHRIDINONES AND TETRAHYDROCYCLOPENTAQUINOLINONES AS PARP AND TUBULIN POLYMERIZATION INHIBITORS

The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) 112-. (canceled)141. A method of claim , wherein:{'sub': 2', '2, 'Y is CH—CH; aryl is phenyl; Het is pyridinyl, pyrimidinyl, benzimidazolyl or indazolyl;'}{'sub': 1-6', '1-6', '1-6', '1', '2', '3', '2', '2', '1-6', '1-6, 'sup': 8', '9', '8', '16', '2', '3', '4', '5', '6', '2', '8', '9, 'each aryl or Het can be substituted with one or two substituents each independently selected from halo, cyano, Calkyl, Calkyloxycarbonyl, —CalkylNRRor —OR; Xis CHor N—CH; Xis CH, C═O or O; Ris phenyl which can be substituted with cyano; Ris methyl; Rand Rare hydrogen; Rand Rare hydrogen; Ris hydrogen; and each Rand Ris independently selected from hydrogen, halo, Calkyl or trihaloCalkyl.'}151. A method of claim , wherein Y is CH—CH; Ris phenyl , pyridinyl or pyrimidinyl; each phenyl , pyridinyl or pyrimidinyl can be substituted with one or two substituents each independently selected from halo , cyano or Calkyloxy; Xis CH; Xis O; Ris phenyl substituted with cyano; Ris methyl; Rand Rare hydrogen; Rand Rare hydrogen; and Ris hydrogen.18. A method of claim 17 , wherein:{'sub': 2', '2, 'Y is CH—CH; aryl is phenyl; Het is pyridinyl, pyrimidinyl, benzimidazolyl or indazolyl;'}{'sub': 1-6', '1-6, 'claim-text': {'sub': 1-6', '1', '2', '3', '2', '2', '1-6', '1-6, 'sup': 8', '9', '8', '10', '2', '3', '4', '5', '6', '7', '8', '9, '—CalkylNRRor —OR; Xis CHor N—CH; Xis CH, C═O or O; Ris phenyl which can be substituted with cyano; Ris methyl; Rand Rare hydrogen; Rand Rare hydrogen; Ris hydrogen; and each Rand Ris independently selected from hydrogen, halo, Calkyl or trihaloCalkyl.'}, 'each aryl or Het can be substituted with one or two substituents each independently selected from halo, cyano, Calkyl, Calkyloxycarbonyl,'}19. A method of claim 17 , wherein Y is CH—CH; Ris phenyl ...

Compounds and Formulations Suitable for Radical Scavenging

The present invention relates to compositions and methods of using free radical scavengers with reduced Ogeneration. In certain embodiments, these compositions and methods of use relate to fullerene-derived ketolactams and fullerene-derived ketolactam derivatives, fullerene derivatives, and/or fullerenes. In yet other embodiments, the invention relates to cosmetic or dermatological compositions comprising said free radical scavengers with reduced Ogeneration. 17-. (canceled)10. The composition of claim 9 , wherein X is H or alkyl; Ris C-Calkyl; and Ris CH.11. The composition of claim 9 , wherein X is H; Ris a Calkyl; and Ris CH.12. The composition of claim 8 , wherein the Cfullerene-derived ketolactam of formula I is CAS#943912-75-2 claim 8 , or 2a-Aza-1 claim 8 ,2(2a)-homo-1 claim 8 ,9-seco[5 claim 8 ,6]fullerene-C—I-1 claim 8 ,9-dione claim 8 ,2a-[[4-docosyloxy)-3-methoxyphenyl]methyl].14. The composition of claim 8 , wherein the composition has an absorbance value of greater than about 0.25 at a wavelength of 570 nm.17. The Cfullerene-derived ketolactam of claim 16 , wherein X is H or alkyl; Ris C-Calkyl; and Ris CH.18. The Cfullerene-derived ketolactam of claim 16 , wherein X is H; Ris a Calkyl; and Ris CH.19. The Cfullerene-derived ketolactam of claim 15 , wherein the Cfullerene-derived ketolactam of formula I is CAS#943912-75-2 claim 15 , or 2a-Aza-1 claim 15 ,2(2a)-homo-1 claim 15 ,9-seco[5 claim 15 ,6]fullerene-C—I-1 claim 15 ,9-dione claim 15 ,2a-[[4-docosyloxy)-3-methoxyphenyl]methyl].20. The Cfullerene-derived ketolactam of claim 15 , wherein the one or more additional addends or modification is an azafulleroid modification of the fullerene cage. This application is a continuation of U.S. patent application Ser. No. 12/516,992, now U.S. Pat. No. 8,580,810, issued Nov. 12, 2013, which is a §371 national stage application based on Patent Cooperation Treaty Application serial number PCT/US2007/085879, filed Nov. 29, 2007, which claims the benefit of priority ...

NOVEL CARBO- AND HETEROCYCLIC SPIRO COMPOUNDS AS DONOR MATERIALS FOR ORGANIC PHOTOVOLTAICS AND THEIR PREPARATION

The subject invention provides compositions of and methods of using carbo- and heterocyclic spiro compounds as donor materials for organic photovoltaic (OPV) devices. In preferred embodiments, spiro compounds comprising triarylamine and derivatives thereof demonstrate effective hole-transporting properties in OPV devices, achieving up to 5.46% of power conversion efficiency. Advantageously, preferred compounds provided herein are thermally stable and volatile enough to form thin films for the photoactive layer of an OPV device by vacuum deposition or by spin-coating. 2. The compound according to claim 1 , wherein A claim 1 , B claim 1 , C claim 1 , and D are claim 1 , independently claim 1 , 5- or 6-membered rings selected from benzenes claim 1 , pyridines claim 1 , thiophenes claim 1 , furans claim 1 , fused-thiophenes claim 1 , pyrazoles claim 1 , pyrimidines claim 1 , pyrroles claim 1 , selenophenes claim 1 , tellurophenes claim 1 , benzimidazoles claim 1 , benzofurans claim 1 , benzothiazoles claim 1 , benzoxazoles claim 1 , benzophospholes claim 1 , indoles claim 1 , indanes claim 1 , naphthalenes claim 1 , anthracenes claim 1 , pyrenes claim 1 , thiazoles claim 1 , pyrans claim 1 , thiapyrans claim 1 , carbazoles claim 1 , dibenzothiophenes claim 1 , dibenzofurans claim 1 , dibenzosiloles claim 1 , fluorenes claim 1 , and dibenzophospholes claim 1 , each being optionally substituted.3. The compound according to claim 1 , comprising one or more of D claim 1 , D claim 1 , D claim 1 , and D claim 1 , wherein D claim 1 , D claim 1 , D claim 1 , and Dare independently selected from optionally substituted functional groups of alkylaminos claim 1 , arylamines claim 1 , thiophenes claim 1 , oligo-thiophenes claim 1 , fused-thiophenes claim 1 , fluorenes claim 1 , dibenzothiophenes claim 1 , dibenzofurans claim 1 , and dibenzophospholes.4. The compound according to claim 1 , wherein X is present and X is a carbon atom or a heteroatom claim 1 , each being optionally ...

NOVEL COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME

A novel compound is disclosed, which comprises: a 7-membered ring segment, which is formed by a cis-stilbene segment and a bridge atom with four bonds; and an acridine segment connecting to the bridge atom of the 7-membered ring segment. In addition, an organic electronic device is also disclosed, and an organic layer therein comprises the novel compound of the present invention. 1. A compound comprising:a 7-membered ring segment, which is formed by a cis-stilbene segment and a bridge atom with four bonds; andan acridine segment connecting to the bridge atom of the 7-membered ring segment.2. The compound of claim 1 , wherein the bridge atom is C or Si.4. The compound of claim 3 , wherein Rand Rare the same.5. The compound of claim 3 , wherein Rand Rare —NRR claim 3 , and Ris aryl claim 3 , and Ris C-Calkyl or aryl.6. The compound of claim 5 , wherein each of Rand Rindependently is phenyl claim 5 , naphthyl claim 5 , or anthryl unsubstituted or substituted with C-Calkyl claim 5 , C-Calkoxy or —CN.10. The compound of claim 9 , wherein X is H claim 9 , methyl claim 9 , ethyl claim 9 , methoxy claim 9 , or ethoxy.11. The compound of claim 3 , wherein Rand Rare Br claim 3 , pyridyl phenyl claim 3 , naphthyl claim 3 , anthryl or carbazoyl.12. The compound of claim 3 , wherein Rand Rare phenyl unsubstituted or substituted with methoxy claim 3 , ethoxy claim 3 , or —CN.13. The compound of claim 3 , wherein Rand Rare —R-R claim 3 , in which Ris phenylene claim 3 , Ris phenyl unsubstituted or substituted with methoxy claim 3 , ethoxy claim 3 , or —CN.15. The compound of claim 3 , having glass transition temperatures (T) ranged from 118° C. to 163° C. claim 3 , decomposition temperatures (T) ranged from 400° C. to 465° C. and/or oxidation potentials ranged from 0.06 V to 0.87 V or the reduction potential ranged from −1.89 to −2.32 V.16. The compound of claim 3 , which is applied to an organic light emitting device claim 3 , an organic solar cell device claim 3 , an organic ...

Morphan and Morphinan Analogues, and Methods of Use

The present application relates to analogues of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof. 2. (canceled)3. (canceled)4. (canceled)7. (canceled)8. (canceled)9. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)16. (canceled)17. (canceled)18. (canceled)19. (canceled)21. The compound of claim 1 , wherein the compound is a μ opioid receptor agonist having an Emax of 5% to 45% in a GTPγS binding assay.22. The compound of claim 21 , wherein the Emax is 15% to 35% in a GTPγS binding assay.23. (canceled)24. The compound of claim 1 , having a maximal dopamine efflux in the nucleus accumbens of 125% to 300% over baseline in a rat.25. The compound of claim 24 , having a maximal dopamine efflux in the nucleus accumbens of 200% to 300% over baseline in a rat.26. The compound of claim 1 , wherein the compound does not attenuate thermal pain in a rodent hot plate model when administered at a dose of at least 1 mg/kg.27. The compound of claim 26 , wherein the compound does not attenuate thermal pain in a rodent hot plate model when administered at a dose of at least 3 mg/kg.28. The compound of claim 26 , wherein the compound does not attenuate thermal pain in a rodent hot plate model when administered at a dose of 10 mg/kg.29. (canceled)30. A method of treating a depressive symptom in a subject in need thereof claim 26 , the method comprising administering to the subject an effective amount of a μ opioid receptor agonist that exhibits an Emax of 5% to 45% in a GTPγS binding assay.31. (canceled)32. (canceled)33. A method of treating a depressive symptom in a subject in need thereof claim 26 , the method comprising administering to the subject an effective amount of a compound having a maximal dopamine efflux in the nucleus accumbens of 125% to 300% over base line in a rat.34. (canceled)35. A method of treating a ...

COMPOSITIONS AND METHODS OF USING THE COMPOSITIONS FOR PLAQUE SOFTENING

Disclosed herein is a compound for use in a composition applied to a blood vessel, wherein the compound softens and/or disrupts the crystalline matrix of calcified plaque. Methods of treatment comprising applying the disclosed composition are also disclosed. Plaque-softening compounds are also disclosed. 1. (canceled)316.-. (canceled)17. A method of softening plaque in a treatment zone of a blood vessel comprising a plaque matrix; the method comprising:applying a bolus of a composition comprising a plaque-softening compound to the treatment zone of the blood vessel, wherein the blood vessel is an artery or a vein.18. (canceled)19. The method of claim 17 , wherein the composition is provided in a bolus in an amount sufficient to provide a high systemic concentration.20. The method of claim 17 , wherein the plaque softening compound is applied for a period of time from about 1 second to about 1 hour.21. The method of claim 17 , wherein the plaque matrix comprises lesions ranging in length from about 4 to about 9 cm.22. The method of claim 17 , wherein the plaque-softening compound penetrates a greasy portion of the plaque matrix and/or the plaque-softening compound crosses the membrane of cells of the plaque matrix and controls the calcium concentration inside the cells.23. (canceled)25. The method of claim 17 , wherein the plaque-softening compound is selected from the group consisting of EDTA-like ligands claim 17 , luciferin-based ligands claim 17 , polyether ligands claim 17 , phosphate-based ligands claim 17 , and organic acids.26. The method of claim 25 , wherein the EDTA-like ligand is selected from the group consisting of ethylene glycol tetraacetic acid (EGTA); diethylene triamine pentaacetic acid (DTPA); 1 claim 25 ,2-bis[o-aminophenoxy)ethane-N claim 25 ,N claim 25 ,N′N′-tetraacetic acid (BAPTA); and amino-5-(3-dimethylamino-6-dimethylammonio-9-xanthenyl) phenoxy]-2-(2-amino-5-methylphenoxy)ethane-N claim 25 ,N claim 25 ,N′ claim 25 ,N′-tetraacetic acid.27. ...

NUCLEIC ACID MODIFYING REAGENTS AND USES THEREOF

The present disclosure includes compounds, compositions, and methods for nucleic acid amplification reactions. In particular, the present disclosure provides compounds, compositions, and methods for viability PCR (vPCR) applications, in which the compounds that selectively bind to nucleic acids from non-viable cells. 1. A compound or a salt thereof , the compound comprising:(A) a nucleic acid binding moiety (“NAB moiety”);(B) a live/dead cell differentiating moiety (“LDCD moiety”); and(C) a nucleic acid modifying moiety (“NAM moiety”).2. The compound of claim 1 , or a salt thereof claim 1 , wherein the compound has the structure:A-B-Cwherein A is the NAB moiety, B is the LDCD moiety, C is the nucleic acid modifying moiety.3. (canceled)4. The compound of claim 1 , or a salt thereof claim 1 , wherein the NAB moiety is a groove-binding moiety claim 1 , an intercalating moiety claim 1 , or a mixed-mode binding moiety.5. The compound of claim 1 , or a salt thereof claim 1 , wherein the NAB moiety comprises a bibenzimidazole moiety or a phenylphenanthridium moiety.7. The compound of claim 1 , or a salt thereof claim 1 , wherein the NAM moiety comprises a bischloroethylamine (nitrogen mustard) moiety claim 1 , a platinum-based moiety claim 1 , a 1-(chloromethyl)-2 claim 1 ,3-dihydro-1H-benzo[e]indolyl moiety claim 1 , or a pyrrolo[2 claim 1 ,1-c][1 claim 1 ,4]benzodiazepine (PBD) moiety.9. The compound of claim 1 , or a salt thereof claim 1 , wherein the LDCD moiety comprises at least one charged moiety.10. The compound of claim 9 , wherein the LDCD moiety comprises at least one quaternary ammonium group.11. The compound of claim 1 , or a salt thereof claim 1 , wherein the LDCD moiety comprises at least one poly(ethylene glycol) moiety having formula:{'br': None, 'sub': 2', '2', 'n, '—(CH—CHO)—'}wherein n is 2, 3, 4, 5, 6, 7, 8, 9, or 10.1214.-. (canceled)16. A method of detecting a viable microorganism or cell in a sample claim 1 , the method comprising:{'claim-ref': {'@ ...

USE OF ORGANIC OXYIMIDES AS FLAME RETARDANT FOR PLASTIC MATERIALS AND ALSO FLAME-RETARDANT PLASTIC MATERIAL COMPOSITION AND MOULDED PARTS PRODUCED THEREFROM

The present invention relates to the use of organic oxy imides as flame retardants for plastics. According to the present invention, a flame-retardant plastics composition is likewise specified, including an oxy imide as flame retardant. Additionally specified are mouldings produced from an inventive flame-retardant polymer composition. 116-. (canceled)21. The oxyimide according to claim 20 , wherein R═H or acyl.22. A plastic material composition comprising a plastic material and an oxyimide according to claim 17 , wherein the plastic materials are thermoplastic claim 17 , elastomeric or duroplastic polymers claim 17 , and when they are thermoplastic polymers claim 17 , they are selected from the group consisting ofa) polymers made of olefins or diolefins, polyethylene (LDPE, LLDPE, VLDPE, ULDPE, MDPE, HDPE, UHMWPE), metallocene-PE (m-PE), polypropylene, polyisobutylene, poly-4-methylpentene-1, polybutadiene, polyisoprene, polycyclooctene, polyalkylene-carbon monoxide copolymers, and copolymers in the form of stochastic or block structures. polypropylene-polyethylene (EP), EPM or EPDM, ethylene-vinyl acetate (EVA), ethylene-acrylic ester, ethylene-butyl acrylate, ethylene-acrylic acid and the salts thereof (ionomers), and terpolymers, ethylene-acrylic acid-glycidylacrylate, graft polymers, polypropylene-g-maleic anhydride, polypropylene-g-acrylic acid, or polyethylene-g-acrylic acid,b) polystyrene, polymethylstyrene, polyvinylnaphthalene, styrene-butadiene (SB), styrene-butadiene-styrene (SBS), styrene-ethylene-butylene-styrene (SEBS), styene-ethylene-propylene-styrene, styrene-isoprene, styrene-isoprene-styrene (SIS), styrene-butadiene-acrylonitrile (ABS), styrene-acrylonitrile-acrylate (ASA), styrene-ethylene, styrene-maleic anhydride polymers including corresponding graft copolymers, styrene grafted on butadiene, maleic anhydride grafted on SBS or SEBS, and also graft copolymers made of methylmethacrylate, styrene-butadiene or ABS (MABS),c) halogen-containing ...

BICYCLIC ROR-GAMMA MODULATORS

Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing ROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds. 11. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein X is —NR— or —C(R)(R)—.12. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Q is attached to the ring carbon atoms at a and b.13. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Q is attached to the ring carbon atoms at c and d.14. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Q is attached to the ring carbon atoms at a and c.15. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Q is attached to the ring carbon atoms at b and d.19. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein each Rand each Rare hydrogen.20. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein t is 1 , 2 , or 3.21. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein t is 1.22. The compound of any one of - , or a pharmaceutically acceptable salt , solvate , or stereoisomer thereof , wherein Ris C-Calkyl , C-Cheteroaryl , (C-Cheteroaryl)-C-Calkylene- , —S(O)R , —C(O)R , —C(O)OR , or —C(O)—C-Calkylene-OR , wherein C-Cheteroaryl and (C-Cheteroaryl)-C-Calkylene- are optionally substituted with 1 or 2 groups each independently selected from halo , C-Calkyl , C-Chaloalkyl , and hydroxyl.23. The compound of any one of - , or a pharmaceutically acceptable salt , solvate ...

CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS

The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R, R, R, R, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTHfunction. 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris{'br': None, '-Q-W—V;'}{'sub': 3', '2, 'Q is —C(O)—, —C(O)O—, —C(O)N(CH)— or —CH—;'}{'sub': 1', '4, 'W is C-Calkylene; and'}{'sub': '2', 'V is —COH.'}4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris C-Calkyl claim 1 , C-Ccycloalkyl claim 1 , —CH—(C-Ccycloalkyl) claim 1 , or phenyl.5. The compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris methyl claim 4 , ethyl claim 4 , cyclopropyl claim 4 , cyclobutyl claim 4 , —CH-cyclopropyl claim 4 , or phenyl.7. The compound of or a pharmaceutically acceptable salt thereof claim 6 , wherein Y is —C(O)—.13. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound is selected from the group consisting of:4-[{cis,cis-4-[(Benzyloxy)carbonyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]quinolin-9-yl}(cyclopropyl)amino]-4-oxobutanoic acid;4-[{cis,cis-4-[(benzyloxy)carbonyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]quinolin-9-yl}(phenyl)amino]-4-oxobutanoic acid;4-{ethyl[cis,cis-4-{[4-(trifluoromethoxy)phenyl]carbonyl}-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]quinolin-9-yl]amino}-4-oxobutanoic acid;4-{cyclopropyl[cis,cis-4-{[4-(trifluoromethoxy)phenyl]carbonyl}-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]quinolin-9-yl]amino}-4-oxobutanoic acid;4-[{cis,cis-4-[(benzyloxy)carbonyl]-6-fluoro-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]quinolin-9-yl}(cyclopropyl)amino]-4-oxobutanoic acid;4-{cyclopropyl[cis,cis-6-fluoro-4-[(4-phenoxyphenyl ...

TETRACYCLINE COMPOUNDS

The present invention is directed to a compound represented by Structural Formula (I): 160.-. (canceled)62. The compound of claim 61 , wherein:{'sup': '4', 'Ris H, methyl, ethyl or propyl; and'}{'sup': '4′', 'R is selected from H, ethyl or propyl.'}64. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound of .66. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound of . This application is a continuation of U.S. application Ser. No. 15/400,674, filed on Jan. 6, 2017, which is a continuation of U.S. application Ser. No. 14/424,765 (now U.S. Pat. No. 9,573,895), filed on Feb. 27, 2015, which is the U.S. National Stage of International Application No. PCT/US2013/057690, filed Aug. 30, 2013, which claims the benefit of U.S. Provisional Application No. 61/695,947, filed on Aug. 31, 2012. The entire teachings of the above application are incorporated herein by reference.The tetracyclines are broad spectrum anti-microbial agents that are widely used in human and veterinary medicine. The total production of tetracyclines by fermentation or semi-synthesis is measured in the thousands of metric tons per year.The widespread use of tetracyclines for therapeutic purposes has led to the emergence of resistance to these antibiotics, even among highly susceptible bacterial species. Therefore, there is need for new tetracycline analogs with improved antibacterial activities and efficacies against other tetracycline responsive diseases or disorders.A first embodiment of the present invention is directed to a compound represented by Structural Formula (I):or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein.Another embodiment of the present invention is directed to a compound represented by Structural Formula (II):or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein.Another ...

BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS

Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. 2. The compound of selected from the group consisting of:{'sup': '3', '1-(6,9-ethano-4-phenyl-6,7,8,9-tetrahydro-5H-pyrido[3,2-c]azepin-2-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine;'}{'sup': '3', '1-(1,4-ethano-8-(4-fluorophenyl)-1,2,3,4-tetrahydro-1,5-naphthyridin-6-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine;'}{'sup': '3', '1-(1,4-ethano-8-(3-fluorophenyl)-1,2,3,4-tetrahydro-1,5-naphthyridin-6-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine;'}{'sup': '3', '1-(1,4-ethano-8-(3-trifluoromethylphenyl)-1,2,3,4-tetrahydro-1,5-naphthyridin-6-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine;'}{'sup': '3', '1-(1,4-ethano-8-(3-methoxyphenyl)-1,2,3,4-tetrahydro-1,5-naphthyridin-6-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine; and'}{'sup': '3', '1-(1,4-ethano-8-(2-methylphenyl)-1,2,3,4-tetrahydro-1,5-naphthyridin-6-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine.'}6. The compound of selected from the group consisting of:{'sup': '3', '1-(4-chloro-5,8-ethano-5,6,7,8-tetrahydrophthalazine-1-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine;'}{'sup': '3', '1-(4-(2-chlorophenyl)-5,8-ethano-5,6,7,8-tetrahydrophthalazine-1-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine;'}{'sup': '3', '1-(4-(3-cyanophenyl)-5,8-ethano-5,6,7,8-tetrahydrophthalazine-1-yl)-N-(4-(4-(pyrrolidin-1-yl)piperidinyl)-3-fluorophenyl)-1H-1,2,4-triazole-3,5-diamine;'}{'sup ...

CHEMOPROTEOMIC APPROACH FOR DISCOVERING COVALENT LIGANDS FOR DIVERSE PROTEIN TARGETS

Despite its power in identifying highly potent ligands for select protein targets, conventional medicinal chemistry is limited by its low throughput and lack of proteomic selectivity information. We seek to develop a chemoproteomic approach for discovering covalent ligands for protein targets in an unbiased, high-throughput manner. Tripartite probe compounds composed of a heterocyclic core, an electrophilic ‘warhead’ and an alkyne tag have been designed and synthesized for covalently labeling and identifying targets in cells. We have developed a novel condensation reaction to prepare 2-chloromethylquinoline (2-CMQ), a novel electrophilic heterocycle. These chloromethylquinolines potently and covalently bind to a number of cellular protein targets including Prostaglandin E Synthase 2 (PTGES2), a critical regulator of cell proliferation, apoptosis, angiogenesis, inflammation, and immune surveillance. 2. The compound of wherein PCis Caryl claim 1 , or Cheteroaryl.4. The compound of wherein LKor LKis Calkyl claim 1 , Caryl claim 1 , or Cheteroaryl.5. The compound of wherein Lm is Cl claim 1 , CH═CH claim 1 , or N═C═S.8. The compound of wherein:{'sub': 2', '1, 'Lm is halo or CH(X)R;'}{'sub': '2', 'Xis a leaving group; and'}{'sub': 1', '1-6, 'Ris H or Calkyl.'}19. A method of finding covalent ligands comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'contacting a protein-containing sample with any of the compounds of to form a modified protein; and'}{'sub': 1', '2', '1', '2', '2', '1', '1', '2, 'contacting the modified protein with a probe compound that includes an alkyne-containing moiety Rfor azido-containing moiety Rf, with the proviso that when Rfis an alkyne-containing moiety, Rfis an azido-containing moiety or when Rfis an alkyne-containing moiety, Rfis an azido-containing moiety wherein Rfreacts with Rfto form a ring.'}20. The method of wherein the probe compound includes a fluorophore. This application claims the benefit of U.S. provisional application ...

MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES

The present invention relates to compounds of the formula (1) and mixture comprising these compounds, which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which comprise these compounds and mixtures.

ORGANIC LIGHT-EMITTING DISPLAY APPARATUS

An organic light-emitting display apparatus includes a substrate, an organic light-emitting device disposed above the substrate, and an encapsulation unit disposed above the organic light-emitting device and sealing the organic light-emitting device, wherein the encapsulation unit includes a compound represented by Formula 1. 2. The organic light-emitting display apparatus of claim 1 , wherein{'sub': '1', 'Aris selected from a benzene group, a naphthalene group, an anthracene group, a phenanthrene group, a pyrene group, a chrysene group, a triphenylene group, an indene group, a fluorene group, a benzofluorene group, a spiro-bifluorene group, a carbazole group, a dibenzofuran group, a dibenzothiophene group, a pyridine group, a pyrazine group, a pyrimidine group, a pyridazine group, a pyrrole group, an imidazole group, a quinoline group, an isoquinoline group, a quinoxaline group, a quinazoline group, a triazine group, an indeno pyrazine group, an indeno pyridine group, a phenanthroline group, and a phenanthridine group.'}3. The organic light-emitting display apparatus of claim 1 , wherein{'sub': 1', '5', '9, 'Lto Land Lare each independently selected from{'sub': 2', '1', '20', '2', '20', '2', '20, '*—S—*′, *—O—*′, *—C(═O)—*′, *—S(═O)—*′, *—S(═O)—*′, a C-Calkylene group, a C-Calkenylene group, a C-Calkynylene group, a phenylene group, a pentalenylene group, an indenylene group, a naphthylene group, an azulenylene group, an indacenylene group, an acenaphthylene group, a fluorenylene group, a spiro-bifluorenylene group, a spiro-benzofluorene-fluorenylene group, a benzofluorenylene group, a dibenzofluorenylene group, a phenalenylene group, a phenanthrenylene group, an anthracenylene group, a fluoranthenylene group, a triphenylenylene group, a pyrenylene group, a chrysenylene group, a perylenylene group, a pentaphenylene group, a pyrrolylene group, a thiophenylene group, a furanylene group, a silolylene group, an imidazolylene group, a pyrazolylene group, a thiazolylene ...

INDENOTRIPHENYLENE DERIVATIVES AND ORGANIC LIGHT EMITTING DEVICE USING THE SAME

The present invention discloses a new indenotriphenylene derivatives and organic light emitting device using the derivatives. The organic light emitting device employing new indenotriphenylene derivatives as host material can lower driving voltage, prolong half-lifetime, increasing efficiency. The new indenotriphenylene derivatives are represented by the following formula (A): 9. According to claim 8 , an organic light emitting device comprising a layer of indenotriphenylene derivatives and functions as host material of a light emitting layer.10. According to claim 8 , an organic light emitting device comprising a layer of indenotriphenylene derivatives and functions as blue emitting host material of a light emitting layer. The present invention generally relates to indenotriphenylene derivatives and organic light emitting device using the derivatives. More specifically, the present invention relates to indenotriphenylene derivatives having general formula (A), an organic light emitting device employing indenotriphenylene derivatives as emissive layer material can lower driving voltage, prolong half-lifetime, increasing efficiency and increasing the stability of organic light emitting device.Organic light-emitting devices (OLEDs) have received much attention due to their potential applications to full-colored flat panel displays. Especially small size AMOLED panels had been installed in smart phone these years. Larger size AMOLED panels also had been installed in TV for prototype DEMO. OLEDs are generally composed of functionally divided organic multi-layers, e.g., hole injection layer (HIL), hole transporting layer (HTL), emissive layer (EML), electron transporting layer (ETL) and electron injection layer (EIL) and so on. A emissive material have good charge carrier mobility and excellent operational durability can lower driving voltage and power consumption, Increasing efficiency and half-lifetime of OLED.For full-colored flat panel displays in AMOLED, the ...

PROCESS FOR THE PREPARATION OF EXO-TERT-BUTYL N-(3-AZABICYCLO[3.2.1]OCTAN-8-YL)CARBAMATE

The present invention relates to a process for the preparation of a compound (I) or pharmaceutically acceptable salt thereof, which is useful as the key intermediate for the synthesis of compounds for prophylaxis and treatment of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome. 2. A process according to claim 1 , characterized in that the formation of the compound (IV) in step b) is performed in the presence of a reducing reagent at 0° C.-70° C. claim 1 , wherein the reducing reagent is selected from Na claim 1 , Pd/c and Raney-Ni; particularly the reaction is performed in the presence of Raney-Ni at 20° C.-30° C.3. A process according to or claim 1 , characterized in that the amount of (R)-(−)-Mandelic acid used in step c) is 0.1-2.0 eq. claim 1 , particularly 0.6 eq.4. A process according to any one of to claim 1 , characterized in that the compound (VI) synthesized in step d) is purified through recrystallization claim 1 , which was performed in a solvent claim 1 , wherein the solvent is selected from n-heptane claim 1 , hexane and petroleum ether; particularly the solvent is n-heptane.5. A process according to any one of to claim 1 , characterized in that the reduction reaction in step d) is performed at 20° C.-100° C. claim 1 , particularly at 65° C.-75° C. The present invention relates to a process for the preparation of a compound (I),or pharmaceutically acceptable salt thereof, which is useful as the key intermediate for the synthesis of compounds for prophylaxis and treatment of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi- ...

Process for the Preparation of Cycloheptapyridine CGRP Receptor Antagonists

The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process. 2. The compound of where Aris 2 claim 1 ,3-difluorophenyl and Ris hydrogen or a salt thereof.3. The compound of which is the dihydrochloride salt.4. The compound of where Aris 2 claim 1 ,3-difluorophenyl and Ris triisopropylsilyl or a salt thereof.5. The compound of which is the dihydrochloride salt. This Divisional application claims the benefit of U.S. Ser. No. 13/236,072 filed Sep. 19, 2011, now allowed, which in turn is a U.S. Non-Provisional application which claims the benefit of U.S. Provisional application Ser. No 61/392,183 filed Oct. 12, 2010, now expired.The disclosure generally relates to a synthetic process for preparing compounds of formula I including the preparation of chemical intermediates useful in this process.CGRP inhibitors are postulated to be useful in pathophysiologic conditions where excessive CGRP receptor activation has occurred. Some of these include neurogenic vasodilation, neurogenic inflammation, migraine, cluster headache and other headaches, thermal injury, circulatory shock, menopausal flushing, and asthma. CGRP antagonists have shown efficacy in human clinical trials. See Davis C D, Xu C. 2008 8(16):1468-79; Benemei S, Nicoletti P, Capone J G, Geppetti P. 2009 9(1):9-14. Epub 2009 Jan. 20; Ho T W, Ferrari M D, Dodick D W, Galet V, Kost J, Fan X, Leibensperger H, Froman S, Assaid C, Lines C, Koppen H, Winner P K. 2008 372:2115. Epub 2008 Nov. 25; Ho T W, Mannix L K, Fan X, Assaid C, Furtek C, Jones C J, Lines C R, Rapoport A M; 2008 70:1304. Epub 2007 Oct. 3.CGRP receptor antagonists have been disclosed in PCT publications WO 2004/092166, WO 2004/092168, and WO 2007/120590. The compound (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl4-(2-oxo-2,3-dihydro-1H-imidazo [4,5-1)]pyridin-1-yl)piperidine-1-carboxylate is an inhibitor of the ...

G-protein biased opioid receptor agonist/analgesics with reduced arrestin recruitment

In some aspects, the present disclosure provides compounds of the formula: wherein the variables are as defined herein. In some embodiments, these compounds may be used to reduce the pain of a patient. These compounds may be used in pain relief and show an improved pharmaceutical profile relative to other commonly used opiates and opioid derivatives.

SPIRO-COMPOUNDS AS SIP MODULATORS

The invention relates to heterocyclic compounds of formula (I) as SIP modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment or alleviation of diseases or disorders mediated by an SIP receptor. 2. A compound according to wherein m and n are both 0 or both 1.4. A compound according to wherein R1 is selected from the group consisting of -1 claim 3 ,3-cyclobutylene-R2 and —(C1-3)alkylene-R2 claim 3 , wherein the (C1)alkyl is unsubstituted claim 3 , and the (C2)alkyl and the (C3)alkyl are substituted with up to two CHgroups claim 3 , with (CH)to form a cyclopropyl moiety or with (CH)to form a cyclobutyl moiety.5. A compound according to wherein X is CH.6. A compound according to wherein R3 is selected from the group consisting of:(C3-6)cycloalkyl, preferably cyclohexyl, optionally substituted with (C1-4) alkyl; halogen,', 'cyano,', '(C1-4)alkyl optionally substituted with one or more fluoro atoms,', '(C1-4)alkoxy optionally substituted with one or more fluoro atoms or with (C3-6)cycloalkyl,', '(C3-5)cycloalkoxy optionally substituted with one or more fluoro atoms; and', '(C3-6)cycloalkyl optionally substituted with (C1-4)alkyl, (C1-4)alkoxy or a halogen atom,, 'monocyclic heterocycle, preferably oxanyl or pyridyl, optionally substituted with 1 or 2 substituents independently selected from the group consisting ofindanyl, optionally substituted with one or two halogen atoms8-10 membered fused bicyclic group, preferably preferably 2,3-dihydrobenzofuranyl, indanyl, indoly or 1,3-dioxaindanyl, optionally substituted with one or two halogen atoms; halogen,', 'cyano,', '(C1-4)alkyl optionally substituted with one or more fluoro atoms,', '(C1-4)alkoxy optionally substituted with one or more fluoro atoms or with (C3-6)cycloalkyl,', '(C3-5)cycloalkoxy optionally substituted with one or more fluoro atoms; and', '(C3-6)cycloalkyl optionally substituted with (C1-4)alkyl, (C1-4)alkoxy or a halogen atom., 'phenyl optionally substituted ...

CYCLIC AMINE SURFACE MODIFIER AND ORGANIC ELECTRONIC DEVICES COMPRISING SUCH CYCLIC AMINE SURFACE MODIFIER

The present invention relates to a cyclic amine surface modifier. In addition the present invention also relates to organic electronic devices comprising such cyclic amine surface modifier. 2. Self-assembled monolayer comprising the moiety according to claim 1 , wherein Xis selected from the group consisting of —S— claim 1 , —S—S— claim 1 , —C(═S)—S— claim 1 , —SO— claim 1 , —S—SO— claim 1 , —POH— and —POH—.3. Self-assembled monolayer comprising the moiety according to claim 1 , wherein Xis —S—.4. Self-assembled monolayer comprising the moiety according to claim 1 , wherein Ris —CH—.6. Self-assembled monolayer comprising the moiety according to claim 1 , wherein a is 0 or 1 claim 1 , b is 0 or 1 claim 1 , c is 0 or 1 claim 1 , and d is 0 or 1.7. Self-assembled monolayer comprising the moiety according to claim 1 , wherein a+b+c+d≧1.8. Self-assembled monolayer comprising the moiety according to claim 1 , wherein Xis C—Rand Rand Rtogether may be —(C—R)— claim 1 , with Rbeing selected from the group consisting of H claim 1 , F claim 1 , methyl claim 1 , ethyl claim 1 , methyl wherein one or more hydrogen is replaced by fluorine claim 1 , ethyl wherein one or more hydrogen is replaced by fluorine claim 1 , or two neighboring groups Rmay together form an aromatic ring system having from 6 to 24 aromatic ring atoms claim 1 , which may in turn be substituted by Rbeing selected from the group consisting of H claim 1 , F claim 1 , ethyl claim 1 , methyl wherein one or more hydrogen is replaced by fluorine claim 1 , ethyl wherein one or more hydrogen is replaced by fluorine.9. Self-assembled monolayer comprising the moiety according to claim 1 , wherein{'sup': 3', '4', '9, 'sub': '4', '(i) Rand Rtogether may be —(C—R)—; or'}{'sup': 4', '7', '3', '7', '9, 'sub': '3', '(ii) Xis N—Rand Rand Rtogether may be —(C—R)—; or'}{'sup': 4', '7', '3', '4', '7', '9', '9, 'sub': 2', '3, '(iii) Xis N—Rand R, Rand Rtogether may be —(C—R)—N—(C—R)—; or'}{'sup': 3', '6, '(iv) Xis N—R; or'}{'sup ...

FLUOROPHORE-BASED KINASE SENSORS

Disclosed are metal-binding analytical reagents that exhibit chelation-enhanced fluorescence (CHEF) upon binding to Mg. Also disclosed are methods of using the reagents for detecting the presence of or quantifying the activity of individual kinases or groups of kinases in a sample. 1112.-. (canceled)114117.-. (canceled)118. A method , comprising the step of:determining phosphorylation of a compound using fluorescence of the compound; wherein:the compound is an oligopeptide comprising a fluorophore; and a (phospho)S, a (phospho)T, or a (phospho)Y residue at the +2 or −2 position relative to the fluorophore.119120.-. (canceled)1221. The compound of claim , wherein the compound is X-EEPIY*V-C(Sx)-FG-Z (SEQ ID NO: 531) , or X-EEPIY*V-C(Sx)-VK-Z (SEQ ID NO: 547).123. The compound of claim 121 , wherein the compound is X-C(Sx)-HS*LPRFNR-Z (SEQ ID NO: 1409).124. The compound of claim 121 , wherein the compound is X-EDPEY*I-C(Sx)-IP-Z (SEQ ID NO: 304).125. The compound of claim 121 , wherein the compound is X-KKKKVKKRPQRADS*D-C(Sx)-FA-Z (SEQ ID NO: 3457).126. The compound of claim 121 , wherein the compound is X-EEPIY*I-C(Sx)-VP-Z (SEQ ID NO: 30) claim 121 , or X-GAEEPIY*I-C(Sx)-VPAKKKG-Z (SEQ ID NO: 42).127. The compound of claim 121 , wherein the compound is X-C(Sx)-KT*PKKAKKL-Z (SEQ ID NO: 212) claim 121 , or X-C(Sx)-QS*PKKG-Z (SEQ ID NO: 207).128. The compound of claim 121 , wherein the compound is X-DANPLMA-C(Sx)-GT*LTRRHQNGRF-Z (SEQ ID NO: 1200).129. The compound of claim 121 , wherein the compound is X-C(Sx)-FS*LRRKAK-Z (SEQ ID NO: 220).130. The compound of claim 121 , wherein the compound is X-RLPWWR-C(Sx)-YT*WVRARQVNTKQR-Z (SEQ ID NO: 4513).131. The compound of claim 121 , wherein the compound is X-LKP-C(Sx)-AS*FKKFA-Z (SEQ ID NO: 5485).132. The compound of claim 121 , wherein the compound is X-KKKKVKKRPQRAHS*D-C(Sx)-FS-Z (SEQ ID NO: 3470).133. The compound of claim 121 , wherein the compound is X-SR-C(Sx)-SS*PHQ[pS]EDEEE-Z (SEQ ID NO: 4741) claim 121 ,134. The ...

MORPHINAN COMPOUNDS

This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a σreceptor agonist that also has NMDA antagonist activity. 1. (canceled)3. The method of claim 2 , wherein the subject is suffering from or susceptible to diabetic neuropathic pain.4. The method of claim 2 , wherein the subject is suffering from or susceptible to epileptic seizures.5. The method of claim 2 , wherein the neurological disorder is schizophrenia. This application is a continuation of U.S. patent application Ser. No. 14/208,968, filed Mar. 13, 2014, which is a continuation of U.S. patent application Ser. No. 13/119,905, filed Jul. 1, 2011 (now U.S. Pat. No. 8,710,072), which is a National Stage application under 35 U.S.C. §371 of International Application No. PCT/US2009/057476, filed Sep. 18, 2009, which claims priority to U.S. Provisional Application Ser. No. 61/098,511, filed Sep. 19, 2008, which are incorporated by reference herein in their entirety.This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a sigma-1 receptor agonist that also has NMDA antagonist activity.Dextromethorphan, also known by its chemical name (+)-3-methoxy-17-methyl-(9α,13α,14α)-morphinan, is currently one of the most widely used antitussives.In addition to the physiological activity noted above, dextromethorphan is also an agonist of the σ2 receptor, an N-methyl-D-aspartate (NMDA) antagonist, and an α3β4 nicotinic receptor antagonist. Dextromethorphan inhibits neurotransmitters, such as glutamate, from activating receptors ...

MULTI-LAYER DEVICE FOR SELECTIVELY DETERMINING MAGNESIUM ION

The invention relates to devices comprising a sensor layer capable of binding magnesium ions and a scavenging layer that preferentially binds to calcium ions in the presence of both magnesium ions and calcium ions. The sensor layers can comprise known or novel luminionophores. The invention further relates to methods of selectively detecting magnesium ion concentration in the presence of calcium ions. 2. The device according to wherein the luminoionophore comprises an ionophore having one or more chelating moieties capable of binding to magnesium claim 1 , and a luminophoric moiety.5. The device according to claim 4 , wherein Z has the general formula (a) and one of Rand Ris —NH and the other is selected from the group consisting of hydrogen claim 4 , a lipophilic group claim 4 , a hydrophilic group and a reactive group for coupling to a polymer.6. The device according to claim 4 , wherein Z has the general formula (b) and Ris a bond.7. The device according to claim 4 , wherein Z has the general formula (c) and Ris a bond claim 4 , and wherein Rand Rare independently selected from hydrogen and methyl.10. The device according to wherein the luminoionophore is potassium 2 claim 1 ,2′-(4-(3-carboxylato-4-(2 claim 1 ,7-dichloro-6-oxido-3-oxo-3H-xanthen-9-yl)benzamido)-2-(carboxylatomethoxy)phenylazanediyl)diacetate claim 1 , and mixtures thereof.11. The device according to wherein the luminoionophore is potassium 2 claim 10 ,2′-(4-(3-carboxylato-4-(2 claim 10 ,7-dichloro-6-oxido-3-oxo-3H-xanthen-9-yl)benzamido)-2-(carboxylatomethoxy)phenylazanediyl)diacetate.12. The device according to wherein the substrate comprises a high-clarity polymer.13. The device according to wherein the substrate comprises high-clarity polyester film which is pretreated to promote adhesion.14. The device according to wherein the scavenging layer comprises a compound having one or more chelating moieties capable of selectively binding calcium ions in the presence of a mixture of calcium ions and ...

INDENOPYRIDINE-BASED COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Provided are an indenopyridine-based compound and an organic light-emitting device including the same. The indenopyridine-based compound is represented by Formula 1: 120.-. (canceled)22. The indenopyridine-based compound as claimed in claim 21 , wherein:{'sub': '1', 'Lis selected from an anthracenylene group, a chrysenylene group, and a pyrenylene group.'}23. The indenopyridine-based compound as claimed in claim 21 , wherein n1 is an integer of 1 or 2.25. The indenopyridine-based compound as claimed in claim 21 , wherein Rand Rare each independently selected from a hydrogen atom claim 21 , a deuterium atom and a methyl group.26. The indenopyridine-based compound as claimed in claim 21 , wherein Rto R claim 21 , and Rare each independently selected from a hydrogen atom claim 21 , a deuterium atom claim 21 , a fluorine atom claim 21 , a cyano group claim 21 , a nitro group claim 21 , and a methyl group.27. The indenopyridine-based compound as claimed in claim 21 , wherein:a2 is 1, 2, or 3, and{'sub': '4', 'Ris selected fromi) a phenyl group, a naphthyl group, and an anthryl group; andii) a phenyl group, a naphthyl group, and an anthryl group, each substituted with at least one selected from a hydrogen atom, a deuterium atom, a halogen atom, a hydroxyl group, a cyano group, a nitro group, a methyl group, an ethyl group, an n-propyl group, an iso-propyl group, a tert-butyl group, a phenyl group, a naphthyl group, and an anthryl group.28. The indenopyridine-based compound as claimed in claim 21 , wherein:a2 is 1, 2, or 3, and{'sub': '4', 'Ris selected from a phenyl group, a 1-naphthyl group, and a 2-naphthyl group.'}29. The indenopyridine-based compound as claimed in claim 21 , wherein a2 is an integer of 0 or 1.30. The indenopyridine-based compound as claimed in claim 21 , wherein:a2 is 1; anda1 is 3.34. An organic light-emitting device (OLED) claim 21 , comprising:a first electrode;a second electrode facing the first electrode; andan organic layer that is disposed ...

Fluorene compound and organic electroluminescent device using the same

The present invention discloses a new fluorene compound and organic EL device using the compound. The organic EL device employing the new fluorene compound as host material can lower driving voltage, prolong half-lifetime. The fluorene compound can functions as blue emitting host material of a light emitting layer and improve CIE colour purity in blue emitting device. The fluorene compound are represented by the following formula(A): Wherein R 1 to R 6 are identical or different. R 1 to R 6 are independently selected from the group consisting of a hydrogen atom, a halide, alkyl group having 1 to 20 carbon atoms, a substituted or unsubstituted aryl group having 6 to 30 carbon atoms, a substituted or unsubstituted aralkyl group having 6 to 30 carbon atoms, a substituted or unsubstituted heteroaryl group having 6 to 30 carbon atoms. R 7 ˜R 13 are identical or different R 7 to R 13 are independently selected from the group consisting of hydrogen atom, halide, alkyl group, aryl group, heteroaryl group. m and n are independently an integer of 0 to 3, X is selected from carbon or nitrogen.

RADICAL ORBITAL SWITCHING

Described herein are distonic radical anion species of formula (I): RAD-L-NEG; wherein RAD is a group comprising a radical; NEG is a group comprising an anion, which is capable of bonding to a proton or other cation; L is a linker that links NEG to RAD; and the radical of RAD is not π-conjugated to the anion of NEG. 194-. (canceled)96. The structure of Formula (I) as defined in claim 95 , wherein the lowest Singly-Occupied Molecular Orbital (SOMO) of RAD is lower in energy than a Doubly-Occupied Molecular Orbital (DOMO) of NEG; and wherein the SOMO of RAD is higher in energy than the DOMOs of NEG when the negative point charge of NEG is neutralized.97. The structure of Formula (I) as defined in claim 95 , wherein NEG is a surface or structure capable of bearing and/or carrying a negative point charge claim 95 , and where the negative point charge is capable of being neutralised claim 95 , wherein the structure capable of bearing and/or carrying a negative point charge is optionally selected from the group comprising: an electrode claim 95 , a metallic or non-metallic structure claim 95 , or graphene.98. The structure of Formula (I) as defined in claim 95 , wherein the negative point charge is selected from the group comprising an electron claim 95 , an electric charge claim 95 , a negative potential claim 95 , or a negative coulombic charge; and where the negative point charge is capable of being neutralised by the substantial removal claim 95 , dissipation or inversion of that charge.99. The structure of Formula (I) as defined in claim 95 , wherein the negative point charge is a group comprising an anion claim 95 , which is capable of being neutralised by bonding to a proton or other cation claim 95 , wherein the anion optionally comprises a sterically and/or electronically destabilised anion.100. The structure of Formula (I) as defined in claim 99 , where neutralisation is achieved by:removal of the proton or other cation bonded to the anion of NEG;increasing the ...

HERBICIDAL COMPOUNDS

The present invention relates to compounds of Formula (I), wherein R1, R2, R3, R4 and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants. 2. A compound of according to claim 1 , wherein Ris 1-propynyl claim 1 , Ris methyl or methoxy and Ris methyl or methoxy.3. A compound according to claim 1 , wherein Ris methyl.4. A compound according to claim 1 , wherein Ris methyl.5. A compound according to claim 1 , wherein Ris methoxy.6. A compound according to claim 1 , wherein Ris —S(O)NRR.7. A compound according to claim 1 , wherein Ris —S(O)(═NR)R.8. A compound according to claim 1 , wherein G is hydrogen.9. A compound according to claim 1 , wherein G is —C(O)C-Calkyl.10. A compound according to claim 1 , wherein G is —C(O)—O—C-Calkyl.11. A herbicidal composition comprising a compound of Formula (I) according to and an agriculturally acceptable formulation adjuvant.12. A herbicidal composition according to claim 11 , further comprising at least one additional pesticide.13. A herbicidal composition according to claim 12 , wherein the additional pesticide is a herbicide or herbicide safener.14. A method of controlling weeds at a locus comprising application to the locus of a weed controlling amount of a composition according to .15. A method of controlling weeds by applying a compound of Formula (I) as defined in . The present invention relates to novel herbicidal compounds, to processes for their preparation, to herbicidal compositions which comprise the novel compounds, and to their use for controlling weeds.Herbicidal cyclic dione compounds substituted by a phenyl which has an alkynyl-containing substituent are disclosed in, for example, WO2014/096289 and WO2015/197468. The present invention relates to novel herbicidal cyclohexanedione derivatives with improved properties.Thus, according to the present invention there is ...

DEXTRORPHAN PRODRUGS AND PROCESSES FOR MAKING AND USING THEM

The presently described technology provides compositions of one or more of oxoacids, polyethylene glycols, and/or vitamin compounds chemically conjugated to dextrorphan, (+)-17-methylmorphinan-3-ol), to form novel prodrugs and compositions of dextrorphan. 2. The compound of claim 1 , wherein Land Yare present claim 1 , Gis at least one oxoacid claim 1 , and m is 1-3.3. The compound of claim 1 , wherein Gis at least one oxoacid selected from the group consisting of aliphatic carboxylic acid claim 1 , aryl carboxylic acid claim 1 , dicarboxylic acid claim 1 , polycarboxylic acid claim 1 , standard amino acids claim 1 , non-standard amino acids claim 1 , and synthetic amino acids claim 1 , and combinations thereof.4. The compound of wherein Gis a combination of at least two oxoacids claim 3 , wherein at least one of the at least two oxoacids is selected from the group consisting of aliphatic carboxylic acid claim 3 , aryl carboxylic acid claim 3 , dicarboxylic acid claim 3 , and polycarboxylic acid claim 3 , and combinations thereof claim 3 , and at least one of the at least two oxoacids is selected from standard amino acids claim 3 , non-standard amino acids claim 3 , synthetic amino acids claim 3 , and combinations thereof.5. The compound of claim 4 , wherein the at least one of the at least two oxoacids is valine.8. The compound of claim 7 , wherein where Land Yare absent claim 7 , M is —(CRR) claim 7 , Gis at least one oxoacid claim 7 , and m is 1-3.9. The compound of claim 7 , wherein the at least one oxoacid is acetic acid.12. The compound of claim 11 , wherein at least one of Gand Gis at least one oxoacid.13. The compound of claim 12 , wherein Gand Gare each acetic acid.15. A composition wherein the composition comprises the compound of 39 or a pharmaceutically acceptable salt of the compound.16. A composition wherein the composition comprises the compound of or a pharmaceutically acceptable salt of the compound.17. The composition of claim 15 , wherein the ...

QUINOLINE DERIVATIVE COMPOUND, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

The present invention relates to a novel quinoline derivative compound, an optical isomer thereof, a pharmaceutically acceptable salt thereof, and a hydrate or a solvate thereof. The novel quinoline derivative compound, the optical isomer thereof, the pharmaceutically acceptable salt thereof, and the hydrate or the solvate thereof accelerates gastrointestinal movement, and thus can effectively prevent or treat gastrointestinal motility disorders. 3. The quinoline derivative compound of represented by Chemical Formula 1 claim 1 , the optical isomer claim 1 , the pharmaceutically acceptable salt claim 1 , or the hydrate or solvate thereof claim 1 , wherein the quinoline derivative compound represented by Chemical Formula 1 is (S)-4-oxo-4-(1 claim 1 ,2 claim 1 ,9 claim 1 ,10-tetramethoxy-4 claim 1 ,5 claim 1 ,6a claim 1 ,7-tetrahydro-dibenzo[de claim 1 ,g]quinoline-6-yl)-butyric acid ethyl ester.5. The method of claim 4 , wherein Rto Rare methoxy claim 4 , Ris ethyl claim 4 , and X is Cl.7. The pharmaceutical composition of claim 6 , wherein the compound represented by Chemical Formula 1 is (S)-4-oxo-4-(1 claim 6 ,2 claim 6 ,9 claim 6 ,10-tetramethoxy-4 claim 6 ,5 claim 6 ,6a claim 6 ,7-tetrahydro-dibenzo[de claim 6 ,g]-quinoline-6-yl)-butyric acid ethyl ester. The present invention relates to a quinoline derivative compound, an optical isomer thereof, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, a method for the preparation thereof, and a pharmaceutical composition comprising the same.Pathological mechanisms of functional gastrointestinal diseases such as gastrointestinal motility disorders act together, manifesting one or usually multiple symptoms. Depending on the symptoms, functional gastrointestinal diseases are classified into ulcer-like dyspepsia, dysmotility-like dyspepsia, reflux-like dyspepsia, nonspecific or unspecified functional dyspepsia.Functional gastrointestinal disorders have been found in 25˜50% of the world population ...

CONDENSED CYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

A condensed cyclic compound having the following structure and an organic light-emitting device including the same are provided: 2. The condensed cyclic compound of claim 1 , wherein{'sub': 1', '2', '11', '12, 'rings B, B, B, and Bin Formulae 2A to 2F and 3B are each independently selected from a benzene group, a naphthalene group, an anthracene group, a phenanthrene group, a pyrene group, a chrysene group, a triphenylene group, an indene group, a fluorene group, a benzofluorene group, a spiro-bifluorene group, a carbazole group, a dibenzofuran group, a dibenzothiophene group, a pyridine group, a pyrazine group, a pyrimidine group, a pyridazine group, a pyrrole group, an imidazole group, a quinoline group, an isoquinoline group, a quinoxaline group, a quinazoline group, a triazine group, an indenopyrazine group, an indenopyridine group, a phenanthroline group, and a phenanthridine group.'}3. The condensed cyclic compound of claim 1 , wherein{'sub': 1', '23', '24, 'Xin Formulae 2B, 2D, and 2F is O, S, or C(R)(R).'}4. The condensed cyclic compound of claim 1 , wherein{'sub': 1', '2', '11', '21', '22, 'L, L, L, L, and Lin Formulae 1, 2A to 2F, and 3C are each independently selected froma phenylene group, a pentalenylene group, an indenylene group, a naphthylene group, an azulenylene group, an indacenylene group, an acenaphthylene group, a fluorenylene group, a spiro-bifluorenylene group, a spiro-benzofluorene-fluorenylene group, a benzofluorenylene group, a dibenzofluorenylene group, a phenalenylene group, a phenanthrenylene group, an anthracenylene group, a fluoranthenylene group, a triphenylenylene group, a pyrenylene group, a chrysenylene group, a perylenylene group, a pentaphenylene group, a pyrrolylene group, a thiophenylene group, a furanylene group, a silolylene group, an imidazolylene group, a pyrazolylene group, a thiazolylene group, an isothiazolylene group, an oxazolylene group, an isoxazolylene group, a pyridinylene group, a pyrazinylene group, a ...

SULFONIC ACID DERIVATIVE COMPOUND, PHOTOACID GENERATOR, RESIST COMPOSITION, CATIONIC POLYMERIZATION INITIATOR, AND CATIONICALLY POLYMERIZABLE COMPOSITION

Provide are: a sulfonic acid derivative compound which has high absorbance for light having a wavelength of 365 nm and exhibits high solubility in organic solvents and good acid generation rate; a photoacid generator; a resist composition; a cationic polymerization initiator; and a cationically polymerizable composition. The sulfonic acid derivative compound is represented by the following Formula (I): 2. The sulfonic acid derivative compound according to claim 1 , wherein said X is an alkyl group having 4 carbon atoms.3. The sulfonic acid derivative compound according to claim 1 , wherein said R is a perfluoroalkyl group having 1 to 8 carbon atoms.4. A photoacid generator comprising the sulfonic acid derivative compound according to .5. A cationic polymerization initiator comprising the sulfonic acid derivative compound according to .6. A resist composition comprising the photoacid generator according to .7. A cationically polymerizable composition comprising the cationic polymerization initiator according to . The present invention relates to a sulfonic acid derivative compound, a photoacid generator, a resist composition, a cationic polymerization initiator, and a cationically polymerizable composition. More particularly, the present invention relates to: a sulfonic acid derivative compound which has high absorbance for light having a wavelength of 365 nm and exhibits high solubility in organic solvents and good acid generation rate; a photoacid generator; a resist composition; a cationic polymerization initiator; and a cationically polymerizable composition.Sulfonyloxyimides having a naphthalimino group which is a radioactive functional group are substances that generate an acid when irradiated with an energy beam such as light, and they are used as, for example, photoacid generators in photolithography resist compositions used for the formation of an electronic circuit such as a semiconductor, and as cationic polymerization initiators contained in ...

ANTIDIABETIC TRICYCLIC COMPOUNDS

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia. 4. The compound according to wherein n is 1; or a pharmaceutically acceptable salt thereof.5. The compound according to wherein Ris hydrogen; or a pharmaceutically acceptable salt thereof.6. The compound according to wherein X is oxygen; or a pharmaceutically acceptable salt thereof.7. The compound according to whereinT is selected from the group consisting of: CH and N;U is selected from the group consisting of: CH and N;V is selected from the group consisting of: CH and N; andW is selected from the group consisting of: CH and N,provided that one of T, U, V and W is N;or a pharmaceutically acceptable salt thereof.8. The compound according to wherein T is CH; U is CH; V is N; and W is CH; or a pharmaceutically acceptable salt thereof.9. The compound according to whereinA is a bicyclic aryl ring,{'sup': a', 'a', '8, 'sub': 1-6', '1-6, 'wherein each bicyclic aryl ring is unsubstituted or substituted with one to six substituents selected from R, and wherein two Rsubstituents together with the carbon atom to which they are attached may form a 3-6 membered cycloalkyl ring, or a 3-6 membered cycloheteroalkyl ring containing 0 to 3 heteroatoms independently selected from oxygen, sulfur, and NR, and wherein each 3-6 membered cycloalkyl and each 3-6 membered cycloheteroalkyl ring is unsubstituted or substituted with 1 to 4 substituents selected from: —Calkyl, —O—Calkyl, halogen and OH;'}or a ...

CYCLIC AMINE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS

There is described a novel group of cyclic amine derivative compounds, having an EPreceptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. 2. A cyclic amine compound of formula (I) according to wherein Ar is phenyl having in 4 position one substituent selected from fluorine claim 1 , cyano or trifluorormethyl.3. A cyclic amine compound of formula (I) according to wherein Ris hydrogen and Ris methyl or both Rand Rare fused together to form a cyclopropyl ring.5. A cyclic amine compound of formula (IB) according to wherein Ar is phenyl having in 4-position at least one substituent selected from the group consisting of: fluorine claim 4 , cyano and trifluoromethyl.6. A cyclic amine compound of formula (IB) according to wherein Rand Rare methyl or are linked together to form a cyclopropyl ring.7. A cyclic amine compound of formula (IB) according to anyone of wherein Ris hydrogen.8. A cyclic amine compound of formula (IB) according to wherein Rand Rare independently selected from hydrogen claim 4 , fluorine claim 4 , methyl or are fused together to form a cyclopropyl ring.9. A cyclic amine compound of formula (IB) according to wherein n is 1 and Rand Rare independently selected from hydrogen claim 4 , fluorine claim 4 , methyl.10. A cyclic amine compound of formula (IB) according to wherein n is 2 and Ar is phenyl substituted in 4 position with at least one substituent selected from the group consisting of: fluorine claim 4 , cyano and trifluoromethyl.11. A cyclic amine compound of formula (IB) according to wherein n is 2 claim 4 , both Rand Rare fluorine or are fused together to form a cyclopropyl ring.13. A cyclic amine compound of formula (IC) according to wherein Ar is phenyl having in 4-position at least one substituent selected from the group consisting of: fluorine claim 12 , cyano and trifluoromethyl.14. A cyclic amine compound of formula (IC) according to ...