Methods and compositions for heavy metal detoxification

Compositions and methods for enhancing heavy metal detoxification are described. The compositions and methods described provide enhanced activity of key detoxification systems including that the induction of phase II detoxification enzymes, such as glutathione S-transferases (GSTs), and NADPH quinone reductase (NQO1) activity.

GENES FOR BIOSYNTHESIS OF TETRACYCLINE COMPOUNDS AND USES THEREOF

The invention relates to tetracycline products produced by genetically engineered cells, and to therapeutic methods using such tetracyclines. The present invention is based on the cloning and heterologous expression of genes encoding the chelocardin biosynthetic pathway. 3. Use of a compound of for the treatment of bacterial or fungal infections claim 1 , treatment of malaria claim 1 , a neurodegenerative disease claim 1 , Parkinson's disease claim 1 , Huntington's claim 1 , disease claim 1 , periodontitis claim 1 , an autoimmune condition claim 1 , multiple sclerosis claim 1 , atherosclerosis claim 1 , rheumatoid arthritis claim 1 , osteoporosis claim 1 , tumour invasion claim 1 , cancer and inflammatory states.4. Use of a compound of for the treatment of bacterial or fungal infections.5. Use of a compound of for the treatment of bacterial or fungal infections claim 2 , treatment of malaria claim 2 , a neurodegenerative disease claim 2 , Parkinson's disease claim 2 , Huntington's claim 2 , disease claim 2 , periodontitis claim 2 , an autoimmune condition claim 2 , multiple sclerosis claim 2 , atherosclerosis claim 2 , rheumatoid arthritis claim 2 , osteoporosis claim 2 , tumour invasion claim 2 , cancer and inflammatory states.6. Use of a compound of for the treatment of bacterial or fungal infections. This application is a divisional of U.S. patent application Ser. No. 12/536,622 filed Aug. 6, 2009, now U.S. Pat. No. 8,361,777, which claims the benefit of EP Application No. 08014141.9 filed Aug. 7, 2008, the entire disclosures of which are incorporated herein by reference.This invention relates to genetically engineered cells, and to proteins and genes useful in the production of tetracycline compounds, to methods of producing tetracycline compounds, and to tetracyclines thereby produced. The present invention is based on the cloning and heterologous expression of genes encoding the chelocardin biosynthetic pathway.Tetracyclines are a large group of drugs with a ...

SHIP1 MODULATORS AND RELATED METHODS

Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, Rand A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed. 19. A composition comprising a compound of in combination with a pharmaceutically acceptable carrier or diluent.20. A method for modulating SHIP1 comprising administering an effective amount of a composition of to an animal in need thereof.21. A method for treating a disease claim 19 , disorder or condition comprising administering an effective amount of a composition of to an animal in need thereof claim 19 , where the disease claim 19 , disorder or condition is an autoimmune disease claim 19 , disorder or condition claim 19 , an inflammatory disease claim 19 , disorder or condition claim 19 , or a neoplastic or cell proliferative disease claim 19 , disorder or condition.22. The method of wherein the disease claim 21 , disorder or condition is an autoimmune disease claim 21 , disorder or condition selected from idiopathic pulmonary fibrosis claim 21 , an inflammatory bowel disease claim 21 , rheumatoid arthritis claim 21 , Still's Disease claim 21 , Sjögren's Syndrome claim 21 , systemic lupus erythematosus claim 21 , and systemic sclerosis.23. The method of claim 22 , wherein the disease claim 22 , disorder or condition is an inflammatory bowel disease selected from Crohn's Disease and ulcerative colitis.24. The method of wherein the disease claim 21 , disorder or condition is an inflammatory disease ...

INHIBITORS OF BETA-SECRETASE

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. 2. A compound according to or a pharmaceutically acceptable salt thereof for use as a medicament.3. A pharmaceutical composition comprising at least one compound according to or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.4. A compound according to or a pharmaceutically acceptable salt thereof for use in the treatment of a BACE1 mediated disorder or disease.5. A compound or a pharmaceutically acceptable salt thereof for use according to claim 4 , wherein the BACE1 mediated disorder or disease is selected from the group consisting of a neurodegenerative disorder claim 4 , cognitive decline claim 4 , cognitive impairment claim 4 , dementia claim 4 , and disease characterized by the production of β-amyloid deposits or neurofibrillary tangles.6. A compound or a pharmaceutically acceptable salt thereof for use according to claim 5 , wherein the disorder or disease is selected from the group consisting of Alzheimer's disease claim 5 , Trisomy 21 (Down Syndrome) claim 5 , Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-type (HCHWA-D) claim 5 , senile dementia claim 5 , cerebral amyloid angiopathy claim 5 , degenerative dementia claim 5 , dementias of mixed vascular and degenerative origin claim 5 , dementia associated with Parkinson's disease claim 5 , dementia associated with progressive supranuclear palsy claim 5 , dementia associated with cortical basal degeneration claim 5 , diffuse Lewy body type of Alzheimer's disease claim 5 , dry age related ...

SYNTHESIS OF RESVERATROL-BASED COMPOUNDS

A compound having the structure: This application claims priority of U.S. Provisional Application No. 61/400,111, filed Jul. 21, 2010, the contents of which are hereby incorporated by reference.Throughout this application, various publications are referenced by citation in parentheses. The disclosures of these publications in their entireties are hereby incorporated by reference into this application in order to more fully describe the state of the art as known to those skilled therein as of the date of the invention described and claimed herein.The past decade has witnessed tremendous interest in the relatively small natural product resveratrol (1, ) based primarily on its possession of a promising and selective array of in vitro and in viva activity against a collection of disease states, including inflammation, heart disease, aging, and cancer [1]. In fact, its truly unique biochemical profile, coupled with its relatively high concentration in red wine (˜100 mM) and near absence in white varietals and grape juice, has led to the popularly held notion that resveratrol is the main protagonist for the so-called “French paradox” [2]. Amazingly, however, virtually no effort has been devoted to the large family of resveratrol-based oligomers (such as 2-8) [3] produced combinatorially by plants throughout the world in response to environmental stress, compounds which initial screening suggest should have unique, if not superior, activity profiles to resveratrol itself [4].In one embodiment, this invention provides a compound having the structureThis invention provides a compound having the structureIn some embodiments, the invention includes the compound wherein in the compound each occurrence of Ris independently H, CH, C(O)CH, P(O)(OR), SOOR, SOR, or C(O)R,In some embodiments, the invention includes the compound wherein in the compoundIn some embodiments, the invention includes the compoundwherein the structure isor a salt thereof.In some embodiments, the invention ...

COMPOUNDS FROM INVASIVE SALVINIAS AND METHODS OF USING THE SAME

In some embodiments, the compositions and methods relate to compounds isolated from plants in the Salviniaceae family, pharmaceutical compositions comprising the same, and methods of using the same. 4. (canceled)611.-. (canceled)12. The compound of claim 1 , wherein the compound is isolated from a plant in the Salviniaceae family.13Salvinia. The compound of claim 12 , wherein the compound is isolated from a plant in the genus.14S. auriculata, S. biloba, S. cucullata, S. cyathiformis, S. hastate, S. herzogii, S. minima, S. molesta, S. natans, S. nymphellula, S. oblongifolia, S. radula, S. rotundifoliaS. sprucei.. The compound of claim 12 , wherein the compound is isolated from claim 12 , or15Azolla. The compound of claim 12 , wherein the compound is isolated from a plant in the genus.16. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) the compound according to or a pharmaceutically acceptable salt thereof; and'}(b) an excipient.17. A method of treating cancer in a patient in need thereof claim 1 , comprising administering to the patient a pharmaceutical composition comprising a compound according to in an amount sufficient to treat the cancer.18. The method of claim 17 , wherein the cancer is melanoma claim 17 , cervical cancer claim 17 , breast cancer claim 17 , ovarian cancer claim 17 , prostate cancer claim 17 , testicular cancer claim 17 , urothelial carcinoma claim 17 , bladder cancer claim 17 , non-small cell lung cancer claim 17 , small cell lung cancer claim 17 , sarcoma claim 17 , colorectal adenocarcinoma claim 17 , gastrointestinal stromal tumors claim 17 , gastroesophageal carcinoma claim 17 , colorectal cancer claim 17 , pancreatic cancer claim 17 , kidney cancer claim 17 , hepatocellular cancer claim 17 , malignant mesothelioma claim 17 , leukemia claim 17 , lymphoma claim 17 , myelodysplastic syndrome claim 17 , multiple myeloma claim 17 , transitional cell carcinoma claim 17 , neuroblastoma claim 17 , ...

Cosmetic Composition Comprising Vetiver Root Extract

A cosmetic composition is provided, which comprises a carrier and a Vetiver root extract, in particular an extract from exhausted Vetiver root. This composition provides a stimulation of sebum production, stimulation of sebum antimicrobial, lipids production, activation of adipocytes volume increase, skin hydration, skin tonicity booster, skin fatigue reduction, perilabial wrinkles reduction, skin replumping, and fragrance long-lastingness enhancement. 1. A cosmetic composition comprising a carrier and at least one active cosmetic ingredient , wherein the at least one active cosmetic ingredient comprises a Vetiver root extract.2. The cosmetic composition according to claim 1 , wherein the cosmetic composition is a skin care composition.3. The cosmetic composition according to claim 1 , wherein the at least one active cosmetic ingredient comprises an aqueous extract of Vetiver root.4. The cosmetic composition according to claim 1 , wherein the at least one active cosmetic ingredient comprises an extract of exhausted Vetiver root.5. A method of preparing an active cosmetic ingredient claim 1 , comprising the step of: extracting Vetiver root.6. The method according to claim 5 , comprising the steps of:(i) providing exhausted Vetiver root; and(ii) extracting the exhausted Vetiver root.7. The method according to claim 5 , wherein the extraction is performed using water.8. (canceled)9. A method of stimulating the sebum production claim 1 , of stimulating sebum antimicrobials claim 1 , of stimulating the lipids production claim 1 , of activating the adipocytes volume increase claim 1 , of improving the skin hydration claim 1 , of boosting the skin tonicity claim 1 , of reducing skin fatigue claim 1 , of reducing perilabial wrinkles claim 1 , of replumping skin claim 1 , and/or of enhancing fragrance long-lastingness claim 1 , the method comprising the step of: applying the cosmetic composition of to human skin. The present invention relates to cosmetic compositions ...

Preparation of Ambrox from Labdanes of Dysoxylum hongkongense, and the Preparation of New Diterpenoids from Dysoxylum hongkongense

The present invention discloses eight new diterpenoids, i.e. Dysongensins A to H, extracted from the leaves and twigs of Dysoxylum hongkongense , wherein AMBROX® which is applicable in the perfume industry is prepared from Dysongensin A via a series of chemical reactions, and the cytotoxicity of Dysongensins A to H against human cancer cell lines and their antiviral and anti-inflammatory activities are determined. Therefore, in the present invention, AMBROX® prepared from Dysongensin A is a new idea for application as an odorous compound in the perfume industry, and the novel diterpenoids can be prepared as a pharmaceutical compositions and/or a drug having antiviral, anti-inflammatory and/or anti-cancer activities.

1,3-DI-OXO-INDENE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT OR OPTICAL ISOMER THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ANTIVIRAL, ACTIVE INGREDIENT

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media. 3. The 1 claim 1 ,3-Dioxoindene derivatives claim 1 , pharmaceutically-acceptable salt thereof or optical isomer thereof as set forth in claim 1 , wherein claim 1 , A claim 1 , A claim 1 , Aand Aare claim 1 , either independently or optionally claim 1 , any one selected from a group consisting of —H claim 1 , halogen and —NRR;{'sup': 1', '2', '1', '2, 'G is —OH, —NR(C═O)Ror —NR(C═O)OR;'}{'sup': 1', '2', '3', '4', '1', '2, 'sub': 1', '10, 'D, D, Dand Dare, either independently or optionally, any one selected from a group consisting of halogen, C˜Cstraight- or side-chain alkyl and —NR(C═O)R;'}{'sup': 1', '1', '1', '1', '2, 'E is —H, —OH, —OR, —O(C═O)R, —O(C═O)ORor —O(C═O)NRR;'}{'sup': 1', '2', '3, 'sub': 1', '8', '1', '4', '6', '10, 'R, Rand Rare, each independently, hydrogen, nonsubstituted or phenyl-substituted C˜Cstraight- or side-chain alkyl, nonsubstituted or phenyl-substituted C˜Cstraight- or side-chain alkenyl or C˜Caryl;'}X and Y are oxygen;{'sup': 1', '2', '3, 'Z, Zand Zare carbon;'}n is integer between 1˜3; and{'img': {'@id': 'CUSTOM- ...

INHIBITION OF DYRK1A KINASE

Novel compounds which inhibit DYRK1A activity comprise thymoquinone derivatives including a pair of substituted or unsubstituted six-membered carbon rings selected from phenyl and cyclohexadiene linked by an alkyl or alkenyl linker. Each six-membered ring includes at least one oxygen-bearing substituent selected from carbonyl oxygens, hydroxyls, alkoxyls, and halogenated derivatives thereof. The compounds can be administered to mammalian subjects for inhibition of DYRK1A kinase proteins. 2. The one or more compounds of claim 1 , wherein at least one of R2 or R4 in compound I is a methyl group claim 1 , or wherein at least one R2′ or R4′ in compound II is a methyl group.3. The one or more compounds of claim 1 , where the linker -[ ]-is a methylene bridge.4. The one or more compounds of claim 1 , at least one of R2 or R1 in compound I is an isopropyl group claim 1 , or wherein at least one R1′ or R2′ in compound II is an isopropyl group.7. The one or more compounds of claim 1 , said compounds selected from the group consisting of the isomers claim 1 , tautomers claim 1 , esters claim 1 , metal complexes claim 1 , and salts of the structures.8. A composition comprising a plurality of one or more compounds of dispersed in a carrier.9. The composition of claim 8 , comprising a plurality of compounds according to structure I and a plurality of compounds according to structure II dispersed in said carrier.10. A method of inhibiting DYRK1A activity comprising the step of contacting DYRK1A kinase with an effective amount of a thymoquinone derivative comprising a pair of substituted or unsubstituted six-membered carbon rings selected from the group consisting of phenyl and cyclohexadiene linked by a linker bonded to both of said six-membered rings claim 8 , at least one of said six-membered rings having a pair of oxygen-bearing substituents selected from the group consisting of carbonyl oxygens claim 8 , hydroxyls claim 8 , alkoxyls claim 8 , and halogenated derivatives ...

KETONE OR OXIME COMPOUND, AND HERBICIDE

There is provided novel agricultural chemicals, in particular herbicides. A ketone or oxime compound or a salt thereof of Formula (1): 2. The compound according to claim 1 , wherein R is —O-A.3. The compound according to claim 2 , wherein A is a hydrogen atom.4. The compound according to claim 2 , wherein q=3 and each Z is independently a halogen atom claim 2 , Calkyl claim 2 , or —OR.5. The compound according to claim 2 , wherein q=3 and a first Z represents a bromine claim 2 , a second Z represents methyl claim 2 , and a third Z represents —OCH.7. The compound according to claim 1 , wherein R is ═O.8. The compound according to claim 7 , wherein q=3 and each Z is independently a halogen atom claim 7 , Calkyl claim 7 , or —OR.9. The compound according to claim 7 , wherein q=3 and a first Z represents a bromine claim 7 , a second Z represents methyl claim 7 , and a third Z represents —OCH.11. The compound according to claim 7 , wherein q=3 and a first Z represents —OCH claim 7 , a second Z represents methyl claim 7 , and a third Z represents —OCH.13. The compound according to claim 7 , wherein q=3 and a first Z represents methyl claim 7 , a second Z represents methyl claim 7 , and a third Z represents —OCH. The present invention relates to a novel ketone or oxime compound or a salt thereof, and agricultural chemicals, in particular herbicides, containing the ketone or oxime compound or the salt thereof as an active component. The agricultural chemical in the present invention means an insecticide/acaricide, a nematicide, a herbicide, and a bactericide in agricultural and horticultural fields.For example, certain types of ketone or oxime compounds have been described in Patent Documents 1 to 4. The ketone or the oxime compound according to the present invention, however, has not been described at all.An object of the present invention is to provide a chemical substance that surely shows effect on various weeds in a low application amount of the chemical substance, has ...

COMPOUNDS FROM INVASIVE SALVINIAS AND METHODS OF USING THE SAME

In some embodiments, the compositions and methods relate to compounds isolated from plants in the Salviniaceae family, pharmaceutical compositions comprising the same, and methods of using the same. 415.-. (canceled)16. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) the compound according to and/or a pharmaceutically acceptable salt thereof; and'}(b) an excipient.17. A method of treating cancer in a patient in need thereof ,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'comprising administering to the patient a pharmaceutical composition, the composition comprising an effective amount of a compound according to .'}18. The method of claim 17 , wherein the cancer is melanoma claim 17 , cervical cancer claim 17 , breast cancer claim 17 , ovarian cancer claim 17 , prostate cancer claim 17 , testicular cancer claim 17 , urothelial carcinoma claim 17 , bladder cancer claim 17 , non-small cell lung cancer claim 17 , small cell lung cancer claim 17 , sarcoma claim 17 , colorectal adenocarcinoma claim 17 , gastrointestinal stromal tumors claim 17 , gastroesophageal carcinoma claim 17 , colorectal cancer claim 17 , pancreatic cancer claim 17 , kidney cancer claim 17 , hepatocellular cancer claim 17 , malignant mesothelioma claim 17 , leukemia claim 17 , lymphoma claim 17 , myelodysplastic syndrome claim 17 , multiple myeloma claim 17 , transitional cell carcinoma claim 17 , neuroblastoma claim 17 , plasma cell neoplasms claim 17 , Wilm's tumor claim 17 , or hepatocellular carcinoma.1921.-. (canceled)22. The method of claim 17 , wherein said patient is further administered a distinct cancer therapy.2324.-. (canceled)25. The method of claim 17 , wherein the compound is isolated from a plant in the Salviniaceae family.26Salvinia. The method of claim 25 , wherein the compound is isolated from a plant in the genus.27Azolla. The method of claim 25 , wherein the compound is isolated from a plant in the genus.28. The method of claim ...

KETONE OR OXIME COMPOUND, AND HERBICIDE

There is provided novel agricultural chemicals, in particular herbicides. A ketone or oxime compound or a salt thereof of Formula (1): 2. The ketone compound or the salt thereof according to claim 1 , wherein A is a hydrogen atom claim 1 , Calkyl claim 1 , or —C(O)R;{'sup': '2', 'sub': '1-8', 'Ris Calkyl;'}{'sup': 6', '15', '16', '17', '1, 'sub': 1-6', '1-6', '3-8', '2-6', 'q1, 'Ris Calkyl, (C) alkyl arbitrarily substituted with R, Ccycloalkyl, Calkenyl, —C(═NOR)R, phenyl, phenyl substituted with (Z), or D1-32;'}{'sup': 8a', '16a', '17a, 'sub': '1-6', 'Ris a hydrogen atom, Calkyl, —C(O)OR, or —C(O)R;'}{'sup': '9a', 'sub': '1-6', 'Ris a hydrogen atom or Calkyl;'}{'sup': 8b', '9b, 'Rand Rare hydrogen atoms;'}{'sup': 10', '1', '12, 'R, R, and Rare hydrogen atoms;'}{'sup': 15', '16, 'sub': '3-8', 'Ris a halogen atom, Ccycloalkyl, —OR, or phenyl;'}{'sup': 16', '16a', '17', '17a, 'sub': '1-6', 'R, R, R, and Rare each independently Calkyl;'}{'sup': '1', 'sub': '1-6', 'Xis halo (C) alkyl;'}{'sup': a', 'c', '45', '41', '3, 'sub': 1-6', '3-8', '2-6', '2-6', '2-6', 'q3, 'Zand Zare each independently a hydrogen atom, a halogen atom, Calkyl, Ccycloalkyl, Calkenyl, (C) alkenyl arbitrarily substituted with R, Calkynyl, —OR, phenyl, phenyl substituted with (Z), D1-7, D1-11, D1-22, D1-32, or D1-37;'}{'sup': '1', 'Zis a halogen atom;'}{'sup': '3', 'sub': 1-6', '1-6', '1-6', '1-6', '1-6, 'Zis a halogen atom, Calkyl, halo (C) alkyl, Calkoxy, halo (C) alkoxy, or Calkylthio;'}{'sup': 41', '45, 'sub': 1-6', '1-6, 'Ris Calkyl, (C) alkyl arbitrarily substituted with R, phenyl, D1-32, or D1-34;'}{'sup': '45', 'Ris a halogen atom, phenyl, or D1-34;'}g2, g3, and p are 0;q1 and q3 are integers of 1; andg4, m, and n are each independently an integer of 0 or 1.3. The ketone compound or the salt thereof according to claim 2 , whereinB is B-1-a;{'sup': 'a', 'sub': 1-6', '1-6, 'Zis a halogen atom, Calkyl, or Calkoxy; and'}{'sup': c', '45', '41', '3, 'sub': 1-6', '3-8', '2-6', '2-6', '2-6', 'q3, 'Zis ...

USAGE OF OBLONGIFOLIN C, A NATURAL COMPOUND FROM GARCINIA YUNNANENSIS HU, ON TREATING CANCER AS METASTASIS INHIBITOR AND AUTOPHAGIC FLUX INHIBITOR

Disclosed is a natural compound, Oblongifolin C, isolated from a natural plant comprising species such as Hu, for its effects of anti-migration and anti-invasion against cancer and its use as an anticancer drug. The treated cancers comprise cervical cancers and esophageal cancers. The cancer treatment comprises inhibition of cancer metastasis and inhibition of autophagic flux. 2. The composition according to claim 1 , wherein said compound comprising Oblongifolin C.3. The composition according to claim 1 , wherein said compound is isolated from a natural plant.4Garcinia. The composition according to claim 3 , wherein said natural plant comprising species.5GarciniaGarcinia yunnanesis. The composition according to claim 4 , wherein said species comprising Hu.6. The composition according to claim 1 , wherein the treated cancers comprising cervical cancers and esophageal cancers.7. The composition according to claim 1 , wherein the cancer treatment comprising inhibition of cancer metastasis and inhibition of autophagic flux.8. A use of the composition according to for manufacture of anticancer medicaments.9. The use according to claim 8 , wherein said composition is used as an autophagy inhibitor.10. A method of treating cancer using composition according to by administering said composition to a subject in need of such treatment.11. The method according to wherein said composition is administered by injection. This application claims the benefit of U.S. Provisional Patent Application No. 61/750,870 filed Jan. 10, 2013 and of Chinese Standard Patent Application Serial Number 201310101235.5 filed Mar. 26, 2013; both disclosures of which are incorporated herein by reference in their entirety.The present invention relates to a chemical entity isolated from natural sources for its therapeutic uses. More particularly, it relates to a compound that is naturally occurring in the plant of Hu and its biological activity of antitumor effects.Esophageal cancer is one of the most ...

5-substituted-5-hydroxy-5-aryl-3-oxo-pentanoate derivatives and their enantiopure forms

The present invention relates to novel tertiary alcohol derivatives substituted with aryl and trifluoromethyl, and optical isomers thereof. In addition, the present invention also relates to methods for the preparation and use as enantiomer recognition agent thereof. The present invention provides pharmaceutical composition and use as therapeutically active substance 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 ...

Herbicidally Active 2-(Substituted-Phenyl)-Cyclopentane-1,3-Dione Compounds and Derivatives Thereof

The present invention relates to a compound of formula (I): wherein: Rand R, independently of each other, are hydrogen, fluorine or C-Calkyl; Ris hydrogen or methyl (preferably hydrogen); and the other substituents are as defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be 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 plants or to the locus thereof. 2. The compound as claimed in , wherein G is hydrogen; an agriculturally acceptable metal , or an agriculturally acceptable sulfonium or ammonium group; or G is —C(X)—Ror —C(X)—X—R , wherein X , R , X , Xand Rare as defined in .3. The compound as claimed in claim 1 , wherein X claim 1 , Xand Xare oxygen;{'sup': 'a', 'sub': 1', '10', '2', '6', '2', '6', '3', '6', '3', '6', '1', '4', '1', '4', '1', '2', '1', '1', '2', '1', '1', '2', '1', '1', '2', '1', '1', '2', '1', '1', '2', '1, 'Ris C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Ccycloalkyl-methyl-, C-CalkoxyC-Calkyl, phenyl-methyl- (in which the phenyl is optionally substituted by 1 or 2 of, independently, C-Calkyl, Cfluoroalkyl, C-Calkoxy; Cfluoroalkoxy, fluorine, chlorine or cyano); phenyl or phenyl substituted by 1 or 2 of, independently, C-Calkyl, Cfluoroalkyl, C-Calkoxy, Cfluoroalkoxy, fluorine, chlorine or cyano; or monocyclic heteroaryl or monocyclic heteroaryl substituted by 1 or 2 of, independently, C-Calkyl, Cfluoroalkyl, C-Calkoxy, Cfluoroalkoxy, fluorine, chlorine or cyano;'}and{'sup': 'b', 'sub': 1', '10', '2', '5', '2', '2', '4', '2', '5', '2', '2', '4', '3', '6', '3', '6', '1', '4', '1', '4', '1', '2', '1', '1', '2', '1', '1', '2', '1', '1', '2', '1', '1', '2', '1', '1', '2', '1, 'Ris C-Calkyl, C-Calkenyl-CH—, C- ...

NOVEL COMPOUND, PREPARING METHOD THEREOF, AND USE THEREOF AS INHIBITORS OF HISTONE DEMETHYLASE

Provided are a novel compound, preparing method thereof, and use thereof as inhibitor of histone demethylase. The compound represented by Chemical Formula 1 has activity which inhibits histone demethylase and thus is capable of specifically and effectively inhibit activity of histone demethylase. 2. The compound claim 1 , the isomer claim 1 , the derivative claim 1 , or the pharmaceutically acceptable salt of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently hydrogen claim 1 , a hydroxyl group claim 1 , or a substituted or unsubstituted Cto Calkly group.3. The compound claim 1 , the isomer claim 1 , the derivative claim 1 , or the pharmaceutically acceptable salt of claim 1 , wherein R claim 1 , R claim 1 , and Rare each independently a hydroxyl group.4. The compound claim 1 , the isomer claim 1 , the derivative claim 1 , or the pharmaceutically acceptable salt of claim 1 , wherein Ris a Cto Calkly group substituted with two or more halogen atoms.5. The compound claim 1 , the isomer claim 1 , the derivative claim 1 , or the pharmaceutically acceptable salt of claim 1 , wherein Ris a Cto Calkly group substituted with two halogen atoms.7StreptomycesStreptomyces. A genus SNC023 strain producing the compound of claim 1 , wherein the genus SNC023 strain is deposited under Korean Collection for Type Cultures (KCTC) Accession number KCTC12494BP.8StreptomycesCopris tripartitus.. The genus SNC023 strain of claim 7 , wherein the strain is separated or derived from an epidermis or body of a larva included in a brood ball of9. A method of producing the compound of claim 1 , the method comprising:{'i': Streptomyces', 'Streptomyces, 'culturing a genus SNC023 strain in a culturing medium, wherein the genus SNC023 strain is deposited under KCTC Accession number KCTC12494BP; and'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'separating the compound of from the culturing medium.'}10. The method of claim 1 , wherein the ...

COMPOSITIONS AND METHODS FOR THE MODULATION OF CYTOKINES

A method for modulating production of a cytokine, or molecule upregulated or down regulated by a cytokine, in a patient in need thereof, including administering to a patient a composition comprising at least one of a strontium-containing compound, a cysteine-based antioxidant, a polyhydroxyphenol and beta hydroxybutyric acid to the patient, whereby an amount of a cytokine in the patient is modulated. 1. A method for modulating production of a cytokine , or molecule upregulated or down regulated by a cytokine , comprising:administering to a patient in need thereof an effective amount of a composition comprising at least one compound selected from the group consisting of a strontium-containing compound, a cysteine-based antioxidant, a polyhydroxyphenol and beta hydroxybutyric acid, whereby an amount of a cytokine in the patient is modulated.2. The method of claim 1 , wherein the composition comprises a complex of a strontium-containing compound claim 1 , a cysteine-based antioxidant claim 1 , and at least one of polyhydroxyphenol and beta hydroxybutyric acid claim 1 , wherein the cysteine-based anti-oxidant and the at least one of polyhydroxyphenol and beta hydroxybutyric acid are optionally conjugated together by a cleavable bond.3. The method of claim 1 , wherein the cytokine is associated with inflammation.4. The method of claim 3 , wherein the cytokine or a molecule upregulated or down regulated by the cytokine is selected from the group consisting of Eotaxin-3 claim 3 , soluble tumor necrosis factor-alpha (sTNF-α) claim 3 , vascular cell adhesion molecule 1 (VCAM-1) claim 3 , interleukin-1 alpha (IL-1α) claim 3 , interferon gamma-induced protein 10 (IP-10) claim 3 , interferon-inducible T-cell alpha chemoattractant (I-TAC) claim 3 , interleukin-8 (IL-8) claim 3 , serum amyloid A protein (SAA) claim 3 , monocyte chemoattractant protein-1 (MCP-1) claim 3 , prostaglandin E2 (sPGE2) claim 3 , intercellular adhesion molecule 1 (ICAM-1) claim 3 , monokine induced by ...

Inhibitors of beta-secretase

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.

Cyclohexanone compounds and herbicides comprising the same

The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH 2 , O, S, S(O) or S(O) 2 ; R 1 represents a hydrogen atom or a methyl group; R 2 and R 3 represents a hydrogen atom, a C 1-6 alkyl group and the like; R 4 represents a C 6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C 1-6 alkyl group and the like; is useful as an active ingredient for herbicides.

Substituted Tropolone Derivatives and Methods of Use

The compositions and methods described herein relate generally to substituted tropolone derivatives, which, among other features, are useful as histone deacetylase (HDAC) inhibitors.

Pharmaceutical composition containing verbenone derivative for treating or preventing neurodegenerative disease

The present invention relates to a pharmaceutical composition or a functional health food comprising a verbenone derivative and pharmaceutically acceptable salts thereof as active ingredients for treating or preventing a neurodegenerative disease. More specifically, the verbenone derivative according to the present invention reduces neuronal cell death and oxidative stress, and is highly effective in preventing ischemic brain damage and inflammatory cell migration in rats, thereby providing the pharmaceutical composition or the functional health food which is useful in treating neurodegenerative diseases.

15-Oxospiramilactone Derivatives, Preparation Method and Uses Thereof

The invention relates to a derivative of 15-oxospiramilacton, particularly to a compound of Formula I or II, or an isomer, a solvate or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the compound as pharmaceutically active ingredient, a method for preparing the same, and use thereof in manufacture of an anti-tumor agent. The derivative of 15-oxospiramilactone of the invention have an activity against multiple tumor cell lines, and the anti-tumor activity is positively correlated to an activity inhibiting the Wnt signaling pathway.

Inhibitors of beta-secretase

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates.

INHIBITORS OF BETA-SECRETASE

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. 113-. (canceled)15. The method of claim 14 , wherein the BACE1 mediated disorder or disease is selected from the group consisting of neurodegenerative disorder claim 14 , cognitive decline claim 14 , cognitive impairment claim 14 , dementia and disease characterized by the production of β-amyloid deposits or neurofibrillary tangles.16. The method of claim 15 , wherein the disorder or disease is selected from the group consisting of Alzheimer's disease claim 15 , Trisomy 21 (Down Syndrome) claim 15 , Hereditary Cerebral Hemorrhage with Amyloidosis of the Dutch-type (HCHWA-D) claim 15 , senile dementia claim 15 , cerebral amyloid angiopathy claim 15 , degenerative dementia claim 15 , dementias of mixed vascular and degenerative origin claim 15 , dementia associated with Parkinson's disease claim 15 , dementia associated with progressive supranuclear palsy claim 15 , dementia associated with cortical basal degeneration claim 15 , diffuse Lewy body type of Alzheimer's disease claim 15 , dry age related macular degeneration (AMD) claim 15 , and glaucoma.1718-. (canceled) This application is a continuation of U.S. application Ser. No. 14/011,183, filed Aug. 27, 2013, which claims the benefit of U.S. Provisional Application Ser. No. 61/693,512, filed Aug. 27, 2012, U.S. Provisional Application Ser. No. 61/788,839, filed Mar. 15, 2013, and U.S. Provisional Application Ser. No. 61/816,458, filed Apr. 26, 2013. The entire teachings of each of the above applications are incorporated herein by reference.The instant application contains a Sequence Listing which ...

ANTICANCER AGENTS AND PROCESS OF MAKING THEREOF

Provided herein are compositions and processes of making of anticancer compounds useful for cancer treatments. These cyclohexenone compounds show an unexpected result against certain cancer cells compared to their known analogs. 3. The compound of claim 1 , wherein R is a hydrogen claim 1 , C(═O)CH claim 1 , C(═O)CH claim 1 , or C(═O)CH.4. The compound of claim 1 , wherein each of R claim 1 , Rand Rindependently is hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl claim 1 , hexyl claim 1 , or heptyl.5. The compound of claim 1 , wherein each of Rand Rindependently is (CHCH═C(CH)(CH))—R.6. The compound of claim 5 , wherein Ris H claim 5 , NH claim 5 , NHCH claim 5 , N(CH) claim 5 , OCH claim 5 , OCH claim 5 , C(═O)CH claim 5 , C(═O)CH claim 5 , C(═O)OCH claim 5 , C(═O)OCH claim 5 , C(═O)NHCH claim 5 , C(═O)NHCH claim 5 , C(═O)NH claim 5 , OC(═O)CH claim 5 , OC(═O)CH claim 5 , OC(═O)OCH claim 5 , OC(═O)OCH claim 5 , OC(═O)NHCH claim 5 , OC(═O)NHCH claim 5 , or OC(═O)NH.7. The compound of claim 5 , wherein Ris CHC(CH)OH claim 5 , CHC(CH)OCH claim 5 , CHCOOH claim 5 , CHCOOH claim 5 , CHOH claim 5 , CHOH claim 5 , CHPh claim 5 , CHPh claim 5 , CHCH═C(CH)(CHO) claim 5 , CHCH═C(CH)(C(═O)CH) claim 5 , 5 or 6-membered lactone claim 5 , aryl claim 5 , or glucosyl claim 5 , wherein 5 or 6-membered lactone claim 5 , aryl claim 5 , and glucosyl are optionally substituted with one or more substituents selected from NRR claim 5 , OR claim 5 , OC(═O)R claim 5 , C(═O)OR claim 5 , C(═O)R claim 5 , C(═O)NRR claim 5 , C-Calkyl claim 5 , C-Calkenyl claim 5 , C-Calkynyl claim 5 , C-Ccycloalkyl claim 5 , and C-Chaloalkyl.8. The compound of claim 7 , wherein Ris C—C alkyl optionally substituted with one or more substituents selected from NRR claim 7 , OR claim 7 , OC(═O)R claim 7 , C(═O)OR claim 7 , C(═O)R claim 7 , C(═O)NRR claim 7 , C-Calkyl claim 7 , C-Calkenyl claim 7 , C-Calkynyl claim 7 , C-Ccycloalkyl claim 7 , and C-Chaloalkyl.9. The ...

Novel synthesis routes for prostaglandins and prostaglandin intermediates using metathesis

Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.

ANTAGONISTS OF THE TOLL-LIKE RECEPTOR 1/2 COMPLEX

Provided are compounds, compositions and methods for treating Toll-like receptor 1/2 complex (TLRI/2) related inflammatory disorders. Small molecules, based on the benzotropolone scaffold, capable of influencing downstream signaling are disclosed as well as methods of making and modifying these molecules. Also provided are methods for treating a subject for a clinical condition associated with Toll-like receptor complex 1/2 activation, comprising administering to the subject an effective amount of a benzotropolone compound. 2. The compound of claim 1 , wherein n is 5 claim 1 , 7 claim 1 , or 9.12. A pharmaceutical composition comprising a compound of claim 1 , or a salt thereof claim 1 , and a pharmaceutically acceptable excipient.13. A method for treating a clinical condition associated with signaling mediated by TLR1/2 comprising administering to a subject in need of such a treatment a therapeutically effective amount of a compound of .14. The method of claim 13 , wherein the clinical condition is a chronic inflammatory disease or an acute inflammatory disease.15. The method of claim 14 , wherein the chronic inflammatory disease or the acute inflammatory disease is atopic dermatitis claim 14 , psoriasis claim 14 , acne vulgaris or sepsis.16. The method of claim 14 , wherein the chronic inflammatory disease or the acute inflammatory disease is caused by human cytomegalovirus claim 14 , lymphocytic choriomeningitis virus claim 14 , or herpes simplex virus 1.17. The method of claim 13 , wherein the clinical condition is pulmonary tumor metastasis. This invention was made with government support under grant numbers DA026950, DA025740 and NS067425 awarded by the National Institutes of Health. The U.S. government has certain rights in the invention.Embodiments herein report compositions, methods, and uses for treating Toll-like receptor 1/2 complex (TLR1/2) related immune disorders. Some embodiments of the present invention provide small molecules capable of ...

Processes for the preparation of hydroxylated cyclohexyl compounds

The present application relates to processes for the preparation of polyhydroxylated cyclohexyl compounds such as the compounds of Formula I:

1,3-DI-OXO-INDENE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT OR OPTICAL ISOMER THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ANTIVIRAL, ACTIVE INGREDIENT

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hapatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, cold, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media. 3. The 1 claim 1 ,3-Dioxoindene derivatives as set forth in claim 1 , pharmaceutically-acceptable salt thereof or optical isomer thereof claim 1 , wherein claim 1 , A claim 1 , A claim 1 , Aand Aare claim 1 , either independently or optionally claim 1 , any one selected from a group consisting of —H claim 1 , halogen and —NRR;{'sup': 1', '2', '1', '2, 'G is —OH, —NR(C═O)Ror —NR(C═O)OR;'}{'sup': 1', '2', '3', '4', '1', '2, 'sub': 1', '10, 'D, D, Dand Dare, either independently or optionally, any one selected from a group consisting of halogen, C˜Cstraight- or side-chain alkyl and —NR(C═O)R;'}{'sup': 1', '1', '1', '1', '2, 'E is —H, —OH, —OR, —O(C═O)R, —O(C═O)ORor —O(C═O)NRR;'}{'sup': 1', '2', '3, 'sub': 1', '8', '1', '4', '6', '10, 'R, Rand Rare, each independently, hydrogen, nonsubstituted or phenyl-substituted C˜Cstraight- or side-chain alkyl, nonsubstituted or phenyl-substituted C˜Cstraight- or side-chain alkenyl or C˜Caryl;'}X and Y are oxygen;{'sup': 1', '2', '3, 'Z, Zand Zare carbon;'}n is integer between 1˜3; and{'img': {'@id': 'CUSTOM- ...

TETRAHYDRO-ISOHUMULONE DERIVATIVES, METHODS OF MAKING AND USING

The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPARγ, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPARγ modulation such as diabetes. 1. A method of inhibiting inflammation or treating a condition associated with inflammation in a subject in need thereof comprising administering a therapeutically effective amount of a tetrahydro-iso-alpha acid (THIAA) derivative selected from the group consisting of(4R,5R)-3,4-dihydroxy-4-(1-hydroxy-4-methylpentyl)-2-(N-methoxy-3-methylbutanimidoyl)-5-(3-methylbutyl)cyclopent-2-en-1-one (KDT0005), (4R,5R)-4-hydroxy-2-{1-[(2-hydroxyethyl)amino]-3-methylbutylidene}-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopentane-1,3-dione (KDT0017), (4R,5R)-4-hydroxy-5-[3-methylbutyl)-2-methyl-1-(methylamino)butylidene]-4-(4-methylpentanoyl)cyclopentane-1,3-dione (KDT0020), (4R,5R)-2-[1-(benzylamino)-3-methylbutylidene]-4-hydroxy-5-(3-methylbutyl)-4-(4-methylpentanoyl)cyclopentane-1,3-dione (KDT0024), (1S,5R)-2-hydroxy-3-(3-methylbutanoyl)-5-(3-methylbutyl)-1-(4-methylpentanoyl)-4-oxocyclopent-2-en-1-yl 2,2-dimethylpropanoate (KDT0033), (1S,5R)-2-hydroxy-3-(3-methylbutanoyl)-5-(3-methylbutyl)-1-(4-methylpentanoyl)-4-oxocyclopent-2-en-1-yl 3,3-dimethylbutanoate (KDT0034), but-3-yn-1-yl (1S,5R)-2-hydroxy-3-(3-methylbutanoyl)-5-(3-methylbutyl)-1-(4-methylpentanoyl)-4-oxocyclopent-2-en-1-yl carbonate (KDT0035), (1S,5R)-2-hydroxy-5-(3-methylbutyl)-1-(4-methylpentanoyl)-3-(2-methylpropanoyl)-4-oxocyclopent-2-en-1-yl decanoate (KDT0036), (1S,5R)-2-hydroxy-5-(3-methylbutyl)-1-(4-methylpentanoyl)-3-(2-methylpropanoyl)-4-oxocyclopent-2-en-1-yl 2-methylpropyl carbonate (KDT0037), 5-[(1S,5R)-1,2-dihydroxy-3-(3-methylbutanoyl)-5-(3-methylbutyl)-4-oxocyclopent-2-en-1-yl]-2- ...

SYNTHESIS OF DELTA 12-PGJ3 AND RELATED COMPOUNDS

In one aspect, the present invention provides novel derivatives of Δ-PGJand modular synthetic pathways to obtaining Δ-PGJand derivatives thereof. In some aspects, the present derivatives of Δ-PGJare useful as chemotherapeutic agents. The present disclosure also describes compositions of these derivatives as well as methods of use of the derivatives thereof. 46.-. (canceled)7. The compound of claim 1 , wherein Yis O.8. The compound of claim 1 , wherein Yis N—OH or N—OMe.9. The compound of claim 8 , wherein Yis N—OMe.1095.-. (canceled)97. The compound of claim 96 , wherein Ais alkenediyl.98. (canceled)99. The compound of claim 96 , wherein z is 1 claim 96 , 2 claim 96 , 3 claim 96 , or 4.100101.-. (canceled)102. The compound of claim 96 , wherein Xis O.103. The compound of claim 96 , wherein Xis alkenyl.104. (canceled)107. A pharmaceutical composition comprising a compound of and an excipient.108. (canceled)109. The pharmaceutical composition of claim 107 , wherein the composition is formulated for oral claim 107 , topical claim 107 , intraarterial claim 107 , intraperitoneal claim 107 , or intravenous administration.110114-. (canceled)115. A method of treating a disease or disorder in a patient in need thereof comprising administering to the patient a pharmaceutically effective amount of a compound or composition of or a pharmaceutically acceptable salt or optical isomer thereof.116. The method of claim 115 , wherein the disease is cancer.117118.-. (canceled)119. The method of claim 116 , wherein the cancer is leukemia.120130.-. (canceled)132293.-. (canceled)295434.-. (canceled) This application claims the benefit of U.S. Provisional Application 61/882,093, filed on Sep. 25, 2013, U.S. Provisional Application 61/897,681, filed on Oct. 30, 2013, U.S. Provisional Application 61/920,302, filed on Dec. 23, 2013, U.S. Provisional Application 61/954,295, filed on Mar. 17, 2014, and U.S. Provisional Application 61/979,276, filed on Apr. 14, 2014, the entire contents of each ...

POLYPRENYLATED PHLOROGLUCINOL COMPOUNDS AS POTENT P-GLYCOPROTEIN INDUCERS

The present invention relates to the polyprenylated phloroglucinol compounds of formulae I and II. The present invention also provides synthesis and p-glycoprotein induction activity of the alkyl- and acyl-polyprenylated phloroglucinol compounds. Further, use of the compounds as p-glycoprotein inducers and methods of treatment of Alzheimer's disease using compounds of the invention are also provided. 2. The compound as claimed in claim 1 , wherein the substitution on the alkyl or the acyl group is at one or more positions and selected from the group comprising of chloro claim 1 , fluoro claim 1 , iodo claim 1 , and nitro.3. The compound as claimed in wherein the benzyl group is selected from the group comprising of 2-iodo benzyl claim 1 , 2-chloro claim 1 , 6-fluoro benzyl claim 1 , 2 claim 1 ,6-dichloro benzyl claim 1 , 4-chloro benzyl claim 1 , 2-nitro benzyl claim 1 , and 3-nitro benzyl.5. A process for the preparation of the compounds of formula I and II as claimed in claim 1 , comprising the steps of—(i) reacting garcinol or isogarcinol with alkyl or acyl halide in presence of a base in a solvent at a temperature ranging between 0 to 35° C. for a period of time between 0 to 60 minutes to obtain a crude mixture; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(ii) optionally purifying the crude mixture column chromatography using an eluent to obtain the compounds of .'}6. The process as claimed in wherein the alkyl halide is selected from group comprising of methyl halide claim 5 , ethyl halide claim 5 , propyl halide claim 5 , isopropyl halide claim 5 , n-butyl halide claim 5 , isobutyl halide claim 5 , isovaleryl halide claim 5 , propargyl halide claim 5 , allyl halide claim 5 , prenyl halide claim 5 , geranyl halide claim 5 , and halides of other long aliphatic chains with chain length from C-C claim 5 , and acyl halide is selected from the group comprising of acetyl halide claim 5 , benzyl halide claim 5 , benzoyl halide and butanoyl halide.7. The ...

HERBICIDALLY ACTIVE CYCLIC DIONE COMPOUNDS, OR DERIVATIVES THEREFOR, SUBSTITUTED BY A PHENYL WHICH HAS AN ALKYNYL-CONTAINING SUBSTITUENT

The present invention relates to a compound of formula (I), wherein: X is methyl or chlorine; Ris methyl or chlorine; Ris hydrogen, methyl, ethyl, n-propyl, cyclopropyl, vinyl, ethynyl, fluorine, chlorine, bromine, C-Calkoxy, C-C-fluoroalkoxy, C-Calkoxy-C-Calkoxy- or Cfluoroalkoxy-C-Calkoxy-; and Y is O, S, S(O), S(O), N(C-Calkyl), N(C-Calkoxy), C(O), CRRor —CRRCRR—; and G, R, R, Rand Rare as defined herein; wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. 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 plants or to the locus thereof. 2. The compound as claimed in 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 claim 1 , wherein X claim 1 , R claim 1 , X claim 1 , Xand Rare as defined herein.3. (canceled)4. (canceled)5. The compound as claimed in claim 1 , wherein X is methyl.6. The compound as claimed in claim 1 , wherein X is chlorine.7. The compound as claimed in claim 1 , wherein Ris methyl.8. The compound as claimed in claim 1 , wherein Ris chlorine.9. The compound as claimed in claim 1 , wherein X is methyl claim 1 , and Ris methyl.10. The compound as claimed in claim 1 , wherein X is methyl claim 1 , and Ris chlorine.11. (canceled)12. (canceled)13. (canceled)14. The compound as claimed in claim 1 , wherein Ris methyl or methoxy.15. (canceled)16. (canceled)17. (canceled)18. The compound as claimed in claim 1 , wherein:{'sup': 1', '2, 'Ris chlorine, and Ris methoxy.'}19. (canceled)20. The compound as claimed in claim 1 , wherein R claim 1 , R claim 1 , Rand R claim 1 , independently of each other claim 1 , are hydrogen or C-Calkyl;{'sup': 4 ...

Clostrubins

The present invention relates to a bioactive compound according to general formula (I); to a pharmaceutical composition comprising one or more of the compound(s); and to the use of the compound(s) as an antibiotic, cytotoxic and/or anti—proliferative agent.

KETONE OR OXIME COMPOUND, AND HERBICIDE

There is provided novel agricultural chemicals, in particular herbicides. A ketone or oxime compound or a salt thereof of Formula (1): 3. The ketone compound or the salt thereof according to claim 2 , wherein Q is an oxygen atom.4. The oxime compound or a salt thereof according to claim 2 , wherein Q is ═NOR.5. The ketone compound or the salt thereof according to claim 3 , wherein A is a hydrogen atom claim 3 , Calkyl claim 3 , or —C(O)R;{'sup': '2', 'sub': '1-s', 'Ris Calkyl;'}{'sup': 6', '15', '16', '17', '1, 'sub': 1-6', '1-6', '3-8', '2-6', 'q1, 'Ris Calkyl, (C) alkyl arbitrarily substituted with R, Ccycloalkyl, Calkenyl, —C(═NOR)R, phenyl, phenyl substituted with (Z), or D1-32;'}{'sup': 8a', '16a', '17a, 'sub': '1-6', 'Ris a hydrogen atom, Calkyl, —C(O)OR, or —C(O)R;'}{'sup': '9a', 'sub': '1-6', 'Ris a hydrogen atom or Calkyl;'}{'sup': 8b', '9b, 'Rand Rare hydrogen atoms;'}{'sup': 10', '11', '12, 'R, R, and Rare hydrogen atoms;'}{'sup': 15', '16, 'sub': '3-8', 'Ris a halogen atom, Ccycloalkyl, —OR, or phenyl;'}{'sup': 16', '16a', '17', '17a, 'sub': '1-6', 'R, R, R, and Rare each independently Calkyl;'}{'sup': '1', 'sub': '1-6', 'Xis halo (C) alkyl;'}{'sup': a', 'c', 'e', '45', '41', '3, 'sub': 1-6', '3-8', '2-6', '2-6', '2-6', 'q3, 'Z, Zand Zare each independently a hydrogen atom, a halogen atom, Calkyl, Ccycloalkyl, Calkenyl, (C) alkenyl arbitrarily substituted with R, Calkynyl, —OR, phenyl, phenyl substituted with (Z), D1-7, D1-11, D1-22, D1-32, or D1-37;'}{'sup': '1', 'Zis a halogen atom;'}{'sup': '3', 'sub': 1-6', '1-6', '1-6', '1-6', '1-6, 'Zis a halogen atom, Calkyl, halo (C) alkyl, Calkoxy, halo (C) alkoxy, or Calkylthio;'}{'sup': 41', '45, 'sub': 1-6', '1-6, 'Ris Calkyl, (C) alkyl arbitrarily substituted with R, phenyl, D1-32, or D1-34;'}{'sup': '45', 'Ris a halogen atom, phenyl, or D1-34;'}g2, g3, and p are 0;q1 and q3 are integers of 1; andg4, m, and n are each independently an integer of 0 or 1.6. The ketone compound or the salt thereof according to ...

INHIBITORS OF BETA-SECRETASE

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid aggregates. 1. A compound having the following structure:or a pharmaceutically acceptable salt thereof. This application is a continuation of U.S. patent application Ser. No. 15/383,287, filed on Dec. 19, 2016, which is a continuation of U.S. patent application Ser. No. 14/613,550, filed on Feb. 4, 2015, now U.S. Pat. No. 9,526,727, which is a continuation of U.S. patent application Ser. No. 13/784,032, filed Mar. 4, 2013, now U.S. Pat. No. 8,981,112, which, in turn, claims the benefit of U.S. Provisional Application Ser. No. 61/606,786, filed Mar. 5, 2012; the entire contents of each of the aforementioned applications are incorporated herein by reference.The instant application contains a Sequence Listing which has been submitted in ASCII format via EFS-Web and is hereby incorporated by reference in its entirety. Said ASCII copy, created on Mar. 4, 2013, is named 15161953.txt and is 718 bytes in size.The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the β-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of β-amyloid deposits or neurofibrillary tangles.β-Amyloid (also referred to herein as “Abeta” or “Aβ”) deposits and neurofibrillary tangles are two major pathologic characterizations associated with Alzheimer's disease (AD), including the genetically linked early onset ...

Fluorene compounds

New fluorene derivatives and new methods for forming fluorene derivatives are disclosed. Examples include processes for preparing tert-butyl substituted fluorenes, 1-methyl fluorene, and 4-methyl fluorene.

Vinly-substituted bridged metallocenes

A method is provided for forming a supported cyclopentadiene-type compound comprising contacting a cyclopentadiene-type compound containing an active halogen with an inorganic support having surface hydroxyl group. Also there is provided a method of preparing a supported metallocene comprising reacting the supported cyclopentadiene-type compound with a transition metal compound under suitable conditions. There is also provided a process for producing bridged cyclopentadiene-type ligands having a bridge having branch that has a terminal vinyl group. Also metallocenes of these ligands are provided. Still further there is provided a process for producing bridged cyclopentadiene-type ligands having a bridge having a branch that has a terminal active halogen. The resulting new ligands and supported metallocenes produced therefrom are also provided. There is further provided supported metallocene catalysts wherein at least two metallocenes of differing effectiveness are both bonded to an inorganic support having surface hydroxy groups. Olefin polymerization employing the inventive bridged supported metallocenes is also provided, as well the resulting polymer products.

Process of polymerizing olefins using diphenylsilyl or dimethyl tin bridged 1-methyl fluorenyl metallocenes

Group IVB metal metallocenes of bis(1-methyl fluorenyl) diphenyl silane and bis(1-methyl fluorenyl) dimethyl tin are disclosed, plus their use in the production of polyolefins, including isotactic polypropylene.

Fulvene, metallocene catalysts and preparation method thereof, and preparation of polyolefines copolymer using the same

The present invention relates to a novel fulvene compound and a preparation method thereof, and more particularly to a fulvene compound having substituted groups in the 2- and 5-positions, prepared from an unsaturated ketone having a substituted group in the β- position and a halogen atom in the α-position, and a preparation method thereof. The present invention also relates to a metallocene catalyst having a substituted group in the α-position carbon of the bridge of the cyclopentadienyl group only by reaction of a fulvene compound and an anion group including the cyclopentadienyl group, and a preparation method of a polyolefin copolymer using the same.

Organometallic fluorenyl compounds and use thereof in an alpha-olefin polymerization process

Fluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Metallocenes and processes therefor and therewith

A method is provided for forming a supported cyclopentadiene-type compound comprising contacting a cyclopentadiene-type compound containing an active halogen with an inorganic support having surface hydroxyl group. Also there is provided a method of preparing a supported metallocene comprising reacting the supported cyclopentadiene-type compound with a transition metal compound under suitable conditions. There is also provided a process for producing bridged cyclopentadiene-type ligands having a bridge having branch that has a terminal vinyl group. Also metallocenes of these ligands are provided. Still further there is provided a process for producing bridged cyclopentadiene-type ligands having a bridge having a branch that has a terminal active halogen. The resulting new ligands and supported metallocenes produced therefrom are also provided. There is further provided supported metallocene catalysts wherein at least two metallocenes of differing effectiveness are both bonded to an inorganic support having surface hydroxy groups. Olefin polymerization employing the inventive bridged supported metallocenes is also provided, as well the resulting polymer products.

C2-phenyl-substituted cyclic keto-enols used as pesticides and herbicides

The present invention relates to novel C 2 -phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.

4-phenyl-pyrane-3,5-diones, 4-phenyl-thiopyrane-3,5-diones and cyclohexanetriones as novel herbicides

Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.

Herbicidally active bicyclic 1,3-dione compounds

Bicyclic dione compounds of formule (I), and derivatives thereof, which are suitable for use as herbicides.

Organometallic fluorenyl compounds, preparation and use

Fluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Metallocenes and processes therefor and therewith

A method is provided for forming a supported cyclopentadiene-type compound comprising contacting a cyclopentadiene-type compound containing an active halogen with an inorganic support having surface hydroxyl group. Also there is provided a method of preparing a supported metallocene comprising reacting the supported cyclopentadiene-type compound with a transition metal compound under suitable conditions. There is also provided a process for producing bridged cyclopentadiene-type ligands having a bridge having branch that has a terminal vinyl group. Also metallocenes of these ligands are provided. Still further there is provided a process for producing bridged cyclopentadiene-type ligands having a bridge having a branch that has a terminal active halogen. The resulting new ligands and supported metallocenes produced therefrom are also provided. There is further provided supported metallocene catalysts wherein at least two metallocenes of differing effectiveness are both bonded to an inorganic support having surface hydroxy groups. Olefin polymerization employing the inventive bridged supported metallocenes is also provided, as well the resulting polymer products.

Metallocenes and processes therefor and therewith

A method is provided for forming a supported cyclopentadiene-type compound comprising contacting a cyclopentadiene-type compound containing an active halogen with an inorganic support having surface hydroxyl group. Also there is provided a method of preparing a supported metallocene comprising reacting the supported cyclopentadiene-type compound with a transition metal compound under suitable conditions. There is also provided a process for producing bridged cyclopentadiene-type ligands having a bridge having branch that has a terminal vinyl group. Also metallocenes of these ligands are provided. Still further there is provided a process for producing bridged cyclopentadiene-type ligands having a bridge having a branch that has a terminal active halogen. The resulting new ligands and supported metallocenes produced therefrom are also provided. There is further provided supported metallocene catalysts wherein at least two metallocenes of differing effectiveness are both bonded to an inorganic support having surface hydroxy groups. Olefin polymerization employing the inventive bridged supported metallocenes is also provided, as well the resulting polymer products.

Metallocenes and processes therefor and therewith

A method is provided for forming a supported cyclopentadiene-type compound comprising contacting a cyclopentadiene-type compound containing an active halogen with an inorganic support having surface hydroxyl group. Also there is provided a method of preparing a supported metallocene comprising reacting the supported cyclopentadiene-type compound with a transition metal compound under suitable conditions. There is also provided a process for producing bridged cyclopentadiene-type ligands having a bridge having branch that has a terminal vinyl group. Also metallocenes of these ligands are provided. Still further there is provided a process for producing bridged cyclopentadiene-type ligands having a bridge having a branch that has a terminal active halogen. The resulting new ligands and supported metallocenes produced therefrom are also provided. There is further provided supported metallocene catalysts wherein at least two metallocenes of differing effectiveness are both bonded to an inorganic support having surface hydroxy groups. Olefin polymerization employing the inventive bridged supported metallocenes is also provided, as well the resulting polymer products.

Metallocenes and processes therefor and therewith

A method is provided for forming a supported cyclopentadiene-type compound comprising contacting a cyclopentadiene-type compound containing an active halogen with an inorganic support having surface hydroxyl group. Also there is provided a method of preparing a supported metallocene comprising reacting the supported cyclopentadiene-type compound with a transition metal compound under suitable conditions. There is also provided a process for producing bridged cyclopentadiene-type ligands having a bridge having branch that has a terminal vinyl group. Also metallocenes of these ligands are provided. Still further there is provided a process for producing bridged cyclopentadiene-type ligands having a bridge having a branch that has a terminal active halogen. The resulting new ligands and supported metallocenes produced therefrom are also provided. There is further provided supported metallocene catalysts wherein at least two metallocenes of differing effectiveness are both bonded to an inorganic support having surface hydroxy groups. Olefin polymerization employing the inventive bridged supported metallocenes is also provided, as well the resulting polymer products.

Cyclopentadiene type compounds and method for making

New fluorenyl silane compounds and method for their production are disclosed. The fluorenyl compounds have the formula ##STR1## wherein Z is a substituted or unsubstituted fluorenyl radical and Z' is a substituted or unsubstituted cyclopentadienyl-type radical or a halogen.

Olefin polymerization using silyl-bridged metallocenes

Fluorenyl-containing silyl bridged metallocenes, the process of using such metallocenes to polymerize olefins, and the resulting unusual syndiotactic polypropylene are disclosed.

Organometallic fluorenyl compounds, preparation, and use

Bridged fluorenyl-containing metallocenes of metals of Groups 4-6 and their use in forming homopolymers of alpha olefins or polymers of ethylene and optionally minor amounts of alpha olefins, wherein in each case at least one of the cyclic groups of the bridged ligand is a fluorenyl and the other is selected from indenyl, tetrahydroindenyl, fluorenyl, and in the case of the polymerization of ethylene optionally cyclopentadienyl.

Bis fluorenyl metallocenes and use thereof

Group IVB metal metallocenes of bis(1-methyl fluorenyl) diphenyl silane and bis(1-methyl fluorenyl) dimethyl tin are disclosed, plus their use in the production of polyolefins, including isotactic polypropylene.

Organometallic fluorenyl compounds, preparations, and use

Fluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Organometallic fluorenyl compounds, preparation, and use

Bridged and unbridged fluorenyl-containing metallocenes of the formula R″ x (FlR n )(CpR m )MQ k wherein Fl is a fluorenyl radical, Cp is a cyclopentadienyl, indenyl, tetrahydroindenyl, or fluorenyl radical, each R is an organo radical, R″ is a structural bridge linking (FlR n ) and (CpR m ), M is a metal selected from the group consisting of IVB, VB, and VIB metals, each Q is selected from the group consisting of hydrocarbyl or hydrocarbyloxy radicals and halogen, x is 1 or 0, k is an integer sufficient to fill out the remaining valences of M, n is in the range of 0 to 7, and m is 0 to 7, further characterized by the fact that if (CpR m ) is unsubstituted fluorenyl and metallocene is an unbridged metallocene, then n is 1 to 7 and if R″ is 1,1-dimethylmethylene and (CpR m ) is unsubstituted cyclopentadienyl or 3-methylcyclopentadienyl, then n is 1 to 7.

Organometallic Fluorenyl Compounds, Preparations, and Use

Fluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Syndiotactic polypropylene prepared using silyl bridged metallocenes

Fluorenyl-containing silyl bridged metallocenes, the process of using such metallocenes to polymerize olefins, and the resulting unusual syndiotactic polypropylene are disclosed.

Organometallic fluorenyl compounds and use thereof in olefin polymerization

Unbridged fluorenyl containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Metallocenes and processes therefor and therewith

Cyclopentadiene type compounds and method for making

Processes are disclosed for preparing compounds of the formula Z-R-Z where each Z can be selected from cyclopentadienyl type radicals such as substituted or unsubstituted cyclopentadienyl, indenyl, fluorenyl or tetrahydroindenyl or where one Z is Cl, Br, or I by reacting specific Z precursors with a dihaloalkylene compound. Also new cyclopentadienyl-type compounds are disclosed.

New tert.-butyl-fluorene cpds. - useful as antiviral and fluorenyl-metallocene intermediates and as polyamide and polyurea monomers

1-, 2- or 4-tert.butyl-fluorenes (I) are new. USE - (I) are intermediates for antiviral drugs and fluorenylmetallocene catalysts as well as monomers for the mfr. of polyamides and polyureas. In an example, AlMe3 (4.6 ml.) was added to a suspension of 1-carboxyfluorene (III) (2 g.) in toluene and the mixt. was refluxed, cooled and added to dil. HCl. The organic phase was washed, dried and evaporated to give after extn. (pentane), silica gel purificn. and evapn., 1-tert.butyl-fluorene (I) in quantitative yield.

Cyclopentadiene type compounds and method for making

Processes are disclosed for preparing compounds of the formula Z--R--Z where each Z can be selected from cyclopentadienyl type radicals such as substituted or unsubstituted cyclopentadienyl, indenyl, fluorenyl or tetrahydroindenyl or where one Z is Cl, Br, or I by reacting specific Z precursors with a dihaloalkylene compound. Also new cyclopentadienyl-type compounds are disclosed.

Method for producing fluorenyl-containing metallocene

Organometallic fluorenyl compounds, preparation, and use

Benzofluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Cyclopetadiene type compounds and method for making

Processes are disclosed for preparing compounds of the formula Z-R-Z where each Z can be selected from cyclopentadienyl type radicals such as substituted or unsubstituted cyclopentadienyl, indenyl, fluorenyl or tetrahydroindenyl or where one Z is Cl, Br, or I by reacting specific Z precursors with a dihaloalkylene compound. Also new cyclopentadienyl-type compounds are disclosed.

Metallocenes and processes therefor and therewith

A method is provided for forming a supported cyclopentadiene-type compound comprising contacting a cyclopentadiene-type compound containing an active halogen with an inorganic support having surface hydroxyl group. Also there is provided a method of preparing a supported metallocene comprising reacting the supported cyclopentadiene-type compound with a transition metal compound under suitable conditions. There is also provided a process for producing bridged cyclopentadiene-type ligands having a bridge having branch that has a terminal vinyl group. Also metallocenes of these ligands are provided. Still further there is provided a process for producing bridged cyclopentadiene-type ligands having a bridge having a branch that has a terminal active halogen. The resulting new ligands and supported metallocenes produced therefrom are also provided. There is further provided supported metallocene catalysts wherein at least two metallocenes of differing effectiveness are both bonded to an inorganic support having surface hydroxy groups. Olefin polymerization employing the inventive bridged supported metallocenes is also provided, as well the resulting polymer products.

Metallocenes and processes therefor and therewith

METALOCENOS AND PROCEDURES FOR THEIR PREPARATION AND USE.

SE SUMINISTRA UN METODO PARA FORMAR UN COMPUESTO DE TIPO DEL CICLOPENTADIENO SOPORTADO QUE COMPRENDE LA PUESTA EN CONTACTO DE UN COMPUESTO DEL TIPO DE CICLOPENTADIENO QUE COMPRENDA UN HALOGENO ACTIVO CON UN SOPORTE INORGANICO QUE TENGA UN GRUPO DE HIDROXIL SUPERFICIAL. TAMBIEN SE SUMINISTRA UN METODO PARA PREPARAR UN METALOCENO SOPORTADO QUE COMPRENDE LA REACCION DEL COMPUESTO DEL TIPO DEL CICLOPENTADIENO SOPORTADO CON UN COMPUESTO DE UN METAL DE TRANSICION BAJO CONDICIONES ADECUADAS. TAMBIEN SE SUMINISTRA UN PROCESO PARA PRODUCIR LIGANTES DEL TIPO DEL CICLOPENTADIENO PUENTEADO QUE TENGAN UN PUENTE QUE TENGA UNA RAMA QUE SEA UN GRUPO DE VINIL TERMINAL. TAMBIEN SE SUMINISTRAN METALOCENOS DE ESTOS LIGANTES. AUN MAS SE SUMINISTRA UN PROCESO PARA PRODUCIR LIGANTES DEL CICLOPENTADIENO PUENTEADO QUE TENGA UN PUENTE QUE TENGA UNA RAMA QUE TENGA UN HALOGENO ACTIVO TERMINAL. TAMBIEN SE SUMINISTRAN LOS NUEVOS LIGANTES RESULTANTES Y NUEVOS METALOCENOS SOPORTADOS PRODUCIDOS MEDIANTE ESTE METODO. ADEMASSE SUMINISTRAN CATALIZADORES DE METALOCENO SOPORTADO EN LOS QUE AL MENOS DOS METALOCENOS DE EFECTIVIDAD DIFERENTE SE ENCUENTRAN UNIDOS ENTRE SI A UN SOPORTE INORGANICO QUE TENGA GRUPOS DE HIDROXIDO SUPERFICIAL. TAMBIEN SE SUMINISTRA UNA POLIMERIZACION DE OLEFINA QUE EMPLEA LOS METALOCENOS SOPORTADOS, PUENTEADOS DE LA INVENCION ASI COMO EL PRODUCTO DE POLIMERO RESULTANTE. A METHOD IS PROVIDED TO FORM A COMPOSITE TYPE OF THE SUPPORTED CYCLOPENTADIENE THAT INCLUDES THE SETTING IN CONTACT OF A CYCLOPENTADIEN TYPE COMPOSITE THAT INCLUDES AN ACTIVE HALOGEN WITH AN INorganic SUPPORT THAT HAS A SUPERX GROUP. A METHOD IS ALSO SUPPLIED TO PREPARE A SUPPORTED METALOCENE THAT UNDERSTANDS THE REACTION OF THE CYCLOPENTADIEN TYPE COMPOSITE SUPPORTED WITH A COMPOSITE OF A TRANSITION METAL UNDER ADEQUATE CONDITIONS. A PROCESS IS ALSO PROVIDED TO PRODUCE BINDERS OF THE TYPE OF BRIDGED CYCLOPENTADIEN THAT HAVE A BRIDGE THAT HAS A BRANCH THAT IS A TERMINAL VINYL GROUP. METALOCENOS OF THESE BINDERS ...

Metalloseeneja ja siihen liittyviä menetelmiä

Metallocenes and preparation methods thereof

활성 할로겐을 함유한 시클로펜타디엔-형 화합물을 표면 히드록실 기를 갖는 무기 지지체와 접촉시키는 것으로 구성되는 지지된 시클로펜타디엔-형 화합물 형성 방법이 제공된다. 또한 지지된 시클로펜타디엔-형 화합물을 적합한 조건하에 전이 금속 화합물과 반응시키는 것으로 구성되는 지지된 메탈로센 제조 방법이 제공된다. 또한 말단 비닐기를 갖는 분지를 갖는 가교를 갖는 가교된 시클로펜타디엔-형 리간드 생성 방법이 제공된다. 또한 상기 리단드의 메탈로센이 제공된다. 또한 부가로 말단 활성 할로겐을 갖는 분지를 갖는 가교를 갖는 가교된 시클로펜타디엔-형 리간드 생성방법이 제공된다. 결과얻어진 신규 리간드 및 그로부터 생성된 지지된 메탈로센이 또한 제공된다. 부가로 다른 효과를 갖는 적어도 두개의 메탈로센이 모두 표면 히드록시 기를 갖는 무기 지지체에 결합된 지지된 메탈로센 촉매가 제공된다. 발명의 가교된 지지된 메탈로센을 사용하는 올레핀 중합이 결과 얻어진 중합 생성물과 더불어 또한 제공된다. A method of forming a supported cyclopentadiene-type compound is provided which consists of contacting a cyclopentadiene-type compound containing an active halogen with an inorganic support having a surface hydroxyl group. Also provided is a method for preparing a supported metallocene, consisting of reacting a supported cyclopentadiene-type compound with a transition metal compound under suitable conditions. Also provided is a method of producing a crosslinked cyclopentadiene-type ligand having a crosslink having branches with terminal vinyl groups. Also provided are metallocenes of the reddide. Also provided is a method of producing a crosslinked cyclopentadiene-type ligand having a crosslink having branches with terminally active halogens. The resulting novel ligands and the supported metallocenes produced therefrom are also provided. In addition, a supported metallocene catalyst is provided in which at least two metallocenes with different effects are both bound to an inorganic support having surface hydroxy groups. Olefin polymerization using the crosslinked supported metallocene of the invention is also provided along with the resulting polymerization product.

Vinyl-substituted bridged metallocenes

Metallocenes, their production and use

Metallocener og fremgangsmåte til deres fremstilling og bruk

Det er tilveiebragt en fremgangsmåte til å danne en un- derstøttet syklopentadien-type forbindelse som omfatter å bringe en syklopentadien-type forbindelse som inneholder et aktivt halogen i berøring med en uorganisk understøt- telse som har overflatehydroksylgruppe. Det er også tilveiebragt en framgangsmåte til å fremstille et understøt- tet metallocen som omfatter å omsette den understøttede syklopentadien-type forbindelse med en overgangsmetall- forbindelse under egnede betingelser. Det er også tilveie- bragt en fremgangsmåte til å fremstille brosyklopentadien- type ligander som har en bro som har en gren som har en avsluttende vinylgruppe. Også metallocener av disse ligander er tilveiebragt. Enda ytterligere er det tilveiebragt en fremgangsmåte for å fremstille brosyklopentadien-type ligander som har en bro som har en gren som har et avsluttende aktivt halogen. De resulterende nye ligander og understøttede metallocener produsert derav er også tilveiebragt. Det er videre tilveiebragt understøttede metallocenkatalysatorer hvor minst to metallocener av forskjellig effektivitet begge er bundet til en uorganisk understøttelse som har overflatehydroksygrupper. Alken- polymerisasjon som benytter de understøttede brometal- locener er også tilveiebragt såvel som de resulterende polymerprodukter.

Processos para preparação de compostos do tipo ciclopentadieno suportado e ciclopentadienila com ponte, processo para preparação de um metaloceno e processo para polimerização de uma olefina

[UNK]

Fulvene, metallocene catalysts and preparation method thereof, and preparation of polyolefines copolymer using the same

The present invention relates to a novel fulvene compound and a preparation method thereof, and more particularly to a fulvene compound having substituted groups in the 2- and 5-positions, prepared from an unsaturated ketone having a substituted group in the β-position and a halogen atom in the α-position, and a preparation method thereof. The present invention also relates to a metallocene catalyst having a substituted group in the α-position carbon of the bridge of the cyclopentadienyl group only by reaction of a fulvene compound and an anion group including the cyclopentadienyl group, and a preparation method of a polyolefin copolymer using the same.

Fulvene, metallocene catalysts and preparation method thereof, and preparation of polyolefines copolymer using the same

The present invention relates to a novel fulvene compound and a preparation method thereof, and more particularly to a fulvene compound having substituted groups in the 2- and 5-positions, prepared from an unsaturated ketone having a substituted group in the β-position and a halogen atom in the α-position, and a preparation method thereof. The present invention also relates to a metallocene catalyst having a substituted group in the α-position carbon of the bridge of the cyclopentadienyl group only by reaction of a fulvene compound and an anion group including the cyclopentadienyl group, and a preparation method of a polyolefin copolymer using the same.

Fulvene, metallocene catalysts and preparation method thereof, and preparation of polyolefines copolymer using the same

The present invention relates to a novel fulvene compound and a preparation method thereof, and more particularly to a fulvene compound having substituted groups in the 2- and 5-positions, prepared from an unsaturated ketone having a substituted group in the β-position and a halogen atom in the α-position, and a preparation method thereof. The present invention also relates to a metallocene catalyst having a substituted group in the α-position carbon of the bridge of the cyclopentadienyl group only by reaction of a fulvene compound and an anion group including the cyclopentadienyl group, and a preparation method of a polyolefin copolymer using the same.

Fulvene, metallocene catalysts and preparation method thereof, and preparation of polyolefines copolymer using the same

The present invention relates to a novel fulvene compound and a preparation method thereof, and more particularly to a fulvene compound having substituted groups in the 2- and 5-positions, prepared from an unsaturated ketone having a substituted group in the β-position and a halogen atom in the α-position, and a preparation method thereof. The present invention also relates to a metallocene catalyst having a substituted group in the α-position carbon of the bridge of the cyclopentadienyl group only by reaction of a fulvene compound and an anion group including the cyclopentadienyl group, and a preparation method of a polyolefin copolymer using the same.

Organometallic fluorenyl compounds, preparation, and use

Fluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Organometallic fluorenyl compounds, preparation, and use

Benzofluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

COSMETIC LIGHT PROTECTION AGENTS FOR THE UV-A AREA

Patent FR2430938B1

NOVEL 3-BENZYLIDENE CAMPHOR DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS PROTECTIVE AGENTS AGAINST UV RAYS AND AS MEDICAMENTS

PHARMACEUTICAL COMPOSITIONS CONTAINING CAMPHO-METHYLIDENE CINNAMIC ACID DERIVATIVES

antioxidants

Die vorliegende Erfindung betrifft die Verwendung von Verbindungen der Formel I X-Ar-Y, wobei X und Y jeweils unabhängig voneinander ausgewählt sind aus den Resten H, C<SUB>1-8</SUB>-Alkyl und den Resten gemäß den Formeln Ia, Ib oder Ic, $F1 mit in der Beschreibung definierten sonstigen Resten, als Antioxidans, entsprechende neue Verbindungen und Zubereitungen sowie entsprechende Herstellverfahren für Verbindungen und Zubereitungen. The present invention relates to the use of compounds of the formula I X-Ar-Y, where X and Y are each independently selected from the radicals H, C <SUB> 1-8 </SUB> alkyl and the radicals according to the formulas Ia, Ib or Ic, $ F1 with other radicals defined in the description, as an antioxidant, corresponding new compounds and preparations and corresponding production processes for compounds and preparations.

Cosmetic light-stabilising agent for the UV-A region

Metallocener og fremgangsmåte til polymerisering av olefin

Benzofluorenyl-inneholdende metallocener beskrives sammen med fremgangsmåter for å lage disse metal- locenene. Det er også beskrevet fremgangsmåter for å anvende metallocenene som polymerisasjonskatalysa- torer. l tillegg beskrives polymerene som oppnås fra slike polymerisasjoner.

Fulbene, metallocene catalyst and method for producing the same, and method for producing polyolefin copolymer using the same

Fulvene, metallocene catalysts and preparation method thereof, and preparation of polyolefines copolymer using the same

Organometallic fluorenyl compounds, preparation, and use

Benzofluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Cyclopetadiene type compounds and method for making

Silyl bridged metallocenes and use thereof

Fluorenyl-containing silyl bridged metallocenes, the process of using such metallocenes to polymerize olefins, and the resulting unusual syndiotactic polypropylene are disclosed.

Benzofluorenylmetallocene and method of polymerization of olefins

Benzofluorenyl-containing metallocenes are disclosed along with methods for making the metallocenes. Also disclosed are methods for using the metallocenes as polymerization catalysts. In addition, polymers resulting from such polymerizations are disclosed.

Organometallic fluorenyl compounds, preparation, and use

Use of organometallic flurorenyl compounds.

Fluorenyl-inneholdende metallocener, fremgangsmåte for fremstilling derav og fremgangsmåte for polymerisering av olefiner ved anvendelse av metallocenene

Fluorenyl-inneholdende metallocener er beskrevet sammen med fremgangsmåter for å lage metallo- cenene. Det er også beskrevet fremgangsmåter for anvendelse av metallocenene som polymerisasjons- katalysatorer. I tillegg beskrives polymerer som oppnås fra slike polymerisasjoner.