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1. 发明专利

MX9604420A DERIVADOS DE PIRIMIDINILO COMO INHIBIDORES DE LA INTERLEUCINA. 未知
公开(公告)号：MX9604420A
公开(公告)日：1997-12-31
申请号：MX9604420
申请日：1995-03-29
申请人： SANOFI WINTHROP INC
发明人： DOLLE ROLAND E , PROUTY CATHERIE P , CHATURVEDULA PRASAD V , SCHMIDT STANLEY J
IPC分类号： A61K31/505 , A61K31/506 , A61K38/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07D401/04 , C07D403/12 , C07D239/47 , C07D405/12 , C07D409/04 , C07F9/6512 , C07K5/02 , C07K5/06 , C07K5/078 , C07D409/14 , C07F09/6512 , A61K31/675
摘要： Se describen compuestos, composiciones y métodos para inhibir la actividad de la proteasa interleucina -1 beta(IL-1 beta). Los compuestos metilcetonas alfa-sustituidas del ácido N-(pirmidinil)-aspártico y aldehídos del ácido aspártico tiene la formula (I) establecida en al presente. Estos compuestos son inhibidores de la enzima que convierte la 1 beta y como tales son utiles siempre que se desee tal inhibicion. Por ejemplo, pueden ser utilizados como herramientas de investigacion en estudios farmacologicos de diagnostico y relacionados y en el tratamiento de enfermedades en mamíferos, en las cuales está implicada la actividad de la IL- beta proteasa.

2. 发明申请

WO1995000524A1 PHOSPHONIC DIESTER DERIVATIVE 审中-公开
公开(公告)号：WO1995000524A1
公开(公告)日：1995-01-05
申请号：PCT/JP1994000883
申请日：1994-05-31
申请人： OTSUKA PHARMACEUTICAL FACTORY, INC. , KUROGI, Yasuhisa , MIYATA, Kazuyoshi , NAKAMURA, Shizuo , KONDO, Mitsuyoshi , IWAMOTO, Takeshi , NABA, Chieko , TSUDA, Yoshihiko , INOUE, Yasuhide , KANAYA, Jun , SATO, Keigo
发明人： OTSUKA PHARMACEUTICAL FACTORY, INC.
IPC分类号： C07F09/6512
CPC分类号： C07F9/65583 , C07F9/65128
摘要： A phosphonic diester derivative represented by general formula (1) and useful as remedies for hyperlipidemia, hypertension, diabetes, and so forth. In said formula, A represents oxygen or sulfur; R , R , R and R represent each independently hydrogen, lower alkoxy, nitro, lower alkyl, halogenated lower alkyl or halogen; R represents phenyl, -B-R (wherein B represents oxygen or sulfur; and R represents hydrogen, lower alkyl, cycloalkyl, phenyl, phenylated lower alkyl wherein the phenyl may be halogenated, phenoxylated lower alkyl, lower-alkoxy carbonyl-substituted lower alkyl, carboxylated lower alkyl or lower alkenyl) or -NR R (wherein R and R represent each independently hydrogen, lower alkyl, amino or cycloalkyl, or R and R are combined together to form lower alkylene); and R and R represent each independently hydrogen or lower alkyl.
摘要翻译：由通式（1）表示的膦酸二酯衍生物，可用作高脂血症，高血压，糖尿病等的补救措施。在所述式中，A表示氧或硫; R 1，R 2，R 9和R 10各自独立地表示氢，低级烷氧基，硝基，低级烷基，卤代低级烷基或卤素; R 3表示苯基，-BR 6（其中B表示氧或硫; R 6表示氢，低级烷基，环烷基，苯基，苯基可被卤化的苯基低级烷基，苯氧基低级烷基，低级 - 烷氧基羰基取代的低级烷基，羧基化的低级烷基或低级烯基）或-NR 7 R 8（其中R 7和R 8各自独立地表示氢，低级烷基，氨基或环烷基，或R <7>和R 8组合在一起形成低级亚烷基）; R 4和R 5各自独立地表示氢或低级烷基。

3. 发明申请

WO1993001198A1 PYRAZOLOPYRIMIDINE AND PYRIMIDINYL BISPHOSPHONIC ESTERS AS ANTI-INFLAMMATORIES 审中-公开
标题翻译：作为抗炎药的吡唑并嘧啶和嘧啶二磷酸酯
公开(公告)号：WO1993001198A1
公开(公告)日：1993-01-21
申请号：PCT/US1992005398
申请日：1992-07-01
申请人： THE UPJOHN COMPANY , NUGENT, Richard, Allen , SCHLACHTER, Stephen, Thomas
发明人： THE UPJOHN COMPANY
IPC分类号： C07F09/6512
CPC分类号： C07F9/6561 , C07F9/6512
摘要： Compounds useful in the treatment of inflammation structurally represented as wherein X is O or S and the R groups are as herein defined. The compounds are useful as anti-inflammatory and anti-arthritic agents without inhibiting prostaglandin synthesis.

4. 发明申请

WO1997030060A1 SUBSTITUTED AROMATIC PHOSPHONIC ACID DERIVATIVES 审中-公开
标题翻译：取代芳族膦
公开(公告)号：WO1997030060A1
公开(公告)日：1997-08-21
申请号：PCT/EP1997000733
申请日：1997-02-17
申请人： BASF AKTIENGESELLSCHAFT , ZAGAR, Cyrill , HEISTRACHER, Elisabeth , MENKE, Olaf , HAMPRECHT, Gerhard , MENGES, Markus , SCHÄFER, Peter , WESTPHALEN, Karl-Otto , MISSLITZ, Ulf , WALTER, Helmut
发明人： BASF AKTIENGESELLSCHAFT
IPC分类号： C07F09/6512
CPC分类号： C07F9/6561 , A01N57/24 , A01N57/32 , C07F9/4015 , C07F9/4056 , C07F9/5537 , C07F9/65031 , C07F9/65038 , C07F9/6506 , C07F9/650905 , C07F9/6512 , C07F9/6539 , C07F9/65583 , C07F9/65586
摘要： The invention concerns substituted aromatic phosphonic acid derivatives (I) and their salts, wherein: Eth = 1,2-ethinediyl, an optionally substituted ethane or ethene-1,2-diyl chain; y = O, S; y , y = O, S or -N(R )-; R , R , R , R = H, C1-C6-alkyl, C1-C6 alkyl halide, hydroxy-C1-C4-alkyl, cyano-C1-C4-alkyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy halide-C1-C4-alkyl, C3-C4-alkenyloxy-C1-C4-alkyl, C3-C4-alkinyloxy-C1-C4-alkyl, C3-C8-cycloalkoxy-C1-C4-alkyl, amino-C1-C4-alkyl, C1-C4-alkylamino-C1-C4-alkyl, Di-(C1-C4-alkyl)amino-C1-C4-alkyl, C1-C4-alkylthio-C1-C4-alkyl, C1-C4-alkyl halide-thio-C1-C4-alkyl, C3-C4-alkenylthio-C1-C4-alkyl, C3-C4-alkinylthio-C1-C4-alkyl, C1-C4-alkylsulfinyl-C1-C4-alkyl, C1-C4-alkyl halide sulfinyl-C1-C4-alkyl, C3-C4-alkenylsulfinyl-C1-C4-alkyl, C3-C4-alkinylsulfinyl-C1-C4-alkyl, C1-C4-alkylsulfonyl-C1-C4-alkyl, C1-C4-alkyl halide sulfonyl-C1-C4-alkyl, C3-C4-alkenylsulfonyl-C1-C4-alkyl, C3-C4-alkinylsulfonyl-C1-C4-alkyl, C3-C6-alkenyl, C3-C6-alkenyl halide, cyano-C3-C6-alkenyle, C3-C6-alkenyl halide, cyano-C3-C6-alkenyl, C3-C6-alkinyl, C3-C6-alkinyl halide, cyano-C3-C6-alkinyl, hydroxycarbonyl-C1-C4-alkyl, (C1-C4-alkoxy)-carbonyl-C1-C4-alkyl, (C1-C4-alkylthio)carbonyl-C1-C4alkyl, aminocarbonyl-C1-C4-alkyl, (C1-C4-alkyl)aminocarbonyl-C1-C4-alkyl, Di-(C1-C4-alkyl)aminocarbonyl-C1-C4-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C4-alkyl, phenyl ou phenyl-C1-C4-alkyl optionally substituted 3- to 7-member heterocyclyl or heterocyclyl-C1-C4 alkyl, wherein all the heterocyclenes can optionally contain a carbonyl- or thiocarbonyl ring member; or R and R and/or R and R and/or R and R together are an optionally substituted 1,2-ethanediyl-, 1,3-propylene-, tetramethylene-, pentamethylene or ethyleneoxyethylene chain; or R and R together are an optionally substituted 1,2-phenylene; R = CN, halogen, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy or C1-C4 alkoxy halide; R = H, halogen; and R = a given heterocyclic ring. The invention further concerns the use of these substances as herbicides and for the desiccation/defoliation of plants.
摘要翻译：式（I）化合物及其盐，其中的Eth = 1,2- ethynediyl，GEG。SUBST的取代的芳族膦酸衍生物。乙烷或乙烯-1,2-二基链; Y'> = O，S; ÿ<2>ý<3> = O，S或-N（R <6>） - ; [R <1>，R <2>，R <6> - [R <7> = H，C1-C6-烷基，C1-C6卤代烷基，羟基-C 1 -C 4烷基，氰基C1-C4烷基， C1-C4烷氧基C1-C4烷基，C1-C4卤代烷氧基，C1-C4烷基，C3-C4链烯氧基，C1-C4烷基，C3-C4炔氧基-C 1 -C 4 - 烷基，C 3 -C C8环烷氧基-C 1 -C 4 - 烷基，氨基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷基氨基-C 1 -C 4 - 烷基，二（C1-C4烷基）氨基 - C1-C4烷基，C1- C4烷硫基C1-C4烷基，C1-C4 - 卤代-C 1 -C 4 - 烷基，C 3 -C 4链烯基硫基-C 1 -C 4 - 烷基，C 3 -C 4炔硫基-C 1 -C 4 - 烷基，C1-C4 烷基亚磺酰基，C1-C4烷基，C1-C4卤代烷基亚磺酰基-C 1 -C 4烷基，C 3 -C 4链烯基亚磺酰基-C 1 -C 4烷基，C 3 -C 4炔基亚磺酰基，C1-C4烷基，C1-C4烷基磺酰基 C1-C4烷基，C1-C4卤代烷基磺酰基-C 1 -C 4 - 烷基，C 3 -C 4链烯基磺酰基-C 1 -C 4烷基，C 3 -C 4炔基磺酰基，C1-C4烷基，C3-C6链烯基，C 3 -C C6卤代链烯基，氰基-C 3 -C 6 - 链烯基，C3-C6炔基，C3-C6卤代炔基，氰基-C 3 -C 6 - 炔基，羟基羰基C 1 -C 4 - 烷基，（C1-C4烷氧基）羰基 C1-C4烷基，（C1-C4烷硫基）羰基C1-C4烷基，氨基羰基C1-C4烷基，（C1 1 -C 4 - 烷基）氨基羰基C1-C4烷基，二（C1-C4烷基）氨基羰基C1-C4烷基，未取代或取代的。 C3-C8环烷基，C3-C8环烷基C1-C4烷基，苯基或苯基C1-C4烷基或GEG。SUBST。 3-至7-元杂环基或杂环基-C 1 -C 4 - 烷基，其中所有的杂环可含有一个羰基或硫代羰基环成员，如果需要的话，或R <1>和R <2>和/或R <1>和R < = 6>和/或R <2>和R <7>一起未取代的或取代的。 1,2-乙二基，1,3-亚丙基，四亚甲基，五亚甲基或亚乙氧基亚乙基链，或R <1>和R <2>合起来为= GEG。SUBST。 1,2-亚苯基; [R <3> = CN，卤素，C1-C4烷基，C1-C4卤代烷基，C1-C4烷氧基或C1-C4卤代烷氧基; [R <4> = H，卤素; [R <5> =某些杂环。用途：用作除草剂; 对于植物干燥/落叶。

5. 发明申请

WO1997008178A1 NOVEL BISPHOSPHONATES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新型二硫磷酸酯，其制备方法及含有它们的药物组合物
公开(公告)号：WO1997008178A1
公开(公告)日：1997-03-06
申请号：PCT/IL1996000087
申请日：1996-08-22
申请人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM , ALFERIEV, Ivan, Sergeievitch , BREUER, Eli , GOLOMB, Gershon , ORNOY, Asher
发明人： YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
IPC分类号： C07F09/6512
CPC分类号： C07F9/6539 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/65031 , C07F9/6506 , C07F9/6512
摘要： Bisphosphonate compounds, their preparation and pharmaceutical compositions which contain such compounds as active ingredients. Such compositions are generally administered per os and they are effective for treating irregularities of the calcium metabolism. Preferred compounds have a 2-aminopyrimidine type ring. Similar unsubstituted and substituted heterocyclic compounds were found to have a similar activity.
摘要翻译：双膦酸酯化合物，其制备方法和含有这些化合物作为活性成分的药物组合物。这样的组合物通常每口服给药，并且它们对于治疗钙代谢的不规则性是有效的。优选的化合物具有2-氨基嘧啶型环。发现类似的未取代和取代的杂环化合物具有相似的活性。

6. 发明申请

WO1995024410A1 PHOSPHONIC DIESTER DERIVATIVE 审中-公开
公开(公告)号：WO1995024410A1
公开(公告)日：1995-09-14
申请号：PCT/JP1995000303
申请日：1995-02-27
申请人： OTSUKA PHARMACEUTICAL FACTORY, INC. , KUROKI, Yasuhisa , MIYATA, Kazuyoshi , TSUDA, Yoshihiko , INOUE, Yasuhide , KANAYA, Jun , SATO, Keigo
发明人： OTSUKA PHARMACEUTICAL FACTORY, INC.
IPC分类号： C07F09/6512
CPC分类号： C07F9/65128
摘要： A phosphonic diester derivative represented by general formula (1) and useful as a remedy and preventive for hyperlipidemia, hypertension, diabetes, and so forth. In formula (1) R , R , R and R represent each independently hydrogen, lower alkyl, halogen, nitro, etc.; R represents phenyl, lower alkyl, phenylalkyl, etc.; R represents lower alkyl; R represents lower alkoxy, hydroxy, phenyl, or phenylated lower alkoxy or lower alkylamino wherein the phenyl group may be halogenated; X and X represent each oxygen or sulfur; A represents oxygen or a single bond; and Z represents lower alkylene.
摘要翻译：由通式（1）表示的膦酸二酯衍生物，可用作高脂血症，高血压，糖尿病等的补救和预防。在式（1）中，R 1，R 2，R 3和R 6各自独立地表示氢，低级烷基，卤素，硝基等; R 4表示苯基，低级烷基，苯基烷基等; R 5表示低级烷基; R 7表示低级烷氧基，羟基，苯基或苯基的低级烷氧基或低级烷基氨基，其中苯基可以被卤化; X 1和X 2代表每个氧或硫; A代表氧或单键; Z表示低级亚烷基。

7. 发明申请

WO1995015968A1 PHOSPHONIC ACID DERIVATIVES AS PESTICIDES 审中-公开
标题翻译：膦衍生物作为杀虫剂
公开(公告)号：WO1995015968A1
公开(公告)日：1995-06-15
申请号：PCT/EP1994003931
申请日：1994-11-28
申请人： BAYER AKTIENGESELLSCHAFT , MAURER, Fritz , HARTWIG, Jürgen , ERDELEN, Christoph , TURBERG, Andreas , MENCKE, Norbert
发明人： BAYER AKTIENGESELLSCHAFT
IPC分类号： C07F09/6512
CPC分类号： A01N57/24 , C07F9/6512
摘要： The invention pertains to new phosphonic acid esters of general formula (I) in which R is a possibly substituted alkyl, R is a possibly substituted alkylk or possibly substituted aryl and X is oxygen or sulfur. These new phosphonic acid esters can be used as pesticides.
摘要翻译：本发明涉及其中R代表任选取代的烷基，R <1>是任选取代的烷基或任选取代的芳基，X表示氧或硫，它可被用作杀虫剂的通式（I）的新的膦酸酯，

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