CYCLOHEXANE COMPOUND AND LIQUID CRYSTAL COMPOSITION CONTAINING THE SAME

The present invention intends to provide a novel cyclohexane compound that can form a liquid crystal composition of which response speed is improved when mixed with a nematic liquid crystal and the like and to provide a specified liquid crystal composition in which a novel cyclohexane compound is mixed. The novel cyclohexane compound is represented by the following formula (1). 5. A liquid crystal composition comprising:{'claim-ref': [{'@idref': 'CLM-00003', 'claim 3'}, {'@idref': 'CLM-00004', 'claim 4'}], 'the liquid crystal composition of mixed with at least one kind of a compound of a compound group of the formula (7) of .'}6. A liquid crystal composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'one or two or more kinds of the cyclohexane compound groups of .'}7. Use of the liquid crystal composition described in in an electrooptical application.8. An electrooptical display device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the liquid crystal composition of encapsulated in a liquid crystal cell.'} The present invention relates to a novel cyclohexane compound and a liquid crystal composition containing the new cyclohexane, and intends to improve the response speed of a liquid crystal display.Many liquid crystal display devices that make use of the optical anisotropy (Δn) (hereinafter, referred to as “Δn” in some cases) or the dielectric constant anisotropy (Δε) (hereinafter, referred to as “Δε” in some cases), which are features of a liquid crystal compound, have been manufactured and have been used in watches, calculators, measurement instruments, instrument panels for vehicles, word processors, electronic diaries, portable telephones, printers, computers, TVs and so on. A liquid crystal compound used in liquid crystal display devices has a specific liquid crystal phase, and the phase mode thereof can be roughly divided into a nematic phase, a smectic phase and a cholesteric phase. Among these, a nematic phase is most widely ...

VINYLOGOUS CHALCONE DERIVATIVES AND THEIR MEDICAL USE

The present invention relates to vinylogous chalcone derivatives, in particular the compounds of formula (I) as described and defined herein, pharmaceutical compositions comprising these compounds, and their medical use, including their use in the treatment or prevention of cancer, in particular malignant hematological diseases/disorders. 2. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl) claim 1 , and Ris hydrogen.3. The compound of claim 1 , wherein Rand Rare mutually linked to form a group —CH═CH—.4. The compound of any of to claim 1 , wherein Ris hydrogen claim 1 , and Ris selected from hydrogen claim 1 , halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).5. The compound of any of to claim 1 , wherein Rand Rare mutually linked to form a group —CH— or —CH—CH—.6. The compound of any of to claim 1 , wherein Rand Rare each hydrogen.7. The compound of any of to claim 1 , wherein each Ris independently selected from halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).8. The compound of any of to claim 1 , wherein each Ris independently selected from halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).9. The compound of any of to claim 1 , wherein n is 1.10. The compound of any of to claim 1 , wherein m is 1 or 3.12. A pharmaceutical composition comprising the compound of any of to and a pharmaceutically acceptable excipient for use in the treatment or prevention of cancer.13. A method of treating or preventing cancer claim 1 , the method comprising the administration of the compound of any of to or the pharmaceutical composition of to a subject in need of such a treatment or prevention.14. The compound of any of to or the pharmaceutical composition of or the method of claim 1 , wherein the cancer is a malignant hematological ...

Total Synthesis Of Prostaglandin J Natural Products and Their Intermediates

The present disclosure is directed to methods of preparing prostaglandin J natural products by stereoretentive metatheses reactions and intermediates used in the synthesis of these natural products, including the use of intermediates of Formula (I-A), where Ris defined in the specification 5. The method of claim 4 , wherein the compound of Formula (I-A) or (I-B) has an enantiomeric purity corresponding to that of the compound of Formula (II-A) or (II-B) claim 4 , respectively.6. The method of claim 4 , wherein the organocopper allyl source is derived from the admixture of a copper halide and an allyl Grignard reagent claim 4 , optionally in the presence of an alkyl sulfide and alkali metal halide).7. The method of claim 4 , wherein oxidizing the aldol intermediate to the compound having a structure of Formula (I-A) or (I-B) comprises reacting the aldol intermediate with a sulfonylating agent and a base to form the compound of Formula (I-A) or (I-B).9. The method of claim 8 , wherein the conditions suitable for effecting a retro-Diels Alder reaction comprise treating the compounds of Formula (I-A) and (IB) with a Lewis acid catalyst (e.g. claim 8 , methyl or ethyl aluminum chloride) in the optional presence of an olefin.11. The method of claim 10 , wherein the Z-selective or stereoretentive olefin metathesis catalyst is a Grubbs metathesis catalyst. This application claims priority to U.S. Patent Application No. 62/876,531, filed Jul. 19, 2019, the contents of which are incorporated by reference herein for all purposesThis invention was made with government support under Grant No. GM031332 awarded by the National Institutes of Health. The government has certain rights in the invention.The present disclosure is directed to methods of preparing prostaglandin J natural products by stereoretentive metatheses reactions and intermediates used in the synthesis of these natural products.Δ-prostaglandin J natural products (1-4, ) features a unique cross-conjugated dienone ...

REDUCED COENZYME Q10 CRYSTAL HAVING EXCELLENT STABILITY

With respect to reduced coenzyme Q10, there has been no report about the presence of crystal polymorphism, and it has been considered that a conventionally obtained crystal form is only one form. The present invention relates to a reduced coenzyme Q10 crystal having an endothermic peak indicating melting at 54±2° C. during temperature rise at a rate of 5° C./min by differential scanning calorimetry (DSC), and/or to a reduced coenzyme Q10 crystal showing characteristic peaks at diffraction angles (2θ±0.2°) of 11.5°, 18.2°, 19.3°, 22.3°, 23.0° and 33.3° by powder X-ray (Cu—Kα) diffraction. The crystal form is a novel reduced coenzyme Q10 crystal which has a higher melting point and a lower solubility in a solvent, and is more excellent in stability than the conventionally known reduced coenzyme Q10 crystal. 1. A reduced coenzyme Q10 crystal having an endothermic peak at 54±2° C. during temperature rise at a rate of 5° C./min by differential scanning calorimetry.2. A reduced coenzyme Q10 crystal showing characteristic peaks at diffraction angles (2θ±0.2°) of 11.5° , 18.2° , 19.3° , 22.3° , 23.0° and 33.3° in powder X-ray (Cu—Kα) diffraction.3. The reduced coenzyme Q10 crystal according to claim 2 , wherein the reduced coenzyme Q10 crystal shows a powder X-ray (Cu—Kα) diffraction pattern shown in .4. The reduced coenzyme Q10 crystal according to claim 1 , wherein the reduced coenzyme Q10 crystal shows characteristic absorption peaks at 862±1 cmand 881±1 cmin infrared spectroscopic analysis by a KBr method.5. The reduced coenzyme Q10 crystal according to claim 4 , wherein the reduced coenzyme Q10 crystal shows an infrared spectroscopic spectrum by a KBr method claim 4 , shown in .6. A reduced coenzyme Q10 crystalline solid comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the reduced coenzyme Q10 crystal according to .'}7. A method for producing a reduced coenzyme Q10 crystal or a reduced coenzyme Q10 crystalline solid claim 4 , comprising:subjecting reduced ...

Cyclohexane-1,3-Diones for Use in the Treatment of Amyotrophic Lateral Sclerosis

The present invention relates to the identification of provided cyclohexane-1,3-diones (CHD compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided CHD compounds. 2. The compound according to wherein L is a bivalent saturated branched or unbranched Chydrocarbon chain.3. The compound according to claim 2 , wherein Ring A is a 5-6 membered aryl ring containing 0-4 heteroatoms independently selected from nitrogen claim 2 , oxygen claim 2 , or sulfur.5. The compound according to claim 2 , wherein 1 methylene unit of L is replaced by —NR— claim 2 , —O— claim 2 , —S— claim 2 , —C(O)— claim 2 , or —C(O)O—.6. The compound according to claim 5 , wherein L is selected from a bivalent saturated C-Chydrocarbon chain and a bivalent saturated C-Chydrocarbon chain wherein 1 methylene unit of L is replaced by —O— claim 5 , and wherein L is substituted with 1-2 R groups.8. The compound according to claim 7 , wherein each Ris independently fluorine claim 7 , chlorine claim 7 , methyl claim 7 , ethyl claim 7 , propyl claim 7 , butyl claim 7 , methoxy claim 7 , propoxy claim 7 , butoxy or trifluoromethyl.9. The compound according to claim 8 , wherein m is 1-2.11. The compound according to claim 10 , wherein Ris selected from H claim 10 , methyl and trifluoromethyl.15. The compound according to claim 14 , wherein each of R claim 14 , Rand Ris H.16. The compound according to claim 15 , wherein each R taken together forms a 3-membered ring.17. The compound according to claim 16 , wherein Ring A is substituted phenyl.20. The compound according to claim 19 , wherein Rand Rare H claim 19 , and Rand each R is independently selected from H claim 19 , CHand CF.21. The compound according to claim 20 , wherein Ring A is substituted phenyl.24. The compound according to claim 23 , wherein L is selected from a bivalent saturated C-Chydrocarbon ...

COMPOUNDS HAVING S1P5 RECEPTOR AGONISTIC ACTIVITY

A compound represented by the general formula (V) 3. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 6', '6', '6, 'L is (1) —O—(C2-7 alkyl), (2) —O—(C2-7 alkenyl), (3) —O—(C2-7 alkynyl), (4) —O—(C1-5 alkylene)-OCH, (5) —O—(C1-4 alkylene)-OCHCH, (6) —CHO—(C1-6 alkyl), (7) —CHO—(C2-6 alkenyl), (8) —CHO—(C2-6 alkynyl), (9) —CHCHO—(C1-5 alkyl), (10) —CHCHO—(C2-5 alkenyl), (11) —CHCHO—(C2-5 alkynyl), (12) —S—(C2-7 alkyl), (13) —S—(C2-7 alkenyl), (14) —S—(C2-7 alkynyl), (15) —NR—(C2-7 alkyl), (16) —NR—(C2-7 alkenyl), (17) —NR—(C2-7 alkynyl), (18) a C3-8 alkyl group, (19) a C3-8 alkenyl group, or (20) a C3-8 alkynyl group,'}{'sup': '6', 'Rrepresents a hydrogen atom or a C1-4 alkyl group, and'}wherein a carbon atom in each group is optionally substituted with 1 to 3 halogen atoms.4. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein L is a branched or linear chain group in which the number of atoms in the main chain is 4 to 7.5. The compound or a pharmaceutically acceptable salt thereof according to claim 2 , wherein{'sub': 3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 6', '6', '6, 'L is (1) —O—(C3-6 alkyl), (2) —O—(C3-6 alkenyl), (3) —O—(C3-6 alkynyl), (4) —O—(C1-4 alkylene)-OCH, (5) —O—(C1-3 alkylene)-OCHCH, (6) —CHO—(C2-5 alkyl), (7) —CHO—(C2-5 alkenyl), (8) —CHO—(C2-5 alkynyl), (9) —CHCHO—(C1-4 alkyl), (10) —CHCHO—(C2-4 alkenyl), (11) —CHCHO—(C2-4 alkynyl), (12) —S—(C3-6 alkyl), (13) —S—(C3-6 alkenyl), (14) —S—(C3-6 alkynyl), (15) —NR—(C3-6 alkyl), (16) —NR—(C3-6 alkenyl), (17) —NR—(C3-6 alkynyl), (18) a C4-7 alkyl group, (19) a C4-7 alkenyl group, or (20) a C4-7 alkynyl group,'}{'sup': '6', 'Rrepresents a hydrogen atom or a C1-4 alkyl group, and'}wherein a carbon atom in each group is optionally substituted with 1 to 3 halogen atoms.6. The compound or a pharmaceutically acceptable salt thereof ...

COMPOUNDS HAVING S1P5 RECEPTOR AGONISTIC ACTIVITY

A compound represented by the general formula (V) 3. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 6', '6', '6, 'L is (1) —O—(C2-7 alkyl), (2) —O—(C2-7 alkenyl), (3) —O—(C2-7 alkynyl), (4) —O—(C1-5 alkylene)-OCH, (5) —O—(C1-4 alkylene)-OCHCH, (6) —CHO—(C1-6 alkyl), (7) —CHO—(C2-6 alkenyl), (8) —CHO—(C2-6 alkynyl), (9) —CHCHO—(C1-5 alkyl), (10) —CHCHO—(C2-5 alkenyl), (11) —CHCHO—(C2-5 alkynyl), (12) —S—(C2-7 alkyl), (13) —S—(C2-7 alkenyl), (14) —S—(C2-7 alkynyl), (15) —NR—(C2-7 alkyl), (16) —NR—(C2-7 alkenyl), (17) —NR—(C2-7 alkynyl), (18) a C3-8 alkyl group, (19) a C3-8 alkenyl group, or (20) a C3-8 alkynyl group, and'}{'sup': '6', 'Rrepresents a hydrogen atom or a C1-4 alkyl group,'}provided that a carbon atom in each group may be substituted with 1 to 13 halogen atoms.4. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein L is a branched or linear chain group in which the number of atoms in the main chain is 4 to 7.5. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'sup': 6', '6', '6, 'L is (1) —O—(C3-6 alkyl), (2) —O—(C3-6 alkenyl), (3) —O—(C3-6 alkynyl), (4) —O—(C1-4 alkylene)-OCH, (5) —O—(C1-3 alkylene)-OCHCH, (6) —CHO—(C2-5 alkyl), (7) —CHO—(C2-5 alkenyl), (8) —CHO—(C2-5 alkynyl), (9) —CHCHO—(C1-4 alkyl), (10) —CHCHO—(C2-4 alkenyl), (11) —CHCHO—(C2-4 alkynyl), (12) —S—(C3-6 alkyl), (13) —S—(C3-6 alkenyl), (14) —S—(C3-6 alkynyl), (15) —NR—(C3-6 alkyl), (16) —NR—(C3-6 alkenyl), (17) —NR—(C3-6 alkynyl), (18) a C4-7 alkyl group, (19) a C4-7 alkenyl group, or (20) a C4-7 alkynyl group, and'}{'sup': '6', 'Rrepresents a hydrogen atom or a C1-4 alkyl group,'}provided that a carbon atom in each group may be substituted with 1 to 13 halogen atoms.6. The compound or a pharmaceutically acceptable salt thereof ...

Synthetic Route To Anhydroryanodol, Ryanodol And Structural Analogues

This disclosure is related to methods for producing anhydroryanodol, ryanodol, or analogues thereof and novel compounds prepared thereby. This application is a divisional of U.S. patent application Ser. No. 15/381,595, filed Dec. 16, 2016, which claims the priority of U.S. Provisional Patent Application No. 62/269,760, filed Dec. 18, 2015, both applications of which are incorporated by reference.This invention was made with government support under Grant No. DGE1144469 awarded by the National Science Foundation and Grant RGM097582-01 awarded by the national Institute of General Medical Sciences. The government has certain rights in invention.This disclosure is related to methods for producing anhydroryanodol, ryanodol, and analogues thereof.Terpenes are a large and structurally diverse family of natural products that range from simple hydrocarbons associated with flavors and fragrances, to complex, highly oxidized polycyclic molecules such as the anti-malarial drug artemisinin, and the anticancer compounds ingenol and taxol. Although terpenes are isolated from natural sources, it can be challenging to translate their biological activity into a practical application. In some cases, the hurdle is low natural abundance; other times, it is the difficulty encountered by chemists seeking to precisely edit a terpene's molecular structure in order to improve its drug-like properties or interrogate its role in modulating disease pathways. The development of concise chemical syntheses of terpenes can transform the ability to use these molecules and their synthetic derivatives as biological probes or as lead compounds for the development of new medicines. Furthermore, these scientific efforts often innovate chemical reactivity or synthetic design concepts.The natural product ryanodine (1) and its hydrolysis product ryanodol (2) are among the most highly oxidized and synthetically challenging diterpenoids reported to date.Isolated from the tropical shrub Ryania speciosa Vahl in ...

LIQUID CRYSTAL COMPOUND HAVING BIPHENYLENE, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY DEVICE

Provided are a liquid crystal compound satisfying at least one of physical properties such as high stability to heat or light, a high clearing point (or high maximum temperature), low minimum temperature of a liquid crystal phase, small viscosity, large optical anisotropy, large negative dielectric anisotropy, a suitable elastic constant and good compatibility with other liquid crystal compounds, a liquid crystal composition containing the compound and a liquid crystal display device including the composition. 2. The compound according to claim 1 , wherein claim 1 , in formula (1) claim 1 , A claim 1 , A claim 1 , Aand Aare independently 1 claim 1 ,4-cyclohexylene claim 1 , 1 claim 1 ,4-phenylene claim 1 , decahydronaphthalene-2 claim 1 ,6-diyl claim 1 , 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydronaphthalene-2 claim 1 ,6-diyl or naphthalene-2 claim 1 ,6-diyl claim 1 , and in the groups claim 1 , at least one piece of —CH— may be replaced by —O— claim 1 , and at least one piece of —CHCH— may be replaced by —CH═CH— claim 1 , and in the divalent groups claim 1 , at least one hydrogen may be replaced by fluorine or chlorine.3. The compound according to claim 1 , wherein claim 1 , in formula (1) claim 1 , Z claim 1 , Z claim 1 , Zand Zare independently a single bond claim 1 , —(CH)— claim 1 , —CH═CH— claim 1 , —C≡C— claim 1 , —COO— claim 1 , —OCO— claim 1 , —CFO— claim 1 , —OCF— claim 1 , —CHO— claim 1 , —OCH— or —CF═CF—.12. A liquid crystal display device claim 8 , including the liquid crystal composition according to . The invention relates to a liquid crystal compound, a liquid crystal composition and a liquid crystal display device. More specifically, the invention relates to a liquid crystal compound having a biphenylene ring and negative dielectric anisotropy, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition.In a liquid crystal display device, a classification based on an operating mode for liquid ...

Herbicidally Active (alkynyl-phenyl)-Substituted Cyclic Dione Compounds and Derivatives Thereof

The present invention relates to a compound of formula (I): wherein: X is methyl or chlorine; Ris fluorine or bromine; Ris ethynyl, C-Calkoxy, C-Chaloalkoxy, or C-Calkoxy-C-Calkoxy-; and Q is a pyran-3,5-dione-4-yl, a thiopyran-3,5-dione-4-yl, a piperidine-3,5-dione-4-yl, a cyclohexane-1,3,5-trione-2-yl, a cyclohexane-1,3-dione-2-yl, a cycloheptane-1,3-dione-2-yl, in which each cyclic dione is bridged by alkanediyl, or a derivative thereof (e.g. an enol ketone tautomer derivative thereof), wherein Q is further defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. Preferably, X is methyl; and/or Ris fluorine; and/or Ris —O—R, wherein Ris methyl, ethyl, trifluoromethyl, difluoromethyl, trifluoroethyl, or —CHCHOCH. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the weeds and/or to the plants and/or to the locus thereof. 2. A compound according to wherein X is methyl.3. A compound according to wherein Ris fluorine.4. A compound according to claim 1 , wherein Ris bromine.5. A compound according to wherein Ris —O—R claim 1 , and wherein Ris methyl claim 1 , ethyl claim 1 , trifluoromethyl claim 1 , difluoromethyl claim 1 , trifluoroethyl claim 1 , or —CHCHOCH.6. A compound according to wherein Ris —O—R claim 1 , and wherein Ris methyl claim 1 , ethyl claim 1 , trifluoromethyl or difluoromethyl.7. A compound according to wherein Ris —O—R claim 1 , and wherein Ris methyl.8. A compound according to claim 6 , wherein Ris fluorine and X is methyl.9. A compound according to claim 1 , wherein G is hydrogen; an agriculturally acceptable metal claim 1 , or an agriculturally acceptable sulfonium or ammonium group; or G is —C(X)—Ror —C(X)—X—R.10. A compound according ...

TROPOLONE COMPOUNDS FOR TREATING OR PREVENTING RETROVIRAL INFECTION

Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R, R, and Rare as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV). 2. The compound claim 1 , salt claim 1 , solvate claim 1 , stereoisomer claim 1 , or prodrug of claim 1 , wherein Ris selected from the group consisting of heterocyclyl C-Calkyl claim 1 , C-Calkylamino C-Calkyl claim 1 , C-Cdialkylamino C-Calkyl claim 1 , C-Caryl C-Calkylamino claim 1 , C-Caryl C-Calkylamino C-Calkyl claim 1 , C-Calkylthio C-Calkyl claim 1 , C-Carylthio claim 1 , C-Caryl C-Calkylthio C-Calkyl claim 1 , C-Calkylsulfonyl C-Calkyl claim 1 , C-Carylsulfonyl C-Calkyl claim 1 , C-Carylsulfinyl C-Calkyl claim 1 , hydroxy C-Calkyl group claim 1 , wherein each of alkyl claim 1 , aryl claim 1 , or heterocyclyl moiety may be unsubstituted or substituted with one or more substituents selected from the group consisting of halo claim 1 , hydroxy claim 1 , carboxy claim 1 , phosphoryl claim 1 , phosphonyl claim 1 , phosphono C-Calkyl claim 1 , carboxy C-Calkyl claim 1 , dicarboxy C-Calkyl claim 1 , dicarboxy halo C-Calkyl claim 1 , sulfonyl claim 1 , cyano claim 1 , nitro claim 1 , alkoxy claim 1 , alkylthio claim 1 , acyl claim 1 , acyloxy claim 1 , thioacyl claim 1 , acylthio claim 1 , aryloxy claim 1 , amino claim 1 , alkylamino claim 1 , dialkylamino claim 1 , trialkylamino claim 1 , guanidine claim 1 , aldehydro claim 1 , ureido claim 1 , and aminocarbonyl.3. The compound claim 1 , salt claim 1 , solvate claim 1 , stereoisomer claim 1 , or prodrug of claim 1 , wherein Ris C-Cdialkylamino C-Calkyl.4. The compound claim 1 , salt claim 1 , solvate claim 1 , stereoisomer claim 1 , or prodrug of claim 1 , wherein Ris heterocyclyl C-Calkyl.5. The compound claim 1 ...

Synthetic Route To Anhydroryanodol, Ryanodol And Structural Analogues

This disclosure is related to methods for producing anhydroryanodol, ryanodol, or analogues thereof and novel compounds prepared thereby. 2. The method of claim 1 , wherein each Ris —CH—O-benzyl.3. The method of claim 1 , wherein Ris CH.4. The method of claim 1 , wherein Rand Rare CH.5. The method of claim 1 , wherein the source of carbon monoxide is gaseous CO claim 1 , Co(CO) claim 1 , or Mo(CO)(DMF).6. The method of claim 1 , wherein the catalyst is a rhodium catalyst claim 1 , preferably [RhCl(CO)].7. The method of claim 1 , wherein the compound of formula (I) is produced in a diastereomeric ratio of at least about 3:1.11. The method of claim 10 , wherein the oxidant is selenium dioxide or molecular oxygen.12. The method of claim 10 , wherein the organic solvent is anhydrous.15. The method of claim 14 , wherein the triflating agent is N-(5-chloro-2-pyridyl) bis(trifluoromethanesulfonimide).18. The method of claim 17 , wherein RC(═CH)Sn(Calkyl)is CHC(═CH)SnBu.19. The method of claim 17 , wherein the catalyst is a palladium catalyst.20. The method of claim 17 , wherein the catalyst is PdCl(PPh).23. The method of claim 22 , wherein the reducing agent is a hydride claim 22 , hydrogen claim 22 , or a mixture thereof.24. The method of claim 22 , wherein the reducing agent is lithium borohydride.25. The method of claim 22 , wherein the reducing agent is hydrogen.26. The method of claim 22 , wherein the catalyst is a palladium catalyst.27. The method of claim 26 , wherein the catalyst is Pd(OH)/C.31. The method of claim 29 , wherein the compound of formula (VII) is (+)-ryanodol. This application claims the priority of U.S. Provisional Patent Application No. 62/269,760, filed Dec. 18, 2015, which application is incorporated by reference herein.This invention was made with government support under Grant No. DGE1144469 awarded by the National Science Foundation and Grant RGM097582-01 awarded by the national Institute of General Medical Sciences. The government has certain ...

CARBON-MONOXIDE-RELEASING MOLECULES AND THERAPEUTIC APPLICATIONS THEREOF

Carbon monoxide-releasing organic molecules are described herein. The molecules can be synthesized prior to administration (e.g., ex vivo) or formed in vivo. In those embodiments where the molecules are formed in vivo, reactants are administered under physiological conditions and undergo a cycloaddition reaction to form a product which releases carbon monoxide. In applying such reactions for therapeutic applications in vivo, the cycloaddition and CO release typically occur only under near-physiological or physiological conditions. For example, in some embodiments, the cycloaddition reaction and/or release of carbon monoxide occur at a temperature of about 37° C. and pH of about 7.4. Pharmaceutical compositions and methods for release carbon monoxide are also described. 2. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable excipient.3. A method for generating carbon monoxide in vivo or ex vivo claim 1 , the method comprising allowing a compound according to to react to form an organic molecule that releases carbon monoxide under physiological conditions.4. The method of wherein the compound is bound to a support selected from the group consisting of a solid bead claim 3 , a soluble polymer claim 3 , an insoluble polymer claim 3 , a protein claim 3 , a nucleic acid claim 3 , and a carbohydrate.5. The method of claim 3 , wherein a cycloaddition reaction occurs and carbon monoxide is released under physiological conditions.6. The method of claim 5 , wherein the amount of CO released is from about 10 to about 250 ppm.7. A method for treating an inflammatory condition comprising: administering a compound according to to a subject in need thereof claim 1 , and allowing the compound to react to form an effective amount of carbon monoxide claim 1 , thereby treating the inflammatory condition.8. The method of claim 7 , wherein the inflammatory condition is selected from the group consisting of inflammatory bowel disease claim 7 , ...

Compound, extract isolated from antrodia camphorate, and method of inhibiting cancer cell growth

Disclosed is a compound isolated from Antrodia camphorata , represented by formula I: wherein R1 is a hydrogen atom or an acetyl group; and a method of inhibiting cancer cell growth by using the compound, the cancer is selected from the group consisting of lung cancer, colon cancer, prostate cancer, liver cancer and breast cancer.

TARGETED CONTRAST AGENTS FOR MRI OF ALPHA-SYNUCLEIN DEPOSITION

A liposomal composition (“ADx-003”) is provided, ADx-003 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by Formula I: 10. The liposomal composition of claim 9 , wherein the first phospholipid comprises hydrogenated soy L-α-phosphatidylcholine (“HSPC”).11. The liposomal composition of claim 9 , wherein the sterically bulky excipient that is capable of stabilizing the liposomal composition comprises cholesterol (“Chol”).12. The liposomal composition of claim 9 , wherein the second phospholipid that is derivatized with a first polymer comprises 1 claim 9 ,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy (polyethylene glycol)-2000) (“DSPE-mPEG2000”).15. The liposomal composition of claim 14 , wherein the variable x is 16 (the conjugate: “Gd(III)-DOTA-DSPE”). This application claims priority from U.S. Provisional Patent Application No. 62/975,265, filed on Feb. 12, 2020, which is incorporated by reference herein in its entirety.Neurodegenerative disorders such as Parkinson's disease (“PD”) and Alzheimer's disease (“AD”) are characterized by pathological deposits of misfolded protein aggregates at different locations in the brain. These misfolded protein aggregates include alpha-synuclein (“α-syn”) aggregates in the form of Lewy bodies (“LB”) and Lewy neurites (“LN”) in PD and amyloid-beta (“Aβ”) plaques and hyperphosphorylated tau tangles in AD. PD is the second most common neurodegenerative disease after AD and is characterized clinically by motor symptoms, including bradykinesia, rigidity, tremor, and postural instability. The motor symptoms are caused by degeneration of dopaminergic neurons in the substantia nigra, ...

INHIBITION OF RESPIRATORY COMPLEX III BY LIGANDS THAT INTERACT WITH A REGULATORY SWITCH

The present invention provides methods for inhibiting respiratory complex III in a cell. The present invention also provides methods for treating cancer in a subject. 14. The method of claim 1 , wherein the cell is a cancer cell.15. The method of claim 14 , wherein the cancer cell is in a subject.16. The method of claim 15 , further comprising administering to the subject an amount of the compound effective to inhibit respiratory complex III in the cancer cell. The present application is a division of U.S. application Ser. No. 16/531,511, filed Aug. 5, 2019, which is a continuation of International Patent Application No. PCT/US2018/017638, filed Feb. 9, 2018, which claims priority to U.S. Provisional Appln. No. 62/457,684, filed Feb. 10, 2017, the disclosures of which are herein incorporated by reference in their entirety for all purposes.This invention was made with Government support under Grant No. GM054052 awarded by the National Institutes of Health (NIH). The Government has certain rights in the invention.Ideally, a smart anti-cancer drug should discriminate between cancer and normal cells. One of the recently discovered biochemical variations in cancer cells that distinguish them from normal cells is a higher basal level of reactive oxygen species (ROS), which makes the cancer cells more susceptible to ROS-induced apoptosis (Szatrowski and Nathan (1991) 51:794; Kawanishi et al. (2006) 387:365; Toyokuni et al. (1995) 358:1; and Trachootham et al. (2009) 8:579). However, since cancer cells can adapt to such oxidative stress by up-regulating antioxidant production (Tiligada (2006) 13:S115), to make use of such a mechanism, a drug should induce rapid production and accumulation of ROS and trigger apoptosis in cancer cells before anti-oxidant up-regulation takes effect.The mitochondrial electron transport chain (METC) is one of the major sources of ROS in the cell (Adam-Vizi and Chinopoulos (2006) 27:639; and Lenaz (2001) 52:159), and respiratory complex III (also ...

PROCESS FOR THE STEREOSELECTIVE PREPARATION OF A PYRAZOLE CARBOXAMIDE

The present invention relates to a process for the enantioselective preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ((1S,4R)-9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide of formula Ib. 2. A process according to claim 1 , wherein the enantioselective reduction of the compound of formula II is done via hydrogenation in the presence of a transition metal catalyst.3. A process according to claim 1 , wherein the enantioselective reduction of the compound of formula II is done via transfer hydrogenation in the presence of a transition metal catalyst.4. A process according to claim 1 , wherein the enantioselective reagent is a ruthenium catalyst.5. A process according to claim 2 , wherein the enantioselective reagent is a ruthenium catalyst.6. A process according to claim 3 , wherein the enantioselective reagent is a ruthenium catalyst.7. A process according to claim 1 , wherein the enantioselective reagent is chloro{(R)-(+)-2 claim 1 ,2′-bis[di(3 claim 1 ,5-xylyl)phosphino]-1 claim 1 ,1′-binaphthyl}[(2R)-(−)-1-(4-methoxyphenyl)-1′-(4-methoxyphenyl-kC)-3-methyl-1 claim 1 ,2-butanediamine]ruthenium(II).8. A process according to claim 1 , wherein the enantioselective reagent is dichloro[(4S claim 1 ,5S)-(+)-4 claim 1 ,5-bis(diphenylphosphinomethyl)-2 claim 1 ,2-dimethyl-1 claim 1 ,3-dioxolane][(S)-(+2-(α-methylmethanamine)-1H-benzimidazole]ruthenium(II). The present invention relates to a process for the stereoselective (enantioselective) preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ((1S,4R)-9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide.The compound 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide is described for example in WO 2007/048556. Said compound shows an excellent fungicidal activity and is for example effective for the reduction of mycotoxin contamination in plants. Mycotoxins ( ...

Cyclohexane-1,3-Diones for Use in the Treatment of Amyotrophic Lateral Sclerosis

The present invention relates to the identification of provided cyclohexane-1,3-diones (CHD compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided CHD compounds. 2. The compound according to wherein L is a bivalent saturated branched or unbranched Chydrocarbon chain.3. The compound according to claim 2 , wherein Ring A is a 5-6 membered aryl ring containing 0-4 heteroatoms independently selected from nitrogen claim 2 , oxygen claim 2 , or sulfur.5. The compound according to claim 2 , wherein 1 methylene unit of L is replaced by —NR— claim 2 , —O— claim 2 , —S— claim 2 , —C(O)— claim 2 , or —C(O)O—.6. The compound according to claim 5 , wherein L is selected from a bivalent saturated C-Chydrocarbon chain and a bivalent saturated C-Chydrocarbon chain wherein 1 methylene unit of L is replaced by —O— claim 5 , and wherein L is substituted with 1-2 R groups.8. The compound according to claim 7 , wherein each Ris independently fluorine claim 7 , chlorine claim 7 , methyl claim 7 , ethyl claim 7 , propyl claim 7 , butyl claim 7 , methoxy claim 7 , propoxy claim 7 , butoxy or trifluoromethyl.9. The compound according to claim 8 , wherein m is 1-2.11. The compound according to claim 10 , wherein Ris selected from H claim 10 , methyl and trifluoromethyl.15. The compound according to claim 14 , wherein each of R claim 14 , Rand Ris H.16. The compound according to claim 15 , wherein each R taken together forms a 3-membered ring.17. The compound according to claim 16 , wherein Ring A is substituted phenyl.20. The compound according to claim 19 , wherein Rand Rare H claim 19 , and Rand each R is independently selected from H claim 19 , CHand CF.21. The compound according to claim 20 , wherein Ring A is substituted phenyl.24. The compound according to claim 23 , wherein L is selected from a bivalent saturated C-Chydrocarbon ...

REDUCED COENZYME Q10 CRYSTAL HAVING EXCELLENT STABILITY

With respect to reduced coenzyme Q10, there has been no report about the presence of crystal polymorphism, and it has been considered that a conventionally obtained crystal form is only one form. The present invention relates to a reduced coenzyme Q10 crystal having an endothermic peak indicating melting at 54±2° C. during temperature rise at a rate of 5° C./min by differential scanning calorimetry (DSC), and/or to a reduced coenzyme Q10 crystal showing characteristic peaks at diffraction angles (2θ±0.2°) of 11.5°, 18.2°, 19.3°, 22.3°, 23.0° and 33.3° by powder X-ray (Cu—Kα) diffraction. The crystal form is a novel reduced coenzyme Q10 crystal which has a higher melting point and a lower solubility in a solvent, and is more excellent in stability than the conventionally known reduced coenzyme Q10 crystal. 1. (canceled)2. A composition , comprising:a reduced coenzyme Q10 crystal showing characteristic peaks at diffraction angles in 20±0.2° of 11.5°, 18.2°, 19.3°, 22.3°, 23.0° and 33.3° in powder Cu—Kα X-ray diffraction,wherein the composition is at least one of food, nutritional functional food, specified health food, nutritious supplement, nutrient, animal drug, feed, cosmetic, medicament, treatment drug, prevention drug, and pet food.3. The composition of claim 2 , further comprising:at least one of an excipient, a disintegrator, a lubricant, a binder, an antioxidant, a colorant, an anticoagulation agent, an absorption promoter, and an active ingredient which is not reduced coenzyme Q10.4. The composition of claim 3 , wherein the active ingredient is at least one of amino acid claim 3 , vitamin claim 3 , mineral claim 3 , polyphenol claim 3 , organic acid claim 3 , saccharide claim 3 , peptide claim 3 , and protein.5. The composition of claim 2 , which is in a form of a hard capsule.6. The composition of claim 3 , which is in a form of a hard capsule.7. The composition of claim 4 , which is in a form of a hard capsule.8. The composition of claim 2 , which is in a ...

DECALIN DERIVATIVES, A PROCESS FOR THE PREPARATION AND PHARMACEUTICAL COMPOSITION THEREOF

Decalin derivative compounds of formula (I) are provided, including processes for preparation thereof, and pharmaceutical compositions including the decalin derivative compounds. Methods are provided for treating blood related disorders, such as sickle cell anemia, in a subject in need thereof using a compound of formula (I). 18-. (canceled)15. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'a decalin derivative compound according to , or a stereoisomer thereof, or an ester thereof, or a pharmaceutically acceptable salt thereof; and'}a pharmaceutically acceptable carrier, diluent, or excipient.16. A method for treating a blood related disorder , the method comprising:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'administering a therapeutically effective amount of a decalin derivative compound according to , or a pharmaceutically acceptable salt thereof, to a subject in need thereof.'}17. The method of claim 16 , wherein the blood related disorder is sickle cell anemia. This application is a national-stage application under 35 U.S.C. § 371 of International Application No. PCT/IN2019/050779, filed Oct. 22, 2019, which international application claims benefit of priority to Indian Patent Application No. 201811039715, filed Oct. 22, 2018.The present disclosure relates to decalin derivatives. More particularly, the present disclosure relates to decalin derivative compounds of formula (I), a process for preparation and a pharmaceutical composition thereof. The present disclosure further relates to a method for treating blood related disorders, preferably sickle cell anemia in a subject in need thereof using compound of formula (I).Sickle cell anemia (SCA) is a genetic disorder in which the red blood cells assume a sickle shape instead of a normal disc shape. It occurs due to a mutation in which the amino acid glutamic acid is replaced by valine in the β-globin chain of hemoglobin. The sickle cell patient may suffer from pain ...

Recyclable and Reconfigurable High-Performance Polymer Networks and Uses Thereof

The present invention relates to a composition of polymers comprising dynamic covalent diketoenamine bonds. This composition allows the formulation of polymeric materials with a wide range of architectures and properties, and further allows these materials to be recycled using thermal, chemical, or mechanical processes

New Pleuromutilin Antibiotic Compounds, Compositions and Methods of Use and Synthesis

The present invention is directed to novel pleuroniutilin antibiotic compounds, intermediates which are useful for making these novel amibioiic compounds and related methods and pharmaceutical compositions for treating pathogens, especially bacterial infections, including gram negative bacteria and synthesizing these compounds.

Method of quadratic acid synthesis

FIELD: organic chemistry. SUBSTANCE: product: quadratic acid. Reagent 1: 3-acetoxy-2-cyclobutene-1-one or 1,3-cyclobutanedione. Reagent 2: base. Reaction conditions: halogenation at (-40)-(+40) C, hydrolysis at 50-150 C. Compound is used as drugs. EFFECT: improved method of synthesis. 7 cl 62 оОс пы Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ” 2017 719 ' 5) МК С 07С 49/573, 45/43 13) СЛ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4894613/04, 25.02.1991 (30) Приоритет: 26.02.1990 СН 598/90 (46) Дата публикации: 15.08.1994 (56) Ссылки: Патент Ц$ М 4104308, кл. С 07С 45/00, 1978. (71) Заявитель: Лонца АГ (СН) (72) Изобретатель: Берри Джэксон[СВ], Томас Шолл[СН] (73) Патентообладатель: Лонца АГ (СН) (54) СПОСОБ ПОЛУЧЕНИЯ КВАДРАТНОЙ КИСЛОТЫ (57) Реферат: Использование: в качестве лекарственных средств и гербицидов. Сущность изобретения: продукт - квадратная кислота. Реагент 1: З-ацетокси-2-циклобутен-1-он или 1,3-циклобутандион. Реагент 2: основание. Условия реакции: галогенирование при (-40) - (+40)°С, гидролиз при 50 - 150°С. 6 з.п. ф-лы. 2017719 С1 КО 62 оОс пы Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ (19) ВИ "” 2017 719. 5 21° @ 07 С 49/573, 45/43 13) СЛ (21), (22) АррИсаНоп: 4894613/04, 25.02.1991 (30) Рпогйу: 26.02.1990 СН 598/90 (46) Рае о! рибИсаНоп: 15.08.1994 (71) АррИсапе: ЕОМТЗА АС (СН) (72) шпуетог: ВЕКН! ОИНЕНКЗОМ[СВ], ТОМАЗ$ ЗЭНОЕУСН] (73) Ргорпеюг: [ОМТЗА АС (СН) (54) МЕТНОО ОЕ ОЧАОКАТ!С АСЮО ЗУМТНЕЗ$З!$ (57) АБзГасЕ: НЕГО: огдапс спептгу. ЗОВЗТАМСЕ: ргочисе: Ччцаагайнс — ас49. Кеадет 1: З-асщоху-2-сусорщепе-1-опе ог 1,3-суЧорщапе4юте. Кеадепт 2: Базе. КеасНоп сопаШоОп$: паодепаНоп а (-40)-(+40) С, пуагоуз$ аЁ 50-150 С. Сотроипа 1$ изед аз агид$. ЕЕЕЕСТ: итргоуея теоа ог зутез5. 7 < 2017719 С1 КО 6 оОс ПЧ ГЭ Изобретение относится к циклическим кетонам, В частности, К усовершенствованному способу получения квадратной кислоты. Квадратная кислота представляет собой интересный ...

Herbicidal activity (alkynyl-phenyl) substituted cyclic dione compounds and derivatives thereof

Sphyngosine kinase inhibitors

FIELD: medicine, pharmaceutics. SUBSTANCE: present invention refers to new compounds of formula I or their pharmaceutically acceptable salts showing an ability to inhibit sphingosine kinase, to a based pharmaceutical composition, to a method of inhibiting sphingosine kinase and a method of treating diseases specified in breast cancer, diabetic retinopathy, arthritis and colitis. , wherein X represents -C(R 3 ,R 4 )N(R 5 )-, -C(O)N(R 4 )-; R 1 represents phenyl unsubstituted or substituted by 1 or 2 halogens. The values of R 2 , R 3 , R 4 , R 5 substitutes are such as specified in the patent claim. EFFECT: preparation of new compounds. 17 cl, 24 dwg, 9 tbl, 26 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 447 060 (13) C2 (51) МПК C07C C07C C07C C07C C07D C07D C07D ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИC07D C07D C07D 233/57 255/44 317/32 323/23 317/58 207/02 295/13 295/32 213/24 265/30 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07D C07D C07D C07D C07D C07D C07D A61K A61K A61K 233/54 (2006.01) 277/46 (2006.01) 263/58 (2006.01) 277/82 (2006.01) 257/04 (2006.01) 209/88 (2006.01) 473/34 (2006.01) 31/33 (2006.01) 31/16 (2006.01) 31/13 (2006.01) (см. прод.) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ Приоритет(ы): (30) Конвенционный приоритет: 17.06.2005 US 60/691,563 (73) Патентообладатель(и): ЭПОУДЖИ БИОТЕКНОЛОДЖИ КОРПОРЕЙШН (US) 2 4 4 7 0 6 0 (43) Дата публикации заявки: 27.07.2009 Бюл. № 21 2 4 4 7 0 6 0 R U (56) Список документов, цитированных в отчете о поиске: US 4053509 А, 11.10.1977. US 5595995 А, 21.01.1997. US 4332806 А, 01.06.1982. US 3663565 A, 16.05.1972. US 4349552 A, 14.09.1982. US 6649600 B1, 18.11.2003. US 3657273 A, 18.04.1972. WO 99/26927 A2, 03.06.1999. WO 2004/089470 A2, 21.10.2004. SU 1574586 A1, 30.06.1990. SU 1367194 A1, 10.04.1996. RU 2197467 C2, 27.01.2003. SU 451691 A, 09.07.1975. (см. прод.) C 2 C 2 (45) Опубликовано: 10.04.2012 Бюл. № 10 (85) Дата начала рассмотрения заявки PCT на ...

Compound having S1P5 receptor agonist activity

Provided is a compound in which the balance of the agonist activity against the S1P

Compounds having S1P5 receptor agonistic activity

为了开发对于S1P 5 介导的疾病、例如精神分裂症、宾斯旺格病等神经变性疾病的治疗有用的药物，本发明提供改善了相对于S1P 1 受体的S1P 5 受体激动活性的平衡的化合物。由于通式(V)(式中，全部符号如说明书中所记载)所示的化合物改善了相对于S1P 1 受体的S1P 5 受体激动活性的平衡，因此可以作为S1P 5 介导的疾病、例如精神分裂症、宾斯旺格病等神经变性疾病的治疗剂。

3-oxy-2-cyclobutnene-1-on basic salts and method for their production

FIELD: organic chemistry. SUBSTANCE: desired salts have formula where R is either ammonium group having common formula (where R 1 ,R 2 and R 3 are the same or different and represent hydrogen atom, lower alkyl or cycloalkyl) or atom of alkali metal. Desired salts are prepared by interaction of base with pure 3-acetoxy-2-cyclobutene-1-on, 1,3-cyclobutanedion or vat residue being prepared during production of diketen and comprising 3-acetoxy-2-cyclobutene-1-on. Amine having common formula where R 1 ,R 2 and R 3 are as mentioned above or alcoholate or hydroxide of alkali metal is used as said base. EFFECT: improved quality of desired product. 17 cl 49138 10с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ” 2 078 757. 13) Сл С 07С 49/593, 211/62 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5010885/04, 31.01.1992 (30) Приоритет: 26.02.1990 СН 598/90 (46) Дата публикации: 10.05.1997 (56) Ссылки: Патент ФРГ М 331443, кл. С 07 С ДЭГГОТ, 1984. (61) Номер основного патента: 04894613/04(25.02.91) (71) Заявитель: Лонца АГ (СН) (72) Изобретатель: Берри Джексон[СВ], Томас Шолл[СН] (73) Патентообладатель: Лонца АГ (СН) (54) 3-ОКСИ-2-ЦИКЛОБУТЕН-1-ОН-ОСНОВНЫЕ СОЛИ И СПОСОБ ИХ ПОЛУЧЕНИЯ (57) Реферат: Описаны З-окси-2-циклобутен-1-оновые соли общей формулы о „ } Е энннни Е «Т> = о где К означает либо аммониевую группу общей формулы Е } [1 + нм - к. «тт» Е 3 где К, К2 и Кз, имея одинаковое или разное значение, означают атом водорода, низший алкил или циклоалкил, либо атом щелочного металла. Соли формулы | получают взаимодействием с основанием чистого З-ацетокси-2-циклобутен-1-она, 1,3,-циклобутандиона или кубового остатка, получаемого в производстве дикетена и содержащего 3-ацетокси-2-циклобутен-1-он. В качестве основания используется амин общей формулы Е р |ч- сттт> 2 Е з где Ка, К и К. имеют вышеуказанное значение, или алкоголят или гидроокись щелочного металла. Соли формулы | пригодны для получения квадратной кислоты, причем на ...

New derivatives of 19-nor-testosterones and processes for their preparation

The invention comprises 13b -alkyl homologues of pharmacologically active 18, 19-di-nor-testosterones of the natural series, the alkyl group including straight and branched chains containing from 2 to 18 carbon atoms, together with a process for their preparation by alkylating 6-methoxy-3, 4-dihydronaphthyl-[2, 1-d]-isoxazole in the presence of an alkali metal alcoholate (either directly using an alkyl iodide or indirectly by reaction with an alkenyl bromide followed by hydrogenation of the alkenyl grouping), condensing the resulting 2-cyano-2-alkylated-6-methoxy-tetralone-1 derivative with dimethyl succinate in the presence of an alkaline condensation agent, preferably potassium t-butylate, to form the corresponding 5-methoxy-13b -alkyl-15-methoxycarbonyl-des-A-gona-5, 7, 9, 14-tetraen-17-one, reacting the latter with an alkali metal hydride to effect simultaneous reduction and saponification to form the corresponding 13b -alkyl-15-carboxy-17b - hydroxy -5- methoxy-des-A-gona-5, 7, 9, 14-tetraene and, after resolution of the optically active isomers thereof, decarboxylating the l-isomer by treatment with a mineral acid to yield a 13b -alkyl-17b -hydroxy-5-methoxy-des: A-gona-5, 7, 9, 14-tetraene, catalytically hydrogenating the latter to form the corresponding 13b -alkyl-17b -hydroxy-5-methoxy-des-A-gona-5, 7, 9-triene, reducing this compound by the action of an alkali metal in liquid ammonia to the corresponding 13b -alkyl-17b -hydroxy-des-A-gon-9-en-5-one, esterifying it with an acylating agent derived from an organic carboxylic acid to form a 17b -acyloxy-13b -alkyl-des: A-gon-9-en-5-one, treating the latter with a 1, 3-dihalogeno-2-butene in an inert organic medium to form the corresponding 17b -acyloxy-13b -alkyl-3-halogeno-4, 5-seco-gona-2, 9-dien-5-one, hydrolysing this compound, preferably with sulphuric acid, to form the corresponding 17b -acyloxy-13b -alkyl-4, 5-seco-gon-9-ene-3, 5-dione, catalytically hydrogenating it to yield the corresponding 17b - ...

Novel 19-nor-testosterone analogue, esters thereof and method of preparation

Patent FR2422616B1

Sphingosine kinase inhibitors

Compuesto de fórmula**Fórmula** o una sal farmaceuticamente aceptable, hidrato o solvato del mismo, en la que: Y es -N(R4)-; R1 es fenilo, sustituido con 1 ó 2 halogenos, R2 es arilo, -alquilarilo, heterocicloalquilo, -alquil-heterocicloalquilo, heteroarilo o -alquil-heteroarilo opcionalmente sustituido; R3 es H, alquilo u oxo; en la que la parte de alquilo y anillo de cada uno de los grupos R2 y R3 anteriores esta opcionalmente sustituida con hasta 5 grupos que son independientemente alquilo (C1-C6), halógeno, haloalquilo, -0C(0)(alquilo C1-C6), -C(0)0(alquilo C1-C6), -CONR'R", -0C(0)NR' R", -NR'C(0)R", -CF3, -0CF3, -OH, alcoxilo hidroxialquilo, -CN, -CO2H, -SH, -S-alquilo, -SOR'R", -SO2R', -NO2 o NR'R", en la que R' y R" son independientemente H o alquilo (C1-C6), y en la que cada parte de alquilo de un sustituyente esta opcionalmente sustituida adicionalmente con 1, 2 1:5 3 grupos seleccionados independientemente de halógeno, CN, OH y NH2; y R4 es H o alquilo (C1-C6). Compound of formula ** Formula ** or a pharmaceutically acceptable salt, hydrate or solvate thereof, in which: Y is -N (R4) -; R1 is phenyl, substituted with 1 or 2 halogens, R2 is aryl, -alkylaryl, heterocycloalkyl, -alkyl-heterocycloalkyl, heteroaryl or -alkyl-heteroaryl optionally substituted; R3 is H, alkyl or oxo; wherein the alkyl and ring portion of each of the above R2 and R3 groups is optionally substituted with up to 5 groups that are independently (C1-C6) alkyl, halogen, haloalkyl, -0C (0) (C1-C6 alkyl ), -C (0) 0 (C1-C6 alkyl), -CONR'R ", -0C (0) NR 'R", -NR'C (0) R ", -CF3, -0CF3, -OH, hydroxyalkyl alkoxy, -CN, -CO2H, -SH, -S-alkyl, -SOR'R ", -SO2R ', -NO2 or NR'R", in which R' and R "are independently H or (C1 alkyl) -C6), and in which each alkyl part of a substituent is optionally further substituted with 1, 2 1: 5 3 groups independently selected from halogen, CN, OH and NH2; and R4 ...

NEW CARBAMATES, THEIR PRODUCTION AND THE PHARMACEUTICAL PREPARATIONS CONTAINING THEM

Patent RU2020127745A3

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2020 127 745 A (51) МПК C07D 205/04 (2006.01) A61K 31/396 (2006.01) A61P 25/00 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2020127745, 21.02.2019 (71) Заявитель(и): ОНО ФАРМАСЬЮТИКАЛ КО., ЛТД. (JP) Приоритет(ы): (30) Конвенционный приоритет: 22.02.2018 JP 2018-029549 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 22.09.2020 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2019/163917 (29.08.2019) A Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" R U (57) Формула изобретения 1. Соединение, представленное общей формулой (V), или его фармацевтически приемлемая соль: (V) [где L представляет собой группу разветвленных или линейных цепей, состоящих из атомов, выбранных из атома углерода, атома кислорода, атома азота и атома серы, где число атомов в основной цепи составляет от 3 до 8, и цепная группа может содержать от 1 до 3 гетероатомов, выбранных из атома кислорода, атома азота и атома серы, при условии, что атом углерода в L может быть замещен от 1 до 13 атомами галогена, Y представляет собой Стр.: 1 A 2 0 2 0 1 2 7 7 4 5 (54) СОЕДИНЕНИЯ, ОБЛАДАЮЩИЕ АГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ ПО ОТНОШЕНИЮ К РЕЦЕПТОРУ S1P5 2 0 2 0 1 2 7 7 4 5 JP 2019/006637 (21.02.2019) R U (43) Дата публикации заявки: 22.03.2022 Бюл. № 9 (72) Автор(ы): ВАТАНАБЕ, Тосихиде (JP), КУСУМИ, Кенсуке (JP), ИМАИДЕ, Сатоми (JP), ЕНДО, Тосимицу (JP), КОМИЯ, Такаки (JP), ЦУБУРАЯ, Наоми (JP) или где каждая группа соединена с Z через связь, представленную стрелкой, A представляет собой C3-7 циклоалкиленовую группу, которая может быть замещена, или C1-4 алкиленовую группу, которая может быть замещена, R1 представляет собой C1-4 алкильную группу, C3-6 циклоалкильную группу, которая может быть замещена галогеном, C1-4 алкокси группу, которая может быть замещена галогеном, C1-4 галогеналкильную ...

Cyclic dione compounds (alkyl phenyl) - active substitutes such as herbicides and derivatives thereof

Un compuesto de fórmula (I)**Fórmula** en donde: X es metilo o cloro; R1 es flúor o bromo; R2 es etinilo, alcoxiC1-C3-, haloalcoxiC1-C3- o alcoxiC1-C3-alcoxiC1-C3-; y Q es un grupo de fórmula Q1 o Q2:**Fórmula** en la que: R3, R4 y R5, independientemente entre sí, son hidrógeno, alquilo C1-C5, alquenilo C2-C4, alquinilo C2-C4, fluoroalquilo C1-C2 o alcoxi C1-C3-alquilo C1-C3; R6 es hidrógeno, alquilo C1-C5, alquenilo C2-C4, alquinilo C2-C4, R6AA-C≡C-CH2-, fluoroalquilo C1-C2, alcoxi C1-C3- alquilo C1-C3, alquiltio C1-C3-alquilo C1-C3, alquil C1-C3-sulfinilalquilo C1-C3, alquil C1-C3-sulfonilalquilo C1-C3, cicloalquilo C3-C4, o un heterociclilo monocíclico de 4, 5 o 6 miembros sin sustituir que tiene un heteroátomo de anillo independientemente seleccionado de oxígeno, azufre y nitrógeno, y unido en un átomo de carbono del anillo dentro del heterociclilo, o R6 es T-(CH2)m-CH(R7)-, en la que m es 0 o 1 y o bien R7 es hidrógeno o bien R7 y R5 juntos son un enlace, y T es un heterociclilo opcionalmente sustituido como se define más adelante; o R6 es Het-CH(R8)-, en la que o bien R8 es hidrógeno o bien R8 y R5 juntos son un enlace, y Het es un heteroarilo opcionalmente sustituido como se define más adelante; o R6 es cicloalquil C3-C6-alquil C1-C2-; o es cicloalquil C4-C6-alquil C1-C2-, sustituido en un átomo de carbono del anillo de cicloalquilo que no es el átomo de carbono del anillo unido al resto de -alquil C1-C2- y que no está unido directamente al átomo de carbono del anillo unido al resto -alquil C1-C2-, con uno o dos sustituyentes de anillo que independientemente son: >=NO-R10, oxo (>=O), alcoxi C1-C4, haloalcoxi C1-C2, 2-(alcoxi C1-C3)-etoxi, cicloalquiloxi C3- C5, (cicloalquil C3-C5)metoxi, alquenil C2-C3-CH2-oxi, alquilo C1-C3 o fluoroalquilo C1-C2; o benciloxi en el que el anillo de fenilo está opcionalmente sustituido con uno o dos sustituyentes que son independientemente alquilo C1-C3, fluoroalquilo C1-C2, alquil C1-C3-C(O)-, fluoroalquil C1-C2-C(O)-, ...

Compound used as autophagy regulator, and preparation method therefor and uses thereof

It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.

9,10-ethano anthracene derivatives

1,214,357. 9,10-Ethanoanthracene derivatives. MERCK & CO. Inc. 18 March, 1968 [21 March, 19671, No. 62407/69. Divided out of 1,214,356. Heading C2C. The invention comprises compounds of the Formula I, wherein R represents an alkanoyl group or a ketalized derivative thereof, each of R<SP>3</SP> and R<SP>4</SP> represents a hydrogen or halogen atom or an alkyl, alkoxy, or trifluoromethyl group and X represents an amino, alkoxycarbonylamino, cyano, carboxy or alkoxycarbonyl group, except that X is not amino when R is ketalized alkanoyl and their preparation by reacting a 9-alkanoylanthracene of the Formula II where R‹ represents an alkanoyl group with acrylic acid, an alkyl acrylate or acrylonitrile to form a 9-alkanoyl-9,10-ethano- 11-(carboxy, alkoxycarbonyl, or cyano)dihydroanthracene of the Formula III wherein X<SP>1</SP> represents a carboxy, alkoxycarbonyl or cyano group and optionally ketalizing the product or by reacting a compound of the Formula IV with hydrozoic acid to convert the carboxylic group to a primary amino group or by reacting an ester of the Formula V with hydrazine, treating the resulting hydrazide with nitrous acid to form a urethane of the Formula VI and hydrolysing the latter to produce a compound of the Formula VI.

Compounds from antrodia camphorata, method for preparing the same and use thereof

The invention relates to bioactive compounds purified from mycelium of Antrodia camphorata and the manufacturing method thereof. A method for treatment of cancers by administrating an effective amount of the said compounds selected from the group consisting of AC006, AC007, AC009, AC011, AC012, AC007-H1, AC009-H1, and AC012-H1 wherein the cancers is liver cancer, brain cancer, prostate cancer, breast cancer, colorectal cancer, or melanoma.

15,16-seco-19-nor progestins

15,16-Seco-19-nor progestins are provided which display elevated progestational activity with a minimum of ancillary hormonal activity. Processes for the preparation of the novel progestins are provided as are methods of use. A preferred method of use is in the suppression of ovulation in the human female.

Patent FR2178221A1

Processes and intermediates for the preparations of benzoprostacyclin analogues and benzoprostacyclin analogues prepared therefrom

The invention relates to processes for preparing benzoprostacyclin analogues and intermediates prepared from the process, and the benzoprostacyclin analogues prepared therefrom. The invention also relates to cyclopentenone intermediates in racemic or optically active form.

Cyclohexane compound and liquid crystal composition containing said compound

SUBSTITUTED BETA-DICETONES AND THEIR USE IN THE TREATMENT OF INFLAMMATORY DISEASES OF THE INTESTINE.

COMPUESTOS DE LA FORMULA: DONDE N ES 0 O 1, R SUB 1 Y R SUB 2 SON INDEPENDIENTEMENTE METILO, ETILO O CICLOPROPILO Y R ES UN GRUPO SUSTITUTIVO OPCIONAL FENILO O HETEROARILO O SAL O ESTER DEL MISMO, UTILIZADO EN EL TRATAMIENTO DE LAS ENFERMEDADES INTESTINALES INFLAMATORIAS.

Cyclohexane compound and liquid crystal composition containing the same

The present invention intends to provide a novel cyclohexane compound that can form a liquid crystal composition of which response speed is improved when mixed with a nematic liquid crystal and the like and to provide a specified liquid crystal composition in which a novel cyclohexane compound is mixed. The novel cyclohexane compound is represented by the following formula (1). (In the formula (1), R 1 and R 2 represent the same or different R, ROCO or RCOO, and the R represents an alkyl group. The alkyl group may have an unsaturated bond, and, in the group, —CH 2 — may be substituted with —O—, —CO— or —COO—, and a part of or an entirety of hydrogen atoms may be substituted with a halogen atom or a cyano group. X and Y each independently represents a halogen atom or a hydrogen atom and does not simultaneously represent a hydrogen atom. Further, alternatively, X represents an oxygen atom and Y represents a direct bond to the oxygen atom.)

Illudin analogs, uses thereof, and methods for synthesizing the same

Fluorine-containing chiral smectic liquid crystals

Novel carbamates, their preparation, and pharmaceutical formulations containing these compounds

Novel carbamates derived from substituted cyclic β-keto-alcohols, their preparation, and pharmaceutical formulations which contain these compounds and which may be used as hypnotics in the treatment of sleep disturbance and as sedatives.

S1P5 RECEPTOR AGONIST ACTIVITY COMPOUNDS

é fornecido um composto no qual o equilíbrio da atividade agonista contra o receptor s1p5 em relação ao receptor s1p1 foi aprimorado a fim de desenvolver um produto farmacêutico útil para o tratamento de doenças mediadas por s1p5, como a esquizofrenia e a doença de binswanger e outras doenças neurodegenerativas. um composto representado pela fórmula geral (v), (em que todos os símbolos são definidos no relatório descritivo) possui um equilíbrio aprimorado da atividade agonista contra o receptor s1p5 em relação ao receptor s1p1 e, portanto, pode servir como um agente terapêutico para doenças mediadas por s1p5, como a esquizofrenia e a doença de binswanger e outras doenças neurodegenerativas. a compound is provided in which the balance of agonist activity against the s1p5 receptor in relation to the s1p1 receptor has been improved in order to develop a pharmaceutical product useful for the treatment of s1p5-mediated diseases, such as schizophrenia and binswanger disease and other diseases neurodegenerative. a compound represented by the general formula (v), (where all symbols are defined in the specification) has an improved balance of agonist activity against the s1p5 receptor in relation to the s1p1 receptor and, therefore, can serve as a therapeutic agent for diseases mediated by s1p5, such as schizophrenia and binswanger disease and other neurodegenerative diseases.

Arylpiperazines having activity at the serotonin 1A receptor

A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1 A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

Novel cyclic and acyclic propenones and their use in the preparation of medicaments for treating cns disorders

Arylpiperazines having activity at the serotonin 1A receptor.

Diketone as well as enol ethers, enol esters or ketals thereof with fragrance properties.

ARYLIPIPERASINS WITH ACTIVITY WITH RESPECT TO 1A SEROTONIN RECEPTOR

Ряд соединений арилпиперазина являются эффективными фармацевтическими средствами для лечения состояний, связанных или зависимых от 1A-рецептора серотонина; эти соединения являются особенно эффективными антагонистами к этому рецептору и чрезвычайно полезны для купирования симптомов синдрома отмены никотина и табака.Международная заявка была опубликована вместе с отчетом о международном поиске. A number of arylpiperazine compounds are effective pharmaceuticals for treating conditions associated with or dependent on the 1A serotonin receptor; These compounds are particularly effective antagonists to this receptor and are extremely useful for alleviating the symptoms of nicotine and tobacco withdrawal syndrome. The international application was published along with an international search report.

Novel 1,3-dicarbonyl compound and composition thereof

3-Oxo-4-acyl or carbamyl-bicyclic aromatic and heterocyclic compounds as inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergy and antiinflammatory agents.

Sphingosine kinase inhibitors

The invention relates to substituted adamantane compounds of formula (I), pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, imflammatory disease, or angiogenic disease.

ARILPIPERAZINES THAT HAVE ACTIVITY ON THE SEROTONINE RECEPTOR 1A

Un compuesto de fórmula en la que Ar´ es un radical arilo o heteroarilo mono o bicíclico sustituido con unos a tres sustituyentes seleccionados entre el grupo que consiste en hidrógeno, alquilo (C1 -C6 ), alcoxi (C1 -C6 ), tioalquilo (C1 -C6 ), alquenilo (C2 -C6 ), alquinilo (C2 -C6 ), haloalquilo (C1 -C6 ), cicloalquilo (C3 -C8 ), cicloalquenilo (C3 -C8 ) o halógeno; R1 es hidrógeno, alquilo (C1 -C6 ), alcoxi (C1 -C6 ), tioalquilo (C1 -C6 ); R2 es fenilo, naftilo o cicloalquilo (C3 -C12 ), sustituido con uno o dos sustituyentes seleccionados entre el grupo que consiste en hidrógeno, alquilo (C1 -C6 ), alcoxi (C1 -C6 ), tioalquilo (C1 -C6 ), alquenilo (C2 -C6 ), alquinilo (C2 -C6 ), haloalquilo (C1 -C6 ), cicloalquilo (C3 -C8 ), cicloalquenilo (C3 -C8 ) o halógeno; R3 se selecciona entre el grupo que consiste en hidrógeno, alquilo (C1 -C6 ), alcoxi (C1 -C6 ), tioalquilo (C1 -C6 ), alquenilo (C2 -C6 ), alquinilo (C2 -C6 ), haloalquilo (C1 -C6 ), cicloalquilo (C3 -C8 ), cicloalquenilo (C3 -C8 ) o halógeno; X es -C(=O)-, -CHOH- o -CH2 -; o una sal, racemato, isómero óptico o solvato farmacéuticamente aceptable del mismo. A compound of the formula wherein Ar 'is a mono or bicyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6) alkyl, (C1-C6) alkoxy, (C1-thioalkyl) -C6), (C2 -C6) alkenyl, (C2 -C6) alkynyl, (C1-C6) haloalkyl, (C3 -C8) cycloalkyl, (C3 -C8) cycloalkenyl or halogen; R1 is hydrogen, (C1-C6) alkyl, (C1-C6) alkoxy, (C1-C6) thioalkyl; R2 is phenyl, naphthyl, or (C3-C12) cycloalkyl, substituted with one or two substituents selected from the group consisting of hydrogen, (C1-C6) alkyl, (C1-C6) alkoxy, (C1-C6) thioalkyl, alkenyl (C2-C6), (C2-C6) alkynyl, (C1-C6) haloalkyl, (C3-C8) cycloalkyl, (C3-C8) cycloalkenyl, or halogen; R3 is selected from the group consisting of hydrogen, (C1-C6) alkyl, (C1-C6) alkoxy, (C1-C6) thioalkyl, (C2-C6) alkenyl, (C2 -C6) alkynyl, (C1 - halo) alkyl. C6 ...

Illudin analogs, uses thereof, and methods for synthesizing the same

This invention provides illudin derivatives, intermediates, preparation methods, pharmaceutical compositions and uses thereof. Specific examples include novel synthetic routes to prepare illudin derivatives and an illudin derivative having a positive optical rotation, which has therapeutic value.

Sphingosine kinase inhibitors

본 발명은 하기 화학식 (I)의 치환된 아다만탄 화합물, 그의 약제학적으로 허용가능한 염, 그의 제조 방법, 및 스핑고신 키나제 저해 방법 및 과증식성 질환, 염증성 질환 또는 혈관형성 질환을 치료 또는 예방하는 방법에 관한 것이다. The present invention provides a method for treating or preventing a substituted adamantane compound of formula (I), a pharmaceutically acceptable salt thereof, a method for preparing the same, and a method for inhibiting sphingosine kinase and hyperproliferative disease, inflammatory disease or angiogenic disease. It is about a method. <화학식 I> (I) 스핑고신 키나제, 과증식성 질환, 염증성 질환, 혈관형성 질환, 아다만탄 화합물 Sphingosine kinases, hyperproliferative diseases, inflammatory diseases, angiogenic diseases, adamantane compounds

Novel tetrahydronaphthalene derivatives

The invention comprises 2-cyano-6-methoxy-tetralone-1 derivatives having the formula: <FORM:0979895/C1/1> in which R represents an alkyl group having 2-7 carbon atoms and processes for the preparation thereof by reacting 6-methoxy-3, 4-dihydronapthyl-[2, 1-d]-isoxazole with an alkylating agent in the presence of an alkali metal alcoholate e.g. sodium methylate. Alkylation may be effected either directly with an alkyl iodide or indirectly with an alkenyl halide followed by catalytic reduction.

Sphingosine Kinase Inhibitors

The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.

Arylpiperazines having activity at the serotonin 1a receptor

A series of arylpiperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

NYA 1,3-DICARBONYLFOERENINGAR OCH DERAS ANVAENDNING.

3-Oxo-4-acyl or carbamyl-bicyclic aromatic and heterocyclic compounds as inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergy and antiinflammatory agents.

Fluorine-containing cyclic compound, fluorine-containing polymer compound, resist material and pattern forming method using the same

Patent JPS497250A

Substituted tetralins as selective estrogen receptor-beta agonists

The present invention relates to novel tetralin ER-β agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-β mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory bowel disease, and arthritis.

PHENYLCYCLOHEXANE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

Arylpiperazines having activity at the serotonin 1A receptor

A method for potentiating the action of a serotonin reuptake inhibitor in increasing the availability of serotonin, norepinephrin and dopamine in the brain, comprising administering to a patient in need of such treatment a serotonin reuptake inhibitor in combination with an effective amount of a compound of the formula wherein Ar′ is a mono or bicyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )alkylthio, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 1 -C 6 )alkyl halo, (C 3 -C 8 )cycloalkyl, (C 3 -C 8 )cycloalkenyl or halo; R 1 is hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )alkylthio; R 2 is phenyl, naphthyl or (C 3 -C 12 )cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )alkylthio, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 1 -C 6 )alkyl halo, (C 3 -C 8 )cycloalkyl, (C 3 -C 8 )cycloalkenyl or halo; R 3 is selected from the group consisting of hydrogen (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )alkylthio, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 1 -C 6 )alkylhalo, (C 3 -C 8 )cycloalkyl, (C 3 -C 8 )cycloalkenyl or halo; X is —(C═O)—, —CHOH— or —CH 2 —; or a pharmaceutically acceptable salt, racemate, optical isomer or solvate thereof.

3-hydroxy-2-cyclobuten-1-one salts, their production and use

3-Hydroxy-2-cyclobuten-1-one salts of the general formula: ##STR1## wherein R is an ammonium group of the general formula: ##STR2## wherein R 1 , R 2 and R 3 are the same or different in meaning and each is a hydrogen atom, a lower alkyl group or a cycloalkyl group or R is an alkali metal atom. The salts according for formula I are obtained by the reaction of pure 3-acetoxy-2-cyclobuten-1-one, or 1,3-cyclobutanedione or a distillation residue of the diketene production containing 3-acetoxy-2-cyclobuten-1-one, with a base. The base can be an amine of the general formula: ##STR3## wherein R 1 , R 2 , and R 3 have the above-mentioned meaning, or an alkali metal alcoholate or an alkali metal hydroxide. The salts according to formula I are suitable for the production of squaric acid, by their being halogenated in a first step and then being hydrolyzed to squaric acid in a second step.

Arylpiperazines having activity at the serotonin 1a receptor

A series of arylpiperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

3-hydroxy-2-cyclobuten-1-one salts, their production and use

3-Hydroxy-2-cyclobuten-1-one salts of the general formula: <IMAGE> I wherein R is an ammonium group of the general formula: <IMAGE> II wherein R1, R2 and R3 are the same or different in meaning and each is a hydrogen atom, a lower alkyl group or a cycloalkyl group or R is an alkali metal atom. The salts according for formula I are obtained by the reaction of pure 3-acetoxy-2-cyclobuten-1-one, or 1,3-cyclobutanedione or a distillation residue of the diketene production containing 3-acetoxy-2-cyclobuten-1-one, with a base. The base can be an amine of the general formula: <IMAGE> III wherein R1, R2 , and R3 have the above-mentioned meaning, or an alkali metal alcoholate or an alkali metal hydroxide. The salts according to formula I are suitable for the production of squaric acid, by their being halogenated in a first step and then being hydrolyzed to squaric acid in a second step.

Carbamates, their preparation and pharmaceutical compositions containing them

Novel carbamates derived from substituted cyclic beta -keto-alcohols, their preparation, and pharmaceutical formulations which contain these compounds and which may be used as hypnotics in the treatment of sleep disturbance and as sedatives.

Arylpiperazines having activity at the serotonin 1A receptor

A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1 A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

Malodor counteracting compositions

一种恶臭冲消组合物，包括至少一种式(A)的化合物和至少一种式(B)的化合物其中n、X、Y和R 1 －R 4 如说明书所定义。

Sphingosine kinase inhibitor compounds, compositions comprising them and uses thereof for preparing a medicament for treating disorders characterized by abnormal activation of spingosine kinase

The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease. [WO2006138660A2]

Cryptoclidin analogue, application and synthetic method thereof

本发明提供了隐杯伞素衍生物、中间体、制备方法、药物组合物及其用途。具体的示例包括用于制备隐杯伞素衍生物的新的合成路线和具有治疗价值的具有正旋光性的隐杯伞素衍生物。

Compounds and processes that generate cyclopropenes and substituted cyclopropenes on demand

Compounds and methods that release 1-methylcyclopropene, 1-trifluoromethylcyclopropene, and other substituted cyclopropenes are disclosed. The compounds are of the class of chemical analogue of 2-oxa-bicyclo[2.1.0]penta-3-one useful as vessels for molecular plant ethylene receptor inhibitors. The compounds and methods overcome present limitations for storage, transportation, and application of the cyclopropene containing compounds by using light, including sunlight, and/or heat as the primary release trigger. Additional products released include innocuous gases and value added aryl-group compounds.

Fluorine-containing chiral smectic liquid crystal

Compound and organic light-emitting element using same

本发明提供新型化合物及利用其的有机发光元件，所述新型化合物由化学式1、化学式2或化学式3表示，在化学式1、化学式2和化学式3中，X为O或S，M为碱金属或碱土金属，Z为O或S，Y为CH或N，L为O、S、CO、SO 2 、 或 A为苯、萘或吡啶，B为苯或吡啶，R全部为氢，或者R中的两个一起形成单键且其余为氢，并且化合物 从所述化学式1中排除。

Lewis-acid metal catalyst enclosed in polymer

To enclose a Lewis-acid metal in a polymer and enable the resultant Lewis-acid metal catalyst to be recovered while maintaining the function of the catalyst. The polymer-enclosed Lewis-acid metal catalyst comprises a crosslinked polymer and a Lewis-acid metal enclosed therein, and the crosslinked polymer is one obtained from a crosslinkable polymer by crosslinking crosslinking groups contained in the polymer. The catalyst is characterized in that the crosslinkable polymer has at least one kind of monomer units having a hydrophobic substituent and a hydrophilic substituent having a crosslinking group and that the hydrophobic substituent comprises an aromatic substituent. This catalyst can be obtained by mixing an organic solution containing the crosslinkable polymer and a Lewis-acid metal with a poor solvent and subjecting the resultant polymer micells containing the Lewis-acid metal enclosed therein to a crosslinking reaction. This catalyst is useful as a catalyst for aldol reaction, cyanation reaction, allylation reaction, Michael reaction, Mannich reaction, Diels-Alder reaction, or Friedel-Crafts reaction.

Arylpiperazines having activity at the serotonin 1A receptor

A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1 A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

Reduced coenzyme q10 crystal having excellent stability

With respect to reduced coenzyme Q10, there has been no report about the presence of crystal polymorphism, and it has been considered that a conventionally obtained crystal form is only one form. The present invention relates to a reduced coenzyme Q10 crystal having an endothermic peak indicating melting at 54 ~ 2°C during temperature rise at a rate of 5°C/min by differential scanning calorimetry (DSC), and/or to a reduced coenzyme Q10 crystal showing characteristic peaks at diffraction angles (2.theta. ~ 0.2°) of 11.5°, 18.2°, 19.3°, 22.3°, 23.0° and 33.3° by powder X-ray (Cu-K.alpha.) diffraction. The crystal form is a novel reduced coenzyme Q10 crystal which has a higher melting point and a lower solubility in a solvent, and is more excellent in stability than the conventionally known reduced coenzyme Q10 crystal.

Sphingosine kinase inhibitors

The invention relates to substituted adamantane compounds of formula (I), pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, imflammatory disease, or angiogenic disease.

Reduced coenzyme q10 crystal having excellent stability

With respect to reduced coenzyme Q10, there has been no report about the presence of crystal polymorphism, and it has been considered that a conventionally obtained crystal form is only one form. The present invention relates to a reduced coenzyme Q10 crystal having an endothermic peak indicating melting at 54 ~ 2°C during temperature rise at a rate of 5°C/min by differential scanning calorimetry (DSC), and/or to a reduced coenzyme Q10 crystal showing characteristic peaks at diffraction angles (2.theta. ~ 0.2°) of 11.5°, 18.2°, 19.3°, 22.3°, 23.0° and 33.3° by powder X-ray (Cu-K.alpha.) diffraction. The crystal form is a novel reduced coenzyme Q10 crystal which has a higher melting point and a lower solubility in a solvent, and is more excellent in stability than the conventionally known reduced coenzyme Q10 crystal.

Arylpiperazines having activity at the serotonin 1A receptor

A series of aryl piperazine compounds of the formula: wherein Ar′ is a mono or bicyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; or the pharmaceutically acceptable salt, racemate, optical isomer or solvate thereof. or the pharmaceutically acceptable salts thereof, are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1 A receptor.

Process for the preparation of new 11-hydroxy- or 11-acyloxy-10,11-dihydro-5,10-methano-5H-dibenzo [a, d] cycloheptene compounds

Cyclohexane compound and liquid crystal composition containing said compound

네마틱 액정 등에 혼합하여, 응답 속도를 개량한 액정 조성물을 형성할 수 있는 신규 시클로헥산 화합물을 제공함과 함께, 신규 시클로헥산 화합물이 혼합된 특정 액정 조성물을 제공하는 것이다. 이 신규 시클로헥산 화합물을 이하의 식 (1) 에 나타낸다. (식 (1) 중 R 1 , R 2 는 동일 또는 상이한 R, ROCO, RCOO 를 나타내고, R 은 알킬기를 나타낸다. 그 알킬기는 불포화 결합을 갖고 있어도 되고, 그 기 중 -CH 2 - 는 -O-, -CO- 또는 -COO- 로 치환되어 있어도 되고, 또한, 일부 혹은 전부의 수소 원자가 할로겐 원자 또는 시아노기에 의해 치환되어 있어도 된다. X, Y 는 각각 독립적으로 할로겐 원자 또는 수소 원자를 나타내고, 동시에 수소 원자를 나타내는 경우는 없다. 또한, X 는 산소 원자를 나타내고 Y 는 그 산소 원자에 대한 직접 결합을 나타낸다) To provide a novel cyclohexane compound capable of forming a liquid crystal composition improved in response speed by mixing with a nematic liquid crystal or the like, and to provide a specific liquid crystal composition in which a novel cyclohexane compound is mixed. This novel cyclohexane compound is shown in the following formula (1). (Wherein R 1 and R 2 represent the same or different R, ROCO, and RCOO, and R represents an alkyl group. The alkyl group may have an unsaturated bond, and -CH 2 - , -CO- or -COO-, and some or all of the hydrogen atoms may be substituted by a halogen atom or a cyano group, X and Y each independently represents a halogen atom or a hydrogen atom, and at the same time And X represents an oxygen atom and Y represents a direct bond to the oxygen atom.

Novel cyclic and acyclic propenones for treating cns disorders

The invention relates to novel cyclic and non-cyclic propenone derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are useful as medicaments.

Aryl piperazines exhibiting activity in respect to 1a serotonine receptor

Methods and intermediates for preparing benzoprostacyclin analogs, and benzoprostacyclin analogs prepared therefrom

本发明关于用于制备苯并前列环素类似物的方法和由所述方法制备的中间物，以及由其制得的苯并前列环素类似物。本发明亦关于呈外消旋或光活性形式的环戊烯酮中间物。

Dioxo-alkanes and dioxo-alkenes

Compounds of general formula (I) wherein: R1 and R2 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, optionally substituted -CO-(C1-10alkyl), optionally substituted C3-10cycloalkyl, optionally substituted -CO-(C3-10cycloalkyl), optionally substituted C2-10alkenyl, optionally substituted -CO-(C2-10alkenyl), optionally substituted aryl, and optionally substituted -CO-aryl, or R1 and R2 together represent an optionally substituted saturated or unsaturated C1-10alkylidene group, or an optionally substituted saturated or unsaturated C3-10cycloalkylidene group, or R1 and R2 together with the carbon atom to which they are attached represent an optionally substituted saturated or unsaturated organic ring containing 3, 4, 5, 6, 7 or 8 ring carbon atoms and optionally 1, 2 or 3 ring heteroatoms selected from O, N and S; R3, which may be the same as, or different from, either of R1 and R2, is selected from optionally substituted C1-10alkyl, optionally substituted C3-10cycloalkyl, optionally substituted C2-10alkenyl, and optionally substituted aryl; R4, R5 and R6 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, OH, optionally substituted C1-10alkoxy, halo, optionally substituted aryloxy, optionally substituted (C1-10alkyl)-S(O)n- where n = 0, 1 or 2, optionally substituted aryl-S(O)n- where n = 0, 1 or 2, or R4 is hydrogen and R5 and R6 together represent an optionally substituted saturated or unsaturated organic chain containing 1, 2, 3, 4, 5, 6 or 7 chain carbon atoms and optionally 1, 2 or 3 chain heteroatoms selected from O, N and S, provided that the chain is at least 3 atoms long; with the proviso that, when R1 = R2 = hydrogen, then any optionally substituted C1-10alkyl or optionally substituted C2-10alkenyl for R3 must have a branch point at one or more of the α and β positions counted from the carbonyl group (or tautomeric form thereof) to which R3 is attached; or a physiologically ...

Fluorine-containing cyclic compound, fluorine-containing polymer compound, resist material using same and method for forming pattern

Disclosed is a fluorine-containing cyclic compound represented by the general formula (1) below. R1a represents a cyclic alkyl group having 1-25 carbon atoms, a cyclic alkenyl group or a cyclic alkynyl group; and R2 and R3 independently represent a hydrogen atom, a halogen atom or a straight-chain, branched-chain or cyclic alkyl group having 1-25 carbon atoms. R1a, R2 and R3 may independently include a fluorine atom, an oxygen atom, a sulfur atom, a nitrogen atom or an atomic group having a carbon-carbon double bond.

Agricultural chemicals.

La presente invención se refiere a derivados de compuestos que son conocidos por ser de uso en el campo de agricultura; estos derivados se diferencian del compuesto activo precursor en virtud de que son derivados redox del compuesto activo; esto significa que uno o más de los grupos funcionales en el compuesto activo ha sido convertido hasta otro grupo en uno o más cambios, uno o más de los cuales puede considerarse que representan un cambio de estado de oxidación respecto a los grupos en el compuesto original; se hace referencia a estos compuestos generalmente como derivados redox; los compuestos son de uso como insecticidas, herbicidas y repelentes de insectos.

Polyene compounds

Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method

Hydroxyethyl-cyclopropyl-azolyl derivatives

Novel hydroxyethylcyclopropylazolyl derivatives of the formula …<IMAGE>… in which … …  R<1>, R<2>, X and Y have the meaning given in the description, …  and their acid addition salts and metal salt complexes, …  a plurality of processes for the preparation of the novel substances and their use as microbicides in crop protection and in the protection of materials. … …<??>Novel intermediates, their preparation, and their use for the synthesis of substances of the formula (I).

Compounds having s1p5 receptor agonistic activity

Patent TWI309640B

Method for producing benzyl ketones and method for producing oxirane

Cyclohexane compound and liquid crystal composition containing said compound

Patent FR1580891A