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1. 发明授权

US4921851A Cephem compounds, their production and use 失效
标题翻译：头孢烯化合物，其生产和使用
公开(公告)号：US4921851A
公开(公告)日：1990-05-01
申请号：US396758
申请日：1989-08-22
申请人： Shoji Kishimoto , Kiminori Tomimatsu , Akio Miyake , Yoshinobu Yoshimura
发明人： Shoji Kishimoto , Kiminori Tomimatsu , Akio Miyake , Yoshinobu Yoshimura
IPC分类号： C07D501/00 , C07D501/46 , C07D519/00
CPC分类号： C07D501/46 , C07D501/00 , C07D519/00
摘要： This invention relates to a compound of the formula: ##STR1## wherein Q is nitrogen or CH; R.sup.1 is hydrogen or a lower alkyl group which may be substituted; and ring A is a pyridine or pyridazine ring which is substituted at the ring-constituting carbon atom by a group of the formula:--E--(CH.sub.2).sub.n --R.sup.2in which E is sulfur or NH; R.sup.2 is an amino, carbamoylamino, formylamino, acetylamino, N-formimidoylamino, N-acetimidoylamino, lower alkylamino, hydroxyl or carbamoyloxy group; and n is an integer of 2 to 4, or a pharmaceutically acceptable salt thereof. The compound (I) or a pharmaceutically acceptable sale thereof has excellent antibacterial activity and is used as antibiotics.
摘要翻译：本发明涉及下式的化合物：其中Q是氮或CH; R1是氢或可被取代的低级烷基; 环A为吡啶或哒嗪环，其在环的构成碳原子上被下列基团取代：其中E为硫或NH的-E-（CH2）n-R2; R2是氨基，氨基甲酰基氨基，甲酰氨基，乙酰氨基，N-甲脒基氨基，N-亚氨代乙酰氨基，低级烷基氨基，羟基或氨基甲酰氧基; n为2〜4的整数，或其药学上可接受的盐。化合物（I）或其药学上可接受的销售具有优异的抗菌活性并用作抗生素。

2. 发明授权

US4942159A Cephem compounds, their production and use 失效
标题翻译：头孢烯化合物，其生产和使用
公开(公告)号：US4942159A
公开(公告)日：1990-07-17
申请号：US235566
申请日：1988-08-24
申请人： Shoji Kishimoto , Kiminori Tomimatsu , Akio Miyake
发明人： Shoji Kishimoto , Kiminori Tomimatsu , Akio Miyake
IPC分类号： C07D501/46 , C07D519/00
CPC分类号： C07D501/46 , C07D519/00
摘要： Novel cephem compounds of the general formula: ##STR1## wherein R.sup.1 is a lower alkyl group, and salts and esters thereof, showing excellent and balanced antibacterial activity against a broad spectrum of bacteria, especially by rectal administration, and their production and use as antimicrobial agents are described.

3. 发明授权

US4833134A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4833134A
公开(公告)日：1989-05-23
申请号：US84882
申请日：1987-08-13
申请人： Shoji Kishimoto , Kiminori Tomimatsu , Michiyuki Sendai
发明人： Shoji Kishimoto , Kiminori Tomimatsu , Michiyuki Sendai
IPC分类号： A61K31/545 , C07D501/38 , C07D501/46
CPC分类号： C07D501/46
摘要： Cephem compounds of the formula: ##STR1## wherein Q stands for a nitrogen atom or CH, R.sup.1 stands for a hydrogen atom or an optionally substituted lower alkyl group, R.sup.2 stands for a hydrogen atom or a lower alkyl group, A stands for a sulfur atom or NH, and n denotes an integral number ranging from 2 to 4, or salts thereof, and processes for producing them. The compounds (I) or salts thereof show not only excellent antibacterial activities against a wide range of pathogenic bacteria from gram-positive to gram-negative ones, including a variety of strains isolated clinically but also hydrophilic properties, and therefore they are excellent antibiotic substances having desirable water-solubility when used as injections.
摘要翻译：下式的头孢烯化合物：其中Q代表氮原子或CH，R1代表氢原子或任选取代的低级烷基，R2代表氢原子或低级烷基 A表示硫原子或NH，n表示2〜4的整数，或其盐，及其制造方法。化合物（I）或其盐不仅具有针对从革兰氏阳性至革兰氏阴性菌的广泛病原菌的优良抗菌活性，包括临床分离的各种菌株，而且亲水性，因此它们是优异的抗生素物质当用作注射剂时具有所需的水溶性。

4. 发明授权

US06982344B2 Process for preparation of optically active sulfonamides and intermediates for their synthesis 有权
标题翻译：制备光学活性磺酰胺及其合成中间体的方法
公开(公告)号：US06982344B2
公开(公告)日：2006-01-03
申请号：US10399165
申请日：2001-10-17
申请人： Tomomi Ikemoto , Atsuko Nishiguchi , Kiminori Tomimatsu
发明人： Tomomi Ikemoto , Atsuko Nishiguchi , Kiminori Tomimatsu
IPC分类号： C07C311/51 , C07C311/14 , C07C311/28 , C07C303/40 , C07B57/00
CPC分类号： C07C311/51 , C07B2200/07 , C07C303/40 , C07C303/44 , C07C311/14 , C07C2601/16
摘要： A method including resolution of a diastereomeric mixture represented by the formula wherein R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, only one of R1 and R2 contains one asymmetric carbon, and Ra is an optically active and optionally substituted hydrocarbon group or an optically active and optionally substituted heterocyclic group, or a salt thereof, to produce the diastereomer having a steric configuration of the asymmetric carbon for R1 or R2 of an R configuration or an S configuration, or a salt thereof.
摘要翻译：一种包括由下式表示的非对映异构体混合物的拆分方法，其中R 1和R 2相同或不同，并且各自为任选取代的烃基或任选取代的杂环基团中，R 1和R 2中只有一个含有一个不对称碳，R a是光学活性和任选取代的烃基或光学活性和任选取代的杂环基或其盐，以产生R构型的R 1或R 2的不对称碳的立体构型的非对映异构体或 S构型或其盐。

5. 发明授权

US06743924B2 Method for producing 1-substituted-1,2,3-triazole derivative 失效
标题翻译： 1-取代-1,2,3-三唑衍生物的制备方法
公开(公告)号：US06743924B2
公开(公告)日：2004-06-01
申请号：US10019264
申请日：2002-04-19
申请人： Tomomi Ikemoto , Tatsuya Ito , Kiminori Tomimatsu , Yasuhiro Sawai , Hirohiko Nishiyama , Yasushi Isogami
发明人： Tomomi Ikemoto , Tatsuya Ito , Kiminori Tomimatsu , Yasuhiro Sawai , Hirohiko Nishiyama , Yasushi Isogami
IPC分类号： C07D24904
CPC分类号： C07D249/04
摘要： A method for producing a compound of the formula: (1) in a secondary or tertiary alcohol in the presence of a base, or (2) in the absence of a base is provided. According to this method, a 1-substituted-1,2,3-triazole compound having a tyrosine kinase inhibitory action can be produced efficiently in a high yield at an industrial large scale by a convenient method
摘要翻译：制备下式化合物的方法：（1）在仲醇或叔醇中，在碱的存在下，或（2）在不存在碱的情况下。根据该方法，可以通过方便的方法以工业大规模高效率地产生具有酪氨酸激酶抑制作用的1-取代-1,2,3-三唑化合物

6. 发明授权

US5246948A Pyridine derivatives, their production and use 失效
标题翻译：吡啶衍生物，其生产和使用
公开(公告)号：US5246948A
公开(公告)日：1993-09-21
申请号：US880641
申请日：1992-05-07
申请人： Muneo Takatani , Taketoshi Saijo , Kiminori Tomimatsu
发明人： Muneo Takatani , Taketoshi Saijo , Kiminori Tomimatsu
IPC分类号： C07D213/68 , C07D213/70 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/38 , A61K31/425
CPC分类号： C07D213/70 , C07D213/68 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D417/14
摘要： There is disclosed a pharmaceutical composition for providing antiinflammatory, antipyretic, analgesic, antiallergic, immunosuppressing or immunomodulating activity which comprises a pyridine derivative of the formula (I): ##STR1## wherein R is an optionally substituted pyridine ring, X is a oxygen atom or --S(O)n--, wherein n is 0, 1 or 2, A is a bivalent C.sub.1-15 hydrocarbon residue whose branched moiety may have a substituent, Y is an oxygen or sulfur atom, R.sub.3 is a hydrogen atom or an optionally substituted hydrocarbon residue, R.sub.4 is an optionally substituted hydrocarbon residue or an optionally substituted monocyclic or bicyclic heterocyclic group, R.sub.3 and R.sub.4 may be joined together with the carbamoyl group or the thiocarbamoyl group to which they are attached to form an optionally substituted heterocyclic group, or R.sub.3 or R.sub.4 may be independently attached to A to form a ring, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier or diluent.

7. 发明授权

US07038042B2 Process for producing cyclic compound 失效
标题翻译：环状化合物的制备方法
公开(公告)号：US07038042B2
公开(公告)日：2006-05-02
申请号：US11010215
申请日：2004-12-10
申请人： Tomomi Ikemoto , Tatsuya Ito , Kiminori Tomimatsu
发明人： Tomomi Ikemoto , Tatsuya Ito , Kiminori Tomimatsu
IPC分类号： C07D487/00 , C07C313/00
CPC分类号： C07D225/06 , C07D313/08 , C07D313/20
摘要： A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2-Z is not —X1—X2—CH2, -Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.
摘要翻译：一种适用于通过短步安全批量生产用于药物，农药，食品，化妆品和化学产品的环状化合物或其中间体的方法。该方法用于制备由下式表示的化合物：其中Z表示吸电子基团; W表示任选取代的乙烯或任选取代的亚乙烯基; R 3表示氢或任选取代的烃基; 并且X表示二价基团[条件是当W表示任选取代的亚乙烯基时，则-X-CH 2 -Z不是-X 1 - 2 - -CH 2 - ，其中X 1表示硫或任选取代的氮，X 2表示任选取代的亚乙基）]} 或其盐的特征在于，在含有碳酸二酯的溶剂中使式（II）表示的化合物或其盐（其中符号具有与上述相同的含义）进行闭环反应。

8. 发明授权

US5767121A Pyridine derivatives, their production and use 失效
公开(公告)号：US5767121A
公开(公告)日：1998-06-16
申请号：US717022
申请日：1996-09-20
申请人： Muneo Takatani , Taketoshi Saijo , Kiminori Tomimatsu
发明人： Muneo Takatani , Taketoshi Saijo , Kiminori Tomimatsu
IPC分类号： C07D213/68 , C07D213/70 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/495 , A61K31/535 , C07D401/06
CPC分类号： C07D213/70 , C07D213/68 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D417/14
摘要： There is disclosed a pharmaceutical composition for providing antiinflammatory, antipyretic, analgesic, antiallergic, immunosuppressing or immunomodulating activity which comprises a pyridine derivative of the formula (I): ##STR1## wherein R is an optionally substituted pyridine ring, X is a oxygen atom or --S(O).sub.n --, wherein n is 0, 1 or 2, A is a bivalent C.sub.1-15 hydrocarbon residue whose branched moiety may have a substituent, Y is an oxygen or sulfur atom, R.sub.3 is a hydrogen atom or an optionally substituted hydrocarbon residue, R.sub.4 is an optionally substituted hydrocarbon residue or an optionally substituted monocyclic or bicyclic heterocyclic group, R.sub.3 and R.sub.4 may be joined together with the carbamoyl group or the thiocarbamoyl group to which they are attached to form an optionally substituted heterocyclic group, or R.sub.3 or R.sub.4 may be independently attached to A to form a ring, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier or diluent.

9. 发明授权

US5561147A Pyridine derivatives, their production and use 失效
公开(公告)号：US5561147A
公开(公告)日：1996-10-01
申请号：US455170
申请日：1995-05-31
申请人： Muneo Takatani , Taketoshi Saijo , Kiminori Tomimatsu
发明人： Muneo Takatani , Taketoshi Saijo , Kiminori Tomimatsu
IPC分类号： C07D213/68 , C07D213/70 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/42 , C02D473/02
CPC分类号： C07D213/70 , C07D213/68 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D417/14
摘要： There is disclosed a pharmaceutical composition for providing antiinflammatory, antipyretic, analgesic, antiallergic, immunosuppressing or immunomodulating activity which comprises a pyridine derivative of the formula (I): ##STR1## wherein R is an optionally substituted pyridine ring, X is a oxygen atom or --S(O).sub.n --, wherein n is 0, 1 or 2, A is a bivalent C.sub.1-15 hydrocarbon residue whose branched moiety may have a substituent, Y is an oxygen or sulfur atom, R.sub.3 is a hydrogen atom or an optionally substituted hydrocarbon residue, R.sub.4 is an optionally substituted hydrocarbon residue or an optionally substituted monocyclic or bicyclic heterocyclic group, R.sub.3 and R.sub.4 may be joined together with the carbamoyl group or the thiocarbamoyl group to which they are attached to form an optionally substituted heterocyclic group, or R.sub.3 or R.sub.4 may be independently attached to A to form a ring, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier or diluent.

10. 发明授权

US5457106A Pyridine derivatives, their production and use 失效
公开(公告)号：US5457106A
公开(公告)日：1995-10-10
申请号：US334221
申请日：1994-11-04
申请人： Muneo Takatani , Taketoshi Saijo , Kiminori Tomimatsu
发明人： Muneo Takatani , Taketoshi Saijo , Kiminori Tomimatsu
IPC分类号： C07D213/68 , C07D213/70 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , A61K31/535
CPC分类号： C07D213/70 , C07D213/68 , C07D213/81 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D417/14
摘要： There is disclosed a pharmaceutical composition for providing antiinflammatory, antipyretic, analgesic, antiallergic, immunosuppressing or immunomodulating activity which comprises a pyridine derivative of the formula (I): ##STR1## wherein R is an optionally substituted pyridine ring, X is a oxygen atom or --S(O).sub.n --, wherein n is 0, 1 or 2, A is a bivalent C.sub.1-15 hydrocarbon residue whose branched moiety may have a substituent, Y is an oxygen or sulfur atom, R.sub.3 is a hydrogen atom or an optionally substituted hydrocarbon residue, R.sub.4 is an optionally substituted hydrocarbon residue or an optionally substituted monocyclic or bicyclic heterocyclic group, R.sub.3 and R.sub.4 may be joined together with the carbamoyl group or the thiocarbamoyl group to which they are attached to form an optionally substituted heterocyclic group, or R.sub.3 or R.sub.4 may be independently attached to A to form a ring, or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier or diluent.

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