子分类：
| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 81 | COMBINATIONS OF IRS/STAT3 DUAL MODULATORS AND ANTI-CANCER AGENTS FOR TREATING CANCER | PCT/IL2016/050134 | 2016-02-04 | WO2016125169A1 | 2016-08-11 | REUVENI, Hadas; HAVIV, Izhak; KUPERSHMIDT, Lana |
The present invention relates to the treatment of cancer using combination therapy comprising a dual modulator of Insulin Receptor Substrate (IRS) and signal transducer and activator of transcription 3 (Stat3), in combination with (i) a modulator of a protein kinase (PK) selected from an Epidermal Growth Factor inhibitor (EGFR inhibitor) and EGFR antibody; (ii) an inhibitor of mammalian target of rapamycin (m TOR); (iii) a mitogen- activated protein kinase (MEK) inhibitor; (iv) a mutated B-Raf inhibitor; (v) a chemotherapeutic agent like Gemcitabine, 5-FU, Irinotecan and Oxaliplatin; and (vi) certain combinations thereof. The combination can be used to treat a tumor that has developed resistance to an EGFR inhibitor, EGFR antibody, m TOR inhibitor, MEK inhibitor, mutated B-Raf inhibitor, chemotherapeutic agents, and certain combinations thereof, or to prevent acquired resistance of a tumor to any of said inhibitors or agents, or to prevent tumor recurrence following cease of treatment with any of said inhibitors or agents or a combination thereof. The combination provides a therapeutic effect which is at least additive, and is preferably synergistic. The present invention further relates to the treatment of cancer using combination therapy comprising a dual modulator of IRS and Stat3, in combination with an immunotherapy agent. The combination can be used to sensitize a tumor to immunotherapy. |
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| 82 | Histone Deacetylase Inhibitors | PCT/US2007062152 | 2007-02-14 | WO2007095584A3 | 2009-05-22 | BRADNER JAMES ELLIOT; MAZITSCHEK RALPH |
| In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for exmaple. The present invention also provides methods for preparing compounds of the invention and intermediates thereto. | ||||||
| 83 | END-MODIFIED POLY(BETA-AMINO ESTERS) AND USES THEREOF | PCT/US2007073976 | 2007-07-20 | WO2008011561A3 | 2008-11-27 | ZUGATES GREGORY T; ZUMBUEHL ANDREAS; LANGER ROBERTS S; ANDERSON DANIEL G |
| Poly(beta-amino esters) are end-modified to form materials useful in the medical as well as non-medical field. An amine-terminated poly(beta-amino ester) is reacted with an electrophile, or an acrylate-terminated poly(beta-amino ester) is reacted with a nucleophile. The iventive end-modified polymers may be used in any field where polymers have been found useful including the drug delivery arts. The end-modified polymers are particularly useful in delivery nucleic acids such as DNA or RNA. The invention also provides compositions including the inventive end-modified polymers, methods of preparing the inventive polymers, and method of using the inventive polymers. | ||||||
| 84 | NUCLEAR RECEPTOR BINDING AGENTS | PCT/US2008/004908 | 2008-04-16 | WO2008130571A1 | 2008-10-30 | DALTON, James, T.; BARRETT, Christina; MILLER, Duane, D.; HONG, Seoung-soo; HE, Yali; MOHLER, Michael, L.; NARAYANAN, Ramesh; WU, Zhongzhi |
The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity. |
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| 85 | COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS | PCT/US2007018362 | 2007-08-20 | WO2008024302A8 | 2008-05-08 | SUN LIJUN; KOYA KEIZO; CHEN SHOUJUN; DEMKO ZACHARY; XIA ZHI-QIANG |
| Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. | ||||||
| 86 | CROSSLINKED, DEGRADABLE POLYMERS AND USES THEREOF | PCT/US2007070430 | 2007-06-05 | WO2007143659A3 | 2008-03-13 | ANDERSON DANIEL GRIFFITH; BURDICK JASON ALAN; LANGER ROBERT S |
| Acrylate-terminated poly(beta-amino esters) are cross-linked to form materials useful in the medical as well as non-medical field. The polymeric starting material is combined with a free radical initiator, either a thermal initiator or a photoinitiator, and the mixture for cross-linking is heated or exposed to light depending on the initiator used. The resulting materials due to the hydrolysable ester bond in the polymer backbone are biodegradable under physiological conditions. These cross-linked materials are particular useful as drug delivery vehicles, tissue engineering scaffolds, and in fabricating microdevices. The materials may also be used as plastics, coating, adhesives, inks, etc. The cross-linked materials prepared exhibit a wide range of degradation times, mass loss profiles, and mechanical properties. Therefore, the properties of the material may be tuned for the desired use. The high-throughput approach to preparing a library of cross-linked poly(beta-amino esters) allows for the rapid screening and design of degradable polymers for a variety of applications. | ||||||
| 87 | COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS | PCT/US2007/018362 | 2007-08-20 | WO2008024302A3 | 2008-02-28 | SUN, Lijun; KOYA, Keizo; CHEN, Shoujun; DEMKO, Zachary; XIA, Zhi-qiang |
Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. |
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| 88 | SULFUR-CONTAINING COMPOSITIONS AND PROCESSES FOR MAKING SAME | PCT/US2005/005110 | 2005-02-17 | WO2005080325A2 | 2005-09-01 | REFVIK, Mitchell D.; HASENBERG, Daniel M.; BROWN, Chad W.; MATSON, Michael S.; BYERS, Jim D.; SOLAAS, Dale M.; HANKINSON, Michael S.; HERRON, Steven J.; CARSTENS, Leslie L.; XING, Baozhong |
Thiol ester compositions, methods of making the thiol ester compositions, and methods of using the thiol ester compositions are provided. In some embodiments, the thiol ester compositions include thiol esters, hydroxy thiol esters and cross-linked thiol esters. The thiol ester composition can be used to produce cross-linked thiol esters, sulfonic acid-containing esters, sulfonate containing esters and thiocrylates containing esters. The thiol ester composition can be used to produce polythiourethanes. The polythiourethanes can be used in fertilizers and fertilizer coatings. |
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| 89 | LONG-ACTING, CHEMICAL-RESISTANT SKIN EMOLLIENTS, MOISTURIZERS, AND STRENGTHENERS | PCT/US1998/018962 | 1998-09-10 | WO99029294A1 | 1999-06-17 | |
| The present invention relates to compounds that are two-part molecules, and compositions containing such compounds, in which one part is designed to become covalently bonded to the skin (bonding agent) and the other part (a characteristic use agent) is designed to impart some characteristic use, such as emolliency, moisturizing effect, anti-acne, anti-wrinkle, anti-pain, antimicrobial, antifungal, antiviral, anti-irritation, skin tanning and skin lightening effects, extended protection of the skin (e.g., from ultraviolet light, by incorporation of a sunscreen component; from toxic and/or irritating substances; from insects and skin parasites, by incorporation of insecticides and/or insect repellants; from free radicals or other agents, as in aging, by incorporation of antioxidants), or dyeing of hair, skin nails, wool or fur. The covalently bonded part may also be useful to impart skin strengthening effect (e.g., from shear forces) or as wound healing agents. | ||||||
| 90 | Aromatic and aromatic/heteroaromatic molecular structures with controllable electron conducting properties | US13368468 | 2012-02-08 | US09169208B2 | 2015-10-27 | Roger Harquail French; Ross Getty; Simona Percec |
| Aromatic and aromatic/heteroaromatic molecular structures with controllable electron conducting properties are derived from the incorporation of electron active substituents in selective positions. | ||||||
| 91 | Controlled chemical release of hydrogen sulfide | US13989971 | 2011-12-01 | US09096504B2 | 2015-08-04 | Ming Xian; Yu Zhao |
| Agents of formula: where R1 and R2 vary independently and are acyl, sulfonyl, phosphoryl, alkyl, substituted alkyl, halogen, aryl, arylalkyl, substituted aryl, heteroaryl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, heterocycle, or heteroatoms; and R3 is H or a member of a ring structure which includes R2, are provided; as are agents of formula: where R1, R2 and R3 vary independently and: R1=OH, OR′, NHR′, NR′R″ (with R′ R″=alkyl, aryl, heteroaryl, etc); R2=acyl, alkyl, aryl, sulfonyl, etc; R3=alkyl, aryl, substituted aryl, heteroaryl, etc; and R4 and R5 are (independently) H, methyl or alkyl, substituted alkyl, aryl, substituted aryl, etc. Methods of using the agents to treat e.g. cardiovascular disease, stroke, shock, injuries caused by hypoxia, male erectile dysfunction, and Alzheimer's are provided. | ||||||
| 92 | Compounds for treating proliferative disorders | US12918703 | 2009-02-20 | US08581004B2 | 2013-11-12 | Teresa Kowalczyk-Przewloka; Lijun Sun |
| Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. | ||||||
| 93 | Organosulfur Compounds, a Method of Making Organosulfur Compounds and their Use for Inhibiting the Growth of Tumour Cells | US13057960 | 2009-08-05 | US20110190368A1 | 2011-08-04 | Catherine Hart Kaschula; Roger Hunter; Mohamed Iqbal Parker |
| Organosulfur compounds of the general formula (2) are described, wherein R1 and R2 are linear or branched C1-C5 alkyl; linear or branched C1-C5 alkenyl with the proviso that R1 is not prop-1-enyl (allyl); substituted linear or branched C1-C5 alkenyl or substituted linear or branched C1-C5 alkyl, in which the substituents are selected from OR3, NR4R5, COOR6, CON—R7R8, in which R3 is selected from H, COR9, para-methoxybenzyl and trialkylsilyl, in which R9 is alkyl or substituted alkyl; R4 N and R5 are alkyl or R4 and R5 together form a phthalimido group; R6 is alkyl or substituted alkyl; and R7 and R8 are alkyl or substituted alkyl; substituted or unsubstituted aromatic specifically where R1 and R2 are benzyl, para-methoxybenzyl and/or ortho,para-methoxybenzyl and substituted or unsubstituted heteroaromatic. The compounds can be used for inhibiting the growth of tumour cells and for treating cancer. A pharmaceutical composition and a method of preparing the compounds are also described. | ||||||
| 94 | Polymerization with living characteristics | US11805929 | 2007-05-25 | US07662986B2 | 2010-02-16 | Tam Phuong Le; Graeme Moad; Ezio Rizzardo; San Hoa Thang |
| This invention concerns a free radical polymerization process, selected chain transfer agents employed in the process and polymers made thereby, in which the process comprises preparing polymer of general Formula (A) and Formula (B) comprising contacting: (i) a monomer selected from the group consisting of vinyl monomers (of structure CH2═CUV), maleic anhydride, N-alkylmaleimide, N-arylmaleimide, dialkyl fumarate and cyclopolymerizable monomers; (ii) a thiocarbonylthio compound selected from Formula (C) and Formula (D) having a chain transfer constant greater than about 0.1; and (iii) free radicals produced from a free radical source; the polymer of Formula (A) being made by contacting (i), (ii) C and (iii) and that of Formula (B) by contacting (i), (ii) D, and (iii); and (iv) controlling the polydispersity of the polymer being formed by varying the ratio of the number of molecules of (ii) to the number of molecules of (iii); wherein Q, R, U, V, Z, Z′, m, p and q are as defined in the text. | ||||||
| 95 | Monomolecular conductive complex, conductive self-assembled film and assembly of electrode composed of metal and semiconductor making use of the same | US11886725 | 2006-03-17 | US07659416B2 | 2010-02-09 | Masamichi Fujihira; Fumie Sato; Yuuki Takayama; Go Ono |
| Enediyne compounds of the formula: (1) characterized in that the structure thereof is very simple and the production process is easy, and that the molecular length thereof is shorter than those of compounds having been proposed. Consequently, electrode assemblies comprising any of these enediyne compounds are highly promising in the application to nanomolecular wiring (nanomolecular wire) whose production has been difficult. | ||||||
| 96 | Fatty acid analogues for equilibrating bone mineral density | US11989004 | 2006-07-10 | US20100029973A1 | 2010-02-04 | Rolf Berge |
| The invention comprises the use of compounds comprising non β-oxidizable fatty acid entities according to formula (I) or (II) for the preparation of a pharmaceutical composition for the prevention and/or treatment of conditions associated with low/decreased bone mineral density (BMD), and/or for increasing the BMD by decreasing the bone resorption. | ||||||
| 97 | Biphenyl derived thiamides as calpain inhibitors | US11579737 | 2005-05-06 | US07476754B2 | 2009-01-13 | Bernardo Herradon Garcia; Mercedes Alonso Giner; Esperanza Benito Cano; Antonio Chana Lopez; Ana Montero Aguado |
| The present invention relates to compounds derived from biphenyl with activity as calpain inhibitors. One compound of the present invention is a 2,2′-disubstituted biphenyl, where the substituents in the 2 and 2′ positions of the biphenyl skeleton are chains containing structures related to amino acids, including fragments of aminocarbonylic compounds where at least one of the substituents in said 2- or 2′-positions is bonded to the biphenyl skeleton via a thiocarbonyl group, forming compounds with thioamide functionality. The present invention also encompasses any of the conformational isomers (atropisomers) of said compound of formula I. The compounds of formula I have application in the preventive or therapeutic treatment of a degenerative disease. | ||||||
| 98 | Synthesis of taxol enhancers | US12231217 | 2008-08-29 | US20090005594A1 | 2009-01-01 | Shoujun Chen; Lijun Sun; Zhi-Qiang Xia; Keizo Kova; Mitsunori Ono |
| Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)-(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent. | ||||||
| 99 | Malononitrile compound and use thereof | US10522764 | 2003-08-26 | US07439266B2 | 2008-10-21 | Satoshi Okada; Daisuke Oohira; Ken Otaka |
| The present invention relates to a novel malononitrile compound represented by the formula (A): wherein, R1 represents C1 to C6 alkyl that may be substituted with halogen, C2 to C6 alkenyl that may be substituted with halogen, etc; R2 represents hydrogen atom or C1 to C6 alkyl that may be substituted with halogen; R3 represents hydrogen atom or C1 to C6 alkyl; R4 represents hydrogen atom or C1 to C6 alkyl; R5 represents C1 to C6 alkyl that may be substituted with halogen, C3 to C6 alkenyl that may be substituted with halogen, etc, or R4 and R5 may be combined at their terminal and represent ethylene that may be substituted with C1 to C3 alkyl or trimethylene that may be substituted with C1 to C3 alkyl; and Z1 and Z2, which are the same or different, represent oxygen atom or sulfur atom. The malononitrile compound has an efficient pesticidal activity and can control effectively pests such as insect pests, acarine pests, nematode pests and the like. | ||||||
| 100 | Synthesis Of Trithiocarbonate Raft Agents And Intermediates Thereof | US11578268 | 2005-05-11 | US20080039651A1 | 2008-02-14 | William Farnham |
| This invention provides an efficient method for synthesizing trithiocarbonate RAFT agents, RSC(S)SR′, that can be used in the living polymerization of methacrylates and other olefinic monomers. This invention also provides an efficient method of synthesizing bis(alkylsulfanylthiocarbonyl) disulfides that are useful as intermediates in the synthesis of trithiocarbonate RAFT agents. | ||||||
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