公开(公告)号：US4758580A

公开(公告)日：1988-07-19

申请号：US874547

申请日：1986-06-16

Applicant: Yoso Numasaki ,  Koichiro Takahashi ,  Isao Ohata

Inventor： Yoso Numasaki ,  Koichiro Takahashi ,  Isao Ohata

IPC: C07D233/60 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61P35/00 ,  C07D213/63 ,  C07D213/64 ,  C07D213/65 ,  C07D521/00 ,  A61K31/435

CPC classification number: C07D213/64 ,  A61K31/415 ,  A61K31/44 ,  C07D213/65 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

Abstract: This disclosure describes compositions of matter useful as growth inhibitors of transplanted tumors in mammals: and this invention discloses a method of inducing the regression and/or palliation of various types of tumors in mammals (mammary cancer, liver cancer, skin cancer, etc.), said method comprising giving to said mammals an effective amount of a compound of the following formula: ##STR1## [wherein A represents an imidazolyl group or a pyridyl group, l represents 0 or 1, m and n each, which may be the same of different, represents an integer of 1 to 6, and, R represents a hydrogen atom or a lower alkyl group], or a salt thereof; the invention also discloses a method of inhibition (or prevention) of metastasis of the various cancers.The above formula compounds have low toxicity, and it is expected to apply various types of administration thereof such as oral administration and parenteral administration. In particular, it is expected that the compounds are useful as new type of medical (anti-cancer) compounds which can be administered orally.

Abstract translation: 本公开描述了用作哺乳动物移植肿瘤生长抑制剂的物质的组合物：本发明公开了诱导哺乳动物（乳腺癌，肝癌，皮肤癌等）中各种类型肿瘤的消退和/或缓解的方法， 所述方法包括给予所述哺乳动物有效量的下式化合物：其中A代表咪唑基或吡啶基，l代表0或1，m和n各自可以相同 不同，表示1〜6的整数，R表示氢原子或低级烷基]或其​​盐; 本发明还公开了抑制（或预防）各种癌症转移的方法。 上述配方化合物的毒性低，预期可以应用各种类型的给药，例如口服给药和肠胃外给药。 特别地，预期这些化合物可用作可以口服给药的新型医疗（抗癌）化合物。

公开(公告)号：US4886818A

公开(公告)日：1989-12-12

申请号：US198099

申请日：1988-05-24

Applicant: Yoso Numasaki ,  Koichiro Takahashi ,  Isao Ohata

Inventor： Yoso Numasaki ,  Koichiro Takahashi ,  Isao Ohata

IPC: C07D233/60 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61P35/00 ,  C07D213/63 ,  C07D213/64 ,  C07D213/65 ,  C07D521/00

CPC classification number: C07D213/64 ,  A61K31/415 ,  A61K31/44 ,  C07D213/65 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

Abstract: This disclosure describes compositions of matter useful as growth inhibitors of transplanted tumors in mammals; and this invention discloses a method of inducing the regression and/or palliation of various types of tumors in mammals and which are susceptible to treatment by certain substituted phenoxy dimethyl alkanoic acids, esters or salts, said method comprising giving to said mammals an effective amount of a compound of the following formula: ##STR1## [wherein A represents an imidazolyl group or a pyridyl group,l represents 0 or 1,m and n each, which may be the same or different, represents an integer of 1 to 6, and,R represents a hydrogen atom or a lower alkyl group],or a salt thereof; the invention also discloses a method of inhibition (or prevention) of metastasis of the various cancers.The above formula compounds have low toxicity, and it is expected to apply various types of administration thereof such as oral administration and parenteral administration.

公开(公告)号：US4565823A

公开(公告)日：1986-01-21

申请号：US507024

申请日：1983-06-23

Applicant: Isao Ohata ,  Nobuo Sakamoto

Inventor： Isao Ohata ,  Nobuo Sakamoto

IPC: C07D211/90 ,  A61K31/44 ,  A61K31/455 ,  A61P3/06 ,  A61P9/10

CPC classification number: A61K31/44 ,  Y10S514/824

Abstract: A medical agent for suppressing arteriosclerosis or a hypolipemic agent comprising a composition containing nicardipine or a pharmaceutically acceptable salt thereof as the effective component.

Abstract translation: 用于抑制动脉硬化的药剂或含有尼卡地平或其药学上可接受的盐的组合物作为有效成分的降血糖药。

公开(公告)号：US4798838A

公开(公告)日：1989-01-17

申请号：US913722

申请日：1986-09-30

Applicant: Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

Inventor： Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

IPC: C07C43/225 ,  C07C51/353 ,  C07C59/68 ,  C07D213/65 ,  C07D233/60 ,  C07D233/61 ,  C07D277/22 ,  C07D277/24 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D311/16 ,  C07D417/04 ,  C07D521/00 ,  A61K31/425 ,  A61K31/44

CPC classification number: C07D231/12 ,  C07C43/225 ,  C07C51/353 ,  C07C59/68 ,  C07D213/65 ,  C07D233/56 ,  C07D249/08 ,  C07D277/24 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D311/16 ,  C07D417/04

Abstract: The present invention relates to novel phenoxy derivatives represented by the formula (I): ##STR1## wherein: A is an imidazolyl group, a pyridyl group, a pyridyloxy group, an oxo-substituted chromenyloxy group, a lower alkyl group, an amino group which may be substituted with a phenyl group or a lower alkyl group, or a carbamoyl group substituted with a cyclohexylamino group or an imidazolylalkyl group;B is a single bond, a thiazolyl group which may be substituted with a lower alkyl group, a group represented by the formula: --(CH.sub.2).sub.n --O--, --(CH.sub.2).sub.n CONH(CH.sub.2).sub.k -- or --(CH.sub.2).sub.n --N(R.sup.4)-- wherein k is 0 or an integer of 1 to 5, n is an integer of 1 to 6 and R.sup.4 is hydrogen or a lower alkyl group;m is 0 or an integer of 1 to 6;R.sup.1 is a hydroxyl group, an amino group or a lower alkoxy group;R.sup.2 and R.sup.3 which may be the same or different, represent a hydrogen atom or a lower alkyl group hereafter the same:and salts thereof.In the definition of the groups appearing in the formulae in the specification, the term "lower" refers to a straight or branched carbon chain having 1 to 5 carbon atoms, preferably 1 to 3 carbon atoms. Accordingly, specific examples of lower alkyl groups include a methyl group, an ethyl group, a propyl group, an isopropyl group, a butyl group, an isobutyl group, a sec-butyl group, a tert-butyl group, a pentyl (or amyl) group, an isopentyl group, a neopentyl group, a tert-pentyl group, etc.

公开(公告)号：US4795753A

公开(公告)日：1989-01-03

申请号：US913513

申请日：1986-09-30

Applicant: Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

Inventor： Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

IPC: C07C43/225 ,  C07C51/353 ,  C07C59/68 ,  C07D213/65 ,  C07D233/60 ,  C07D233/61 ,  C07D277/22 ,  C07D277/24 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D311/16 ,  C07D417/04 ,  C07D521/00 ,  A61K31/415 ,  A61K31/44

CPC classification number: C07D231/12 ,  C07C43/225 ,  C07C51/353 ,  C07C59/68 ,  C07D213/65 ,  C07D233/56 ,  C07D249/08 ,  C07D277/24 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D311/16 ,  C07D417/04

Abstract: The present invention relates to novel phenoxy derivatives represented by the formula (I): ##STR1## wherein: A is an imidazolyl group, a pyridyl group, a pyridyloxy group,B is group represented by the formula: --(CH.sub.2).sub.n --O--, --(CH.sub.2).sub.n CONH(CH.sub.2).sub.k -- or --(CH.sub.2).sub.n-N (R.sup.4)-- wherein k is 0 or an integer of 1 to 5, n is an integer of 1 to 6 and R.sup.4 is hydrogen or a lower alkyl group;m is 0 or an integer of 1 to 6;R.sup.1 is a hydroxyl group, an amino group or a lower alkoxy group;R.sup.2 and R.sup.3 which may be the same or different represent, a hydrogen atom or a lower alkyl group hereafter the same, having lipid lowering activity, and salts thereof.

公开(公告)号：US4690932A

公开(公告)日：1987-09-01

申请号：US871155

申请日：1986-05-30

Applicant: Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

Inventor： Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

IPC: A61K31/415 ,  A61K31/44 ,  A61K31/443 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  C07D233/56 ,  C07D233/64 ,  C07D311/16 ,  C07D405/12 ,  C07D521/00

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D311/16 ,  C07D405/12

Abstract: Novel coumarin compounds of the formula ##STR1## wherein R.sup.1 represents an imidazolyl group or a pyridyloxy group which may be substituted by lower alkyl group(s); R.sub.2 represents a hydrogen atom or a lower alkyl group; and m represents an integer of 1 to 6; and the salts thereof, which inhibit platelets aggregation.

Abstract translation: 式中，R1表示可被低级烷基取代的咪唑基或吡啶氧基的新型香豆素化合物。 R2表示氢原子或低级烷基; m表示1〜6的整数。 及其盐，其抑制血小板聚集。

公开(公告)号：US4942242A

公开(公告)日：1990-07-17

申请号：US261552

申请日：1988-10-21

Applicant: Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

Inventor： Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

IPC: C07C43/225 ,  C07C51/353 ,  C07C59/68 ,  C07D213/65 ,  C07D277/24 ,  C07D277/38 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D311/16 ,  C07D417/04 ,  C07D521/00

CPC classification number: C07D231/12 ,  C07C43/225 ,  C07C51/353 ,  C07C59/68 ,  C07D213/65 ,  C07D233/56 ,  C07D249/08 ,  C07D277/24 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D311/16 ,  C07D417/04

Abstract: Thiazolyl phenoxy derivatives are provided as well as pharmaceutical compositions containing such derivatives. The compositions are useful for lowering lipid activity in a subject and accordingly useful for reducing cholesterol and triglycerides.

Abstract translation: 提供噻唑基苯氧基衍生物以及含有这些衍生物的药物组合物。 该组合物可用于降低受试者的脂质活性，因此可用于降低胆固醇和甘油三酯。

公开(公告)号：US4794113A

公开(公告)日：1988-12-27

申请号：US203

申请日：1987-01-02

Applicant: Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

Inventor： Tadao Kojima ,  Shunji Kageyama ,  Minoru Okada ,  Isao Ohata ,  Noboru Sato

IPC: C07C43/225 ,  C07C51/353 ,  C07C59/68 ,  C07D213/65 ,  C07D233/60 ,  C07D233/61 ,  C07D277/22 ,  C07D277/24 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D311/16 ,  C07D417/04 ,  C07D521/00 ,  A61K31/415

CPC classification number: C07D231/12 ,  C07C43/225 ,  C07C51/353 ,  C07C59/68 ,  C07D213/65 ,  C07D233/56 ,  C07D249/08 ,  C07D277/24 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D311/16 ,  C07D417/04

Abstract: Imidazolyl phenoxy derivatives are provided as well as pharmaceutical compositions containing such derivatives. The compositions useful for lowering lipid activity in a subject and accordingly useful for reducing cholesterol and triglycerides.

Abstract translation: 提供咪唑基苯氧基衍生物以及含有这些衍生物的药物组合物。 该组合物可用于降低受试者的脂质活性，因此可用于降低胆固醇和甘油三酯。