公开(公告)号：US08470829B2

公开(公告)日：2013-06-25

申请号：US11662289

申请日：2005-09-09

申请人： Kazutaka Tachibana ,  Haruhiko Sato ,  Masateru Ohta ,  Mitsuaki Nakamura ,  Takuya Shiraishi ,  Hitoshi Yoshino ,  Takashi Emura ,  Akie Honma ,  Etsuro Onuma ,  Hiromitsu Kawata ,  Kenji Taniguchi

发明人： Kazutaka Tachibana ,  Haruhiko Sato ,  Masateru Ohta ,  Mitsuaki Nakamura ,  Takuya Shiraishi ,  Hitoshi Yoshino ,  Takashi Emura ,  Akie Honma ,  Etsuro Onuma ,  Hiromitsu Kawata ,  Kenji Taniguchi

IPC分类号： A61K31/426 ,  A61K31/454 ,  A61K31/428 ,  A61K31/4166 ,  C07D401/12 ,  C07D403/12 ,  C07D277/82 ,  C07D233/72 ,  C07D233/70

CPC分类号： C07D417/04 ,  C07D211/58 ,  C07D233/74 ,  C07D233/86 ,  C07D277/82 ,  C07D401/04

摘要： An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted C1-4 alkyl group; E is independently selected from a C1-6 alkyl group; R2 and R3 are independently selected from C1-6 alkyls; X1 and X2 are independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is —CON(—Ra)—, —CO—, —OOO—, —NRa—C(═NH)NRb—, —NRa—C(═N—CN)NRb—, —N(—Ra)COO—, —C(═NH)—, —SO2—, —SO2N(—Ra)—, —SO2NR1—, —N(—Ra)CO—, —N(—Ra)CON(—Rb)—, —N(COR1)CO—, —N(—Ra)SO2—, —N(SO2R1)SO2—, —N(—Ra)— or —N(—Ra)SO2N(—Rb)—; R1 is independently a hydrogen atom, a hydroxyl group, or substituted or unsubstituted group selected from C1-6 alkyl group, heterocyclic group, aryl group, C3-8 cycloalkyl group and C3-8 cycloalkenyl group; or salt or prodrug thereof.

摘要翻译： 由式（I）表示的咪唑衍生物：其中Q是：A是氢，卤素或取代或未取代的C1-4烷基; E独立地选自C 1-6烷基; R2和R3独立地选自C1-6烷基; X1和X2独立地选自O和S; Y选自取代或未取代的亚芳基和取代或未取代的二价5元或6元单环或8至10元稠合杂环基; Z是-CON（-R a） - ， - CO - ， - OO-，-NR a -C（= NH）NR b - ， - NR a -C（= N-CN）NR b - ， - N（-R a） ，-C（= NH） - ， - SO 2 - ， - SO 2 N（-R a） - ， - SO 2 NR 1 - ， - N（-R a）CO - ， - N（-R a）CON（-R b） COR 1）CO - ， - N（-R a）SO 2 - ， - N（SO 2 R 1）SO 2 - ， - N（-R a） - 或-N（-R a）SO 2 N（-R b） R 1独立地为氢原子，羟基或取代或未取代的选自C 1-6烷基，杂环基，芳基，C 3-8环烷基和C 3-8环烯基的基团; 或其盐或前药。

公开(公告)号：US20110306615A1

公开(公告)日：2011-12-15

申请号：US11662289

申请日：2005-09-09

申请人： Kazutaka Tachibana ,  Haruhiko Sato ,  Masateru Ohta ,  Mitsuaki Nakamura ,  Takuya Shiraishi ,  Hitoshi Yoshino ,  Takashi Emura ,  Akie Honma ,  Etsuro Onuma ,  Hiromitsu Kawata ,  Kenji Taniguchi

发明人： Kazutaka Tachibana ,  Haruhiko Sato ,  Masateru Ohta ,  Mitsuaki Nakamura ,  Takuya Shiraishi ,  Hitoshi Yoshino ,  Takashi Emura ,  Akie Honma ,  Etsuro Onuma ,  Hiromitsu Kawata ,  Kenji Taniguchi

IPC分类号： A61K31/454 ,  C07D233/74 ,  C07D417/10 ,  C07D403/12 ,  C07D233/86 ,  C07D413/12 ,  A61K31/4166 ,  A61K31/428 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/5377 ,  A61P35/00 ,  A61P13/08 ,  A61Q7/00 ,  A61P15/00 ,  A61P17/10 ,  C07D401/04

CPC分类号： C07D417/04 ,  C07D211/58 ,  C07D233/74 ,  C07D233/86 ,  C07D277/82 ,  C07D401/04

摘要： According to the present invention, a compound represented by formula (I): wherein Q is: A is a hydrogen atom, a halogen atom, —ORa or a C1-4 alkyl group which may be substituted by one or more halogen atoms; E is independently selected from a C1-6 alkyl group; m is selected from integers from 0 to 3; R2 and R3 are independently selected from a C1-6 alkyl group; X1 and X2 are independently selected from O and S; Y is selected from an arylene group and a divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group, wherein the arylene group and the heterocyclic group may be substituted by 1 to 3 substituents independently selected from E1; E1 is independently selected from a hydroxyl group, a halogen atom, a C1-4 alkyl group, a cyano group, a C1-4 alkoky group, a carbamoyl group, a C1-4 alkylcarbamoyl group, a di(C1-4 alkyl)carbamoyl group, an amino group, a C1-4 alkylamino group, a di(C1-4 alkylamino group, a sulfamoyl group, a C1-4 alkylsulfamoyl group and a di(C1-4 alkyl)sulfamoyl group; Z is —CON(—Ra)—, —CO—, —COO—, —NRa—C(═NH)NRb—, —NRa—C(═N—CN)NRb—, —N(—Ra)COO—, —C(═NH)—, —SO2—, —SO2N(—Ra)—, —SO2NR1—, —N(—Ra)CO—, —N(—Ra)CON(—Rb)—, —N(COR1)CO—, —N(—Ra)SO2—, —N(SO2R1)SO2—, —N(—Ra)— or —N(—Ra)SO2N(—Rb)—; R1 is independently a hydrogen atom, a hydroxyl group, a C1-6 alkyl group which may be substituted by one or more substituents, a heterocyclic group which may be substituted by one or more substituents, an aryl group which may be substituted by one or more substituents, a C3-8 cycloalkyl group which may be substituted by one or more substituents or a C3-8 cycloalkenyl group which may be substituted by one or more substituents, or a salt, prodrug or solvate thereof is provided. Furthermore, a pharmaceutical composition containing the compound, and the like are also provided.

公开(公告)号：US4732906A

公开(公告)日：1988-03-22

申请号：US840680

申请日：1986-03-18

申请人： Hiroshi Koga ,  Takashi Dan ,  Haruhiko Sato ,  Etsuro Onuma

发明人： Hiroshi Koga ,  Takashi Dan ,  Haruhiko Sato ,  Etsuro Onuma

IPC分类号： A61K31/357 ,  A61K31/42 ,  A61P7/10 ,  C07D261/00 ,  C07D317/00 ,  C07D498/04 ,  C07D261/20

CPC分类号： C07D498/04

摘要： Dioxolobenzisoxazole derivatives of the formula ##STR1## wherein R.sub.1 is a phenyl group which may be substituted with a halogen atom, a lower alkyl group having 1-3 carbon atoms or a lower haloalkyl group, or a thienyl group; R.sub.2 is a hydrogen atom or a lower alkyl group having 1-4 carbon atoms; and X and Y which may be the same or different represent a hydrogen atom or a halogen atom, as well as non-toxic salts thereof wherein R.sub.2 is a hydrogen atom, a process for preparing the same and a pharmaceutical composition containing the same are disclosed.The derivatives have diuretic and uricosuric activities and, therefore, are useful as a drug for treating hyperuricemia or hypertension.

摘要翻译： 其中R 1是可以被卤素原子取代的苯基，具有1-3个碳原子的低级烷基或低级卤代烷基，或噻吩基的式Ⅱ的二氧代联苯并恶唑衍生物; R2是氢原子或具有1-4个碳原子的低级烷基; 和可以相同或不同的X和Y表示氢原子或卤素原子，以及其中R2是氢原子的无毒盐，其制备方法和含有它们的药物组合物 。 衍生物具有利尿和尿酸活性，因此可用作治疗高尿酸血症或高血压的药物。

公开(公告)号：US4791209A

公开(公告)日：1988-12-13

申请号：US860210

申请日：1986-05-06

申请人： Haruhiko Sato ,  Hiroshi Koga ,  Takashi Dan ,  Etsuro Onuma

发明人： Haruhiko Sato ,  Hiroshi Koga ,  Takashi Dan ,  Etsuro Onuma

IPC分类号： C07D498/04 ,  A61K31/42

CPC分类号： C07D498/04

摘要： Novel furobenzisoxazole derivatives of the formula (I): ##STR1## (wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 which may be the same or different represent a hydrogen atom, a halogen atom, or a lower alkyl group having 1-4 carbon atoms; R.sub.5 is a hydroxymethyl group, a carboxyl group or a lower alkoxy carbonyl group having 1-3 carbon atoms; and X is a sulfur atom or a --CH.dbd.CH-- group), as well as intoxic salts thereof when R.sub.5 is a carboxyl group, and process for preparing the same are disclosed.The derivatives of formula (I) and nontoxic salts thereof have hypotensive, uricosuric and diuretic activities and hence ae useful as therapeutics for treating hyperuricemia, edema and hypertension.

摘要翻译： 式（I）的新型呋喃苯并异恶唑衍生物：其中R 1，R 2，R 3和R 4可以相同或不同，表示氢原子，卤素原子或具有1-4个碳原子的低级烷基 碳原子; R5是羟基甲基，羧基或具有1-3个碳原子的低级烷氧基羰基; X是硫原子或-CH = CH-基团），以及当其为R5时的中性盐 羧基，及其制备方法。 式（I）的衍生物及其无毒盐具有降血压，尿酸和利尿活性，因此可用作治疗高尿酸血症，水肿和高血压的治疗剂。

公开(公告)号：US07655227B1

公开(公告)日：2010-02-02

申请号：US10019501

申请日：2000-07-03

申请人： Etsuro Ogata ,  Etsuro Onuma ,  Toshiaki Tsunenari ,  Hidemi Saito ,  Yumiko Azuma

发明人： Etsuro Ogata ,  Etsuro Onuma ,  Toshiaki Tsunenari ,  Hidemi Saito ,  Yumiko Azuma

IPC分类号： A61K39/395 ,  A61K38/22 ,  C07K16/26 ,  C12P21/08

CPC分类号： C07K16/26

摘要： The present invention provides an agent for ameliorating low vasopressin level, which comprises, as an active ingredient, a substance capable of inhibiting the binding between parathyroid hormone-related peptide (PTHrP) and a receptor thereof; and an agent for ameliorating a symptom caused by a decrease in vasopressin level, which comprises, as an active ingredient, a substance capable of inhibiting the binding between parathyroid hormone-related peptide (PTHrP) and a receptor thereof.

摘要翻译： 本发明提供一种用于改善低加压素水平的药剂，其包含作为活性成分的能够抑制甲状旁腺激素相关肽（PTHrP）与其受体之间的结合的物质; 以及用于改善由加压素水平降低引起的症状的药剂，其包含作为活性成分的能够抑制甲状旁腺激素相关肽（PTHrP）与其受体之间的结合的物质。