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 |
|---|---|---|---|---|---|---|
| 41 | PDK4 INHIBITOR AND USE THEREOF | US14655631 | 2013-12-26 | US20150344404A1 | 2015-12-03 | Satoshi OMURA; Hirofumi NAKANO; Kenzaburo YAMAJI; Tsuyoshi YAMAMOTO; Hiroshi KIDO; Kazuhiko YAMANE; Toshiaki SUNAZUKA; Tomoyasu HIROSE |
| The present invention to provide a novel pyruvate dehydrogenase kinase inhibitors. A pyruvate dehydrogenase kinase inhibitor comprising a compound represented by the general formula (I) as an active ingredient (wherein, ring A represents a 6-membered aromatic hydrocarbon ring optionally substituted with 2-4 substituents, R1 and R4, which are the same or different, represent a hydrogen atom, a hydroxyl group, an optionally substituted C1-6 alkyl group, R2 and R3, which are the same or different, represent a hydrogen atom, a carboxyl group, an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group, or a group represented by —C (═R9)—R10), a pharmaceutical composition for treatment or prophylaxis of diseases or disorders that pyruvate dehydrogenase kinase relates to its development or aggravation, and a cosmetic composition, and the like. | ||||||
| 42 | Anti-leishmanial compound and anti-leishmanial drug | US13583345 | 2011-10-13 | US08809555B2 | 2014-08-19 | Junji Kimura; Shohei Horie; Harumi Marushima; Yoshitsugu Matsumoto; Chizu Sanjoba; Yasutaka Osada |
| Provided is an anti-leishmanial compound represented by formula (1): | ||||||
| 43 | ANTI-LEISHMANIAL COMPOUND AND ANTI-LEISHMANIAL DRUG | US13583345 | 2011-10-13 | US20130245288A1 | 2013-09-19 | Junji Kimura; Shohei Horie; Harumi Marushima; Yoshitsugu Matsumoto; Chizu Sanjoba; Yasutaka Osada |
| Provided is an anti-leishmanial compound represented by formula (1): | ||||||
| 44 | Anthracyclinone derivatives and their use in amyloidosis | US395202 | 1999-09-14 | US6096888A | 2000-08-01 | Antonino Suarato; Jacqueline Lansen; Michele Caruso; Dario Ballinari; Tiziano Bandiera |
| The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described. | ||||||
| 45 | Method of making vitamin K1 | US764289 | 1996-12-12 | US5744624A | 1998-04-28 | Manfred Dorner |
| A process for the preparation of vitamin K.sub.1 by the oxidation of an alkali metal salt of dihydrovitamin K.sub.1 with hydrogen peroxide in the presence of an iron (III) salt at a pH of 13.7 to 14.3. The dihydrovitamin K.sub.1 alkali metal salt is produced by the saponification of a dihydrovitamin K.sub.1 diester with sodium hydroxide or potassium hydroxide. Conveniently, the oxidation process follows the saponification of dihydrovitamin K.sub.1 without isolation of the product of the saponification reaction. | ||||||
| 46 | 4-substituted anthracyclinones and their preparation | US646594 | 1991-01-25 | US5218130A | 1993-06-08 | Walter Cabri; Silvia De Bernardinis; Franco Francalanci; Sergio Penco |
| 4-substituted anthracyclinones of formula (I) ##STR1## wherein R represents a hydrogen atom or a straight or branched alkyl, alkenyl or alkynyl group having from 1 to 10 carbon atoms, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX): ##STR2## wherein R is as defined above and R.sub.1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof. | ||||||
| 47 | Quinone derivatives, their production and use | US1893 | 1987-01-09 | US5180742A | 1993-01-19 | Shinji Terao; Yoshitaka Maki |
| Quinone derivatives of the general formula: ##STR1## (wherein R.sup.1 and R.sup.2 are the same or different, and independently are a hydrogen atom or a methyl or methoxy group, or R.sup.1 and R.sup.2 combine with each other to represent --CH.dbd.CH--CH.dbd.CH--R.sup.3 is a hydrogen atom or a methyl group; R.sup.4 is an aliphatic, aromatic or heterocyclic group which may be substituted; R.sup.5 is a methyl or methoxy group, a hydroxymethyl group which may be substituted or a carboxyl group which may be esterified or amidated; Z is a group represented by --C.dbd.C--, --CH.dbd.CH--, ##STR2## n is an integer of 0 to 10; m is an integer of 0 to 3; k is an integer of 0 to 5, provided, however, that in the case of m being 2 or 3, Z and k can vary arbitrarily within the bracketed repeating units) are novel compounds, possess metabolism ameliorating action for polyunsaturated fatty acids, particularly production inhibitory activity of lipid peroxides (antioxidant activity), thromboxane A.sub.2 receptor antagonism, or production inhibitory activity of 5-lipoxygenase metabolites in mammals, and of use as drugs, such as antiasthmatic, antiallergic agent and cerebral-circulatory metabolism ameliorating agent. | ||||||
| 48 | Method of obtaining an antiplatelet effect | US738936 | 1985-05-29 | US4992469A | 1991-02-12 | Takayuki Ozawa; Morimitsu Nishikimi; Hiroshi Suzuki; Yoshiharu Shimomura; Isao Yamatsu; Shinya Abe; Kouji Yamada; Tohru Fujimori; Takanobu Takamura |
| A quinone derivative of the formula (I): ##STR1## in which A is a group of the formula (IV): ##STR2## or a group of the formula (V): ##STR3## in which X and Y are either the same as or different from each other and each are hydroxy, methoxy or hydrogen; and n is an integer of 1 to 5,is disclosed. The compound is useful as a medicament. | ||||||
| 49 | Benzoquinone derivatives and production thereof | US390871 | 1989-08-08 | US4943645A | 1990-07-24 | Shinji Terao; Hisayoshi Okazaki; Isuke Imada |
| A novel benzoquinone derivative of the general formula: ##STR1## [wherein R.sub.1 and R.sub.2 are the same or different and each is methyl or methoxy; n is an integer of 0 to 21; m is 0 or 1, Z is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen or an alkyl group which may optionally be substituted or, R.sub.3 and R.sub.4 together with the adjacent nitrogen atom form a morpholino group), a group of the formula: --COR.sub.5 (wherein R.sub.5 is an .alpha.-amino acid residue or a substituted or unsubstituted glucosamine residue), a group of the formula: ##STR3## (wherein R.sub.6 is a divalent hydrocarbon group of 1 to 3 carbon atoms), a group of the formula: ##STR4## (wherein R.sub.6 has the same meaning as defined above) or a group of the formula: ##STR5## (wherein l is an integer of 1 to 4 and R.sub.7 is hydroxy, methoxy or methyl)] has protocollagen-proline hydroxylase inhibiting activity, collagen biosynthesis inhibiting activity and 5-lipoxygenase suppressant activity, and is useful for the prevention and treatment of such diseases as pulmonary fibrosis, hepatocirrhosis, nephrosclerosis, arteriosclerosis, scleroderma, myelofibrosis and chronic arthritis or for the prevention and treatment of asthma, allergic rhinitis, urticaria, etc. | ||||||
| 50 | Benzoquinone derivatives | US168321 | 1988-03-18 | US4808339A | 1989-02-28 | Shinji Terao; Hisayoshi Okazaki; Isuke Imada |
| A novel benzoquinone derivative of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each is methyl or methoxy; n is an integer of 0 to 21; m is 0 or 1, Z is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen or an alkyl group which may optionally be substituted or, R.sub.3 and R.sub.4 together with the adjacent nitrogen atom form a morpholino group), a group of the formula: --COR.sub.5 (wherein R.sub.5 is an .alpha.-amino acid residue or a substituted or unsubstituted glucosamine residue), a group of the formula: ##STR3## (wherein R.sub.6 is a divalent hydrocarbon group of 1 to 3 carbon atoms), a group of the formula: ##STR4## (wherein R.sub.6 has the same meaning as defined above) or a group of the formula: ##STR5## (wherein l is an integer of 1 to 4 and R.sub.7 is hydroxy, methoxy or methyl) has protocollagen-proline hydroxylase inhibiting activity, collagen biosynthesis inhibiting activity and 5-lipoxygenase suppressant activity, and is useful for the prevention and treatment of such diseases as pulmonary fibrosis, hepatocirrhosis, nephrosclerosis, arteriosclerosis, scleroderma, myelofibrosis and chronic arthritis or for the prevention and treatment of asthma, allergic rhinitis, urticaria, etc. | ||||||
| 51 | Hydroquinone ether compounds | US741888 | 1985-06-06 | US4631252A | 1986-12-23 | Frederick H. Howell |
| New hydroquinone ether compounds of formula I are described: ##STR1## wherein p is 1 or 2 and q is 0 or 1, provided that p+q is 1 or 2, R is a residue of formula II ##STR2## and R.sub.o, R.sub.oo, R.sub.1, R.sub.2, R.sub.3, Q, n and k are as defined in the specification.The new compounds are useful e.g. as stabilizers in photographic material. | ||||||
| 52 | Benzo-1,4-quinones | US489360 | 1983-04-28 | US4608435A | 1986-08-26 | Frederick H. Howell |
| New benzo-1,4-quinones and salts thereof with organic or inorganic acid and bases have the formula I ##STR1## wherein p is 1 or 2 and q is 0 or 1, provided that p+q is 1 or 2, R is a residue of formula II ##STR2## wherein Q is selected from the residues --CO.sub.2 R.sub.4, --CON(R.sub.4)(R.sub.5), --OR.sub.5, --OCOR.sub.7, --N(R.sub.8)(R.sub.9), --PO(OR.sub.10)([O].sub.x R.sub.11), --SO.sub.2 R.sub.12, --CN, Halogen, --NO.sub.2 or --COR.sub.13, n is an integer from 1 to 20, k is 1 or 2 and x is 0 or 1, and R.sub.1 to R.sub.5 and R.sub.7 to R.sub.13 are as defined in the specification.The compounds of formula I are useful in photographic materials such as bleaching inhibitors in films of photographic silver dye bleach materials. | ||||||
| 53 | Quinone derivatives and use | US471457 | 1983-03-02 | US4533554A | 1985-08-06 | Shinji Terao; Mitsuru Shiraishi; Kaneyoshi Kato |
| New quinone derivatives of the formula ##STR1## wherein R.sup.1 is methyl or methoxy, or two of R.sup.1 combine to represent --CH.dbd.CH--CH.dbd.CH--, R is amino which may be substituted or --OR.sup.4 wherein R.sup.4 is hydrogen, C.sub.1-4 alkyl or --CH.sub.2 --CH.dbd.C(CH.sub.3 --CH.sub.2).sub.m H (wherein m is an integer of 1 to 10), and n is an integer of 1 to 10 when R is amino which may be substituted, or n is an integer of 2 to 10 when R is --OR.sup.4, and their hydroquinone forms, have useful physiological activities such as blood-pressure decreasing and antiallergic activities. | ||||||
| 54 | Benzoquinone derivatives and production thereof | US484232 | 1983-04-12 | US4526719A | 1985-07-02 | Shinji Terao; Hisayoshi Okazaki; Isuke Imada |
| A novel benzoquinone derivative of the general formula: ##STR1## [wherein R.sub.1 and R.sub.2 are the same or different and each is methyl or methoxy; n is an integer of 0 to 21; m is 0 or 1, Z is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen or an alkyl group which may optionally be substituted or, R.sub.3 and R.sub.4 together with the adjacent nitrogen atom form a morpholino group), a group of the formula: --COR.sub.5 (wherein R.sub.5 is an .alpha.-amino acid residue or a substituted or unsubstituted glucosamine residue), a group of the formula: ##STR3## (wherein R.sub.6 is a divalent hydrocarbon group of 1 to 3 carbon atoms), a group of the formula: ##STR4## (wherein R.sub.6 has the same meaning as defined above) or a group of the formula: --CH.dbd.CH.sub.l --COR.sub.7 (wherein l is an integer of 1 to 4 and R.sub.7 is hydroxy, methoxy or methyl)] has protocollagen-proline hydroxylase inhibiting activity, collagen biosynthesis inhibiting activity and 5-lipoxygenase suppressant activity, and is useful for the prevention and treatment of such diseases as pulmonary fibrosis, hepatocirrhosis, nephrosclerosis, arteriosclerosis, scleroderma, myelofibrosis and chronic arthritis or for the prevention and treatment of asthma, allergic rhinitis, urticaria, etc. | ||||||
| 55 | Quinone compounds and their use in suppressing the production of SRS-A in mammals | US248042 | 1981-03-26 | US4393075A | 1983-07-12 | Shinji Terao; Mitsuru Shiraishi; Yoshitaka Maki |
| New quinone compounds of the formula: ##STR1## wherein R.sup.1 is methyl or methoxy, or the two R.sup.1 groups jointly represent --CH.dbd.CH--CH.dbd.CH--; X is --CH.dbd.CH-- or --C.dbd.C--; Y.sup.1 is hydrogen, hydroxyl, carboxyl, cyano, acyloxy or --COZ in which Z is amino which may be substituted; m is zero or an integer of 1 to 3; n is zero or an integer of 1 to 10; n' is an integer of 1 to 5; k is an integer of 1 to 3; and when k is 2 or 3, n' is optionally variable within the range of 1 to 5 in each occurrence of the --X--(CH.sub.2).sub.n' group; and their hydroquinone forms and salts, have useful physiological activities such as antiasthmatic, antiallergic and bloodpressure decreasing activities. | ||||||
| 56 | Photographic material suited for use in diffusion transfer photography | US249508 | 1981-03-31 | US4371604A | 1983-02-01 | Christian C. Van de Sande; Wilhelmus Janssens; Wolfgang Lassig; Ernst Meier |
| A photographic material for diffusion transfer photography containing a quinonoid compound, which is capable in reduced state and under alkaline conditions of releasing a photographically useful group and corresponds to one of the following general formulae: ##STR1## wherein: each of (Nuox).sup.1 and (Nuox).sup.2 (same or different) represents an oxidized nucleophilic group,Z represents a bivalent atom or bivalent atomic group, which is electro-negative,Q together with the group Z represents a releasable photographically useful group,Y.sup.1 and Y.sup.2 together represent the necessary atoms to close a p-quinonoid ring substituted with (a) directly linked monovalent organic ring or ring system substituent(s) having aromatic character,Y.sup.3 represents the necessary atoms to close a o-quinonoid ring substituted with (a) directly linked monovalent organic ring or ring system substituent(s) having aromatic character, andeach of R.sup.1 and R.sup.2 (same or different) represents hydrogen or a (substituted) hydrocarbon group, and at least one of R.sup.1, R.sup.2 and a substituent on the quinonoid ring being or carrying a ballasting group. | ||||||
| 57 | Aralkyl carboxylic acid compounds | US573158 | 1975-04-30 | US4139545A | 1979-02-13 | Hiroshi Morimoto; Isuke Imada; Masazumi Watanabe; Mitsuru Kawada |
| Novel compounds of the formulae ##STR1## wherein R represents lower alkyl or lower alkoxy, A represents --CH.sub.2 --, --CO-- or ##STR2## n represents an integer of 1 to 8, X represents hydrogen or hydroxyl which may be protected and Y represents hydroxyl which may be protected, and their esters show an excellent action on the lysosomal membranes of cells, and exhibit excellent pharmacological activities such as physiologic host defense control activity, especially immuno-potentiating activity. | ||||||
| 58 | 4-hexenoic compounds | US42431473 | 1973-12-13 | US3879448A | 1975-04-22 | MORIMOTO HIROSHI; WATANABE MASAZUMI; IMADA ISUKE |
| Compounds of the formula
WHEREIN Z is acetoxy or halogen and Y2 is hydrogen or a lower alkyl group, which are useful in preparing quinones having strong anti-inflammatory activity. |
||||||
| 59 | Quinone derivatives | US12454771 | 1971-03-15 | US3849453A | 1974-11-19 | MORIMOTO H; NISHIKAWA M; WATANABE M; IMADA I |
| 1. A MEMBER SELECTED FROM THE GROUP CONSISTING OF A COMPOUND OF THE FORMULA
1,4-DI(O=),2-(H3C-),3-(R-OOC-CH(-A'')-CH(-A)-CH2-)-1,4- DIHYDRONAPHTHALENE WHEREIN ONE OF A AND A'' IS HYDROGEN AND THE OTHER IS LOWER ALKYL, AND R IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL OF 1-6 CARBON ATOMS, CYCLOALKYL OF UP TO 6 CARBON ATOMS AND ALLYL, AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF. |
||||||
| 60 | 3-substituted 1, 4-naphthoquinones | US14035050 | 1950-01-24 | US2589686A | 1952-03-18 | GEORGE FAWAZ |
QQ群二维码
意见反馈
意见反馈