公开(公告)号：JP2010195793A

公开(公告)日：2010-09-09

申请号：JP2010060698

申请日：2010-03-17

Applicant: Lonza Ag ,  ロンザ アーゲー

Inventor： HANSELMANN PAUL ,  HILDBRAND STEFAN

IPC: C07D233/64 ,  A61K31/417 ,  A61P3/10 ,  A61P17/18 ,  A61P27/12 ,  A61P39/06 ,  C07B61/00 ,  C07C209/48 ,  C07C237/02 ,  C07C279/14 ,  C07D233/54 ,  C07D239/20

CPC classification number: C07D233/64 ,  Y02P20/55

Abstract: PROBLEM TO BE SOLVED: To provide a production method in which using of a protecting group or an expensive derivative is not needed, and which is suitable for composing amides of beta-alanine useful as a medicine like carcinine, and to provide a novel synthetic intermediate in the production method. SOLUTION: Cyanoacetic acid amide which is expressed by formula (IV), wherein R 1 is a 1-6C imidazol-4-ylmethyl, which is optionally substituted, and R 2 is hydrogen, is useful as a synthetic intermediate of amides of beta-alanine. In addition, the production method obtains the amides of beta-alanine by catalyst-hydrogenation of the synthetic intermediate under the presence of a metal catalyst based on rhodium. COPYRIGHT: (C)2010,JPO&INPIT

Abstract translation: 要解决的问题：提供不需要使用保护基或昂贵的衍生物的制造方法，其适用于组合用作药物如癌的β-丙氨酸的酰胺，并且提供一种 新型合成中间体的生产方法。 解决方案：由式（Ⅳ）表示的氰基乙酰胺，其中R 1是选自被取代的1-6C咪唑-4-基甲基，R 2 = / SP>是氢，可用作β-丙氨酸酰胺的合成中间体。 此外，生产方法通过在基于铑的金属催化剂存在下合成中间体的催化氢化获得β-丙氨酸的酰胺。 版权所有（C）2010，JPO＆INPIT

公开(公告)号：JP2529825B2

公开(公告)日：1996-09-04

申请号：JP2137186

申请日：1986-02-04

Applicant: MERRELL DOW PHARMA

Inventor： MAIKERU KORUBU ,  MAIKERU JEI JANGU ,  JOSEFU PII BURUKAATO ,  FURITSUTSU II GEEHAATO ,  YUUJIN ERU GIROTSUKUSU ,  DANIERU JII SUCHIRURIN ,  BAANAADO NEISESU

IPC: C07K5/00 ,  A61K31/13 ,  A61K31/16 ,  A61K31/165 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K38/00 ,  A61K38/55 ,  A61P7/02 ,  A61P7/06 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C221/00 ,  C07C225/02 ,  C07C225/16 ,  C07C227/00 ,  C07C227/16 ,  C07C227/18 ,  C07C229/02 ,  C07C229/04 ,  C07C229/22 ,  C07C229/24 ,  C07C229/26 ,  C07C233/01 ,  C07C233/31 ,  C07C237/02 ,  C07C237/06 ,  C07C237/12 ,  C07C237/20 ,  C07C237/22 ,  C07C239/00 ,  C07C271/06 ,  C07C271/22 ,  C07C273/04 ,  C07C279/18 ,  C07D207/16 ,  C07D209/42 ,  C07D498/10 ,  C07K1/113 ,  C07K5/02 ,  C07K5/04 ,  C07K5/06 ,  C07K5/062 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097 ,  C07K7/06 ,  C07K14/81 ,  C12N9/99

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

公开(公告)号：JP3338445B2

公开(公告)日：2002-10-28

申请号：JP50466892

申请日：1992-03-02

IPC: B01F17/00 ,  B01F17/16 ,  B01F17/22 ,  B01F17/26 ,  B01F17/42 ,  C07C233/17 ,  C07C233/18 ,  C07C233/22 ,  C07C233/69 ,  C07C235/02 ,  C07C235/48 ,  C07C237/02 ,  C07C311/08 ,  C07C311/14 ,  C07C311/29 ,  G03C1/38

公开(公告)号：JPH11315056A

公开(公告)日：1999-11-16

申请号：JP5073299

申请日：1999-02-26

Applicant: SHISEIDO CO LTD

Inventor： FUKUNISHI HIROTADA ,  MAGARA TSUNAO ,  KOBAYASHI KOJI

IPC: C07D295/08 ,  A61K8/00 ,  A61K8/30 ,  A61K8/42 ,  A61K8/49 ,  A61Q5/00 ,  A61Q5/02 ,  A61Q7/00 ,  A61Q19/00 ,  C07C235/40 ,  C07C237/02 ,  C07C237/24 ,  C07C271/12 ,  C07C271/20 ,  C07C271/64 ,  C07C275/60 ,  C07D233/61 ,  C07D295/12 ,  A61K7/00 ,  A61K7/06 ,  A61K7/48

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound having an excellent trichogenous action, an excellent hair growth-stimulating action, and an excellent hair falling- preventing action, and useful as an active ingredient for hair tonics and skin preparations for external uses. SOLUTION: This compound is a compound of formula I [one of A and B is a 10-30C hydrocarbon group, and the other is (CH2 )n -NR R (R and R are H, a lower alkyl, phenyl or bezyl, or R and R together form a three to seven-membered heterocyclic ring or the like); Z is O, OCO, OCONR (R is H, a lower alkyl or the like) or NR ; R is a halogen, a lower alkyl, a lower acyl or the like; R is H, a lower alkyl or the like; (m) is 0-2; (n) is 0-5]. For example, a compound of formula II. The compound of formula I is obtained, for example, by reacting a compound of formula III with an amine of formula IV.

公开(公告)号：JP2544557B2

公开(公告)日：1996-10-16

申请号：JP33482591

申请日：1991-12-18

Applicant: KAO CORP

Inventor： FUJINAMI SHIGEAKI ,  MORIMURA MOTOHIRO ,  AIZAWA KAZUNORI ,  NISHIMOTO UICHIRO ,  KATO TOORU

IPC: C07C67/08 ,  C07C69/24 ,  C07C69/52 ,  C07C219/06 ,  C07C219/08 ,  C07C231/02 ,  C07C233/04 ,  C07C233/09 ,  C07C233/36 ,  C07C233/38 ,  C07C237/02

公开(公告)号：JP2005502697A

公开(公告)日：2005-01-27

申请号：JP2003526873

申请日：2002-09-04

Applicant: ロンザ ア−ゲ−

Inventor： ハンセルマン、ポール ,  ヒルドブランド、シュテファン

IPC: C07D233/64 ,  C07B61/00 ,  C07C209/48 ,  C07C237/02 ,  C07C279/14 ,  C07D233/54 ,  C07D239/20

CPC classification number: C07D233/64 ,  Y02P20/55

Abstract: 下記一般式のβアラニンアミド［式中、R
1 は水素またはC
1-6 -アルキルであり、該アルキルはヒドロキシ、アミノ、カルボキシ、カルバモイル、メチルメルカプト、グアニド、置換もしくは非置換のアリールもしくはヘテロアリールで置換されるかまたは非置換で、且つR
2 が水素であるか、或いはR
1 およびR
2 が一緒になって式-(CH
2 )
n -（ここで、nは3または4である）の基を形成する］は、対応するアミンをシアノ酢酸エステルと反応させてシアノ酢酸アミドを生じさせ、続いて、アミノ保護基を使用することなく触媒的に水素化することにより製造される。 この方法は、天然に存在する偽ジペプチドであるカルニシン（βアラニルヒスタミン、R
1 ＝イミダゾール-4-イルメチル、R
2 ＝H)の製造に特に適しており、これは抗酸化作用をもった薬物として医薬および化粧品に使用される。
【化１】

公开(公告)号：JPH10502911A

公开(公告)日：1998-03-17

申请号：JP50275496

申请日：1995-06-16

IPC: C07D263/44 ,  A01N37/18 ,  A01N37/20 ,  A01N37/44 ,  A01N43/16 ,  C07C231/02 ,  C07C237/02 ,  C07C237/06 ,  C07C237/08 ,  C07C269/04 ,  C07C271/04 ,  C07C271/06 ,  C07C271/22 ,  C07D311/58

公开(公告)号：JPS61183253A

公开(公告)日：1986-08-15

申请号：JP2137186

申请日：1986-02-04

Applicant: MERRELL DOW PHARMA

Inventor： MAIKERU KORUBU ,  MAIKERU JIEI JIYANGU ,  JIYOSEFU PII BURUKAATO ,  FURITSUTSU II GEEHAATO ,  YUUJIN ERU GIROTSUKUSU ,  DANIERU JII SUCHIRURIN ,  BAANAADO NEISESU

IPC: C07K5/00 ,  A61K31/13 ,  A61K31/16 ,  A61K31/165 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K38/00 ,  A61K38/55 ,  A61P7/02 ,  A61P7/06 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P17/00 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C221/00 ,  C07C225/02 ,  C07C225/16 ,  C07C227/00 ,  C07C227/16 ,  C07C227/18 ,  C07C229/02 ,  C07C229/04 ,  C07C229/22 ,  C07C229/24 ,  C07C229/26 ,  C07C233/01 ,  C07C233/31 ,  C07C237/02 ,  C07C237/06 ,  C07C237/12 ,  C07C237/20 ,  C07C237/22 ,  C07C239/00 ,  C07C271/06 ,  C07C271/22 ,  C07C273/04 ,  C07C279/18 ,  C07D207/16 ,  C07D209/42 ,  C07D498/10 ,  C07K1/113 ,  C07K5/02 ,  C07K5/04 ,  C07K5/06 ,  C07K5/062 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097 ,  C07K7/06 ,  C07K14/81 ,  C12N9/99

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

公开(公告)号：JPS4948644A

公开(公告)日：1974-05-11

申请号：JP5123973

申请日：1973-05-10

IPC: C07C255/24 ,  A61K20060101 ,  A61K31/165 ,  C07C20060101 ,  C07C49/76 ,  C07C67/00 ,  C07C221/00 ,  C07C225/22 ,  C07C233/00 ,  C07C237/00 ,  C07C237/02 ,  C07C237/04 ,  C07C237/06 ,  C07C253/00 ,  C07D20060101 ,  C07D335/00 ,  C07C103/50

公开(公告)号：JP2000086611A

公开(公告)日：2000-03-28

申请号：JP37494598

申请日：1998-12-11

Applicant: FUJI CHEMICAL IND LTD

Inventor： FUJISAWA TETSUNORI ,  KOTAKE SHINJIRO ,  HONGO KAZUYA ,  OTANI YOSHIKAZU ,  YASUDA JUNKO ,  MORIKAWA TADANORI

IPC: C07D295/22 ,  A61K31/00 ,  A61K31/16 ,  A61K31/165 ,  A61K31/21 ,  A61K31/215 ,  A61K31/27 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61K31/44 ,  A61K31/4409 ,  A61K31/445 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/66 ,  A61K31/70 ,  A61K31/7028 ,  A61P5/00 ,  A61P25/04 ,  A61P27/00 ,  A61P37/00 ,  C07C237/02 ,  C07C259/06 ,  C07C271/64 ,  C07C279/24 ,  C07D213/53 ,  C07D233/74 ,  C07F9/40 ,  C07H15/18

Abstract: PROBLEM TO BE SOLVED: To obtain a new compound capable of inhibiting matrix metalloproteinases derived from vertebrates or a tumor necrosis factor-α converting enzyme, and excellent in biological activity such as oral absorptivity. SOLUTION: This compound is represented by formula I [R1 is H, a (substituted) aralkyl or the like; R2 is H, a (substituted) aralkyloxycarbonyl or the like; R3 is H, a (substituted) alkyl or the like; R4 is a (substituted) alkyl or the like; R5 and R6 are each H, a (substituted) alkyl or the like; R7 is H, a (substituted) alkyl or the like; R8 is H, a (substituted) alkyl or the like; R9 is H, OH, amino or the like], e.g. Na-t-butyloxycarbonyl-Ne-benzyloxycarbonyl-L- lysine N-methylamide. The compound represented by formula I is obtained by converting an ester site of a compound represented by formula II into an amide bond-containing site and, as desired, respectively converting groups R11 and R14 (R11 is the same meaning as that of R3 or the like; R12 has the same meaning as that of R4 or the like; R13 has the same meaning as that of R5 or the like; R14 has the same meaning as that of R9 or the like) into the groups R3 to R5 and R9.