Novel Indicator Platform

A novel indicator platform comprises a plurality of 1H-lndol-3-yl indicator compounds that are capable of converting to a signalophore compound in response to an external stimulus. In one class of indicator compounds, the resulting signalophores are 2-benzylideneindoline compounds that are formed by an intermolecular Aldol-type process; in a further class of indicator compounds, the resulting signalophores are 10H-indolo[1,2-a]indole compounds that are formed by an intramolecular Aldol-type process. The indicators can be used in a wide array of applications relating, for example, to biological systems or optical data storage.

Wnt inhibitors for human stem cell differentiation

Methods and small molecule compounds for stem cell differentiation and treatment of animals with diseases are provided. One example of a class of compounds that may be used is represented by the compound of Formula I and II: or a pharmaceutically acceptable salt or solvate thereof, wherein A, X, Q, R 1 , R 2 , R 3 , R 4 are as described herein.

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

There are described RORγ modulators of the formula (I), 10. The compound according to wherein{'sup': 1', '1a', '1a, 'sub': '1-6', 'Ris halo, phenyl substituted with 0-3 R, or Calkyl substituted with 0-3 R;'}{'sup': 1a', 'a', '2e', '2f', 'b', '2e', '2f', 'a, 'sub': 3', '1-6, 'Ris, independently at each occurrence, hydrogen, CF, halo, Calkyl substituted with 0-3 R, —(CRR)r-OR, and —(CRR)r-phenyl substituted with 0-3 R,'}{'sup': '1b', 'sub': 3', '3', '1', '4, 'Ris, independently at each occurrence, hydrogen, CD, halo, CF, and C-Calkyl;'}{'sup': 2', '2c', '2a', '2b', '2d', '11', '11', 'a, 'sub': 2', '1-6', '2', 'p, 'Ris hydrogen, SOR, Calkyl substituted with 0-3 R, COR, —C(O)R, —C(O)NRR; or a 5-7 membered heterocycle comprising carbon atoms, and 1-4 heteroatoms selected from N, O, P(═O) and S(O)substituted with 0-4 R,'}{'sup': 2a', 'a, 'sub': '1-6', 'Ris hydrogen or Calkyl substituted with 0-3 R;'}{'sup': 2b', 'a', 'a', '2e', '2f', 'a', '2e', '2f', 'a, 'sub': 1-6', '3-6', 'p, 'Ris hydrogen, Calkyl substituted with 0-2 R, Ccycloalkyl substituted with 0-3 R, —(CRR)r-5-7 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O, P(═O) and S(O)substituted with 0-4 R, or —(CRR)r-phenyl substituted with 0-3 R;'}{'sup': 2c', 'a', 'a', 'a', 'a', '2e', '2f', 'a, 'sub': 1-6', '2-6', '3-10', '6-10', 'p, 'Ris, independently at each occurrence, hydrogen, Calkyl substituted with 0-3 R, Calkenyl substituted with 0-3 R, Ccycloalkyl substituted with 0-3 R, Caryl substituted with 0-3 R, or —(CRR)r-5-10-membered heterocycle containing 1-4 heteroatoms selected from N, O, P(═O) and S(O), substituted with 0-4 R;'}{'sup': 2d', 'd', '11', '11', 'd', '2e', '2f', 'a', 'a, 'sub': 1-6', '1-6', '3-10', 'p, 'Ris, independently at each occurrence, hydrogen, Calkyl substituted with 0-3 R, Chaloalkyl, C(O)NRR, Ccycloalkyl substituted with 0-2 R, (CRR)r-phenyl substituted with 0-2 R, or a 4-10 membered heterocycle containing 1-4 heteroatoms selected from N, O, P(═O) and S(O), ...

DIARYLAMINE-BASED COMPOUND, ANTI-AGING AGENT, AND POLYMER COMPOSITION

The present invention provides a diarylamine-based compound represented by General Formula (1): 5. The diarylamine-based compound according to claim 1 , wherein Aand Aare a 1 claim 1 ,4-phenylene group.8. The composition according to claim 7 , wherein Rand Reach independently represent a linear or branched Cto Calkyl group which may have a substituent claim 7 , or a phenyl group which may have a substituent.10. The composition according to claim 1 , wherein a weight ratio of the diarylamine-based compound to the condensed heterocyclic compound is 30:1 to 1:30 as “diarylamine-based compound:condensed heterocyclic compound”.11. An antioxidant comprising the diarylamine-based compound according to claim 1 , or the composition according to any one of to .12. The antioxidant according to claim 11 , wherein the antioxidant is an antioxidant for a polymer.13. A polymer composition comprising a polymer and the antioxidant according to .14. The polymer composition according to claim 13 , wherein the polymer is a synthetic resin.15. The polymer composition according to claim 13 , wherein the polymer is a rubber.16. The polymer composition according to claim 15 , wherein the rubber is an acrylic rubber.17. The polymer composition according to claim 13 , wherein a content of the antioxidant is 0.05 to 30 parts by weight relative to 100 parts by weight of the polymer.18. An antioxidant comprising the composition according to . The disclosure relates to a novel diarylamine-based compound which has an excellent antioxidant effect on polymer materials required to have high heat resistance (for example, heat resistance in a high temperature range of 190° C. or more) and can be suitably used as an antioxidant, and an antioxidant and a polymer composition comprising such a diarylamine-based compound.With development of petrochemistry, polymers composed of organic compounds have contributed to human development in a variety of forms such as plastics, rubber, fibers, and films. Because ...

STRIGOLACTAM DERIVATIVES AS PLANT GROWTH REGULATING COMPOUNDS

The present invention relates to novel strigolactam derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds. 1. A compound of Formula (II).whereinW is O or S;{'sub': 1', '3, 'R2 and R3 are independently hydrogen, or C-Calkyl;'}{'sub': 1', '3', '1', '3', '1', '3', '1', '3', '1', '3, 'R4 and R5 are independently hydrogen, halogen, nitro, cyano, C-Calkyl, C-Chaloalkyl, C-Calkoxy, hydroxyl, —OC(O)R9, amine, N—C-Calkyl amine, or N,N-di-C-Calkyl amine;'}{'sub': 1', '6', '1', '6', '1', '6, 'R9 is hydrogen, C-Calkyl, C-Calkoxy, or C-Chaloalkyl;'}{'sub': 1', '6', '1', '6', '1', '8', '1', '8', '1', '8', '1', '6', '1', '6', '1', '8', '1', '8', '1', '8, 'R8 is hydrogen, nitro, cyano, C-Calkyl, C-Chaloalkyl, halogen, C-Calkylthio, C-Chaloalkylthio, C-Calkylsulfinyl, N—C-Calkyl amine, N,N-di-C-Calkyl amine, C-Chaloalkylsulfinyl, C-Calkylsulfonyl, or C-Chaloalkylsulfonyl;'}{'sub': 1', '6', '1', '6', '1', '6', '1', '6', '1', '8', '1', '8, 'R1 is hydrogen, C-Calkoxy, hydroxyl, amine, N—C-Calkyl amine, N,N-di-C-Calkyl amine, C-Calkyl optionally substituted by one to five R10, C-Calkylcarbonyl, C-Calkoxycarbonyl, aryl optionally substituted by one to five R10, heteroaryl optionally substituted by one to five R10, or benzyl optionally substituted by one to five R10;'}{'sub': 1', '6', '1', '6', '1', '6', '2', '6', '2', '6, 'R10 is hydrogen, cyano, nitro, halogen, C-Calkyl, C-Calkoxy, C-Chaloalkyl, C-Calkenyl, or C-Calkynyl;'}{'sub': 1', '2', '3', '4', '1', '2', '3', '4', '1', '2', '3', '4, 'A, A, Aand Aare each independently C—X, C—Y or nitrogen, wherein each X or Y may be the same or different, and provided that no more than two of A, A, Aand Aare nitrogen and that at least one of A, A, Aand Ais C—X;'}{'sub': 1', '6', '1', '6', '1', '6', '1', '3', '1', '6', '1', '6, 'Y is hydrogen, halogen, cyano, hydroxyl, —OC(O)R9, ...

METHODS OF PREPARING TECOVIRIMAT

Disclosed are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. 128.-. (canceled)30. The method of claim 29 , wherein a base is present in the reaction of step (a) claim 29 , wherein said base is selected from the group consisting of: pyridine claim 29 , 4-dimethylaminopyridine claim 29 , triethylamine and diisopropylethylamine.31. The method of claim 29 , wherein step (a) is carried out under nitrogen atmosphere at a temperature below about 20° C.32. The method of claim 29 , wherein step (b) is carried out in the presence of dimethylformamide claim 29 , methyl 2 claim 29 ,2-difluoro-2-(fluorosulfonyl)acetate and copper (I) iodide.33. The method of claim 29 , wherein said N-[(3aR claim 29 ,4R claim 29 ,4aR claim 29 ,5aS claim 29 ,6S claim 29 ,6aS)-3 claim 29 ,3a claim 29 ,4 claim 29 ,4a claim 29 ,5 claim 29 ,5a claim 29 ,6 claim 29 ,6a-octahydro-1 claim 29 ,3-dioxo-4 claim 29 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide collected in step (c) is further purified by column chromatography.3436.-. (canceled) This application claims the benefit of U.S. Provisional Patent Application No. 61/683,905, filed on Aug. 16, 2012, the disclosure of which is hereby fully incorporated herein by reference.Described herein are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Tecovirimat, with a proprietary name of ST246®, has a chemical name of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide.The Orthopox genus (Orthopoxviridae) is a member of the Poxviridae family and the Choropoxivirinae subfamily. The genus consists of numerous ...

METHODS OF PREPARING TECOVIRIMAT

Disclosed are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. 111.-. (canceled)13. The method of claim 12 , wherein step (a) is carried out in anhydrous toluene under nitrogen atmosphere and reactants heated to reflux.14. The method of claim 12 , wherein said acid in step (b) is HCl.15. The method of claim 12 , wherein compound 10 is dissolved in i-PrOAc prior to the reaction of step (b).16. The method of claim 12 , wherein a base is present in the reaction of step (c) claim 12 , wherein said base is selected from the group consisting of: pyridine claim 12 , 4-dimethylaminopyridine claim 12 , triethylamine and diisopropylethylamine.17. The method of claim 12 , wherein said 4-(trifluoromethyl)benzoyl halide is 4-(trifluoromethyl)benzoyl chloride.18. The method of claim 12 , wherein step (c) is carried out at a temperature of about 10 to about 25° C.19. The method of claim 12 , wherein step (d) is carried out in toluene under nitrogen atmosphere at a temperature above about 110° C.20. The method of claim 12 , wherein said N-[(3aR claim 12 ,4R claim 12 ,4aR claim 12 ,5aS claim 12 ,6S claim 12 ,6aS)-3 claim 12 ,3a claim 12 ,4 claim 12 ,4a claim 12 ,5 claim 12 ,5a claim 12 ,6 claim 12 ,6a-octahydro-1 claim 12 ,3-dioxo-4 claim 12 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide collected in step (e) is further purified by column chromatography.2135.-. (canceled)37. (canceled) This application claims the benefit of U.S. Provisional Patent Application No. 61/683,905, filed on Aug. 16, 2012, the disclosure of which is hereby fully incorporated herein by reference.Described herein are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the ...

FULLERENE DERIVATIVE AND LUBRICANT

A fullerene derivative, used as a lubricant, includes, in a molecule: a fullerene backbone; and n pyrrolidine rings each being condensed to the fullerene backbone, each of the pyrrolidine rings including one aryl group including a group including m perfluoropolyether chains, “m” being an integer from 2 to 5 and “n” being an integer from 1 to 5. 1. A fullerene derivative comprising , in a molecule:a fullerene backbone; andn pyrrolidine rings each being condensed to the fullerene backbone,each of the pyrrolidine rings including one aryl group including a group including m perfluoropolyether chains, “m” being an integer from 2 to 5 and “n” being an integer from 1 to 5.3. The fullerene derivative according to claim 2 , wherein the “R” is an alkyl group or an aryl group whose carbon number is less than or equal to 24.4. The fullerene derivative according to claim 1 , wherein the fullerene backbone is C.5. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains includes at least a partial structure selected from —(CF)O— in which “x” is an integer from 1 to 5.6. The fullerene derivative according to claim 5 , wherein the group including perfluoropolyether chains includes a partial structure expressed by —(CFCFO)(CFO)— in which each of “y” and “z” is an integer from 1 to 50.7. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains is configured only by a perfluoropolyether structure.8. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains is a straight-chain.9. A lubricant comprising the fullerene derivative according to .10. The lubricant according to claim 9 , further comprising a perfluoropolyether chemical compound that does not include a fullerene backbone. This application is a continuation-in-part application filed under 35 U.S.C. 111(a) claiming the benefit under 35 U.S.C. 120 and 365(c) of PCT International Application No. PCT ...

FULLERENE DERIVATIVE AND N-TYPE SEMICONDUCTOR MATERIAL

The present invention is a material that exhibits excellent properties as an n-type semiconductor, in particular for use in organic thin-film solar cells. The present invention relates to a fullerene derivative represented by formula (1): 3. The fullerene derivative according to claim 2 , wherein Rand Rare the same or different claim 2 , and each represents a hydrogen atom or a fluorine atom;{'sup': 1a', '1b, 'at least one of Rand Ris a fluorine atom;'}{'sup': 1c', '1d, 'Rand Rare the same or different, and each represents a hydrogen atom or a fluorine atom;'}{'sup': 2', '2, 'i': a', 'b, 'Rand Rare the same or different, and each represents a hydrogen atom, a fluorine atom, alkyl, or alkoxy; and'}{'sup': 2', '2, 'i': c', 'd, 'Rand Reach represents a hydrogen atom.'}4. The fullerene derivative according to claim 1 , wherein the ring A is Cfullerene or Cfullerene.5. An n-type semiconductor material consisting of the fullerene derivative according to .6. The n-type semiconductor material according to claim 5 , which is for use in an organic thin-film solar cell.7. An organic power-generating layer comprising the n-type semiconductor material according to .8. A photoelectric conversion element comprising the organic power-generating layer according to .9. The photoelectric conversion element according to claim 8 , which is an organic thin-film solar cell. The present invention relates to a fullerene derivative, an n-type semiconductor material, and the like.Organic thin-film solar cells are formed by a coating technique with a solution of an organic compound, which is a photoelectric conversion material. The cells have various advantages: for example, 1) device production cost is low; 2) area expansion is easy; 3) the cells are more flexible than inorganic materials, such as silicon, thus enabling a wider range of applications; and 4) resource depletion is less likely. As such, organic thin-film solar cells have been developed, and the use of the bulk heterojunction ...

NOVEL METAL COMPLEX, METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING GAMMA-LACTAM COMPOUND USING SAME

The present invention relates to a novel metal complex, a method for producing same, and a method for producing a gamma-lactam compound using same, and the metal complex according to the present invention is used as a catalyst for producing a gamma-lactam compound and can efficiently produce a gamma-lactam compound with an excellent yield and excellent selectivity. 3. The method of preparing a gamma-lactam compound of claim 1 , wherein the metal complex is used at 0.01 to 0.1 mol with respect to 1 mol of the dioxazol-one compound.4. The method of preparing a gamma-lactam compound of claim 1 , wherein the base is one or two or more selected from NaBAr(sodium tetrakis [3 claim 1 ,5-bis (trifluoromethyl)phenyl]borate) claim 1 , AgSbF(silver hexafluoroantimonate(V)) claim 1 , AgNTf(silver bis(trifluoromethanesulfonyl)imide) claim 1 , AgBF(silver tetrafluoroborate) claim 1 , AgPF(silver hexafluorophosphate) claim 1 , AgOTf (silver trifluoromethanesulfonate) claim 1 , and AgOAc (silver acetate).5. The method of preparing a gamma-lactam compound of claim 1 , wherein the base is used at 0.01 to 0.1 mol with respect to 1 mol of the dioxazol-one compound.6. The method of preparing a gamma-lactam compound of claim 1 , wherein the amidating is performed at 20 to 60° C.8. The method of preparing a gamma-lactam compound of claim 2 , wherein{'sub': a1', 'a5, 'Rto Rare independently of each other hydrogen, (C1-C20)alkyl, or (C3-C20)heterocycloalkyl;'}{'sub': a6', 'a5', 'a6, 'Ris independently of each other hydrogen, (C1-C20)alkyl, (C3-C20)cycloalkyl, (C2-C20)alkenyl, (C2-C20)alkynyl, (C6-C20)aryl, or (C3-C20)heteroaryl, or Rand Rmay be connected to form a (C5-C8)spiro ring,'}{'sub': a2', 'a3', 'a1', 'a2, 'Rand Rmay be connected by (C2-C10)alkenylene to form a (C6-C12)aromatic ring, and in this case, Rand Rare not present,'}{'sub': a3', 'a6, 'Rand Rmay be connected to each other to form a (C3-C20)alicyclic ring with or without an aromatic ring,'}{'sub': a3', 'a4', 'a6, 'Rand Rand ...

POLYMORPHIC FORMS OF ST-246 AND METHODS OF PREPARATION

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions. 110.-. (canceled)11. A polymorph Form II of ST-246 which shows a X-ray powder diffraction pattern having characteristic peaks at a reflection angle 20 according to .12. An isolated polymorph according to that is at least about 70% free of other forms.13. An isolated polymorph according to that is at least about 80%% free of other forms.14. An isolated polymorph according to that is at least about 90% % free of other forms.15. An isolated polymorph according that is at least about 95% % free of other forms.16. An isolated polymorph according that is at least about 99% free of other forms.17. A pharmaceutical composition comprising the polymorph of and further comprising one or more pharmaceutically acceptable ingredients selected from the group consisting of carriers claim 11 , excipients claim 11 , diluents claim 11 , additives claim 11 , fillers claim 11 , lubricants and binders.18. The pharmaceutical composition of claim 17 , wherein the composition is formulated for oral administration.19. A method of treating Orthopoxvirus infections comprising administering to a patient in need thereof a therapeutically effective amount of the polymorph of .2021. A method of treating eczema vaccinatum comprising administering to a patient in need thereof a therapeutically effective amount of the polymorph of claim .2163.-. (canceled)64. A method of producing crystal polymorphic Form II of ST-246 claim 11 , comprising the steps of:a) dissolving ST-246 in at least one solvent to make a solution;b) cooling said solution to a temperature that causes the preferential crystallization of said ST-246 polymorphic Form II; andc) optionally drying the formed crystals of ST-246,wherein said solvent is selected from the group consisting of ethyl acetate, chloroform and 1- ...

INHIBITORS OF METALLO-BETA-LACTAMASES

The present invention relates to compounds of Formula (I) that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection. (Formula (I)) 2. A compound of Formula I according to claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , for use in the treatment of a bacterial infection in combination with a beta-lactam antibiotic.3. A compound according to any one of or claim 1 , wherein Ris selected from hydrogen or (1-4C)alkyl which is optionally substituted by one or more substituent groups selected from oxo claim 1 , halo claim 1 , or (1-2C)alkoxy.4. A compound according to any one of to claim 1 , wherein Ris hydrogen.5. A compound according to any one of to claim 1 , wherein Ris selected from:(i) —C(O)OH;{'sub': 2B', '2C', '2B', '2C, 'sup': 'A', '(ii) —C(O)NRR; wherein Rand Rare each independently selected from hydrogen, (1-6C)alkyl, (3-8C)cycloalkyl, aryl or heteroaryl, each of which is optionally substituted by one or more substituent groups R;'}{'sub': 2D', '2B', '2C', '2D', '2B', '2C, '(iii) —C(O)NRNRR; wherein Ris selected from hydrogen or (1-2C)alkyl and Rand Rare as defined above;'}(iv) tetrazolyl;{'sub': 2F', '2G', '2F', '2G', '2F', '2G, '(v) —B(OR)(OR), wherein Rand Rare each independently selected from hydrogen, (1-4C)alkyl or Rand Rare linked such that, together with the B and O atoms, they form a 5 or 6-membered heterocyclic ring, which is optionally substituted by (1-2C)alkyl; or'}(vi) cyano:{'sup': 'A', 'claim-text': {'br': None, 'sup': 2', '2, '—X—Z'}, 'and wherein Ris selected from halo, cyano, or a group of the formula [{'sup': '2', 'sub': '2', 'Xis absent or —C(O)—, —SO—; and'}, {'sup': '2', 'Zis hydrogen, (1-6C)alkyl, aryl, or heteroaryl;'}, {'sup': 2', 'A4', 'A5', 'A4', 'A5, 'and wherein Zis optionally further substituted by one or ...

POLYMORPHIC FORMS OF ST-246 AND METHODS OF PREPARATION

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions. 1116.-. (canceled)117. A method of treating Orthopoxvirus infections comprising administering to a subject in need thereof a therapeutically effective amount of a polymorph Form I of 4-trifluoromethyl-N-(3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-benzamide (ST-246) which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of about 7.63 , 10.04 , 11.47 , 14.73 , 15.21 , 15.47 , 16.06 , 16.67 , 16.98 , 18.93 , 19.96 , 20.52 , 20.79 , 22.80 , 25.16 , 26.5 3 , 27.20 , 27.60 , 29.60 , 30.23 , 30.49 , 30.68 , 31.14 , 33.65 , 34.33 , 35.29 , 35.56 , 36.30 , 37.36 , 38.42 , 38.66 degrees.118. The method of claim 117 , wherein the polymorph Form I is at least about 70% free of other forms.119. The method of claim 117 , wherein the polymorph Form I is at least about 80% free of other forms.120. The method of claim 117 , wherein the polymorph Form I is at least about 90% free of other forms.121. The method of claim 117 , wherein the polymorph Form I is at least about 95% free of other forms.122. The method of claim 117 , wherein the polymorph Form I is at least about 99% free of other forms.123. The method of claim 117 , wherein the polymorph Form I is administered orally.124. A method of treating eczema vaccinatum comprising administering to a patient in need thereof a therapeutically effective amount of a polymorph Form I of 4-trifluoromethyl-N-(3 claim 117 ,3a claim 117 ,4 claim 117 ,4a claim 117 ,5 claim 117 ,5a claim 117 ,6 claim 117 ,6a-octahydro-1 claim 117 ,3-dioxo-4 claim 117 ,6-ethenocycloprop[f]isoindol-2(1H)-benzamide (ST-246) which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of about 7.63 claim 117 , 10.04 claim 117 , ...

CARBON MONOXIDE RELEASING NORBORNENONE COMPOUNDS

The present invention provides organic compounds which are capable of releasing carbon monoxide under physiological conditions or pH trigger, and to the use of such compounds for conditioning a cell, tissue or organ, for example, to protect against ischaemic injury during a transplant event. 2. The norbornenone compound of claim 1 , wherein X is selected from halo claim 1 , ONO claim 1 , OP(O)(OR) claim 1 , OC(O)R claim 1 , OS(O)R claim 1 , OS(O)OR claim 1 , SR claim 1 , S(O)R claim 1 , S(O)R claim 1 , OR claim 1 , and NRR; and Rand Rare each independently selected from hydrogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , aryl claim 1 , arylalkyl and arylhaloalkyl.3. The norbornenone compound of claim 1 , wherein X is selected from halo claim 1 , OS(O)R claim 1 , and OS(O)OR; and Ris independently selected from hydrogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , aryl claim 1 , arylalkyl and arylhaloalkyl.4. The norbornenone compound of claim 1 , wherein X is selected from iodo claim 1 , bromo claim 1 , chloro claim 1 , SR claim 1 , S(O)R claim 1 , S(O)R claim 1 , OS(O)R claim 1 , and OS(O)OR; and Ris independently selected from hydrogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , phenyl claim 1 , phenylalkyl and phenylhaloalkyl.5. The norbornenone compound of claim 1 , wherein R claim 1 , R claim 1 , Rand R claim 1 , are each independently selected from hydrogen claim 1 , halo claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , monocyclic or bicyclic Ccarbocyclyl claim 1 , and monocyclic or bicyclic Cheterocyclyl claim 1 , polyethylene glycol claim 1 , and a saccharide; wherein the alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , carbocyclyl claim 1 , and heterocyclyl group claim 1 , are each optionally substituted with 1-3 substituents independently selected from halo claim 1 , CN claim 1 , NO claim 1 , OC(O)R claim 1 , C(O)R claim 1 , C(O)OR claim 1 , OR claim 1 , OS(O)R claim 1 , NRR claim 1 , SR claim 1 , polyethylene glycol claim 1 ...

FULLERENE DERIVATIVE AND N-TYPE SEMICONDUCTOR MATERIAL

The present invention is a material having excellent performance as an n-type semiconductor material, in particular for organic thin-film solar cells. 2. The n-type semiconductor material according to claim 1 , which is for use in an organic thin-film solar cell.3. An organic power-generating layer comprising the n-type semiconductor material according to and a p-type semiconductor material.4. The organic power-generating layer according to claim 3 , wherein the p-type semiconductor material consists of a donor-acceptor type π-conjugated polymer claim 3 , the donor-acceptor type π-conjugated polymer including as a donor unit benzodithiophene claim 3 , dithienosilole claim 3 , or N-alkyl carbazole and as an acceptor unit benzothiadiazole claim 3 , thienothiophene claim 3 , or thiophene pyrrole dione.5. The organic power-generating layer according to claim 4 , wherein the donor-acceptor type π-conjugated polymer is poly(thieno[3 claim 4 ,4-b]thiophene-co-benzo[1 claim 4 ,2-b:4 claim 4 ,5-b′]thiophene) claim 4 , or poly(dithieno[1 claim 4 ,2-b:4 claim 4 ,5-b′][3 claim 4 ,2-b:2′ claim 4 ,3′-d]silole-alt-(2 claim 4 ,1 claim 4 ,3-benzothiadiazole).6. The organic power-generating layer according to claim 4 , wherein the donor-acceptor type π-conjugated polymer is poly(thieno[3 claim 4 ,4-b]thiophene-co-benzo[1 claim 4 ,2-b:4 claim 4 ,5-b′]thiophene).7. The organic power-generating layer according to claim 3 , wherein the p-type semiconductor material is poly-3-hexylthiophene claim 3 , or poly[[4 claim 3 ,8-bis[(2-ethylhexyl)oxy]benzo[1 claim 3 ,2-b:4 claim 3 ,5-b′]dithiophene-2 claim 3 ,6-diyl][3-fluoro-2-[(2-ethylhexyl)carbonyl]thieno[3 claim 3 ,4-b]thiophenediyl]].8. The organic power-generating layer according to claim 3 , further comprising diiodooctane.9. A photoelectric conversion element comprising the organic power-generating layer according to .10. The photoelectric conversion element according to claim 9 , which is an organic thin-film solar cell. The present ...

AMORPHOUS TECOVIRIMAT PREPARATION

Disclosed are methods for the preparation of amorphous N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Also disclosed are methods for the preparation of amorphous solid dispersion of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide. 122-. (canceled)23. A method for producing amorphous solid dispersion of N-[(3aR ,4R ,4aR ,5aS ,6S ,6aS)-3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide , said method comprising:(a) heating a solid form of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide in the presence of at least one polymer at a temperature sufficient to cause melting and produce a liquid solution; and(b) cooling the solution of step (a) and thus producing said amorphous dispersion.24. The method of claim 23 , wherein said polymer is selected from the group consisting of: Polyethylene glycol claim 23 , Gelucire claim 23 , Glycerol mono and di stearate claim 23 , methacrylic acid copolymer claim 23 , Hydroxypropyl methyl cellulose (HPMC) claim 23 , HPMCP-H55 claim 23 , CAP claim 23 , PVAP claim 23 , HPMCAS-L claim 23 , HPMCAS-M claim 23 , HPMCAS-H claim 23 , Hypromellose claim 23 , HPC claim 23 , Poloxamer claim 23 , PVP-VA claim 23 , PVP (neutral) claim 23 , hydroxypropyl cellulose claim 23 , methyl cellulose claim 23 , ethyl cellulose claim 23 , and mixtures thereof.25. The method of claim 24 , wherein said polymer is Polyethylene glycol.26. The method of claim 23 , wherein said liquid solution comprises a surfactant.27. The method of claim 26 , wherein said ...

Method Of Preparing Fused Ring Indeno Compounds

The present invention relates to methods of preparing fused ring indeno compounds that involves reacting together a dienophile and a lactone compound, in the presence of a catalyst, and a carboxylic acid anhydride. With some embodiments, the fused ring indeno compound is represented by the following Formula (I-A), the dienophile is represented by the following Formula (II-A), and the lactone compound is represented by the following Formula (III-A): 3. The method of wherein claim 2 , the metal M of Formula (V) and Formula (VI) is independently selected from Bi claim 2 , B claim 2 , Al claim 2 , Hf claim 2 , Sc claim 2 , Cu claim 2 , Yb claim 2 , Ti claim 2 , Sn claim 2 , Fe claim 2 , Zn claim 2 , Ag claim 2 , Y claim 2 , In claim 2 , Nb and Mg claim 2 , Ris selected from C-Clinear or branched alkyl claim 2 , and C-Clinear or branched perfluoroalkyl claim 2 , and X is selected from F claim 2 , Cl claim 2 , I claim 2 , and Br.4. The method of wherein said method is conducted in the presence of a solvent claim 1 , said solvent being selected from benzene claim 1 , toluene claim 1 , xylene claim 1 , methylene chloride claim 1 , 1 claim 1 ,2-dichloroethane claim 1 , C-Clinear or branched perhaloalkyl claim 1 , acetonitrile claim 1 , nitromethane claim 1 , and combinations thereof.6. The method of wherein for Formula (I-B) and Formula (II-B) Zis N—R claim 5 , and Ris claim 5 , or is converted to claim 5 , a group L represented by the following Formula (VII) claim 5 , and{'sup': '1', 'claim-text': {'br': None, 'sub': 1', 'c', '1', '2', 'd', 'd′', '2', '3', 'e', 'e′', '3', '4', 'f', 'f′', '5, '—[S]-[Q-[S]]-[Q-[S]]-[Q-[S]]—S—P\u2003\u2003Formula (VII)'}, 'optionally for Formula (I-B) at least one Rindependently for each n, is selected from said group L represented by the following Formula (VII),'}wherein:{'sub': 1', '2', '3, '(a) Q, Q, and Qfor each occurrence, are independently selected from a divalent group selected from optionally substituted aryl, optionally substituted ...

SUBSTITUTED (1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS

The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. 158-. (canceled)60. The process according to claim 59 , wherein n is 1.61. The process according to claim 59 , wherein Y is CR.62. The process according to claim 61 , wherein Ris H or C-Chaloalkyl.63. The process according to claim 61 , wherein Ris H or trifluoromethyl.64. The process according to claim 59 , wherein Ris selected from the group consisting of H claim 59 , cyano claim 59 , C-Chaloalkoxy and C-Chaloalkyl.65. The process according to claim 59 , wherein Ris selected from the group consisting of H claim 59 , cyano claim 59 , trifluoromethoxy and trifluoromethyl.66. The process according to claim 59 , wherein Ris selected from the group consisting of cyclobutyl claim 59 , cyclohexyl claim 59 , cyclopentyl claim 59 , and cyclopropyl.67. The process according to claim 59 , wherein Z is CR.68. The process according to claim 67 , wherein Ris selected from the group consisting of H claim 67 , cyano claim 67 , C-Chaloalkoxy and C-Chaloalkyl.69. The process according to claim 67 , wherein Ris selected from the group consisting of H claim 67 , cyano claim 67 , trifluoromethoxy and trifluoromethyl. The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple ...

AMORPHOUS TECOVIRIMAT PREPARATION

Disclosed are methods for the preparation of amorphous N-[(aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Also disclosed are methods for the preparation of amorphous solid dispersion of N-[(aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1 H)-yl]-4-(trifluoromethyl)-benzamide. 1. A method for producing amorphous N-[(3aR ,4R ,4aR ,5aS ,6S ,6aS)-3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide , said method comprising:(a) heating a solid form of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide at a temperature sufficient to cause melting; and(b) cooling the melted form of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide and thus producing amorphous N-[( 3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide.2. The method of claim 1 , wherein said heating is carried out at a temperature of at least about 196° C.3. The method of claim 1 , wherein said heating is carried out at a temperature of up to about 230° C.4. The method of claim 1 , wherein said heating is carried out at a temperature from about 196° C. to about 230° C.5. The method of claim 1 , wherein said cooling step is carried out at a temperature below about 0° C.6. The method of claim 1 , wherein said cooling step is carried out at a temperature of less than about −50 ° C.7. The method of claim 1 , wherein said cooling step is carried out in liquid nitrogen.8. The method of claim 1 ...

TRICYCLIC PYRROLE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS

The invention refers to compounds of general formula (I) 2. The compound according to claim 1 , wherein Ris selected from —COOR claim 1 , —CONHR claim 1 , —CONRR claim 1 , more preferably it is —COOR.3. The compound according to of claim 2 , wherein Ris —COOH or a salt thereof.4. The compound according to claim 1 , wherein Ris hydrogen.5. The compound according to claim 1 , wherein Ris substituted or unsubstituted alkenyl claim 1 , preferably unsubstituted alkenyl.6. The A compound according to claim 5 , wherein Ris 1-propenyl.7. The compound according to claim 1 , Ris substituted or unsubstituted alkenyl claim 1 , preferably unsubstituted alkenyl.8. The compound according to claim 7 , wherein Ris 1-propenyl.10. A process for the preparation of a compound of formula general (I) as defined in claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , or solvate thereof claim 1 , wherein the process comprises the step of isolating a compound of formula (I) above from a culture broth of a microorganism.11Paraconiothyrium. The process according to claim 10 , wherein the microorganism is a fungal strain claim 10 , more preferably a sp.12Paraconiothyrium. The process according to claim 11 , wherein the fungal strain is sp. HL-78-gCHSP3-B005 which has been deposited in the Colección Española de Cultivos Tipo at the Universidad de Valencia claim 11 , Spain under the accession number CECT 20841.13. A pharmaceutical composition comprising at least one compound of general formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , or solvate thereof and a pharmaceutically acceptable excipient.14. A method for inhibiting angiogenesis in a subject comprising administering to the subject a compound of general formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , or solvate thereof.15. The method according to claim 14 , for the treatment and/or prophylaxis of ...

RESIN COMPOSITIONS

The present disclosure is directed to resins and to polymers, copolymers, and blends formed therefrom. 3. The resin of claim 2 , wherein each of (A)and (A)are different.4. The resin of claim 2 , wherein (A)comprises a vinyl benzyl group; and{'sub': s', '2', '2, 'wherein (A)is —CH—CH═CH.'}5. The resin of claim 2 , wherein (A)is —CH-phenyl-CH═CH.6. The resin of claim 2 , wherein (Z)is an unsubstituted alkyl group having from 2 to 6 carbon atoms.8. The resin of claim 7 , wherein when T is -phenyl claim 7 , or —CH-phenyl claim 7 , and Y is —CH═CH claim 7 , —CH═CH—CH claim 7 , or an alkyne group claim 7 , z is 1.9. The resin of claim 1 , wherein a Dk value ranges from about 1.5 to about 3.10. The resin of claim 1 , wherein a Df value ranges from about 0.0001 to about 0.004 The present application claims the benefit of the filing date of U.S. patent application Ser. No. 15/601,880 filed May 22, 2017, and claims the benefit of the filing date of U.S. Provisional Patent Application 62/435,369 filed Dec. 16, 2016, the disclosure of which is hereby incorporated by reference herein in its entirety.The present disclosure is directed to thermosetting resin compositions that are useful for the next-generation wireless standard (i.e. namely 5th generation mobile networks or “5G”).5G is the follow-up to the current wireless standard known as 4G or long term evolution (LTE). It is believed to be able to enable data transmission rates of more than 10 Gbps or 100 times the throughput of LTE. Basically, 5G technology consists of three separate elements—enhanced mobile broadband (1,000 times more capacity and one-tenth the latency), the Internet of Things (IOT) and other Wi-Fi based technology, and machine-to-machine (M2M) type communications.Today's LTE networks (servers, router base station, etc.) are believed to operate from 700 MHz to 3.5 GHz. In comparison, 5G will not only co-exist with LTE, but will also operate in unlicensed or millimeter wave bands. This involves the spectrum ...

Polymorphic forms of st-246 and methods of preparation

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

RESIN COMPOSITIONS

The present disclosure is directed to resins and to polymers, copolymers, and blends formed therefrom. 3. The resin of claim 2 , wherein at least one (Alkyl)group is —CHCH.4. The resin of claim 2 , wherein each [Alkyl] group is independently —CH— claim 2 , —CH(CH)— claim 2 , or —C(CH)— claim 2 , —CH claim 2 , —CHCH claim 2 , or —CH(CH).5. The resin of claim 1 , wherein Rcomprises a substituted phenyl group.6. The resin of claim 1 , wherein Rcomprises a branched alkyl group comprising between 1 and 10 carbon atoms.8. The resin of claim 1 , wherein each (A)is independently H claim 1 , allyl claim 1 , benzyl claim 1 , or vinylbenzyl.12. The product of claim 11 , wherein f is 0.14. The compound of claim 13 , wherein each (A)is independently H claim 13 , allyl claim 13 , benzyl or vinylbenzyl.17. The compound of claim 16 , wherein at least one (Alkyl)group is —CHCH.18. The compound of claim 16 , wherein each [Alkyl] group is independently —CH— claim 16 , —CH(CH)— claim 16 , or —C(CH)— claim 16 , —CH claim 16 , —CHCH claim 16 , or —CH(CH).19. A printed circuit board comprising the compound of .20. An electronic device comprising the printed circuit board of .21. An underfill comprising the compound of .22. A printed circuit board comprising the underfill of . The present application is a continuation-in-part of U.S. patent application Ser. No. 15/861,133 filed on Jan. 3, 2018, which is a continuation of U.S. patent application Ser. No. 15/601,880 filed May 22, 2017, which application claims the benefit of the filing date of U.S. Provisional Patent Application 62/435,369 filed Dec. 16, 2016; the present application is also a continuation-in-part of PCT Application No. PCT/US2017/033869 filed on Mary 22, 2017, which application claims the benefit of the filing date of U.S. Provisional Patent Application 62/435,369 filed Dec. 16, 2016, the disclosures of which are hereby incorporated by reference herein in their entireties.The present disclosure is directed to thermosetting ...

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT AND PREVENTION OF ORTHOPOXVIRUS INFECTIONS AND ASSOCIATED DISEASES

Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. 119-. (canceled)21. The process of claim 20 , wherein the ratio of compound 1(b) to 4-trifluoromethylbenzhydrazide is 0.89 to 1.22. The process of claim 20 , wherein the solvent is ethanol.23. The process of claim 20 , wherein the reaction occurs at above room temperature.24. The process of claim 20 , wherein the reaction occurs under argon.25. The process of claim 20 , wherein the solvent is removed by evaporation.26. The process of claim 20 , wherein N-[(3aR claim 20 ,4S claim 20 ,4aS claim 20 ,5aR claim 20 ,6R claim 20 ,6aS)-3 claim 20 ,3a claim 20 ,4 claim 20 ,4a claim 20 ,5 claim 20 ,5a claim 20 ,6 claim 20 ,6a-octahydro-1 claim 20 ,3-dioxo-4 claim 20 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide is further purified by chromatography.28. The method of claim 27 , wherein said first solvent comprises xylenes.29. The method of claim 27 , wherein said second solvent is ethanol. This application is a continuation-in-part of U.S. application Ser. No. 11/785,998 filed Apr. 23, 2007, which is a continuation-in-part of U.S. application Ser. No. 10/561,153 filed Apr. 5, 2006, now U.S. Pat. No. 7,737,168, which is a national stage filing of corresponding international application number PCT/US04/19552, filed on Jun. 18, 2004, which claims priority of U.S. Provisional Application No. 60/480,182, filed Jun. 20, 2003, all of which are hereby incorporated by reference in their entirety.This invention was made with U.S. government support under Grant No. 7R43AI056409 and Contract HHSN266200600014C awarded by the National Institute of Health (NIH). The U.S. Government has certain rights in the invention.The present invention relates to the ...

INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects. 3. The method of claim 1 , wherein the AKR1C3 polypeptide is present within a subject.4. The method of claim 3 , wherein the subject is a mammal.5. The method of claim 3 , wherein the subject is a male and the AKR1C3 polypeptide is present in the prostate of the subject.6. The method of claim 5 , wherein the prostate of the subject comprises a tumor claim 5 , optionally a castrate-resistant tumor.9. The method of claim 7 , wherein the subject is a mammal.10. The method of claim 9 , wherein the subject is a male and the undesirable AKR1C3 biological activity is present in a tumor claim 9 , optionally a castrate-resistant tumor claim 9 , present in the prostate of the subject.13. The method of claim 11 , wherein the prostate tumor is a castrate-resistant prostate tumor.14. The method of claim 11 , wherein the administering is via a route selected from the group consisting of peroral claim 11 , intravenous claim 11 , intraperitoneal claim 11 , inhalation claim 11 , intraprostatic claim 11 , and intratumoral. This application is a divisional of U.S. patent application Ser. No. 16/530,907, filed Aug. 2, 2019 (pending), which itself is a divisional of U.S. patent application Ser. No. 15/899,171, filed Feb. 19, 2018 (now U.S. Pat. No. 10,398,678), which itself is a U.S. patent application Ser. No. 15/132,937, filed Apr. 19, 2016 (now U.S. Pat. No. 9,895,351), which itself is a continuation of U.S. patent application Ser. No. 14/352,421, filed Apr. 17, ...

COMPOUNDS FOR THE INHIBITION OF CYCLOPHILINS AND USES THEREOF

The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of cyclophilins, and for the treatment of cyclophilin-related disorders. 117-. (canceled)19. The method of claim 18 , wherein the disease or disorder is selected from viral infections claim 18 , inflammation claim 18 , neurologic disorders claim 18 , cardiac failure and cancer.20. The method of claim 18 , wherein the disease or disorder is selected from Alzheimer's disease claim 18 , Parkinson's disease claim 18 , Amyotrophic Lateral Sclerosis (ALS) claim 18 , Dementia claim 18 , Multiple Sclerosis claim 18 , and Huntington's disease.21. The method of claim 18 , wherein each R′ is independently —R claim 18 , —OR claim 18 , or —N(R).22. The method of claim 21 , wherein each R′ is independently H claim 21 , -Me claim 21 , -Et claim 21 , —OH claim 21 , or —NH.23. The method of claim 18 , wherein X is CH.24. The method of claim 18 , wherein X claim 18 , and the bonds attached to X claim 18 , are absent.25. The method of claim 18 , wherein each Ris independently H claim 18 , Me claim 18 , or -Et.26. The method of claim 25 , wherein each Ris independently —H or -Me.27. The method of claim 18 , wherein Rand Rtaken together with the atom to which they are attached form a cyclopropyl claim 18 , cyclobutyl claim 18 , cyclopentyl claim 18 , or cyclohexyl claim 18 , each of which is optionally substituted. This application claims the benefit of U.S. Provisional application No. 62/315,890, filed on Mar. 31, 2016, the content of which is incorporated in its entirety by reference.The present invention relates to dioxo-hexahydroisoindolyl compounds useful as inhibitors of Cyclophilins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.Cyclophilins or peptidyl-prolyl isomereases (PPAses) are widely expressed enzymes which ...

Strigolactam derivatives as plant growth regulating compounds

The present invention relates to novel strigolactam derivatives of formula (I), to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.

RESIN COMPOSITIONS

The present disclosure is directed to resins and to polymers, copolymers, and blends formed therefrom. 2. The resin of claim 1 , wherein t is 1; and Rand Rare each H.3. The resin of claim 2 , wherein Y is —CH═CH.4. The resin of claim 1 , wherein m is 2 claim 1 , and a first A group comprises a vinyl benzyl moiety; and wherein a second A group is —CH—CH═CH.7. The resin of claim 1 , wherein the resin comprises at least one A moiety terminating in one of a —CH═CHgroup claim 1 , a —CH═CH—CHgroup claim 1 , or an alkyne group.8. A polymer or copolymer derived from the resin of .9. The polymer or copolymer of claim 8 , wherein the polymer or copolymer has a room temperature viscosity of 100 to 1 claim 8 ,000 claim 8 ,000 mPa*s.10. The polymer or copolymer of claim 8 , wherein the polymer or copolymer comprises a glassy material which can be ground into a fine powder.11. The polymer or copolymer of claim 8 , wherein the polymer or copolymer is soluble in an organic solvent selected from the group consist of MEK claim 8 , Xylenes claim 8 , NMP claim 8 , DMF claim 8 , DCM claim 8 , Acetonitrile claim 8 , Acetone claim 8 , DMSO claim 8 , THF.12. The polymer or copolymer of claim 8 , wherein the polymer or copolymer comprises a molecular weight ranging from between about 200 to about 1 claim 8 ,000 claim 8 ,000 Da.13. The polymer or copolymer of claim 8 , further comprising an additive selected from the group consisting of adhesion agents claim 8 , peroxides claim 8 , crosslinking agents claim 8 , antioxidants claim 8 , flame retardants claim 8 , diluents and fillers.14. The polymer or copolymer of claim 8 , wherein the polymer or copolymer has a Dk value ranging from about 1.5 to about 3.15. The polymer or copolymer of claim 8 , wherein the polymer or copolymer polymer has a Df value ranging from about 0.0001 to 0.004.16. A polymer or copolymer comprising (i) a resin of ; and (ii) a second component selected from the group consisting of polyethylenes claim 1 , polypropylenes ...

Tricyclic sulfones as ror gamma modulators

There are described RORγ modulators of the formula (I), and formula (II) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects. 519-. (canceled)20. A method for inhibiting a biological activity of an aldo-keto reductase family 1 claim 1 , member C3 (AKR1C3) polypeptide claim 1 , the method comprising contacting the AKR1C3 polypeptide with an effective amount of a compound of .22. The method of claim 20 , wherein the AKR1C3 polypeptide is present within a subject.23. The method of claim 22 , wherein the subject is a mammal.24. The method of claim 22 , wherein the subject is a male and the AKR1C3 polypeptide is present in the prostate of the subject.25. The method of claim 24 , wherein the prostate of the subject comprises a tumor claim 24 , optionally a castrate-resistant tumor.26. A method for inhibiting undesirable aldo-keto reductase family 1 claim 1 , member C3 (AKR1C3) biological activity in a subject claim 1 , the method comprising administering to the subject an effective amount of a compound of .28. The method of claim 26 , wherein the subject is a mammal.29. The method of claim 28 , wherein the subject is a male and the undesirable AKR1C3 biological activity is present in a tumor claim 28 , optionally a castrate-resistant tumor claim 28 , present in the prostate of the subject.30. A method for treating a prostate tumor in a subject claim 1 , the method comprising administering the subject a therapeutically effective amount of a compound of .32. The method of claim 30 , wherein the prostate tumor is a castrate-resistant prostate tumor.33. The method of claim 30 , ...

Indomethacin analogs for the treatment of castrate-resistant prostate cancer

Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Aromatic amine derivative and organic electroluminescence element using same

An aromatic amine derivative represented by formula (1): wherein L 1 , L 2 , Ar 1 , Ar 2 , R 1 , R 2 , a, b, and Q are as defined in the specification. An organic electroluminescence device having at least one organic thin film layer which includes the aromatic amine derivative has high emission efficiency and long lifetime.

COMPOUNDS FOR THE INHIBITION OF CYCLOPHILINS AND USES THEREOF

The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of cyclophilins, and for the treatment of cyclophilin-related disorders. 2. The compound of claim 1 , wherein Ring A is phenyl.3. The compound of claim 2 , wherein Ring A is phenyl which is fused with a 7-9 membered saturated or partially unsaturated heterocyclic mono- or bicyclic ring having 1-3 heteroatoms independently selected from nitrogen claim 2 , oxygen claim 2 , or sulfur; which is optionally substituted.4. The compound of claim 1 , wherein each R′ is independently —R claim 1 , —OR claim 1 , or —N(R).5. The compound of claim 4 , wherein each R′ is independently H claim 4 , -Me claim 4 , -Et claim 4 , —OH claim 4 , or —NH.7. The compound of claim 1 , wherein X is CH.8. The compound of claim 1 , wherein X is O.9. The compound of claim 1 , wherein X claim 1 , and the bonds attached to X claim 1 , are absent.10. The compound of claim 1 , wherein each Ris independently —H or -Me.11. The compound of claim 1 , wherein Rand Rtaken together with the atom to which they are attached form a cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , or cyclohexyl claim 1 , each of which is optionally substituted.16. The compound of claim 1 , selected from Table 1.17. A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable adjuvant claim 1 , carrier claim 1 , or vehicle.18. A method for treating a cyclophilin-mediated disease or disorder in a subject in need thereof claim 1 , comprising the step of administering to said subject a compound of .19. The method of claim 18 , wherein the disease or disorder is selected from viral infections claim 18 , inflammation claim 18 , neurologic disorders claim 18 , cardiac failure and cancer.20. The method of claim 18 , wherein the disease or disorder is selected from Alzheimer's disease claim 18 , Parkinson's disease claim 18 , Amyotrophic Lateral Sclerosis (ALS) claim ...

Indomethacin analogs for the treatment of castrate-resistant prostate cancer

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

METHODS OF PREPARING TECOVIRIMAT

Disclosed are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. 120-. (canceled)22. The method of claim 21 , wherein step (a) is carried out in anhydrous toluene under nitrogen atmosphere and reactants heated to reflux.23. The method of claim 21 , wherein step (b) is carried out under nitrogen atmosphere at a temperature of at least about 75° C.24. The method of claim 21 , wherein said acid in step (c) is HCl.25. The method of claim 21 , wherein compound 6 is dissolved in in i-PrOAc prior to the reaction of step (c).26. The method of claim 21 , wherein a base is present in the reaction of step (d) claim 21 , wherein said base is selected from the group consisting of: pyridine claim 21 , 4-dimethylaminopyridine claim 21 , triethylamine and diisopropylethylamine.27. The method of claim 21 , wherein step (d) is carried out at a temperature of less than about 20° C.28. The method of claim 21 , wherein said N-[(3aR claim 21 ,4R claim 21 ,4aR claim 21 ,5aS claim 21 ,6S claim 21 ,6aS)-3 claim 21 ,3a claim 21 ,4 claim 21 ,4a claim 21 ,5 claim 21 ,5a claim 21 ,6 claim 21 ,6a-octahydro-1 claim 21 ,3-dioxo-4 claim 21 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide collected in step (e) is further purified by column chromatography.2935-. (canceled)37. (canceled) This application claims the benefit of U.S. Provisional Patent Application No. 61/683,905, filed on Aug. 16, 2012, the disclosure of which is hereby fully incorporated herein by reference.Described herein are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Tecovirimat, with a proprietary name of ST-246®, has a chemical name of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a ...

Thermosetting ring-opening metathesis polymerization materials with thermally degradable linkages

The present invention provides a new class of thermosetting ring-opening metathesis polymerization materials based on norbornene and oxanorbornene dicarboximide moieties containing at least one acetal ester group linkage. The acetal ester group is degradable when subjected to heat or acidic aqueous hydrolysis. The polymerization materials can be used in reworkable thermosetting compositions. R1-Rs, X, and n are defined herein.

MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES

The present invention describes indenocarbazole derivatives having electron- and hole-transporting properties, in particular for use in the emission and/or charge-transport layer of electroluminescent devices or as matrix material. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same. 116-. (canceled)19. The compound according to claim 17 , wherein R is selected from H claim 17 , D claim 17 , N(Ar) claim 17 , a substituted or unsubstituted arylamine claim 17 , a straight-chain alkyl group having 1 to 20 C atoms claim 17 , a branched alkyl group having 3 to 20 C atoms claim 17 , or an aromatic or heteroaromatic ring system having 5 to 40 ring atoms.20. The compound according to claim 19 , wherein the aromatic or heteroaromatic ring system here is selected from substituted or unsubstituted phenyl claim 19 , naphthyl claim 19 , pyridine claim 19 , triazine claim 19 , pyrimidine claim 19 , benzimidazole claim 19 , thiophene claim 19 , triphenylamine or combinations of these groups.21. The compound according to claim 17 , wherein Ris selected on each occurrence claim 17 , independently of one another claim 17 , from alkyl claim 17 , substituted or unsubstituted triazine claim 17 , pyridine claim 17 , pyrimidine claim 17 , pyrazine claim 17 , phenyl claim 17 , biphenyl claim 17 , terphenyl claim 17 , naphthyl claim 17 , anthracenyl and carbazole claim 17 , and two radicals Rwhich are bonded to the same C atom together with the atom(s) to which they are bonded may also form an aliphatic claim 17 , aromatic or heteroaromatic ring.22. An electronic device comprising at least one compound according to .23. An organic electroluminescent device which comprises the compound according claim 17 , to is employed in an emitting layer and/or as electron-transport material and/or as hole-transport material and/or as hole-injection material and/or as hole-blocking material.24. An ...

POLYMORPHIC FORMS OF ST-246 AND METHODS OF PREPARATION

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions. 1138-. (canceled)139. A polymorph Form IV of 4-trifluoromethyl-N-(3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide (ST-246) which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of 6.97 , 9.75 , 11.21 , 12.13 , 13.54 , 16.82 , 18.17 , 18.79 , 19.69 , 20.51 , 23.31 , 24.78 , 27.24 , 30.20 , and 33.52 degrees.140. An isolated polymorph according to that is at least about 70% free of other forms.141. An isolated polymorph according to that is at least about 80% free of other forms.142. An isolated polymorph according to that is at least about 90% free of other forms.143. An isolated polymorph according that is at least about 95% free of other forms.144. An isolated polymorph according that is at least about 99% free of other forms.145. A pharmaceutical composition comprising the polymorph of and further comprising one or more pharmaceutically acceptable ingredients selected from the group consisting of carriers claim 139 , excipients claim 139 , diluents claim 139 , additives claim 139 , fillers claim 139 , lubricants and binders.146. The pharmaceutical composition of claim 145 , wherein the composition is formulated for oral administration.147. Use of the polymorph of in the preparation of a medicament for treating Orthopoxvirus infections.148. Use of the polymorph of in the preparation of a medicament for treating eczema vaccinatum.149. A method of producing crystal polymorphic Form IV of ST-246 claim 139 , comprising the steps of: 'dissolving 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide (ST-246) in at least one solvent to make a solution wherein said solvent is selected from the group ...

TRICYCLIC SULFONES AS RORy MODULATORS

There are described RORγ modulators of the formula (I), 10. A compound according to wherein{'sup': 1', '1a', '1a, 'sub': '1-6', 'Ris halo, phenyl substituted with 0-3 R, or Calkyl substituted with 0-3 R;'}{'sup': 1a', 'a', '2e', '2f', 'b', '2e', '2f', 'a, 'sub': 3', '1-6, 'Ris, independently at each occurrence, hydrogen, CF, halo, Calkyl substituted with 0-3 R, —(CRR)r-OR, and —(CRR)r-phenyl substituted with 0-3 R,'}{'sup': '1b', 'sub': 3', '3', '1', '4, 'Ris, independently at each occurrence, hydrogen, CD, halo, CF, and C-Calkyl;'}{'sup': 2', '2c', '2a', '2b', '2d', '11', '11', 'a, 'sub': 2', '1-6', '2', 'p, 'Ris hydrogen, SOR, Calkyl substituted with 0-3 R, COR, —C(O)R, —C(O)NRR; or a 5-7 membered heterocycle comprising carbon atoms, and 1-4 heteroatoms selected from N, O, P(═O) and S(O)substituted with 0-4 R,'}{'sup': 2a', 'a, 'sub': '1-6', 'Ris hydrogen or Calkyl substituted with 0-3 R;'}{'sup': 2b', 'a', 'a', '2e', '2f', 'a', '2e', '2f', 'a, 'sub': 1-6', '3-6', 'p, 'Ris hydrogen, Calkyl substituted with 0-2 R, Ccycloalkyl substituted with 0-3 R, —(CRR)r-5-7 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O, P(═O) and S(O)substituted with 0-4 R, or —(CRR)r-phenyl substituted with 0-3 R;'}{'sup': 2c', 'a', 'a', 'a', 'a', '2e', '2f', 'a, 'sub': 1-6', '2-6', '3-10', '6-10', 'p, 'Ris, independently at each occurrence, hydrogen, Calkyl substituted with 0-3 R, Calkenyl substituted with 0-3 R, Ccycloalkyl substituted with 0-3 R, Caryl substituted with 0-3 R, or —(CRR)r-5-10-membered heterocycle containing 1-4 heteroatoms selected from N, O, P(═O) and S(O), substituted with 0-4 R;'}{'sup': 2d', 'd', '11', '11', 'd', '2e', '2f', 'a', 'a, 'sub': 1-6', '1-6', '3-10', 'p, 'Ris, independently at each occurrence, hydrogen, Calkyl substituted with 0-3 R, Chaloalkyl, C(O)NRR, Ccycloalkyl substituted with 0-2 R, (CRR)r-phenyl substituted with 0-2 R, or a 4-10 membered heterocycle containing 1-4 heteroatoms selected from N, O, P(═O) and S(O), ...

Amido Compounds And Their Use As Pharmaceuticals

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. 138-. (canceled)39. A compound , which is N-methyl-5-[4-(1-{[3-oxo-1′H ,3H-spiro[2-benzofuran-1 ,3′-pyrrolidin]-1′-yl]carbonyl}cyclopropyl)phenyl]pyridine-2-carboxamide , wherein one or more hydrogen atoms are replaced by deuterium; or a pharmaceutically acceptable salt thereof.40. A compound , which is N-methyl-5-[4-(1-{[(1R)-3-oxo-1′H ,3H-spiro[2-benzofuran-1 ,3′-pyrrolidin]-1′-yl]carbonyl}cyclopropyl)phenyl]pyridine-2-carboxamide , wherein one or more hydrogen atoms are replaced by deuterium; or a pharmaceutically acceptable salt thereof.41. A compound , which is N-methyl-5-[4-(1-{[(1R)-3-oxo-1′H ,3H-spiro[2-benzofuran-1 ,3′-pyrrolidin]-1′-yl]carbonyl}cyclopropyl)phenyl]pyridine-2-carboxamide , wherein one or more hydrogen atoms are replaced by deuterium.42. A pharmaceutical composition comprising the compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , and a pharmaceutically acceptable carrier.43. A pharmaceutical composition comprising the compound of claim 40 , or a pharmaceutically acceptable salt thereof claim 40 , and a pharmaceutically acceptable carrier.44. A pharmaceutical composition comprising the compound of claim 41 , and a pharmaceutically acceptable carrier. This application is a continuation of U.S. Ser. No. 14/808,337, filed Jul. 24, 2015, which is a continuation of U.S. Ser. No. 13/243,565, filed Sep. 23, 2011, now issued as U.S. Pat. No. 9,126,927 on Sep. 8, 2005, which is a continuation of U.S. Ser. No. 12/817,887 filed Jun. 17, 2010, now issued as U.S. Pat. No. 8,058,288 on Nov. 15, 2011, which is a continuation of U.S. ...

THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION

Disclosed herein are compounds of formula (I), or a salt thereof and compositions comprising compounds of formula I that exhibit antibacterial activities, when tested alone and/or in combination with a bacterial efflux pump inhibitor. Also disclosed are methods of treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I alone or in combination with the administration of a bacterial efflux pump inhibitor. 2. The compound of claim 1 , wherein Ris (C-C)alkyl substituted with one NRRand wherein the (C-C)alkyl is optionally substituted with one or more halo claim 1 , hydroxyl or phenyl wherein the phenyl is optionally substituted independently with one or more halo claim 1 , cyano claim 1 , (C-C)alkyl claim 1 , or (C-C)haloalkyl claim 1 , and Ris hydrogen or (C-C)alkyl claim 1 , or Rand Rtogether with the atoms to which they are attached form a 5 or 7-membered carbocycle wherein the carbocycle is substituted with one NRRand wherein the carbocycle is optionally substituted with one or more halo claim 1 , hydroxyl claim 1 , or (C-C)alkyl.3. The compound of claim 1 , wherein Ris (C-C)alkyl substituted with one NRRand Ris hydrogen claim 1 , or Rand Rtogether with the atoms to which they are attached form a 5 or 7-membered carbocycle wherein the carbocycle is substituted with one NRR.4. The compound of claim 1 , wherein Ris (C-C)alkyl substituted with one NRRand Ris hydrogen.6. The compound of claim 5 , wherein Ris hydrogen or (C-C)alkyl optionally substituted with one or more halo claim 5 , hydroxyl claim 5 , NRRor phenyl wherein the phenyl is optionally substituted independently with one or more halo claim 5 , cyano claim 5 , (C-C)alkyl claim 5 , or (C-C)haloalkyl and Ris hydrogen or (C-C)alkyl optionally substituted with one or more halo claim 5 , hydroxyl claim 5 , oxo claim 5 , or NRR.7. The compound of claim 5 , wherein Ris hydrogen or (C-C)alkyl optionally substituted with one or more halo claim 5 , ...

NOVEL METAL COMPLEX, METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING GAMMA-LACTAM COMPOUND USING SAME

The present invention relates to a novel metal complex, a method for producing same, and a method for producing a gamma-lactam compound using same, and the metal complex according to the present invention is used as a catalyst for producing a gamma-lactam compound and can efficiently produce a gamma-lactam compound with an excellent yield and excellent selectivity. 4. The metal complex of claim 3 , wherein A is —CO— claim 3 , Rand Rare independently of each other (C1-C20)alkoxy claim 3 , and n is an integer of 1.5. The metal complex of claim 1 , wherein the metal complex is used as a catalyst for preparing a gamma-lactam compound from a dioxazol-one compound.7. The method of preparing a metal complex of claim 6 , wherein the base is any one or two or more selected from NaOAc claim 6 , NaCO claim 6 , NaHNO claim 6 , Cu(OAc) claim 6 , Cu(OAc).HO claim 6 , and NEt.8. The method of preparing a metal complex of claim 6 , wherein the base is used at 2 to 10 mol with respect to 1 mol of the metal precursor compound of Chemical Formula 3A claim 6 , and the quinoline-based compound of Chemical Formula 3B is used at 1.5 to 2.5 mol with respect to 1 mol of the metal precursor compound of Chemical Formula 3A.11. The method of preparing a gamma-lactam compound of claim 9 , wherein the metal complex is used at 0.01 to 0.1 mol with respect to 1 mol of the dioxazol-one compound.12. The method of preparing a gamma-lactam compound of claim 9 , wherein the base is one or two or more selected from NaBAr(sodium tetrakis[3 claim 9 ,5-bis(trifluoromethyl)phenyl]borate) claim 9 , AgSbF(silver hexafluoroantimonate(V)) claim 9 , AgNTf(silver bis(trifluoromethanesulfonyl)imide) claim 9 , AgBF(silver tetrafluoroborate) claim 9 , AgPF(silver hexafluorophosphate) claim 9 , AgOTf (silver trifluoromethanesulfonate) claim 9 , and AgOAc (silver acetate).13. The method of preparing a gamma-lactam compound of claim 9 , wherein the base is used at 0.01 to 0.1 mol with respect to 1 mol of the dioxazol- ...

CARBON MONOXIDE RELEASING NORBORNENONE COMPOUNDS

The present invention provides organic compounds which are capable of releasing carbon monoxide under physiological conditions or pH trigger, and to the use of such compounds for conditioning a cell, tissue or organ, for example, to protect against ischaemic injury during a transplant event. 2. The norbornenone compound of claim 1 , wherein X is selected from halo claim 1 , ONO claim 1 , OP(O)(OR) claim 1 , OC(O)R claim 1 , OS(O)R claim 1 , OS(O)OR claim 1 , SR claim 1 , S(O)R claim 1 , S(O)R claim 1 , OR claim 1 , and NRR; and Rand Rare each independently selected from hydrogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , aryl claim 1 , arylalkyl and arylhaloalkyl.3. The norbornenone compound of claim 1 , wherein X is selected from halo claim 1 , OS(O)R claim 1 , and OS(O)OR; and Ris independently selected from hydrogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , aryl claim 1 , arylalkyl and arylhaloalkyl.4. The norbornenone compound of claim 1 , wherein X is selected from iodo claim 1 , bromo claim 1 , chloro claim 1 , SR claim 1 , S(O)R claim 1 , S(O)R claim 1 , OS(O)R claim 1 , and OS(O)OR; and Ris independently selected from hydrogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , phenyl claim 1 , phenylalkyl and phenylhaloalkyl.5. The norbornenone compound of claim 1 , wherein R claim 1 , R claim 1 , Rand R claim 1 , are each independently selected from hydrogen claim 1 , halo claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , monocyclic or bicyclic Ccarbocyclyl claim 1 , and monocyclic or bicyclic Cheterocyclyl claim 1 , polyethylene glycol claim 1 , and a saccharide; wherein the alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , carbocyclyl claim 1 , and heterocyclyl group claim 1 , are each optionally substituted with 1-3 substituents independently selected from halo claim 1 , CN claim 1 , NO claim 1 , OC(O)R claim 1 , C(O)R claim 1 , C(O)OR claim 1 , OR claim 1 , OS(O)R claim 1 , NRR claim 1 , SR claim 1 , polyethylene glycol claim 1 ...

Novel tricyclic compounds and preparation thereof

The present invention provides novel tricyclic compound of Formula I or its stereoisomer or ester or pharmaceutically acceptable salts and preparation thereof useful for treatment of cancer.

POLYMORPHIC FORMS OF ST-246 AND METHODS OF PREPARATION

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions. 140.-. (canceled)41. A polymorph Form VI of 4-trifluoromethyl-N-(3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide (ST-246) which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of 6.43 , 7.10 , 8.23 , 10.46 , 12.62 , 13.72 , 15.71 , 17.84 , 19.34 , 21.52 , 23.73 , 24.17 , 24.71 , 26.71 , 27.26 , 30.11 and 31.00 degrees.42. An isolated polymorph according to that is at least about 70% free of other forms.43. An isolated polymorph according to that is at least about 80% free of other forms.44. An isolated polymorph according to that is at least about 90% free of other forms.45. An isolated polymorph according to that is at least about 95% free of other forms.46. An isolated polymorph according to that is at least about 99% free of other forms.47. A pharmaceutical composition comprising the polymorph of claim and further comprising one or more pharmaceutically acceptable ingredients selected from the group consisting of carriers claim 41 , excipients claim 41 , diluents claim 41 , additives claim 41 , fillers claim 41 , lubricants and binders.48. The pharmaceutical composition of claim 47 , wherein the composition is formulated for oral administration.49. A method of treating Orthopoxvirus infections comprising administering to a patient in need thereof a therapeutically effective amount of the polymorph of .50. A method of treating eczema vaccinatum comprising administering to a patient in need thereof a therapeutically effective amount of the polymorph of .5183.-. (canceled)84. A method of producing crystal polymorphic Form VI of ST-246 claim 41 , comprising the steps of:a) dissolving ST-246 in at least one solvent to make a solution;b) cooling said solution ...

INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects. 5. A method for producing an indomethacin derivative that substantially lacks cyclooxygenase inhibitory activity but that has aldo-keto reductase family 1 , member C3 (AKR1C3) inhibitory activity , the method comprising performing a microwave-assisted reaction between (a) a Cto Calkoxy- or halo-substituted phenylhydrazine or salt thereof and (b) a cyclic or acyclic aliphatic ketoacid or alkyl ester thereof thereby providing an indole alkyl carboxylic acid or ester thereof , wherein the indole alkyl carboxylic acid or ester is a synthetic precursor of the indomethacin derivative.6. The method of claim 5 , wherein the microwave-assisted reaction is performed in the presence of sulfuric acid.7. The method of claim 5 , wherein the microwave-assisted reaction is performed in an alcoholic solvent claim 5 , preferably methanol.10. The method of claim 9 , wherein the cyclic or acyclic aliphatic ketoacid or alkyl ester thereof is selected from the group consisting of 3-oxopentanoic acid claim 9 , 4-oxobutanoic acid claim 9 , 4-oxopentanoic acid claim 9 , 5-oxohexanoic acid claim 9 , 4-oxohexanoic acid claim 9 , 4-oxoheptanoic acid claim 9 , 4-oxocyclohexanecarboxylic acid claim 9 , 3-oxocyclohexanecarboxylic acid or a methyl or ethyl ester thereof.12. The method of claim 5 , further comprising reacting the indole alkyl carboxylic acid or ester thereof with an aliphatic or aromatic acid halide to introduce an acyl substituent at the indole nitrogen atom ...

PURIFICATION METHOD

An object of the present disclosure is to provide a method for purifying the following fullerene derivative represented by formula (1) that is advantageous in production costs. The object is achieved by the method for purifying the fullerene derivative represented by formula (1) 2. The purification method according to claim 1 , wherein Ris an aryl group that is substituted with at least one substituent or unsubstituted.3. The purification method according to claim 1 , wherein ring A is a Cfullerene;{'sup': '1', 'Ris an alkyl group that is substituted with at least one substituent or unsubstituted, or an aryl group that is substituted with at least one substituent or unsubstituted; and'}{'sup': '2', 'Ris an aryl group that is substituted with at least one alkyl group or substituted.'}4. The purification method according to claim 1 , wherein n is 1.5. The purification method according to claim 1 , wherein the aluminum-containing inorganic porous adsorbent is activated clay.6. The purification method according to claim 1 , wherein the aluminum-containing inorganic porous adsorbent has a median size of 50 to 500 μm.7. The purification method according to claim 1 , wherein step 1 is a step of introducing the composition containing the fullerene derivative represented by formula (1) claim 1 , which is a target product for purification claim 1 , and the one or more impure fullerene compounds into a column containing activated clay claim 1 , which is a solid phase; and the method further comprises step 2 of allowing a solvent claim 1 , which is a liquid phase claim 1 , to flow through the column having the composition introduced to elute the fullerene derivative represented by formula (1) from the column.8. The purification method according to claim 1 , wherein the flow rate of the fullerene derivative represented by formula (1) per column cross-section area of 0.002 mis 0.001 to 50 g/min.9. The purification method according to claim 1 , wherein the flow rate of the solvent ...

SUBSTITUTED (1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS

Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.

MCBI analogs of CC-1065 and the duocarmycins

Mcbi analogs of cc-1065 and the duocarmycins

MCBI (7-methoxy-1,2,9,9a-tetra-hydrocyclopropa[c]benz[e]indol-4-one) is employable as a DNA alkylating agent and can be incorporated into analogs of CC-1065 and the duocarmycins for constructing regioselective DNA alkylating agents.

Metalosen dan katalis untuk polimerisasi olefin

Metallocenes and catalysts for olefin polymerization

Metallocenes and catalysts for olefin-polymerisation

A class of metallocenes of formula (I): (ZR1m)n(Cp)(A)rMLpL'q (I) wherein (ZR1m)n is a divalent group bridging Cp and A, Cp is a heterocyclic cyclopentadienyl group of formula (II) or (II'), wherein one of X or Y is a single bond, the other being an heteroatom; R?2 and R3¿ are hydrogen, halogen or a hydrocarbon radical, optionally containing heteroatoms; R4 is halogen or an hydrocarbon radical, optionally containing heteroatoms; the group A is a cyclopentadienyl derivative or is equal to Cp; M is Ti, Zr or Hf; m is 1 or 2; n ranges from 0 to 4; r is 0 or 1; p and q range from 0 to 3; and a ranges from 0 to 4. Moreover, are disclosed catalyst systems containing these metallocenes, useful in the polymerization of olefins.

Metallocenes and catalysts for olefin-polymerisation

A class of metallocenes of formula (I): (ZR 1 m ) n (Cp)(A) r ML p L′ q (I) wherein (ZR 1 m ) n , is a divalent group bridging Cp and A, Cp is a heterocyclic cyclopentadienyl group of formula (II) or (II′), wherein one of X or Y is a single bond, the other being an heteroatom; R 2 and R 3 are hydrogen, halogen or a hydrocarbon radical, optionally containing heteroatoms; R 4 is halogen or an hydrocarbon radical, optionally containing heteroatoms; the group A is a cyclopentadienyl derivative or is equal to Cp; M is Ti, Zr or Hf; m is 1 or 2; n ranges from 0 to 4; r is 0 or 1; p and q range from 0 to 3; and a ranges from 0 to 4. Moreover, are disclosed catalyst systems containing these metallocenes, useful in the polymerization of olefins.

METALLOCENES AND CATALYSTS FOR OLEFIN POLYMERIZATION

Metallocenes and catalysts for olefin-polymerisation

A class of metallocenes of formula (I): (ZR 1 m ) n (Cp)(A) r ML p L′ q (I) wherein ZR 1 m ) is a divalent group bridging Cp and A, Cp is a heterocyclic cyclopentadienyl group of formula (II) or (II′), wherein one of X or Y is a single bond, the other being an heteroatom; R 2 and R 3 are hydrogen, halogen or a hydrocarbon radical, optionally containing heteroatoms; R 4 is a halogen or an hydrocarbon radical, optionally containing heteroatoms; the group A is a cyclopentadienyl derivative or is equal to Cp; M is Ti, Zr or Hf; m is 1 or 2; n ranges from 0 to 4; r is 0 or 1; p and q range from 0 to 3; and a ranges from 0 to 4. Moreover, are disclosed catalyst systems containing these metallocenes, useful in the polymerization of olefins.

金属茂和烯烃聚合催化剂

本发明涉及一类式(I)的金属茂：(ZR 1 m ) n (Cp)(A) r ML p L’ q (I)，其中(ZR 1 m ) n 是一个桥连Cp和A的二价基团，Cp是一个式(II)或(II’)的杂环环戊二烯基基团，其中X或Y之一是一个单键，另一个是杂原子；R 2 和R 3 是氢、卤素或一个烃基，任选含有杂原子；R 4 是卤素或一个烃基，任选含有杂原子；基团A是一个环戊二烯基衍生物或等于Cp；M是Ti、Zr或Hf；m是1或2；n范围为0-4；r是0或1；p和q范围为0-3和0-4。此外，这里公开了可用于烯烃聚合的含这些金属茂的催化剂体系。

Catalysts for metallocene and olefin polymerization

Metalocenes and olefins polymerisation catalysts

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1303584 Phthalimides INSTITUT FRANCAIS DU PETROLE DE CARBURANTS ET LUBRIFIANTS and ENTERPRISE DE RECHERCHES ET D'ACTIVITES PETROLIERES-ELF 19 April 1971 [21 Jan 1970] 20036/71 Headings C2C and C2P [Also in Division C5] Novel compounds of the general Formula I where the hydrocarbon ring is a cyclohexanic, aromatic, dihydroaromatic or tetrahydroaromatic ring, each of R 1 ,R 2 ,R 2 and R 4 (which may be similar or dis-similar) is a hydrogen atom or an aliphatic radical, with the proviso that R 1 and R 4 together may represent a divalent C 1-2 radical and that the total number of carbon atoms in R 1 to R 4 is 0-30, n is 2-10, m is 1-10 and R is a univalent aliphatic C 1-30 hydrocarbon radical, are made by reacting a linear amine of formula with an equimolecular amount of an ester-acid or anhydride respectively of formula wherein R 5 is a univalent aliphatic HC radical or an optionally substituted phenyl radical, and removing the water formed during the reaction; the reaction may be carried out in an inert solvent consisting of at least one aromatic hydrocarbon that forms an azeotrope with water, and the water formed during the reaction may thus be removed by azeotropic entrainment. Salts of the compounds of Formula I may be obtained by reaction with a mono- or di-alkyl phosphoric acid of formula R<SP>1</SP>-P(O)-(OH) 2 or (R<SP>1</SP>O) 2 P(O)-OH where R<SP>1</SP>is a univalent saturated aliphatic HC radical and is used in such amount that the number of OH groups does not exceed the number of amine groups. The compounds I and salts thereof are useful as fuel additives (Division C5).

유기 전계 발광 소자

본 발명은 특정 조합의 도판트 화합물 및 호스트 화합물을 함유하는 유기 전계 발광 소자에 관한 것이다. 본 발명에 따른 유기 전계 발광 소자는 황록색 발광을 나타내고, 소자의 전류특성을 개선시킴으로써 소자의 구동전압을 저하시키고 동시에 전력효율과 작동수명을 향상시킨다.

The method of producing pentacyclic compounds

Organic light emitting device

본 발명은 하기 화학식 1로 표시되는 헤테로 고리 화합물 및 이를 포함한 유기막을 구비한 유기 발광 소자에 관한 것이다: The present invention relates to an organic light emitting device having a heterocyclic compound represented by Chemical Formula 1 and an organic film including the same: <화학식 1> <Formula 1> 상기 화학식에 대한 설명은 발명의 상세한 설명을 참조한다. For the description of the above formula, see the detailed description of the invention.

신규 화합물 및 중합체, 및 감방사선성 수지 조성물

방사선에 대한 투명성이 높고, 더욱이 감도, 해상도, 패턴 형상 등의 레지스트로서의 기본 물성이 우수하고, 특히 고해상도이고 DOF가 넓고 LER이 우수한 감방사선성 수지 조성물, 그 조성물에 이용할 수 있는 중합체 및 이 중합체의 합성에 이용되는 신규 화합물을 제공한다. 신규 화합물은 하기 화학식 2로 표시된다. <화학식 2> 화학식 2에 있어서, R 4 는 메틸기, 트리플루오로메틸기 또는 수소 원자를 나타내고, Rf 중 1개 이상은 불소 원자 또는 탄소수 1 내지 10의 직쇄상 또는 분지상의 퍼플루오로알킬기를 나타내고, A는 2가의 유기기 또는 단일 결합을 나타내고, G는 불소 원자를 함유하는 2가의 유기기 또는 단일 결합을 나타내고, M m ＋ 는 금속 이온 또는 오늄 양이온을 나타내고, m은 1 내지 3의 자연수를, p는 1 내지 8의 자연수를 각각 나타낸다. 감방사선성 수지 조성물, 화학 증폭형 레지스트, 집적 회로 소자

新的法呢基转移酶的抑制剂,其制备方法及其药物组合物

通式(I)的新化合物，其制备方法及其药物组合物。通式(I)中：R代表：通式-(CH 2 ) m -X 1 -(CH 2 ) n -Z，其中：X 1 ＝单键或O或S，m＝0或1，n＝0，1或2，CH 2 基可由羧基、烷氧基羰基、氨基甲酰基、烷基氨基甲酰基、二烷基氨基甲酰基、氨基、烷基氨基、二烷基氨基取代和Z代表：羧基，COOR 4 (R 4 ＝烷基)，或CON(R 5 )(R 6 )(R 5 ＝氢或烷基，R 6 ＝氢或视具体情况而定被取代的烷基，或R 5 ＝氢或烷基，R 6 ＝羟基、视具体情况而定被取代烷氧基，或氨基，或PO(OR 7 ) 2 (R 7 代表氢或烷基)，或NH-CO-T基(T＝氢或视具体情况而定取代的烷基，或-CH 2 -N基)R 1 和R 2 ＝氢或卤素或烷基、视具体情况而定取代的烷基氧基，或者R 1 和R 2 彼此相邻，构成一个视具体情况而定取代的含有1或2个杂原子的杂环，或者R 1 ＝氢或卤素或烷基、视具体情况而定取代的烷基氧基，和R 2 ＝硫代烷基，R 3 ＝氢或卤素或烷基、链烯基、烷基氧基、烷基硫代基、羧基或烷基氧羰基，X＝O或S或-NH-，-CO-，亚甲基、亚乙基、亚烷基或1，1-环烷基，和Y＝O或S。通式(I)新化合物是法呢基转移酶抑制剂，它具有显著的抗肿瘤和抗白血病的性质。

Flame retardants and compositions containing them

Flame retardants having good stability at the processing temperatures of high melting polymers are described. The flame retardants are halogen-containing bis-imides, for example, those of the formula ##STR1## R being defined in the specification.

Patterning method, chemically-amplified resist composition, and resist film

고감도, 고해상성, 우수한 러프니스 성능, 및 우수한 드라이 에칭 내성을 동시에 만족함과 아울러 또한 현상 시간 의존성이 우수한 패턴 형성 방법으로서 (가) (A) 산 분해성기를 갖는 풀러렌 유도체와, (B) 활성광선 또는 방사선의 조사에 의해 산을 발생하는 화합물과, (C) 용제를 함유하는 화학증폭형 레지스트 조성물에 의해 막을 형성하는 공정, (나) 상기 막을 노광하는 공정, 및 (다) 유기 용제를 포함하는 현상액을 사용하여 현상하는 공정을 포함하는 네거티브형 패턴 형성 방법을 제공한다. (A) a fullerene derivative having an acid-decomposable group, (B) an actinic ray-curable resin composition comprising (A) a fullerene derivative having an acid-decomposable group, and (C) a step of forming a film by a chemically amplified resist composition containing a solvent, (B) a step of exposing the film, and (C) a step of exposing the film to a developing solution containing an organic solvent And a step of developing the light-emitting layer by using the light-emitting layer.

Metallocenes and catalysts for olefin-polymerisation

取代的四环四氢吡喃、吡咯烷和四氢噻吩衍生物

本发明涉及新的取代的四环四氢吡喃、吡咯烷和四氢噻吩衍生物，其对于血清素受体、尤其是5-HT 2A 和5-HT 2C 受体具有结合亲合性，对于多巴胺受体、尤其是多巴胺D2受体具有结合亲合性，具有去甲肾上腺素再摄取抑制性能，涉及包含按照本发明化合物的药物组合物，其作为药物的用途，尤其是用于预防和/或治疗精神病学和神经病学疾病范围内的疾病，特别是某些精神病、心血管和胃动力学病症，和它们的制备方法。按照本发明的化合物可以由通式(I)代表也包括其药学可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式和其前体药物，其中所有的取代基如权利要求1所定义。

The method of obtaining derivatives of indole-2-carboxylic acid or their salts

Новые замещенные тетрациклические производные тетрагидрофурана, пирролидина и тетрагидротиофена

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2007 125 693 (13) A (51) ÌÏÊ C07D 209/70 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007125693/04, 06.12.2005 (71) Çà âèòåëü(è): ßÍÑÑÅÍ ÔÀÐÌÀÖÅÂÒÈÊÀ Í.Â. (BE) (30) Êîíâåíöèîííûé ïðèîðèòåò: 07.12.2004 EP 04106373.6 (43) Äàòà ïóáëèêàöèè çà âêè: 20.01.2009 Áþë. ¹ 2 (87) Ïóáëèêàöè PCT: WO 2006/061392 (15.06.2006) A Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. À.Â.Ìèö (54) ÍÎÂÛÅ ÇÀÌÅÙÅÍÍÛÅ ÒÅÒÐÀÖÈÊËÈ×ÅÑÊÈÅ ÏÐÎÈÇÂÎÄÍÛÅ ÒÅÒÐÀÃÈÄÐÎÔÓÐÀÍÀ, ÏÈÐÐÎËÈÄÈÍÀ È ÒÅÒÐÀÃÈÄÐÎÒÈÎÔÅÍÀ R U 1. Ñîåäèíåíèå ôîðìóëÛ (I) A 2 0 0 7 1 2 5 6 9 3 (57) Ôîðìóëà èçîáðåòåíè åãî N-îêñèäíà ôîðìà, ôàðìàöåâòè÷åñêè ïðèåìëåìà àääèòèâíà ñîëü èëè ñòåðåîõèìè÷åñêè èçîìåðíà ôîðìà, ãäå ïóíêòèðíà ëèíè îçíà÷àåò íåîá çàòåëüíóþ ñâ çü; i è j îçíà÷àþò öåëûå ÷èñëà, íåçàâèñèìî äðóã îò äðóãà ðàâíûå íóëþ, 1, 2, 3 èëè 4; A è B êàæäûé íåçàâèñèìî äðóã îò äðóãà îçíà÷àþò áåíçî-, íàôòîãðóïïó èëè ðàäèêàë, âûáðàííûé èç ãðóïïû, ñîñòî ùåé èç ôóðî-; òèåíî-; ïèððîëî-; îêñàçîëî-; òèàçîëî-; èìèäàçîëî-; èçîêñàçîëî-; èçîòèàçîëî-; îêñàäèàçîëî-; òðèàçîëî-; ïèðèäèíî-; ïèðèäàçèíî-; ïèðèìèäèíî-; ïèðàçèíî-; èíäîëî-; èíäîëèçèíî-; èçîèíäîëî-; áåíçîôóðî-; èçîáåíçîôóðî-; áåíçîòèåíî-; èíäàçîëî-; áåíçèìèäàçîëî-; áåíçòèàçîëî-; õèíîëèçèíî-; õèíîëèíî-; èçîõèíîëèíî-; ôòàëàçèíî-; õèíàçîëèíî-; õèíîêñàëèíî-; õðîìåíî- è íàôòèðèäèíîãðóïïû; êàæäûé R 9 íåçàâèñèìî äðóã îò äðóãà âûáðàí èç ãðóïïû, ñîñòî ùåé èç âîäîðîäà; ãàëîãåíà; öèàíîãðóïïû; ãèäðîêñèãðóïïû; êàðáîêñèëà; íèòðîãðóïïû; àìèíîãðóïïû; ìîíîÑòðàíèöà: 1 RU 2 0 0 7 1 2 5 6 9 3 (86) Çà âêà PCT: EP 2005/056544 (06.12.2005) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 09.07.2007 (72) Àâòîð(û): ÑÈÄ-ÍÓÍÜÅÑ Õîñå Ìàðè (ES), ÌÅÃÅÍÑ Àíòîíèóñ Àäðèàíóñ Õåíäðèêóñ Ïåòðóñ (BE), ÒÐÀÁÀÍÊÎ-ÑÓÀÐÅÑ Àíäðåñ Àâåëèíî (ES), ÊÎÓÊÍÈ Ìîõàìåä (BE), ÕÎÐÍÀÐÒ Äæîðæ Æîçåô Êîðíåëèóñ (BE), ÊÎÌÏÅÐÍÎËËÅ Ôðàíñ Éîçåô Êîðíåëèóñ (BE), ...

Derivatives of tetrahydrocarbazoles, method of obtaining them and pharmaceutical compositions containing them

FIELD: medicine. SUBSTANCE: invention relates to compounds of general formula (I) and their pharmaceutically acceptable salts and pharmaceutically acceptable asters, possessing activity with respect to LXRα and/or LXRβ receptors. Compounds can be applied for treatment and prevention of diseases mediated by LXRα and/or LXRβ receptors, namely: increased level of lipids and cholesterol level, atherosclerotic diseases, diabetes, metabolic syndrome, dyslipidermia, sepsis, inflammatory diseases, pancreatitis, liver cholestasis/fibrosis, and diseases which include inflammatory component, such as Alzheimer's disease and reduced/improvable cognitive function. In general formula n represents integer number from 0 to 3; R 1 is independently selected from group consisting of halogen, -CN, -NO 2 , -SO 2 Me, lower alkyl, -OR 11 , pyperidinyl and -N(R 11 )(R 11 ), where R 11 is independently selected from lower alkyl and H, X 1 , X 2 , X 3 and X 4 are independently selected from nitrogen and carbon, on condition that, not more than two of X 1 , X 2 , X 3 and X 4 can simultaneously represent nitrogen, and in case when two of X 1 , X 2 , X 3 and X 4 represent nitrogen, n represents 0,1 or 2; k represents integer number 0 or 1; R2 represents H; R 3 represents H, lower alkyl or halogen; R 4 represents aryl, heteroaryl, lower alkylaryl or lower alkylheteroaryl, each of which is optionally substituted with substituents in amount from one to five, which are independently selected from group consisting of halogen, lower alkyl, -OR 41 , lower alkinyl and NR 42 R 43 , where R 41 represents lower alkyl, R 42 and R 43 independently on each other represent hydrogen or lower alkyl, or NR 42 R 43 represents pyrrolidinyl, or R 4 represents lower alkyl; R 5 is selected from group, heteroaryl, consisting of and , said aryl and heteroaryl being optionally substituted in one or more positions with one or more substituents, independently selected from group consisting of H, halogen, lower alkyl ...

Titanocenes, the use thereof, and n-substituted fluoroanilines

Titanocenes containing two 5-membered cyclodienyl gropus, for example cyclopentadienyl, and one or two 6-membered carbocyclic or 5- or 6-membered heterocyclic aromatic rings which are substituted by a fluorine atom in at least one of the two ortho-positions to the titanium-carbon bond and contain, as further substituents, a substituted amino radical, are suitable as photoinitiators for radiation-induced polymerization of ethylenically unsaturated compounds.

Способ получени индолкарбоновойкислоты или ее эфиров

Pyromethene metal complex, pyromethene compound, light emitting device material, light emitting device, display device and lighting device

본 발명의 목적은 발광 효율이 높고, 색순도가 우수한 적색 발광 재료 및 적색 발광 소자를 제공하는 것이다. 본 발명은 특정한 일반식으로 표시되는 피로메텐 금속 착체이다.

Substituted bicycloheptane-2, 3-dicarboximides

Containing hindered phenolic norbornane-2,3-dicarboximides stabilized compositions

Compounds having the formula ##SPC1## Wherein R 1 and R 2 are lower alkyl, X and Y are hydrogen or, when taken together, they form a bond or an ether linkage, m is 0 to 3, and n is 0 to 2, are good ultraviolet light stabilizers for synthetic polymers.

Patent CH615911A5

Polymer parts and compound useful therein

ABSTRACT Compounds of the formula (I) ( I ) where n' is 1, 2, 3 or 4 and X is S or S-S-where each A is where Y is H, C1 or Br, and preferably when used as a flame retardant at least on- Y is C1 or Br or where n2 is 0, 1 and n3 is 0, 1, R1, R2 and R3 are H, or straight or branched alkyl of 1 to 8 carbons, or

Resin compositions

The present disclosure is directed to resins and to polymers, copolymers, and blends formed therefrom.

METHOD OF OBTAINING PENTACYCLIC COMPOUNDS

Polymorphic forms of st-246 compound and methods for producing

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to a polymorphic form of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)benzamide (ST-246 compound), a method for producing the polymorphic form, and a pharmaceutical composition containing said polymorphic form. EFFECT: producing new compounds. 13 cl, 24 dwg, 18 tbl, 11 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 578 606 C2 (51) МПК C07D 209/76 (2006.01) A61K 31/403 (2006.01) A61P 31/20 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2012144818/04, 23.03.2011 (24) Дата начала отсчета срока действия патента: 23.03.2011 Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 27.04.2014 Бюл. № 12 (56) Список документов, цитированных в отчете о поиске: CN 101445478 A, 03.06.2009. US 20080004452 A1, 03.01.2008. RU 2412160 C1, 20.02.2011. (73) Патентообладатель(и): СИГА ТЕКНОЛОДЖИЗ, ИНК (US) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 23.10.2012 2 5 7 8 6 0 6 (45) Опубликовано: 27.03.2016 Бюл. № 9 R U 23.03.2010 US 61/316,747; 12.08.2010 US 61/373,031 (72) Автор(ы): ТЯВАНАГИМАТТ Шантхакумар Р. (US), СТОУН Мелиалани А.К.Л. (US), УЭЙМЕРС Уилльям К. (US), НЕЛЬСОН Дилан (US), БОЛКЕН Тоув К. (US), ХРУБИ Деннис Э. (US), О'НЕЙЛЛ Майкл Х. (US), СВИТЭППЛ Гари (US), МакКЛУН Келли А. (US) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2011/119698 (29.09.2011) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (54) ПОЛИМОРФНЫЕ ФОРМЫ СОЕДИНЕНИЯ ST-246 И СПОСОБЫ ПОЛУЧЕНИЯ (57) Реферат: Изобретение относится к полиморфной форме получения полиморфной формы и 4-трифторметил-N-(3,3a,4,4a,5,5a,6,6a-октагидрофармацевтической композиции, содержащей 1,3-диоксо-4,6-этеноциклопроп[f]изоиндол-2(1H) указанную полиморфную форму. 7 н. и 6 з.п. ф-ил)бензамида (соединение ST-246), к способу лы, 24 ил., 18 табл., 11 пр. R ...

Method for synthesizing cycloalkanyl[b]indoles, cycloalkanyl[b]benzofurans, cycloalkanyl[b]benzothiophenes, compounds and methods of use

A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided.

Indenoindole compounds II

具有如下结构式的化合物及其对映体和盐 式中R是氢或低级烷基或COR 15 R 1 、R 2 、R 11 、和R 12 、是氢或低级烷基， R 3 、R 4 、R 5 、和R 6 是氢、羟基、卤素、低级烷基、低级烷氧基或者一或二-低级烷基氨基、NH 2 或NR 13 COR 14 ， R 7 、R 8 、R 9 和R 10 是氢、羟基、低级烷基、低级烷氧基、一或二-低级烷基氨基、或NR 13 COR 14 ，其中R 13 、R 14 和R 15 是氢或低级烷基，但须：当R是COR 15 时，R 3 -R 10 中至少有一个羟基或一或二-低级烷基氨基，该化合物在医药和非医药领域内作为抗氧化剂是有效的。结构式为IA和IB的化合物有许多是新的，并且叙述了制备它们的各种方法。

Tricyclic derivatives of indenopyrrole as modulators of serotinin receptors, a pharmaceutical composition based on them, and a method for treating diseases, and / or non-trivial necrosis.

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2007 107 494 (13) A (51) ÌÏÊ C07D 209/80 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007107494/04, 26.07.2005 (71) Çà âèòåëü(è): Ýñåðñèñ, Èíê. (US) (30) Êîíâåíöèîííûé ïðèîðèòåò: 29.07.2004 US 60/592047 (43) Äàòà ïóáëèêàöèè çà âêè: 10.09.2008 Áþë. ¹ 25 Àäðåñ äë ïåðåïèñêè: 127055, Ìîñêâà, à/ 11, ïàò.ïîâ. Í.Ê.Ïîïåëåíñêîìó, ðåã. N 31 (54) ÒÐÈÖÈÊËÈ×ÅÑÊÈÅ ÏÐÎÈÇÂÎÄÍÛÅ ÈÍÄÅÍÎÏÈÐÐÎËÀ ÊÀÊ ÌÎÄÓËßÒÎÐÛ R U (57) Ôîðìóëà èçîáðåòåíè 1. Òðèöèêëè÷åñêèå ïðîèçâîäíûå èíäåíîïèððîëà, îõâàòûâàåìûå îáùåé ñòðóêòóðíîé ôîðìóëîé A 2 0 0 7 1 0 7 4 9 4 A ÑÅÐÎÒÈÍÈÍÎÂÛÕ ÐÅÖÅÏÒÎÐÎÂ, ÔÀÐÌÀÖÅÂÒÈ×ÅÑÊÀß ÊÎÌÏÎÇÈÖÈß ÍÀ ÈÕ ÎÑÍÎÂÅ È ÑÏÎÑÎÁ ËÅ×ÅÍÈß ÇÀÁÎËÅÂÀÍÈÉ, ÐÀÑÒÐÎÉÑÒ È/ÈËÈ ÏÀÒÎËÎÃÈ×ÅÑÊÈÕ ÑÎÑÒÎßÍÈÉ, ÑÂßÇÀÍÍÛÕ Ñ ÍÅÎÁÕÎÄÈÌÎÑÒÜÞ ÌÎÄÓËßÖÈÈ ÔÓÍÊÖÈÈ 5-ÍÒ2Ñ ÐÅÖÅÏÒÎÐΠâ êîòîðîé R1 âûáðàí èç ãðóïïû, ñîñòî ùåé èç Í, ãàëîãåíà, Ñ1-10-àëêèëà, Ñ2-àëêåíèëà, Ñ2-10-àëêèíèëà, ïåðãàëîãåíàëêèëà, CN, N(R6)2, SR6, CON(R6)2, NR6COR7, 10 NR6CO2R7, SO2N(R6)2, NR6SO2R7, àðèëà, ãåòåðîàðèëà, Ñ1-10-àëêèëàðèëà è Ñ1-10àëêèëãåòåðîàðèëà; è åñëè m+n=1, òî R1 ìîæåò òàêæå áûòü OR6 èëè OCOR7; R2, R3 è R4 íåçàâèñèìî âûáðàíû èç ãðóïïû, ñîñòî ùåé èç Í, ãàëîãåíà, Ñ1-10-àëêèëà, Ñ2-àëêåíèëà, Ñ2-10-àëêèíèëà, ïåðãàëîãåíàëêèëà, CN, OR6, N(R6)2, SR6, OCOR7, CON(R6)2, 10 NR6COR7, NR6CO2R7, SO2N(R6)2, NR6SO2R7, àðèëà, ãåòåðîàðèëà, Ñ1-10-àëêèëàðèëà è Ñ1-àëêèëãåòåðîàðèëà, èëè R2 è R3 ñîâìåñòíî ñ öèêëîì, ê êîòîðîìó îíè ïðèñîåäèíåíû, 10 îáðàçóþò 5-7-÷ëåííûé êàðáî- èëè ãåòåðîöèêë; R5 âûáðàí èç ãðóïïû, ñîñòî ùåé èç Í, Ñ1-10-àëêèëà, Ñ2-10-àëêåíèëà, Ñ2-10-àëêèíèëà, Ñòðàíèöà: 1 RU 2 0 0 7 1 0 7 4 9 4 (86) Çà âêà PCT: US 2005/026415 (26.07.2005) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 28.02.2007 (72) Àâòîð(û): ÕÀÊ Áåéàðä (US), ÁÅÍÍÀÍÈ Þññåô Ë. (US), ÐÎÁÀÐÄÆ Ìàéêë Äæ. (US) A 2 0 0 7 1 0 7 4 9 4 A R U 2 0 0 7 1 0 7 4 9 4 Ñòðàíèöà: 2 R U ïåðãàëîãåíàëêèëà, CN, OR6, N(R6)2, SR6, OCOR7, CON(R6)2, NR6COR7, NR6CO2R7, NR6SO2R7, ...

POLYMORPHIC COMPOUND FORMS ST-246 AND METHODS FOR PRODUCING

1. Полиморф формы I 4-трифторметил-N-(3,3а,4,4а,5,5а,6,6а-октагидро-1,3-диоксо-4,6-этеноциклопроп[f]изоиндол-2(1Н)-ил)бензамида (соединение ST-246), который демонстрирует картину рентгеновской порошковой дифракции, имеющую характеристические пики при угле отражения 2θ приблизительно 7,63, 10,04, 11,47, 14,73, 15,21, 15,47, 16,06, 16,67, 16,98, 18,93, 19,96, 20,52, 20,79, 22,80, 25,16, 26,53, 27,20, 27,60, 29,60, 30,23, 30,49, 30,68, 31,14, 33,65, 34,33, 35,29, 35,56, 36,30, 37,36, 38,42, 38,66 градусов.2. Полиморф по п.1, который представляет собой изолированный полиморф, и который является по меньшей мере приблизительно на 70% свободным от других форм, предпочтительно является по меньшей мере приблизительно на 80% свободным от других форм, более предпочтительно является по меньшей мере приблизительно на 90% свободным от других форм, еще более предпочтительно является по меньшей мере приблизительно на 95% свободным от других форм, в частности является по меньшей мере приблизительно на 99% свободным от других форм.3. Полиморф формы II 4-трифторметил-N-(3,3а,4,4а,5,5а,6,6а-октагидро-1,3-диоксо-4,6-этеноциклопроп[f]изоиндол-2(1Н)-ил)бензамида (соединение ST-246), который демонстрирует картину рентгеновской порошковой дифракции, имеющую характеристические пики при угле отражения 2θ в соответствии с фиг.2.4. Полиморф по п.3, который представляет собой изолированный полиморф, и который является по меньшей мере приблизительно на 70% свободным от других форм, предпочтительно является по меньшей мере приблизительно на 80% свободным от других форм, более предпочтительно является по меньшей мере приблизительно на 90% свободным от других форм, еще более предпочтительно является по меньшей мере приблизительно на 95% свободным от других форм, в частности является � РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК A61K 31/44 (13) 2012 144 818 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2012144818/04, 23.03.2011 (71) ...

Compound having indenocarbazole ring structure and organic electroluminescent element

고효율, 고내구성의 유기 일렉트로루미네센스 소자용의 재료로서, 정공의 주입·수송성능이 우수하고, 전자 저지능력을 가지며, 박막 상태에서의 안정성이 높고, 발광 효율이 높은 우수한 특성을 가지는 유기 화합물을 제공하고, 이 화합물을 더 이용하여, 고효율, 고내구성의 유기 일렉트로루미네센스 소자를 제공하는 것. 하기 일반식(1)로 표시되는 인데노카바졸 환 구조를 가지는 화합물이고, 한 쌍의 전극과 그 사이에 끼워진 적어도 1층의 유기층을 가지는 유기 일렉트로루미네센스 소자에 있어서, 상기 화합물이, 적어도 1개의 유기층의 구성 재료로서 이용되고 있는 것을 특징으로 하는 유기 일렉트로루미네센스 소자이다. An organic electroluminescence device having high efficiency and high durability and having excellent characteristics of injecting and transporting holes, having electron blocking ability, high stability in a thin film state, And further using this compound to provide an organic electroluminescent device with high efficiency and high durability. An organic electroluminescence device having an indenocarbazole ring structure represented by the following general formula (1), wherein the compound has at least a pair of electrodes and at least one organic layer sandwiched therebetween, Is an organic electroluminescent device characterized by being used as a constituent material of one organic layer.

Materials for organic electroluminescent devices

Die vorliegende Erfindung beschreibt Indenocarbazol-Derivate mit elektronen- und lochtransportierenden Eigenschaften, insbesondere zur Verwendung in der Emissions- und/oder Ladungstransportschicht von Elektrolumineszenzvorrichtungen oder als Matrixmaterial. Die Erfindung betrifft ferner ein Verfahren zur Herstellung der erfindungsgemäßen Verbindungen sowie elektronische Vorrichtungen, enthaltend diese. The present invention describes indenocarbazole derivatives having electron and hole transporting properties, in particular for use in the emission and / or charge transport layer of electroluminescent devices or as matrix material. The invention further relates to a process for the preparation of the compounds according to the invention and to electronic devices containing them.

Organic light-emitting device

Provided is an organic light-emitting device including a first electrode, a second electrode, an emission layer between the first electrode and the second electrode, and a hole transport region between the first electrode and the emission layer, wherein the hole transport region includes an auxiliary layer, the auxiliary layer including at least one amine-based compound represented by Formula 1: where R 11 , R 12 , R 13 , R 14 , R 15 , R 16 , X 11 , L 11 , L 12 , L 13 , a11, a12, a13, b15, and b16 are as defined in the specification.

Organic light-emitting device

유기 발광 소자가 개시된다. An organic light emitting device is disclosed.

Substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives

This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Substituted tetracyclic tetahydrofuran, pyrrolidine and tetrahydrothiophene derivatives

This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT 2A and 5-HT 2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Compound, colorant composition containing the same, and resin composition containing the same

本发明涉及化合物、含有该化合物的色料组合物和含有该化合物的树脂组合物。

DERIVATIVES OF BENZENE AND THEIR PHARMACEUTICAL USE

2-aldehyde indole compound and preparation method thereof

本发明提供了一种2‑醛基吲哚类化合物及其制备方法，以四炔类化合物和2‑苯基‑2‑恶唑啉为原料，在甲苯溶剂反应，得到了一种2‑醛基吲哚类化合物。与现有技术相比，本发明提供了一种全新的2‑醛基吲哚的合成方法，生成一种新的2‑醛基吲哚类化合物。合成的2‑醛基吲哚类化合物具有较高原子经济性，结构更加复杂多样，具有一定的运用前景。

Patent JPH0566952B2

Process for preparing tricyclic aminoacids derivatives

내용 없음.

Multidimensional crosslinkable oligomers

내용 없음. No content.

Isoindoline derivatives

FIELD: chemistry. SUBSTANCE: in general formula (I) , R 1 represents similar or different 2 groups, each of which is selected from group consisting of C 1-3 alkyl, or when R 1 are two adjacent groups, two groups R 1 , taken together, can form saturated or unsaturated 5- or 6-member cyclic group, which can have 1 or 2 oxygens as heteroatom; X represents oxygen or sulphur; values of other radicals are given in invention formula. EFFECT: increase of composition efficiency. 16 cl, 11 tbl, 31 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 343 145 (13) C2 (51) ÌÏÊ C07D 209/46 C07D 401/04 C07D 401/06 C07D 401/12 C07D 401/14 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ C07D 403/04 ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ,C07D 403/12 ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ C07D 405/14 C07D 491/048 C07D 491/056 (12) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) A61K A61K A61K A61K A61K 31/4035 (2006.01) 31/4439 (2006.01) 31/4545 (2006.01) 31/496 (2006.01) 31/551 (2006.01) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2005120003/04, 25.11.2003 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 25.11.2003 (30) Êîíâåíöèîííûé ïðèîðèòåò: 26.11.2002 JP 2002-342399 2 3 4 3 1 4 5 R U (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: Jan Epsztajn et al. Application of organolithium and related reagents in synthesis. Part 23: synthesis strategies based on ortho-aromatic metallation. Synthesis of 4b-arylisoindolo[2,1-a]quinoline derivatives. Tetrahedron, 2000, vol.56, no.27, p.4837-4844. SU 1376941 A3, 23.02.1988. WO 9842666 A1, 01.10.1998. GB 1307205 A (RHONE-POULENC S.A.), 14.02.1973. C 2 C 2 (45) Îïóáëèêîâàíî: 10.01.2009 Áþë. ¹ 1 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 27.06.2005 (86) Çà âêà PCT: JP 03/014986 (25.11.2003) (87) Ïóáëèêàöè PCT: WO 2004/048332 (10.06.2004) Àäðåñ äë ïåðåïèñêè: 103735, Ìîñêâà, óë. Èëüèíêà, 5/2, ÎÎÎ "Ñîþçïàòåíò", ïàò.ïîâ. À.Ï.Àãóðååâó (54) ÏÐÎÈÇÂÎÄÍÛÅ ÈÇÎÈÍÄÎËÈÍÀ (57) Ðåôåðàò: Èçîáðåòåíèå îòíîñèòñ ê íîâûì ñîåäèíåíè ì ôîðìóëû (I) è èõ ...

Novel anthracene derivatives and organic electroluminescent device using the same

본 발명은 신규한 비대칭 안트라센 유도체 및 이를 발광층에 포함하는 유기 발광 소자에 관한 것으로, 보다 상세하게 본 발명에 따른 안트라센 유도체는 하기 화학식1로 표시되며, 비대칭의 고도로 뒤틀린 안트라센 화합물인 것을 특징으로 한다. [화학식 1] [상기 화학식 1에서, R 1 내지 R 4 , X 및 Y는 각각 발명의 상세한 설명에서 정의한 바와 같다.] The present invention relates to a novel asymmetric anthracene derivative and an organic light emitting device including the same in a light emitting layer. More specifically, the anthracene derivative according to the present invention is represented by the following general formula (1) and is an asymmetric highly twisted anthracene compound. [Chemical Formula 1] [Wherein R 1 to R 4 , X and Y are each as defined in the description of the invention].