公开(公告)号：US08440689B2

公开(公告)日：2013-05-14

申请号：US12972333

申请日：2010-12-17

申请人： Yasuyoshi Arikawa ,  Qing Dong ,  Victoria Feher ,  Benjamin Jones ,  Betty Lam ,  Zhe Nie ,  Christopher Smith ,  Masashi Takahashi

发明人： Yasuyoshi Arikawa ,  Qing Dong ,  Victoria Feher ,  Benjamin Jones ,  Betty Lam ,  Zhe Nie ,  Christopher Smith ,  Masashi Takahashi

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P11/06 ,  A61P19/02 ,  A61P17/06 ,  A61P35/00 ,  C07D487/04 ,  A61K31/519

CPC分类号： C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

摘要： Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

公开(公告)号：US08334301B2

公开(公告)日：2012-12-18

申请号：US12680184

申请日：2008-09-24

申请人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Keizo Hirase

发明人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Keizo Hirase

IPC分类号： A61K31/415 ,  C07D233/00

CPC分类号： C07D333/20 ,  C07D231/18 ,  C07D231/38 ,  C07D231/40 ,  C07D231/42 ,  C07D233/24 ,  C07D233/42 ,  C07D333/32 ,  C07D333/34 ,  C07D401/12 ,  C07D403/04 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14

摘要： Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.A compound represented by the formula (I) or a salt thereof: wherein ring A is a saturated or unsaturated 5-membered heterocycle containing, as a ring-constituting atom besides carbon atoms, at least one heteroatom selected from a nitrogen atom, an oxygen atom and a sulfur atom, the ring-constituting atoms X1 and X2 are the same or different and each is C or N, the ring-constituting atoms X3 and X4 are the same or different and each is C, N, O or S (provided that a pyrrole ring wherein X1 is N is excluded from ring A), and when the ring-constituting atom X3 or X4 is C or N, each ring-constituting atom optionally has substituent(s) selected from an optionally substituted alkyl, an acyl, an optionally substituted hydroxy, an optionally substituted mercapto, an optionally substituted amino, a halogen, a cyano and a nitro; R1 and R2 are each a cyclic group optionally having substituent(s); R3 and R4 are each H or alkyl, or R3 and R4 form, together with the adjacent N, an nitrogen-containing heterocycle; and Y is a spacer.

摘要翻译： 提供具有优异的酸分泌抑制作用的化合物，其表现出抗溃疡活性等。 由式（I）表示的化合物或其盐：其中环A是饱和或不饱和的5元杂环，其含有除碳原子之外的构成环的原子，至少一个选自氮原子，氧原子的杂原子 原子和硫原子，构成环的原子X1和X2相同或不同，分别为C或N，构成成环原子X3和X4相同或不同，分别为C，N，O或S（ 条件是其中X1为N的吡咯环不包括在环A）中，并且当构成环的原子X 3或X 4为C或N时，每个构成环的原子任选具有选自任选取代的烷基， 酰基，任选取代的羟基，任选取代的巯基，任选取代的氨基，卤素，氰基和硝基; R1和R2各自为任选具有取代基的环状基团; R3和R4各自为H或烷基，或R3和R4与相邻的N一起形成含氮杂环; Y是间隔物。

公开(公告)号：US20100210696A1

公开(公告)日：2010-08-19

申请号：US12680184

申请日：2008-09-24

申请人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Keizo Hirase

发明人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Keizo Hirase

IPC分类号： A61K31/426 ,  C07D233/61 ,  A61K31/4164 ,  C07D403/06 ,  C07D277/22 ,  C07D411/14 ,  A61K31/337 ,  A61P1/00 ,  A61P1/04

CPC分类号： C07D333/20 ,  C07D231/18 ,  C07D231/38 ,  C07D231/40 ,  C07D231/42 ,  C07D233/24 ,  C07D233/42 ,  C07D333/32 ,  C07D333/34 ,  C07D401/12 ,  C07D403/04 ,  C07D409/14 ,  C07D417/06 ,  C07D417/14

摘要： Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.A compound represented by the formula (I) or a salt thereof: wherein ring A is a saturated or unsaturated 5-membered heterocycle containing, as a ring-constituting atom besides carbon atoms, at least one heteroatom selected from a nitrogen atom, an oxygen atom and a sulfur atom, the ring-constituting atoms X1 and X2 are the same or different and each is C or N, the ring-constituting atoms X3 and X4 are the same or different and each is C, N, 0 or S (provided that a pyrrole ring wherein X1 is N is excluded from ring A), and when the ring-constituting atom X3 or X4 is C or N, each ring-constituting atom optionally has substituent(s) selected from an optionally substituted alkyl, an acyl, an optionally substituted hydroxy, an optionally substituted mercapto, an optionally substituted amino, a halogen, a cyano and a nitro;R1 and R2 are each a cyclic group optionally having substituent(s); R3 and R4 are each H or alkyl, or R3 and R4 form, together with the adjacent N, an nitrogen-containing heterocycle; and Y is a spacer.

摘要翻译： 提供具有优异的酸分泌抑制作用的化合物，其表现出抗溃疡活性等。 由式（I）表示的化合物或其盐：其中环A是饱和或不饱和的5元杂环，其含有除碳原子之外的构成环的原子，至少一个选自氮原子，氧原子的杂原子 原子和硫原子，构成环的原子X1和X2相同或不同，分别为C或N，构成环的原子X3和X4相同或不同，分别为C，N，O或S（ 条件是其中X1为N的吡咯环不包括在环A）中，并且当构成环的原子X 3或X 4为C或N时，每个构成环的原子任选具有选自任选取代的烷基， 酰基，任选取代的羟基，任选取代的巯基，任选取代的氨基，卤素，氰基和硝基; R1和R2各自为任选具有取代基的环状基团; R3和R4各自为H或烷基，或R3和R4与相邻的N一起形成含氮杂环; Y是间隔物。

公开(公告)号：US08592597B2

公开(公告)日：2013-11-26

申请号：US13061078

申请日：2009-08-26

申请人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

发明人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

IPC分类号： C07D401/14

CPC分类号： A61K31/444 ,  C07D401/14

摘要： The present invention relates to a compound represented by the formula: wherein A is pyridyl group having at least one substituent wherein R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, R4 and R6 are each a hydrogen atom, a halogen atom or a C1-6 alkyl group optionally substituted by halogen, R5 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, and R7 is a hydrogen atom or a C1-6 alkyl group optionally substituted by halogen or a salt thereof, or a pharmaceutical composition containing the same.

公开(公告)号：US20100056577A1

公开(公告)日：2010-03-04

申请号：US12547778

申请日：2009-08-26

申请人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

发明人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

IPC分类号： A61K31/444 ,  C07D401/14 ,  A61P1/04

CPC分类号： A61K31/444 ,  C07D401/14

摘要： The present invention relates to a compound represented by the formula: wherein A is pyridyl group having at least one substituent wherein R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, R4 and R6 are each a hydrogen atom, a halogen atom or a C1-6 alkyl group optionally substituted by halogen, R5 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, and R7 is a hydrogen atom or a C1-6 alkyl group optionally substituted by halogen or a salt thereof, or a pharmaceutical composition containing the same.

摘要翻译： 本发明涉及由下式表示的化合物：其中A是具有至少一个取代基的吡啶基，其中R 1，R 2和R 3各自为氢原子，卤素原子，任选被卤素取代的C 1-6烷基或 任选被卤素取代的C 1-6烷氧基，R 4和R 6各自为氢原子，卤素原子或任选被卤素取代的C 1-6烷基，R 5为氢原子，卤素原子，C 1-6烷基 任选被卤素取代或被卤素任意取代的C 1-6烷氧基，R 7是氢原子或任选被卤素或其盐取代的C 1-6烷基，或含有它们的药物组合物。

公开(公告)号：US07456162B2

公开(公告)日：2008-11-25

申请号：US11081615

申请日：2005-03-17

申请人： Shigenori Ohkawa ,  Yasuyoshi Arikawa ,  Kouki Kato ,  Masahiro Okura ,  Masaki Setoh

发明人： Shigenori Ohkawa ,  Yasuyoshi Arikawa ,  Kouki Kato ,  Masahiro Okura ,  Masaki Setoh

IPC分类号： A61K31/33 ,  C07D405/00 ,  C07D411/00 ,  C07D209/00

CPC分类号： C07D307/79 ,  C07D405/04 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06

摘要： Compounds represented by the formula: wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring, W indicates a group represented by the formula: wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, R3 indicates a C6-14 aryl group, or salts thereof. The compounds have an excellent action to inhibit neurodegeneration as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as drugs for nerve degenerative diseases.

摘要翻译： 由下式表示的化合物：其中R 1和R 2是氢原子，烃基或杂环基，或R 1和R 2 可以与相邻的碳原子一起形成3-至8-元的杂环或杂环，W表示由下式表示的基团：其中R 4表示 （1）可以被芳族基团取代的脂族烃基，或（2）含有芳基的酰基，R 5是氢原子，C 1-6 烷基或酰基，R 3表示C 6-14芳基或其盐。 该化合物具有抑制神经变性以及优异的脑渗透性的优异作用，毒性低，因此可用作神经退行性疾病的药物。

公开(公告)号：US20080262042A1

公开(公告)日：2008-10-23

申请号：US12072421

申请日：2008-02-26

申请人： Masahiro Kajino ,  Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Keizo Hirase ,  Koji Ono

发明人： Masahiro Kajino ,  Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Keizo Hirase ,  Koji Ono

IPC分类号： A61K31/444 ,  C07D401/04 ,  A61K31/4439 ,  A61P35/00 ,  A61P1/02 ,  C07D401/14

CPC分类号： C07D401/04

摘要： The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity, which is represented by the formula (I) wherein R1 is an optionally substituted cyclic group, R2 is a substituent, R3 is an optionally substituted alkyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a halogen atom, a cyano group or a nitro group, R4 and R5 are each a hydrogen atom, an optionally substituted alkyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a halogen atom, a cyano group or a nitro group, R6 and R6′ are each a hydrogen atom or an alkyl group, and n is an integer of 0-3, or a salt thereof.

摘要翻译： 本发明提供具有优异的酸分泌抑制作用并显示抗溃疡活性的化合物，其由式（I）表示，其中R 1是任选取代的环状基团，R 2 R 3是取代基，R 3是任选取代的烷基，酰基，任选取代的羟基，任选取代的氨基，卤素原子，氰基或硝基 基团R 4和R 5各自为氢原子，任选取代的烷基，酰基，任选取代的羟基，任选取代的氨基， 卤素原子，氰基或硝基，R 6和R 6'各自为氢原子或烷基，n为0-3的整数 ，或其盐。

公开(公告)号：US20070293532A1

公开(公告)日：2007-12-20

申请号：US11658416

申请日：2005-07-28

申请人： Atsushi Hasuoka ,  Yasuyoshi Arikawa

发明人： Atsushi Hasuoka ,  Yasuyoshi Arikawa

IPC分类号： A61K31/437 ,  A61P1/04 ,  C07D471/04

CPC分类号： C07D471/04

摘要： Provision of a compound having a superior proton pump action, which shows an antiulcer activity and the like after conversion to an in vivo proton pump inhibitor, a production method thereof and use thereof. A pyrrolo[2,3-c]pyridine compound represented by the formula: wherein each symbol is as defined in the specification.

摘要翻译： 提供具有优异的质子泵作用的化合物，其在转化成体内质子泵抑制剂后显示出抗溃疡活性等，其制备方法和用途。 由下式表示的吡咯并[2,3-c]吡啶化合物：其中每个符号如说明书中所定义。

公开(公告)号：US20050187238A1

公开(公告)日：2005-08-25

申请号：US11081615

申请日：2005-03-17

申请人： Shigenori Ohkawa ,  Yasuyoshi Arikawa ,  Kouki Kato ,  Masahiro Okura ,  Masaki Setoh

发明人： Shigenori Ohkawa ,  Yasuyoshi Arikawa ,  Kouki Kato ,  Masahiro Okura ,  Masaki Setoh

IPC分类号： A61P25/28 ,  C07D307/79 ,  C07D405/04 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06 ,  C07D491/056 ,  C07D491/107 ,  A61K31/4747 ,  C07D493/04

CPC分类号： C07D307/79 ,  C07D405/04 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06

摘要： Compounds represented by the formula: wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring, W indicates (i) a group represented by the formula: wherein ring B indicates a 5- to 7-membered ring, or (ii) a group represented by the formula: wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, provided that, when W is Wa, R3 is hydrogen atom, a hydrocarbon group or a heterocyclic group, when W is Wb, R3 indicates a C6-14 aryl group, or salts thereof or prodrugs thereof have an excellent action to inhibit neurodegeneration and the like as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as prophylactic or therapeutic drugs for nerve degenerative diseases and the like.

摘要翻译： 由下式表示的化合物：其中R 1和R 2是氢原子，烃基或杂环基，或R 1和R 2 可以与相邻的碳原子一起形成3-至8-元的杂环或杂环，W表示（i）由下式表示的基团：其中环B表示5-至 或（ii）由下式表示的基团：其中R 4表示（1）可被芳基取代的脂族烃基，或（2）酰基 含有芳基的基团R 5是氢原子，C 1-6烷基或酰基，条件是当W是Wa时，R“ 当W为Wb时，R 3为氢原子，烃基或杂环基，R 3为C 6-14芳基，或其盐 或其前药具有抑制神经变性等优异的作用以及优异的脑渗透性，并且l 因此可用作神经变性疾病等的预防或治疗药物。

公开(公告)号：US08969387B2

公开(公告)日：2015-03-03

申请号：US12547778

申请日：2009-08-26

申请人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

发明人： Haruyuki Nishida ,  Yasuyoshi Arikawa ,  Ikuo Fujimori

IPC分类号： A61K31/4439 ,  C07D401/14 ,  A61K31/444

CPC分类号： A61K31/444 ,  C07D401/14

摘要： The present invention relates to a compound represented by the formula: wherein A is pyridyl group having at least one substituent wherein R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, R4 and R6 are each a hydrogen atom, a halogen atom or a C1-6 alkyl group optionally substituted by halogen, R5 is a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally substituted by halogen or a C1-6 alkoxy group optionally substituted by halogen, and R7 is a hydrogen atom or a C1-6 alkyl group optionally substituted by halogen or a salt thereof, or a pharmaceutical composition containing the same.

摘要翻译： 本发明涉及由下式表示的化合物：其中A是具有至少一个取代基的吡啶基，其中R 1，R 2和R 3各自为氢原子，卤素原子，任选被卤素取代的C 1-6烷基或 任选被卤素取代的C 1-6烷氧基，R 4和R 6各自为氢原子，卤素原子或任选被卤素取代的C 1-6烷基，R 5为氢原子，卤素原子，C 1-6烷基 任选被卤素取代或被卤素任意取代的C 1-6烷氧基，R 7是氢原子或任选被卤素或其盐取代的C 1-6烷基，或含有它们的药物组合物。