公开(公告)号：US06989401B2

公开(公告)日：2006-01-24

申请号：US10333266

申请日：2001-07-19

Applicant: Kazuhiro Maeda ,  Shuji Sonda ,  Tadahiro Takemoto ,  Tomokazu Goto ,  Fujio Kobayashi ,  Masahiko Kajii ,  Naruyasu Komorita ,  Fumihiro Hirayama

Inventor： Kazuhiro Maeda ,  Shuji Sonda ,  Tadahiro Takemoto ,  Tomokazu Goto ,  Fujio Kobayashi ,  Masahiko Kajii ,  Naruyasu Komorita ,  Fumihiro Hirayama

IPC: A61K31/403 ,  C07D207/408

CPC classification number: C07D209/48 ,  A61K31/185 ,  C07C309/11 ,  C07C309/15 ,  C07C309/51

Abstract: The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.

公开(公告)号：US06610729B1

公开(公告)日：2003-08-26

申请号：US09701043

申请日：2000-11-22

Applicant: Tomokazu Gotou ,  Shinji Takeda ,  Kazuhiro Maeda ,  Tomohiro Yoshida ,  Naoki Sugiyama ,  Tadahiro Takemoto

Inventor： Tomokazu Gotou ,  Shinji Takeda ,  Kazuhiro Maeda ,  Tomohiro Yoshida ,  Naoki Sugiyama ,  Tadahiro Takemoto

IPC: C07C25906

CPC classification number: C07D209/48 ,  C07C259/06 ,  C07D209/46 ,  C07D233/72 ,  C07D307/52 ,  C07D309/12 ,  C07D405/12 ,  C07D405/14

Abstract: The present invention relates to a hydroxamic acid derivative of the formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition containing the derivative or a salt thereof, and to pharmaceutical use thereof. The hydroxamic acid derivative and a pharmacologically acceptable salt thereof of the present invention have an inhibitory activity of TNF &agr; production, and are useful for, for example, the prophylaxis and treatment of the diseases such as autoimmune diseases and inflammatory diseases (e.g., sepsis, MOF, rheumatoid arthritis, Crohn's disease, cachexia, myasthenia gravis, systemic lupus erythematosus, asthma, I type diabetes, psoriasis and the like), and the like.

Abstract translation: 本发明涉及式（I）的异羟肟酸衍生物，其中各符号如说明书中所定义，其药理学上可接受的盐，含有其衍生物或其盐的药物组合物及其药学用途。 本发明的异羟肟酸衍生物及其药理学上可接受的盐具有TNFα产生的抑制活性，可用于例如自身免疫性疾病和炎症性疾病（例如败血症， MOF，类风湿关节炎，克罗恩病，恶病质，重症肌无力，系统性红斑狼疮，哮喘，I型糖尿病，牛皮癣等）等。

公开(公告)号：US5262415A

公开(公告)日：1993-11-16

申请号：US850817

申请日：1992-03-13

Applicant: Tadahiro Takemoto ,  Masahiro Eda ,  Mitsuyoshi Hihara ,  Takehiro Okada ,  Hiroshi Sakashita ,  Miyuki Eiraku ,  Chikara Fukaya ,  Norifumi Nakamura ,  Masanori Sugiura ,  Sumio Matzno ,  Maki Goda ,  Yasumi Uchida

Inventor： Tadahiro Takemoto ,  Masahiro Eda ,  Mitsuyoshi Hihara ,  Takehiro Okada ,  Hiroshi Sakashita ,  Miyuki Eiraku ,  Chikara Fukaya ,  Norifumi Nakamura ,  Masanori Sugiura ,  Sumio Matzno ,  Maki Goda ,  Yasumi Uchida

IPC: A61K31/44 ,  A61K31/4406 ,  A61K31/4427 ,  A61K31/495 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07D213/75 ,  C07D213/76 ,  C07D213/77 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  A61K31/54 ,  C07D211/56 ,  C07D211/72 ,  C07D401/00

CPC classification number: C07D213/75 ,  C07D213/76 ,  C07D213/77 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D405/12 ,  C07D413/10

Abstract: An aminopyridine compound represented by the formula: ##STR1## wherein n represents 0 or 1; Z represents .dbd.S, .dbd.O, .dbd.NCN or .dbd.CHNO.sub.2 ; R.sub.1 represents --CN, --NR.sub.3 R.sub.4, --CONR.sub.3 R.sub.4, --NHNR.sub.3 R.sub.4, --NHCONHR.sub.3, --NHSO.sub.2 R.sub.3 or --SR.sub.3 ; R.sub.2 represents H, or substituted or unsubstituted alkyl; R.sub.3 and R.sub.4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R.sub.3 and R.sub.4 may form a heterocyclic ring together with a nitrogen atom to which R.sub.3 and R.sub.4 are bound, through another heteroatom or without it; or an acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.

公开(公告)号：US5371086A

公开(公告)日：1994-12-06

申请号：US53869

申请日：1993-04-29

Applicant: Tadahiro Takemoto ,  Masahiro Eda ,  Mitsuyoshi Hihara ,  Takehiro Okada ,  Hiroshi Sakashita ,  Miyuki Eiraku ,  Chikara Fukaya ,  Norifumi Nakamura ,  Masanori Sugiura ,  Sumio Matzno ,  Maki Goda ,  Yasumi Uchida

Inventor： Tadahiro Takemoto ,  Masahiro Eda ,  Mitsuyoshi Hihara ,  Takehiro Okada ,  Hiroshi Sakashita ,  Miyuki Eiraku ,  Chikara Fukaya ,  Norifumi Nakamura ,  Masanori Sugiura ,  Sumio Matzno ,  Maki Goda ,  Yasumi Uchida

IPC: C07D213/75 ,  C07D213/76 ,  C07D213/77 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D405/12 ,  C07D413/12 ,  A61K31/495 ,  A61K31/54 ,  C07D211/56 ,  C07D401/00

CPC classification number: C07D213/75 ,  C07D213/76 ,  C07D213/77 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D405/12 ,  C07D413/10

Abstract: An aminopyridine compound represented by the formula: ##STR1## wherein n represents 0 or 1; Z represents .dbd.S, .dbd.NCN or .dbd.CHNO.sub.2 ; R.sub.1 represents --NR.sub.3 R.sub.4, --NHNR.sub.3 R.sub.4, --NHCONHR.sub.3 or --NHSO.sub.2 R.sub.3 ; R.sub.2 represents H, or substituted or unsubstituted alkyl; R.sub.3 and R.sub.4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R.sub.3 and R.sub.4 may form a heterocyclic ring together with a nitrogen atom to which R.sub.3 and R.sub.4 are bound, through another heteroatom or without it; an optical isomer thereof or art acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.

Abstract translation: 由下式表示的氨基吡啶化合物：其中n表示0或1; Z表示= S，= NCN或= CHNO2; R 1表示-NR 3 R 4，-NHNR 3 R 4，-NHCONHR 3或-NHSO 2 R 3; R 2表示H或取代或未取代的烷基; R 3和R 4可以相同或不同，表示H，取代或未取代的烷基，芳基，取代或未取代的酰基或烷氧基羰基; 并且R 3和R 4可以与R3和R4连接的氮原子一起通过另一个杂原子或不与其形成杂环; 其光学异构体或其酸性盐，其药理作用优异，作为循环系统疾病药物的副作用被抑制。