公开(公告)号：US20060058298A1

公开(公告)日：2006-03-16

申请号：US11081095

申请日：2005-03-15

Applicant: Daniel Delorme ,  Soon Woo ,  Arkadii Vaisburg ,  Oscar Moradei ,  Silvana Leit ,  Stephane Raeppel ,  Sylvie Frechette ,  Giliane Bouchain

Inventor： Daniel Delorme ,  Soon Woo ,  Arkadii Vaisburg ,  Oscar Moradei ,  Silvana Leit ,  Stephane Raeppel ,  Sylvie Frechette ,  Giliane Bouchain

IPC: A61K31/5377 ,  A61K31/53 ,  A61K31/495 ,  A61K31/454 ,  A61K31/4015

CPC classification number: C07D401/04 ,  A61K31/4015 ,  A61K31/445 ,  A61K31/495 ,  A61K31/513 ,  A61K31/53 ,  A61K31/537 ,  C07C233/44 ,  C07C233/80 ,  C07C235/38 ,  C07C235/42 ,  C07C235/56 ,  C07C235/84 ,  C07C237/20 ,  C07C237/22 ,  C07C237/40 ,  C07C237/42 ,  C07C255/58 ,  C07C255/59 ,  C07C275/34 ,  C07C275/36 ,  C07C311/42 ,  C07C323/32 ,  C07C323/36 ,  C07C323/44 ,  C07C323/60 ,  C07C381/00 ,  C07D213/30 ,  C07D213/74 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D239/91 ,  C07D249/08 ,  C07D251/18 ,  C07D251/52 ,  C07D251/54 ,  C07D263/14 ,  C07D263/24 ,  C07D265/36 ,  C07D271/06 ,  C07D277/42 ,  C07D277/74 ,  C07D277/82 ,  C07D295/155 ,  C07D307/12 ,  C07D307/28 ,  C07D311/56 ,  C07D311/58 ,  C07D333/36 ,  C07D333/38 ,  C07D401/12 ,  C07D403/04 ,  C07D409/12 ,  C07D473/40 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07F7/081 ,  C07F7/0812

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

公开(公告)号：US20050182025A1

公开(公告)日：2005-08-18

申请号：US10510083

申请日：2003-04-30

Applicant: Chi-Ping Tseng

Inventor： Chi-Ping Tseng

IPC: C07C257/12 ,  A01N25/02 ,  A01N25/08 ,  A01N25/30 ,  A01N37/52 ,  A01N47/30 ,  A01N47/42 ,  A01N49/00 ,  A01N55/00 ,  C07C257/10 ,  C07C257/14 ,  C07C275/34 ,  C07C275/70 ,  C07C323/20 ,  C07C323/36 ,  C07C335/18 ,  C07C335/36 ,  C07F7/18 ,  A01N43/40 ,  A01N33/02

CPC classification number: A01N37/52 ,  A01N47/30 ,  A01N49/00 ,  A01N55/00 ,  C07C257/12 ,  C07C257/14 ,  C07C275/70 ,  C07C323/36 ,  C07C335/18 ,  C07C335/36 ,  C07C2601/02 ,  C07F7/1804

Abstract: Compounds of the formula (R5)m-(R6A)-2-(R4)-1-[N═C(R1)N(R2)(R3)]benzene and their agriculturally suitable salts, are disclosed which are useful as fungicides, wherein R1 is H, OH, SH, SO3H, CN, —OR7 or —SR7; C1-C10 alkyl, C2-C10 alkenyl, C2-C5 alkoxycarbonyl, C2-C10 alkynyl, a C3-C6 carbocycle or a 3-, 4-, 5- or 6-membered heterocycle, each optionally substituted; provided that when R1? is a heterocycle containing nitrogen as a ring member, it is not attached to the remainder of Formula I through said nitrogen ring member; R6 is C5-C21 alkyl, C5-C21 alkenyl, C5-C21 alkynyl, C4-C9alkoxycarbonyl, C4-C6 alkylaminocarbonyl, C3-C10 dialkylaminocarbonyl or C3-C12 trialkylsilyl, each optionally substituted; or R6 is C1-C4 alkyl or C2-C9 alkylcarbonyl, each substituted with one or more R12; A is a direct bond, O, S(O)n, or NR10; n is 0, 1 or 2; m is 0, 1, 2 or 3; and R2, R3, R4, R5, R7, R10 and R12 are as defined in the disclosure. Also disclosed are compositions containing the compounds of the formula (R5)m-(R6A)-2-(R4)-1-[N═C(R1)N(R2)(R3)]benzene and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of the formula (R5)m-(R6A)-2-(R4)-1-[N═C(R1)N(R2)(R3)]benzene.

公开(公告)号：US20050171097A1

公开(公告)日：2005-08-04

申请号：US11098440

申请日：2005-04-05

Applicant: Keiji Toriyabe ,  Nobuo Takefuji ,  Minoru Itou ,  Tetsuya Hirade ,  Kiyotoshi Nishiyama ,  Mitsuharu Asahida ,  Yasunobu Maeda ,  Nobuhide Wada ,  Toyokazu Fujisawa ,  Hiroyuki Yano ,  Masaaki Komatsu ,  Osamu Tada

Inventor： Keiji Toriyabe ,  Nobuo Takefuji ,  Minoru Itou ,  Tetsuya Hirade ,  Kiyotoshi Nishiyama ,  Mitsuharu Asahida ,  Yasunobu Maeda ,  Nobuhide Wada ,  Toyokazu Fujisawa ,  Hiroyuki Yano ,  Masaaki Komatsu ,  Osamu Tada

IPC: A01N41/10 ,  A01N43/08 ,  A01N43/10 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/60 ,  A01N43/76 ,  A01N43/78 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/445 ,  A61K31/495 ,  A61K31/498 ,  A61K31/50 ,  A61K31/513 ,  A61K31/53 ,  C07C309/00 ,  C07C317/14 ,  C07C317/22 ,  C07C317/32 ,  C07C323/09 ,  C07C323/18 ,  C07C323/31 ,  C07D211/54 ,  C07D213/52 ,  C07D213/57 ,  C07D213/64 ,  C07D231/12 ,  C07D249/08 ,  C07D253/00 ,  C07D263/32 ,  C07D277/26 ,  C07D307/56 ,  C07D333/24 ,  C07D333/28

CPC classification number: C07D213/12 ,  A01N31/08 ,  A01N31/14 ,  A01N33/10 ,  A01N37/08 ,  A01N37/34 ,  A01N41/10 ,  A01N43/08 ,  A01N43/10 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/76 ,  A01N43/78 ,  A01N47/18 ,  C07C317/32 ,  C07C317/48 ,  C07C323/18 ,  C07C323/20 ,  C07C323/36 ,  C07C323/63 ,  C07D213/32 ,  C07D213/48 ,  C07D213/57 ,  C07D213/64 ,  C07D239/36 ,  C07D239/38 ,  C07D239/40 ,  C07D249/08 ,  C07D333/24

Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.

Abstract translation: 由通式（I）表示的3-芳基苯基硫醚衍生物：其中R是C 2 -C 6烷基，C 2 - -C 6亚烷基，C 2 -C 6亚炔基等，B 0〜B 2个和3个3个是氢原子，卤素原子，氰基，C 1 -C 4卤代烷基或 n为0,1或2，Ar为苯环，吡啶环，噻吩环，吡唑环等），含有3-芳基苯基硫醚衍生物的杀虫剂和杀螨剂为活性成分。

公开(公告)号：US20050059705A1

公开(公告)日：2005-03-17

申请号：US10913168

申请日：2004-08-06

Applicant: Adnan Mjalli ,  Robert Andrews ,  Xiao-Chuan Guo ,  Daniel Christen ,  Devi Gohimmukkula ,  Guoxiang Huang ,  Robert Rothlein ,  Sameer Tyagi ,  Tripura Yaramasu ,  Christopher Behme

Inventor： Adnan Mjalli ,  Robert Andrews ,  Xiao-Chuan Guo ,  Daniel Christen ,  Devi Gohimmukkula ,  Guoxiang Huang ,  Robert Rothlein ,  Sameer Tyagi ,  Tripura Yaramasu ,  Christopher Behme

IPC: A61P31/12 ,  C07C233/87 ,  C07C235/42 ,  C07C235/52 ,  C07C235/60 ,  C07C235/66 ,  C07C237/36 ,  C07C237/42 ,  C07C271/20 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C311/44 ,  C07C317/32 ,  C07C323/36 ,  C07D295/155 ,  C07D41/02 ,  A61K31/4439 ,  C07D43/02

CPC classification number: C07D295/155 ,  C07C233/87 ,  C07C235/42 ,  C07C235/52 ,  C07C235/60 ,  C07C235/66 ,  C07C237/36 ,  C07C237/42 ,  C07C271/20 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C311/44 ,  C07C317/32 ,  C07C323/36 ,  C07C2601/08

Abstract: This invention provides aryl and heteroaryl compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention may be antagonists, or partial antagonist of factor IX and/or factor XI and thus, may be useful for inhibiting the intrinsic pathway of blood coagulation. The compounds may be useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway.

Abstract translation: 本发明提供芳基和杂芳基化合物，其制备方法，包含该化合物的药物组合物及其在治疗人或动物病症中的用途。 本发明的化合物可以是拮抗剂或因子IX和/或因子XI的部分拮抗剂，因此可用于抑制凝血的内在途径。 所述化合物可用于各种应用，包括部分由内在凝血途径引起的疾病的管理，治疗和/或控制。

公开(公告)号：US20050049310A1

公开(公告)日：2005-03-03

申请号：US10913882

申请日：2004-08-06

Applicant: Adnan Mjalli ,  Guoxiang Huang ,  Murty Arimilli ,  Thomas Yokum ,  Jeff Zhu

Inventor： Adnan Mjalli ,  Guoxiang Huang ,  Murty Arimilli ,  Thomas Yokum ,  Jeff Zhu

IPC: A61P31/12 ,  C07C233/87 ,  C07C235/42 ,  C07C235/52 ,  C07C235/60 ,  C07C235/66 ,  C07C237/36 ,  C07C237/42 ,  C07C271/20 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C311/44 ,  C07C317/32 ,  C07C323/36 ,  C07D295/155 ,  A61K31/195 ,  A61K31/137 ,  A61K31/15

CPC classification number: C07D295/155 ,  C07C233/87 ,  C07C235/42 ,  C07C235/52 ,  C07C235/60 ,  C07C235/66 ,  C07C237/36 ,  C07C237/42 ,  C07C271/20 ,  C07C311/08 ,  C07C311/09 ,  C07C311/21 ,  C07C311/44 ,  C07C317/32 ,  C07C323/36 ,  C07C2601/08

Abstract: This invention provides aryl and heteroaryl compounds of Formula (I) as described herein, and methods of their preparation. Also provided are pharmaceutical compositions made with the compounds of Formula (I) and methods for making such compositions. The compounds of Formula (I) may activate an erythropoietin receptor and thus, may be useful to induce red blood cell production. The compounds of Formula (I) and compositions including compounds of Formula (I) may be useful in a variety of applications including the management, treatment and/or control of diseases caused at least in part by deficient (or inefficient) EPO production relative to hemoglobin level.

Abstract translation: 本发明提供了本文所述的式（I）的芳基和杂芳基化合物及其制备方法。 还提供了用式（I）的化合物制备的药物组合物和制备这些组合物的方法。 式（I）的化合物可以激活促红细胞生成素受体，因此可用于诱导红细胞生成。 式（I）化合物和包含式（I）化合物的组合物可用于各种应用，包括至少部分地由EPO生产缺陷（或低效）引起的疾病的管理，治疗和/或控制，相对于 血红蛋白水平。

公开(公告)号：US20040006245A1

公开(公告)日：2004-01-08

申请号：US10349801

申请日：2003-01-23

Inventor： Gordon William Rewcastle ,  Julie Ann Spicer ,  Stephen Douglas Barrett ,  Michael David Kaufman ,  Jared Bruce John Milbank ,  Haile Tecle

IPC: C07C311/45 ,  C07C323/39 ,  C07C237/28

CPC classification number: C07C317/36 ,  C07C259/10 ,  C07C323/36 ,  Y10S514/825

Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.

Abstract translation: 本发明涉及4-取代苯基氨基苯并肟酸衍生物的氧化酯，药物组合物及其使用方法。

公开(公告)号：US06600074B2

公开(公告)日：2003-07-29

申请号：US10206769

申请日：2002-07-29

Applicant: Masanobu Onishi ,  Akihiko Yoshiura ,  Eiji Kohno ,  Kenji Tsubata

Inventor： Masanobu Onishi ,  Akihiko Yoshiura ,  Eiji Kohno ,  Kenji Tsubata

IPC: C07C21100

CPC classification number: C07C323/41 ,  C07C209/68 ,  C07C211/52 ,  C07C213/08 ,  C07C215/76 ,  C07C217/84 ,  C07C233/15 ,  C07C271/14 ,  C07C323/36 ,  C07D209/08

Abstract: The present invention provides an aniline derivative represented by the formula (I) wherein R1 and R2 are each H, (C1-12)alkyl, (C3-8)cycloalkyl, hydroxy(C1-12)alkyl, hydroxycarbonyl (C1-12)alkyl, (C1-6)-alkoxycarbonyl(C1-6)alkyl, —COR8, wherein R8 is H, halo-(C1-12)alkyl, (C3-8)cycloalkyl or (substituted) phenyl, COOR9, wherein R9 is a halo(C1-6)alkyl group, (substituted) phenyl or (substituted) benzyl; R3, R4, R5, R6and R7 are each H, halogen, OH, nitro, halo(C1-12)alkylthio, (substituted)amino-(C1-2)alkyl, (substituted) phenyl, (substituted) benzyl, amino, —N(R10)R11 wherein R10 and R11 are each H, alkyl, cycloalkyl, (substituted) phenyl, (substituted) benzyl, —COR8 or COOR9, or (C2-27)perfluoroalkyl, etc., and a process for producing the aniline derivative. According to the process of the present invention, perfluoroalkylaniline derivatives can be obtained by using various anilines as the substrate with a high position selectivity and high yield.

Abstract translation: 本发明提供由式（I）表示的苯胺衍生物，其中R1和R2各自为H，（C1-12）烷基，（C3-8）环烷基，羟基（C1-12）烷基，羟基羰基（C1-12） 烷基，（C 1-6） - 烷氧基羰基（C 1-6）烷基，-COR 8，其中R 8为H，卤代（C 1-12）烷基，（C 3-8）环烷基或（取代）苯基，COOR 9，其中R 9为 （C 1-6）烷基，（取代的）苯基或（取代的）苄基; R3，R4，R5，R6和R7各自为H，卤素，OH，硝基，卤代（C1-12）烷硫基，（取代的）氨基 - （C1-2）烷基，（取代的）苯基，（取代的） -N（R 10）R 11其中R 10和R 11各自为H，烷基，环烷基，（取代）苯基，（取代的）苄基，-COR 8或COOR 9或（C 2- 27）全氟烷基等， 苯胺衍生物。 根据本发明的方法，可以通过以高位置选择性和高收率使用各种苯胺作为基材来获得全氟烷基苯胺衍生物。

公开(公告)号：US06509354B1

公开(公告)日：2003-01-21

申请号：US09673633

申请日：2000-10-27

Applicant: Keiji Toriyabe ,  Nobuo Takefuji ,  Minoru Itou ,  Tetsuya Hirade ,  Kiyotoshi Nishiyama ,  Mitsuharu Asahida ,  Yasunobu Maeda ,  Nobuhide Wada ,  Toyokazu Fujisawa ,  Hiroyuki Yano ,  Masaaki Komatsu ,  Osamu Tada

Inventor： Keiji Toriyabe ,  Nobuo Takefuji ,  Minoru Itou ,  Tetsuya Hirade ,  Kiyotoshi Nishiyama ,  Mitsuharu Asahida ,  Yasunobu Maeda ,  Nobuhide Wada ,  Toyokazu Fujisawa ,  Hiroyuki Yano ,  Masaaki Komatsu ,  Osamu Tada

IPC: A61K31445

CPC classification number: C07D213/12 ,  A01N31/08 ,  A01N31/14 ,  A01N33/10 ,  A01N37/08 ,  A01N37/34 ,  A01N41/10 ,  A01N43/08 ,  A01N43/10 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/76 ,  A01N43/78 ,  A01N47/18 ,  C07C317/32 ,  C07C317/48 ,  C07C323/18 ,  C07C323/20 ,  C07C323/36 ,  C07C323/63 ,  C07D213/32 ,  C07D213/48 ,  C07D213/57 ,  C07D213/64 ,  C07D239/36 ,  C07D239/38 ,  C07D239/40 ,  C07D249/08 ,  C07D333/24

Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.

Abstract translation: 由通式（I）表示的3-芳基苯基硫醚衍生物:(其中R为C2-C6烷基，C2-C6烯基，C2-C6炔基等，B0至B2和B3为氢原子， 卤素原子，氰基，C 1〜C 4卤代烷基等，n为0,1或2，Ar为苯环，吡啶环，噻吩环，吡唑环等），杀虫剂和杀螨剂 含有3-芳基苯基硫醚衍生物作为活性成分。

公开(公告)号：US06500213B1

公开(公告)日：2002-12-31

申请号：US09446726

申请日：2000-03-14

Applicant: Hans-Juergen Braun ,  Laurent Chassot

Inventor： Hans-Juergen Braun ,  Laurent Chassot

IPC: A61K713

CPC classification number: C07D295/135 ,  A61K8/411 ,  A61Q5/10 ,  C07C211/51 ,  C07C211/52 ,  C07C215/68 ,  C07C217/76 ,  C07C217/80 ,  C07C225/22 ,  C07C229/52 ,  C07C237/30 ,  C07C255/58 ,  C07C271/28 ,  C07C323/36 ,  C07C2602/08 ,  C07D209/08 ,  C07D317/58

Abstract: The object of the present patent application are agents for the oxidative coloring of keratin fibers, particularly hair, based on a developer-coupler combination, characterized in that they contain as the developer at least one 2,5-diamino-1-phenylbenzene derivative of general formula and novel 2,5-diamino-1-phenylbenzene derivatives of formula (I) wherein at least one of the R1 to R10 radicals is different from hydrogen.

Abstract translation: 本专利申请的目的是基于显影剂 - 成色剂组合的角蛋白纤维，特别是毛发的氧化着色的试剂，其特征在于它们作为显影剂含有至少一种2,5-二氨基-1-苯基苯衍生物 通式和式（I）的新的2,5-二氨基-1-苯基苯衍生物，其中R 1至R 10基团中的至少一个不同于氢。

公开(公告)号：US5534037A

公开(公告)日：1996-07-09

申请号：US456814

申请日：1995-06-01

Applicant: Alex Junino ,  Alain Genet ,  Alain Lagrange

Inventor： Alex Junino ,  Alain Genet ,  Alain Lagrange

IPC: C07C233/03 ,  C07C323/32 ,  C07C323/36 ,  A61K7/13

CPC classification number: A61Q5/10 ,  A61K8/46 ,  C07C323/36

Abstract: The invention relates to a dye composition for keratinic fibers comprising an oxidation colorant precursor of the type ortho and/or para and a sulfured metaphenylenediamine having formula (I) ##STR1## wherein Z is alkyl, aralkyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aminoalkyl, as well as the acid salts thereof, with the condition that R.sub.1 and R.sub.2 do not represent simultaneously hydrogen when Z is alkyl or hydroxyalkyl, as well as the acid salts corresponding to the compounds of formula (I).

Abstract translation: 本发明涉及用于角蛋白纤维的染料组合物，其包含邻位和/或对位的氧化着色剂前体和具有式（I）的硫代偏苯二胺其中Z是烷基，芳烷基，单羟基烷基或多羟基烷基，芳基 或氨基烷基，以及其酸式盐，其中当Z是烷基或羟烷基时，R1和R2不同时代表氢，以及与式（I）化合物相应的酸式盐。