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    Trihalomethionine derivative and pharmaceutical product containing the same
    1.
    发明授权
    Trihalomethionine derivative and pharmaceutical product containing the same 失效
    三卤代甲硫氨酸衍生物和含有它们的药物产品

    公开(公告)号：US07868206B2

    公开(公告)日：2011-01-11

    申请号：US12159459

    申请日：2006-12-27

    申请人： Tomoyoshi Nozaki ,  Takeshi Toru ,  Norio Shibata ,  Masaichi Yamamoto

    发明人： Tomoyoshi Nozaki ,  Takeshi Toru ,  Norio Shibata ,  Masaichi Yamamoto

    IPC分类号： C07C233/05 ,  A61K31/16

    CPC分类号： C07C323/60 ,  C07C2602/08

    摘要： A compound represented by the formula (I) is used as an active ingredient in a medicament for treatment or prevention of infectious diseases caused by protozoa or bacterium. X represents halogen, Z represents —(CH2)m— wherein m is an integer of 1-5, and R represents one of the following (i)-(v): (i) hydrogen n represents an integer of 0-5, R1's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. R2's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. (iv) alkyl having 1-5 carbon atoms, (v) hydroxyalkyl having 1-5 carbon atoms.

    摘要翻译： 在由用于治疗或预防由原生动物或细菌引起的感染性疾病的药物中使用由式（I）表示的化合物作为活性成分。 X表示卤素，Z表示 - （CH 2）m - ，其中m为1-5的整数，R表示以下（i） - （v）中的一个：（i）氢n表示0-5的整数， R 1独立地表示氢，卤素，具有1-5个碳原子的烷氧基或具有1-5个碳原子的烷基。 R 2独立地表示氢，卤素，具有1-5个碳原子的烷氧基或具有1-5个碳原子的烷基。 （iv）具有1-5个碳原子的烷基，（v）具有1-5个碳原子的羟烷基。

    NOVEL TRIHALOMETHIONINE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING THE SAME
    2.
    发明申请
    NOVEL TRIHALOMETHIONINE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING THE SAME 失效
    新型三缩水甘油衍生物和含有它们的药物产品

    公开(公告)号：US20100076224A1

    公开(公告)日：2010-03-25

    申请号：US12159459

    申请日：2006-12-27

    申请人： Tomoyoshi Nozaki ,  Takeshi Toru ,  Norio Shibata ,  Masaichi Yamamoto

    发明人： Tomoyoshi Nozaki ,  Takeshi Toru ,  Norio Shibata ,  Masaichi Yamamoto

    IPC分类号： C07C237/06

    CPC分类号： C07C323/60 ,  C07C2602/08

    摘要： A compound represented by the formula (I) is used as an active ingredient in a medicament for treatment or prevention of infectious diseases caused by protozoa or bacterium. X represents halogen, Z represents —(CH2)m— wherein m is an integer of 1-5, and R represents one of the following (i)-(v): (i) hydrogen n represents an integer of 0-5, R1's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. R2's independently represent hydrogen, halogen, alkoxy having 1-5 carbon atoms or alkyl having 1-5 carbon atoms. (iv) alkyl having 1-5 carbon atoms, (v) hydroxyalkyl having 1-5 carbon atoms.

    摘要翻译： 在由用于治疗或预防由原生动物或细菌引起的感染性疾病的药物中使用由式（I）表示的化合物作为活性成分。 X表示卤素，Z表示 - （CH 2）m - ，其中m为1-5的整数，R表示以下（i） - （v）中的一个：（i）氢n表示0-5的整数， R 1独立地表示氢，卤素，具有1-5个碳原子的烷氧基或具有1-5个碳原子的烷基。 R 2独立地表示氢，卤素，具有1-5个碳原子的烷氧基或具有1-5个碳原子的烷基。 （iv）具有1-5个碳原子的烷基，（v）具有1-5个碳原子的羟烷基。

    1-Fluoro-1,1-Bis-(Phenylsulfonyl)Methane and Production Method Thereof
    3.
    发明申请
    1-Fluoro-1,1-Bis-(Phenylsulfonyl)Methane and Production Method Thereof 失效
    1-氟-1,1-二 - （苯基磺酰基）甲烷及其制备方法

    公开(公告)号：US20090131723A1

    公开(公告)日：2009-05-21

    申请号：US12224664

    申请日：2007-03-02

    申请人： Takeshi Toru ,  Norio Shibata ,  Shuichi Nakamura ,  Takeo Fukuzumi

    发明人： Takeshi Toru ,  Norio Shibata ,  Shuichi Nakamura ,  Takeo Fukuzumi

    IPC分类号： C07C317/14 ,  C07C315/04

    CPC分类号： C07C317/14

    摘要： A novel 1-fluoro-1,1-bis(arylsulfonyl)methane is provided which is useful in monofluoromethylation. Also provided is a production method thereof.A method for producing a fluorobis(arylsulfonyl)methane, the method including the steps of: treating a bis(arylsulfonyl)methane represented by the following formula (1), (ArSO2)2CH2  (1) (wherein Ar represents a substituted or unsubstituted phenyl group or naphthyl group) with a base; and then adding a fluorination reagent thereto, to produce fluorobis(arylsulfonyl)methane represented by the following formula (2) (ArSO2)2CHF  (2) (wherein Ar is defined as above), and a fluorobis(arylsulfonyl)methane (2) represented by the above formula (2), which is a novel compound that is very useful in producing a monofluoromethyl.

    摘要翻译： 提供了一种新颖的1-氟-1,1-双（芳基磺酰基）甲烷，其可用于单氟甲基化。 还提供了其制备方法。 一种制备氟双（芳基磺酰基）甲烷的方法，所述方法包括以下步骤：处理由下式（1）表示的双（芳基磺酰基）甲烷，<？在线式描述=“在线式”末端 （“Ar”）2CH2（1）<？in-line-formula description =“In-line formula”end =“tail”？>（其中Ar表示取代或未取代的苯基或萘基） 一个基地 然后向其中加入氟化试剂以产生由下式（2）表示的氟双（芳基磺酰基）甲烷<？in-line-formula description =“In-line Formulas”end =“lead”→（ArSO 2）2CHF （式中，Ar如上所定义），上述式（2）表示的氟双（芳基磺酰基）甲烷（2） ），它是一种在生产单氟甲基中非常有用的新型化合物。

    1-fluoro-1, 1-bis-(phenylsulfonyl)methane and production method thereof
    4.
    发明授权
    1-fluoro-1, 1-bis-(phenylsulfonyl)methane and production method thereof 失效
    1-氟-1,1-双 - （苯基磺酰基）甲烷及其制备方法

    公开(公告)号：US07638654B2

    公开(公告)日：2009-12-29

    申请号：US12224664

    申请日：2007-03-02

    申请人： Takeshi Toru ,  Norio Shibata ,  Shuichi Nakamura ,  Takeo Fukuzumi

    发明人： Takeshi Toru ,  Norio Shibata ,  Shuichi Nakamura ,  Takeo Fukuzumi

    IPC分类号： C07C315/04 ,  C07C317/14

    CPC分类号： C07C317/14

    摘要： A novel 1-fluoro-1,1-bis(arylsulfonyl)methane is provided which is useful in monofluoromethylation. Also provided is a production method thereof.A method for producing a fluorobis(arylsulfonyl)methane, the method including the steps of: treating a bis(arylsulfonyl)methane represented by the following formula (1), (ArSO2)2CH2  (1) (wherein Ar represents a substituted or unsubstituted phenyl group or naphthyl group) with a base; and then adding a fluorination reagent thereto, to produce fluorobis(arylsulfonyl)methane represented by the following formula (2) (ArSO2)2CHF  (2) (wherein Ar is defined as above), and a fluorobis(arylsulfonyl)methane (2) represented by the above formula (2), which is a novel compound that is very useful in producing a monofluoromethyl.

    摘要翻译： 提供了一种新颖的1-氟-1,1-双（芳基磺酰基）甲烷，其可用于单氟甲基化。 还提供了其制备方法。 一种制备氟双（芳基磺酰基）甲烷的方法，所述方法包括以下步骤：处理由下式（1）表示的双（芳基磺酰基）甲烷，（ArSO 2）2 CH 2（1）（其中Ar表示取代或未取代的苯基 基团或萘基）; 然后向其中加入氟化试剂，得到由下式（2）（ArSO 2）2 CHF（2）（其中Ar如上定义）表示的氟双（芳基磺酰基）甲烷和表示为氟代双（芳基磺酰基）甲烷（2） 通过上述式（2），其是在制备单氟甲基中非常有用的新型化合物。

    Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof
    6.
    发明授权
    Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof 失效

    公开(公告)号：US4421914A

    公开(公告)日：1983-12-20

    申请号：US311329

    申请日：1981-10-14

    申请人： Noriaki Okamura ,  Takeshi Toru ,  Takeo Oba ,  Toshio Tanaka ,  Kiyoshi Bannai ,  Kenzo Watanabe ,  Seizi Kurozumi ,  Tatsuyuki Naruchi ,  Keiji Komoriya

    发明人： Noriaki Okamura ,  Takeshi Toru ,  Takeo Oba ,  Toshio Tanaka ,  Kiyoshi Bannai ,  Kenzo Watanabe ,  Seizi Kurozumi ,  Tatsuyuki Naruchi ,  Keiji Komoriya

    IPC分类号： C07D513/04 ,  C07D513/14 ,  A61K31/505

    CPC分类号： C07D513/04

    摘要： A compound selected from thiazolo[3,2-a]pyrimidines or their enolate derivatives represented by the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are identical or different, and each represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 3 to 10 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted cycloaliphatic group having 3 to 8 carbon atoms, a substituted or unsubstituted phenylalkyl group or a substituted or unsubstituted acyl group having 2 to 7 carbon atoms, provided that R.sup.1 and R.sup.2 are not simultaneously hydrogen atoms or substituted or unsubstituted acyl groups having 2 to 7 carbon atoms; and R.sup.1 and R.sup.2, when taken together, may form, with the nitrogen atom to which they are bonded, a 5- or 6-membered ring which may further contain one or more hetero atoms;and acid addition salts of these compounds.The thiazolo[3,2-a]pyrimidines may be prepared by a process comprising (a) reacting a malonic acid derivative of the following general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined with regard to formula (I), and R.sup.4 and R.sup.5 are identical or different and each represents an alkyl group having 1 to 6 carbon atoms,with 2-aminothiazoline under heat, if desired in the presence of an inert organic solvent, to induce cyclocondensation, or (b) performing said condensation reaction in the presence of an alkali metal alkoxide, if desired in the presence of an inert organic solvent, and neutralizing the resulting enolate with an acid; and if desired, reacting the reaction product of (a) or (b) with an acid.The present invention provides also several processes for preparing enolate derivatives thereof.The thiazolo[3,2-a]pyrimidines, their enolate derivatives and acid addition compounds thereof are useful for regulating the immune function of a warm-blooded animal.

    Composition containing fluorescence-generating substrate
    8.
    发明授权
    Composition containing fluorescence-generating substrate 失效
    含荧光发生基质的组合物

    公开(公告)号：US06180844B2

    公开(公告)日：2001-01-30

    申请号：US09264678

    申请日：1999-03-09

    申请人： Satoshi Fujita ,  Naoto Kagiyama ,  Yasumitsu Kondoh ,  Paidi Yella Reddy ,  Takeshi Toru

    发明人： Satoshi Fujita ,  Naoto Kagiyama ,  Yasumitsu Kondoh ,  Paidi Yella Reddy ,  Takeshi Toru

    IPC分类号： C07C1300

    CPC分类号： C12Q1/28

    摘要： A fluorescent dye-forming composition is provided that contains a fluorescence-generating substrate of formula (I): where R1 and R2 are each independently a hydrogen atom, or an electron-donating group selected from a lower alkyl group, a lower alkoxy group, a hydroxyl group, an alkylcarbonyloxy group, an amino group di-substituted with a lower alkyl group, and an aryl group; L is selected from —NHCO— or —CONH—; Y is selected from -alkylene-COOH or formula (II):  where R3, R4 and R5 each independently represent a hydrogen atom, carboxyl group, or an electron-donating group selected from a lower alkyl group, a lower alkoxy group, a hydroxyl group, an alkylcarbonyloxy group, an amino group di-substituted with a lower alkyl group, and an aryl group. Alternatively, two of R3, R4 and R5 form, together with the adjacent carbon atoms to which they bond, a fused 5-membered or 6-membered hydrocarbon ring. Alkylene represents a linear or branched C1-6 alkylene group; and a represents an integer of 0 or 1. The substrate forms a fluorescent dye having good binding to biological samples.

    摘要翻译： 提供荧光染料形成组合物，其含有式（I）的荧光发生底物：其中R 1和R 2各自独立地为氢原子，或者是供体基团，其选自低级烷基，低级烷氧基， 羟基，烷基羰基氧基，被低级烷基二取代的氨基和芳基; L选自-NHCO-或-CONH-; Y选自 - 亚烷基-COOH或式（II） ：其中R3，R4和R5各自独立地表示氢原子，羧基或供体基团，其选自低级烷基，低级烷氧基，羟基，烷基羰基氧基，二取代的氨基 低级烷基和芳基。 或者，R 3，R 4和R 5中的两个与它们键合的相邻碳原子一起形成稠合的5元或6元烃环。 亚烷基表示直链或支链C 1-6亚烷基; a表示0或1的整数。底物形成与生物样品具有良好结合性的荧光染料。

    Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives
    10.
    发明授权
    Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives 失效
    4-羟基环戊-2-烯-1-酮衍生物的制备方法

    公开(公告)号：US4132726A

    公开(公告)日：1979-01-02

    申请号：US642800

    申请日：1975-12-22

    申请人： Seizi Kurozumi ,  Takeshi Toru ,  Toshio Tanaka ,  Shuzi Miura ,  Makiko Kobayashi ,  Sachio Ishimoto ,  Sadakazu Matsubara

    发明人： Seizi Kurozumi ,  Takeshi Toru ,  Toshio Tanaka ,  Shuzi Miura ,  Makiko Kobayashi ,  Sachio Ishimoto ,  Sadakazu Matsubara

    IPC分类号： C07C35/06 ,  C07C45/67 ,  C07D309/12 ,  C07F7/18 ,  C12P7/38 ,  C12P41/00

    CPC分类号： C07C49/707 ,  C07C35/06 ,  C07C45/676 ,  C07D309/12 ,  C07F7/1804 ,  C07F7/1856 ,  C12P41/004 ,  C12P7/38 ,  Y02P20/55

    摘要： Novel optically active compounds of 4-protected hydroxy-cyclopent-2-en-1-ones of the formula ##STR1## wherein R is a splittable protective group for an alcoholic hydroxyl group, and a process for preparing the 4-protected hydroxycyclopent-2-en-1-ones by oxidizing monohydroxy-protected derivatives of cyclopent-1-ene-3,5-diol expressed by the following formula ##STR2## wherein R is the same as defined above. Optically active 4-hydroxycyclopent-2-en-1-one which is an optically active isomer of the compound of formula (2); or optically active cyclopent-1-en-3,5-diol (R-isomer) and a novel diacyl derivative of the diol, a novel monoacylmonosilyl-derivative of the diol and a novel monoacylmonotetrahydropyranol-derivative of the diol, which are intermediates for the protective derivative of formula (1). Processes are also provided for preparing the protective derivatives of formula (1) by converting these intermediates by esterification, hydrolysis, enzymatic processes, etc. The optically active compounds of formula (2) are useful as precursors for the preparation of prostaglandin or its analogues.

    摘要翻译： 新型的具有式（2）的4-保护的羟基 - 环戊-2-烯-1-酮的光学活性化合物，其中R是醇羟基的可裂解的保护基，以及制备4-保护的 羟基环戊-2-烯-1-酮通过氧化由下式（1）表示的环戊-1-烯-3,5-二醇的单羟基保护衍生物，其中R与上述定义相同。 光学活性的4-羟基环戊-2-烯-1-酮，它是式（2）化合物的旋光异构体; 或光学活性的环戊-1-烯-3,5-二醇（R-异构体）和二醇的新型二酰基衍生物，二醇的新型单酰基单甲硅烷基衍生物和二醇的新型单酰基单四氢吡喃醇衍生物，其为 式（1）的保护性衍生物。 还提供了通过酯化，水解，酶法等转化这些中间体来制备式（1）的保护性衍生物的方法。式（2）的光学活性化合物可用作制备前列腺素或其类似物的前体。