公开(公告)号：US5972929A

公开(公告)日：1999-10-26

申请号：US137148

申请日：1998-08-20

申请人： Koji Kobayashi ,  Hirotada Fukunishi ,  Tsunao Magara

发明人： Koji Kobayashi ,  Hirotada Fukunishi ,  Tsunao Magara

IPC分类号： A61K8/49 ,  A61Q7/00 ,  C07D239/90 ,  A61K31/495

CPC分类号： C07D239/90 ,  A61K8/4953 ,  A61Q7/00

摘要： A quinazolinone derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2).sub.n -NR.sup.2 R.sup.3 ; wherein R.sup.1 represents a hydrocarbon group of C.sub.10-30 ; wherein R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group, or a benzyl group, or together represent a heterocyclic ring having 3-7 members; and n represents an integer of 1-5; wherein when A is R.sup.1, B is --(CH.sub.2).sub.n -NR.sup.2 R.sup.3 and when A is --(CH.sub.2).sub.n -NR.sup.2 R.sup.3, B is R.sup.1 ; and wherein R.sup.4 is selected from the group consisting of a hydrogen atom, a halogen atom, a lower alkyl group, a lower acyl group, a nitro group, a cyano group, an amino group, a lower alkoxycarbonyl group, a lower alkylamino group, a lower alkoxy group, a lower acyloxy group, a carbamoyl group, a lower alkylcarbamoyl group, and a lower acylamino group. The quinazolinone derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in humans.

摘要翻译： 由下式（I）表示的喹唑啉酮衍生物或其盐; 其中A和B各自为R 1或 - （CH 2）n -NR 2 R 3; 其中R1表示C10-30的烃基; 其中R2和R3各自表示氢原子，低级烷基，苯基或苄基，或一起表示具有3-7个成员的杂环; n表示1-5的整数， 其中当A为R1时，B为 - （CH2）n-NR2R3，当A为 - （CH2）n-NR2R3时，B为R1; 并且其中R 4选自氢原子，卤素原子，低级烷基，低级酰基，硝基，氰基，氨基，低级烷氧基羰基，低级烷基氨基， 低级烷氧基，低级酰氧基，氨基甲酰基，低级烷基氨基甲酰基和低级酰氨基。 喹唑啉酮衍生物或其盐具有优异的毛发生长和再生长促进作用，其可用于哺乳动物，特别是人类的护发，改善或预防脱发。

公开(公告)号：US06177067B1

公开(公告)日：2001-01-23

申请号：US09169940

申请日：1998-10-13

申请人： Tsunao Magara ,  Yoshiharu Tsuji ,  Masahiro Tajima ,  Koji Kobayashi ,  Hirotada Fukunishi ,  Masazumi Watanabe

发明人： Tsunao Magara ,  Yoshiharu Tsuji ,  Masahiro Tajima ,  Koji Kobayashi ,  Hirotada Fukunishi ,  Masazumi Watanabe

IPC分类号： A61K706

CPC分类号： A61K8/44 ,  A61K8/49 ,  A61K8/4926 ,  A61K8/494 ,  A61Q5/00 ,  A61Q5/006 ,  A61Q5/02 ,  A61Q7/00 ,  Y10S514/88

摘要： Disclosed is a hair revitalizing tonic composition containing a dimethylpropanediol derivative of the formula: wherein R1 and R2 are each independently a C1-30 hydrocarbon group which may be substituted, or a five- or six-membered heterocyclic group which contains 1 to 4 heteroatoms selected from oxygen, sulfur and nitrogen atoms and which may be substituted, R3 is hydrogen atom, an alkyl group which may be substituted, an acyl group, an alkoxycarbonyl group, a phenoxycarbonyl group, or a carbamoyl group which may be substituted, and a and b are each 0 or 1, as well as a method for effecting hair growth promotion, hair growth stimulation, or hair loss prevention in mammals by using such a hair revitalizing tonic composition. Also disclosed is the use of a compound of formula (I) in the preparation of a hair revitalizing tonic composition. Thus, this invention can provide an excellent means of hair revitalization or hair loss prevention in mammals.

摘要翻译： 本发明公开了一种含有下式的二甲基丙二醇衍生物的头发活力补品组合物：其中R 1和R 2各自独立地为可被取代的C 1-30烃基或选自含有1至4个杂原子的五元或六元杂环基 可以被氧，硫和氮原子取代，可以被取代，R3是氢原子，可被取代的烷基，酰基，烷氧基羰基，苯氧基羰基或可被取代的氨基甲酰基，以及 b各自为0或1，以及通过使用这种头发活化的滋补组合物来实现哺乳动物的头发生长促进，毛发生长刺激或脱发防止的方法。 还公开了式（I）化合物在制备头发活化滋补组合物中的用途。 因此，本发明可以提供哺乳动物的头发复兴或脱发预防的优良手段。

公开(公告)号：US06174885B1

公开(公告)日：2001-01-16

申请号：US09257940

申请日：1999-02-26

申请人： Hirotada Fukunishi ,  Tsunao Magara ,  Koji Kobayashi

发明人： Hirotada Fukunishi ,  Tsunao Magara ,  Koji Kobayashi

IPC分类号： A61K31535

CPC分类号： C07D295/205 ,  A61K8/44 ,  A61Q7/00 ,  C07C271/20 ,  C07C2601/16 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D295/13

摘要： A [6-(substituted-methyl)-3-cyclohexenyl]formamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is—(CH2)n-NR2R3; Z is —O—, —OCO—, —OCONR6— or —NR6—; R2 and R3 individually represent a hydrogen, lower alkyl, phenyl or benzyl group, or together represent a heterocycle having 3-7 members; —NR5—(CH2)n-NR2R3 or —NR6—(CH2)n-NR2R3 may be Group W, and —OCONR6—(CH2)n-NR2R3 may be —OCO—W, wherein W is a formula of: wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R2 is a hydrogen, lower alkyl, phenyl or benzyl group; R4 is a halogen, lower alkyl, lower acyl, nitro, cyano, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, lower alkylamino, lower acylamino, lower alkoxy or lower acyloxy group; each of R5 and R6 is a hydrogen, lower alkyl, lower acyl, lower alkylcarbamoyl group, or a part of said Group W; m is an integer of 0-2; and n is an integer of 0-5. The [6-(substituted-methyl)-3-cyclohexenyl]formamide derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.

摘要翻译： 由下式（I）表示的[6-（取代甲基）-3-环己烯基]甲酰胺衍生物或其盐：其中A和B中的一个是由R 1表示的C 10-30的烃基，另一个是 - （CH 2）n -NR 2 R 3; Z是-O - ， - OCO - ， - OCONR 6 - 或-NR 6 - ; R2和R3各自表示氢，低级烷基，苯基或苄基，或一起表示具有3-7个成员的杂环; -NR 5 - （CH 2）n -NR 2 R 3或-NR 6 - （CH 2）n -NR 2 R 3可以是W组，-OCONR 6 - （CH 2）n -NR 2 R 3可以是-OCO-W，其中W是下式的化合物：其中环 E是6或7个成员的杂环，包括两个氮原子，R 2是氢，低级烷基，苯基或苄基; R4是卤素，低级烷基，低级酰基，硝基，氰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基，低级酰基氨基，低级烷氧基或低级酰氧基。 R5和R6各自为氢，低级烷基，低级酰基，低级烷基氨基甲酰基或所述W组的一部分; m是0-2的整数; n为0-5的整数。 [6-（取代甲基）-3-环己烯基]甲酰胺衍生物或其盐具有优异的毛发生长和再生长促进作用，其可用于哺乳动物，特别是人的护理，改善或预防脱发 。

公开(公告)号：US6057337A

公开(公告)日：2000-05-02

申请号：US239960

申请日：1999-01-29

申请人： Koji Kobayashi ,  Hirotada Fukunishi ,  Kenichi Umishio ,  Akihiro Ishino

发明人： Koji Kobayashi ,  Hirotada Fukunishi ,  Kenichi Umishio ,  Akihiro Ishino

IPC分类号： C07D211/22 ,  C07D211/26 ,  C07D401/12 ,  C07D521/00 ,  A61K7/06

CPC分类号： C07D231/12 ,  C07D211/22 ,  C07D211/26 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12

摘要： A 1,2-di-substituted piperidine derivative or a salt thereof expressed by the following Formula (I): ##STR1## wherein one of A and B is a hydrocarbon group of C.sub.1-30 expressed by R.sup.1 and the other is --(CH.sub.2)n-NR.sup.2 R.sup.3 ; Y is --CO--, --CONR.sup.5 -- or --COO--; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.2 and R.sup.3 individually represent a hydrogen a lower alkyl, a phenyl or a benzyl group, or together represent a heterocycle having 3-7 members; --NR.sup.5 --(CH.sub.2)n-NR.sup.2 R.sup.3 and --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 of --(Y).sub.1 --A and --Z--B may be the following Group W: ##STR2## wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R.sup.2 is a hydrogen, a lower alkyl, a phenyl or a benzyl group; R.sup.4 is a hydrogen, a halogen, a lower alkyl, a lower acyl, a nitro, a cyano, a lower alkoxycarbonyl, a carbamoyl, a lower alkylcarbamoyl, a lower alkylamino, a lower acylamino, a lower alkoxy or a lower acyloxy group; each of R.sup.5 and R.sup.6 is a hydrogen, a lower alkyl, a lower acyl, a lower alkylcarbamoyl group, or a part of said ring E; l is 0 or 1; m is an integer of 2-5; and n is an integer of 0-5. The 1,2-di-substituted piperidine derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.

摘要翻译： 由下式（I）表示的1,2-二取代的哌啶衍生物或其盐：其中A和B中的一个为由R1表示的C1-30的烃基，另一个为 - （CH 2）n - NR2R3; Y是-CO - ， - CONR 5 - 或-COO-; Z是-O - ， - OCO - ， - OCONR 6 - 或-NR 6 - ; R2和R3各自表示氢，低级烷基，苯基或苄基，或一起表示具有3-7个成员的杂环; - （Y）1-A和-ZB的-NR 5 - （CH 2）n -NR 2 R 3和-NR 6 - （CH 2）n -NR 2 R 3可以是以下W组：其中环E是6或7个成员的杂环，包括两个 氮原子，R 2为氢，低级烷基，苯基或苄基; R4是氢，卤素，低级烷基，低级酰基，硝基，氰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基，低级酰基氨基，低级烷氧基或低级酰氧基。 R5和R6各自为氢，低级烷基，低级酰基，低级烷基氨基甲酰基或所述环E的一部分; l为0或1; m为2-5的整数; n为0-5的整数。 1,2-二取代的哌啶衍生物或其盐具有优异的毛发生长和再生长促进效果，其可用于哺乳动物，特别是人的护发，改善或预防脱发。

公开(公告)号：US5756505A

公开(公告)日：1998-05-26

申请号：US625992

申请日：1996-04-01

申请人： Chikao Nishino ,  Fumitaka Sato ,  Tomohiro Uetake ,  Hirotada Fukunishi ,  Nao Kojima ,  Koji Kobayashi

发明人： Chikao Nishino ,  Fumitaka Sato ,  Tomohiro Uetake ,  Hirotada Fukunishi ,  Nao Kojima ,  Koji Kobayashi

IPC分类号： C07D295/18 ,  A61K31/495 ,  A61P1/04 ,  A61P31/04 ,  C07D295/185 ,  C07D295/192 ,  C07D295/205 ,  C07D405/12

CPC分类号： C07D295/185 ,  C07D295/192

摘要： An N-acylpiperazine derivative or a salt thereof in accordance with the present invention is represented by the following formula 1: ##STR1## wherein R.sub.1 represents a lower alkyl, hydroxy lower alkyl, lower acyl, or arylcarbonyloxy lower alkyl group; R.sub.2 represents hydrogen atom or a lower alkyl, lower alkoxy, lower alkenyl, amino, or nitro group; R.sub.3 and R.sub.4, which are identical to or different from each other, represent hydrogen atoms, halogen atoms, or cyano, nitro, lower alkyl, or lower alkoxy groups; and n represents 0 or 1. The N-acylpiperazine derivative has anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulsers.

摘要翻译： 根据本发明的N-酰基哌嗪衍生物或其盐由下式1表示：其中R 1表示低级烷基，羟基低级烷基，低级酰基或芳基羰基氧基低级烷基; R2代表氢原子或低级烷基，低级烷氧基，低级烯基，氨基或硝基; R 3和R 4彼此相同或不同，表示氢原子，卤原子或氰基，硝基，低级烷基或低级烷氧基; 并且n表示0或1. N-酰基哌嗪衍生物具有抗溃疡作用或对幽门螺杆菌具有抗菌活性，可用于预防或治愈酏剂。

公开(公告)号：US06339154B1

公开(公告)日：2002-01-15

申请号：US09496258

申请日：2000-02-01

申请人： Koji Kobayashi ,  Hirotada Fukunishi ,  Tokuro Iwabuchi

发明人： Koji Kobayashi ,  Hirotada Fukunishi ,  Tokuro Iwabuchi

IPC分类号： C07D24104

CPC分类号： C07D295/185 ,  A61K8/42 ,  A61K8/445 ,  A61K8/4926 ,  A61K8/494 ,  A61Q7/00 ,  C07C235/34 ,  C07C271/44 ,  C07C271/52 ,  C07C271/64 ,  C07C271/66 ,  C07C281/02 ,  C07D295/088 ,  C07D295/13 ,  C07D295/205

摘要： A (2-substituted oxyphenyl)alkanamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C3-30 expressed by R1 and the other is —(CH2)n—NR2R3; Z is —CO— or —CONR6—; R2 and R3 individually represent H, lower alkyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members; wherein —CONR5—(CH2)n—NR2R3 or —CONR6—(CH2)n—NR2R3 may be the following Group (D): wherein ring Y is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, lower alkyl, lower acyl and etc; R5 and R6 are individually H, lower alkyl, lower acyl or lower alkylcarbamoyl, or may form a part of said Group(II); 1 is 0 or 1; m is 1 or 2; and n is an integer of 0-5. The (2-substituted oxyphenyl)alkanamide derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.

摘要翻译： 由下式（I）表示的（2-取代的氧苯基）烷酰胺衍生物或其盐：其中A和B中的一个是由R 3表示的C3-30的烃基，另一个是 - （CH 2）n -NR 2 R 3 ; Z是-CO-或-CONR 6 - ; R2和R3各自表示H，低级烷基或苄基，或-NR2R3可以是具有3-7个成员的杂环; 其中-CONR 5 - （CH 2）n -NR 2 R 3或-CONR 6 - （CH 2）n -NR 2 R 3可以是下列基团（D）：其中环Y是6或7个成员的杂环; R4选自H，卤素，低级烷基，低级酰基等; R5和R6各自为H，低级烷基，低级酰基或低级烷基氨基甲酰基，或可形成所述组（II）的一部分。 1为0或1; m为1或2; n为0-5的整数。 （2-取代的氧苯基）烷酰胺衍生物或其盐具有优异的毛发生长和再生长促进作用，其可用于哺乳动物，特别是人的护发，改善或预防脱发。

公开(公告)号：US06573297B2

公开(公告)日：2003-06-03

申请号：US09984202

申请日：2001-10-29

申请人： Koji Kobayashi ,  Hirotada Fukunishi ,  Tokuro Iwabuchi

发明人： Koji Kobayashi ,  Hirotada Fukunishi ,  Tokuro Iwabuchi

IPC分类号： A61K3116

CPC分类号： C07D295/185 ,  A61K8/42 ,  A61K8/445 ,  A61K8/4926 ,  A61K8/494 ,  A61Q7/00 ,  C07C235/34 ,  C07C271/44 ,  C07C271/52 ,  C07C271/64 ,  C07C271/66 ,  C07C281/02 ,  C07D295/088 ,  C07D295/13 ,  C07D295/205

摘要： A (2-substituted oxyphenyl)alkanamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C3-30 expressed by R1 and the other is —(CH2)n-NR2R3; Z is —CO— or —CONR6—; R2 and R3 individually represent H, lower alkyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members; wherein —CONR5—(CH2)n-NR2R3 or —CONR6—(CH2)n-NR2R3 may be the following Group (II): wherein ring Y is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, lower alkyl, lower acyl and etc; R5 and R6 are individually H, lower alkyl, lower acyl or lower alkylcarbamoyl, or may form a part of said Group(II); 1 is 0 or 1; m is 1 or 2; and n is an integer of 0-5. The (2-substituted oxyphenyl)alkanamide derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.

摘要翻译： 由下式（I）表示的（2-取代的氧苯基）烷酰胺衍生物或其盐：其中A和B中的一个是由R 3表示的C3-30的烃基，另一个是 - （CH 2）n -NR 2 R 3 ; Z是-CO-或-CONR 6 - ; R2和R3各自表示H，低级烷基或苄基，或-NR2R3可以是具有3-7个成员的杂环; 其中-CONR 5 - （CH 2）n -NR 2 R 3或-CONR 6 - （CH 2）n -NR 2 R 3可以是下列基团（II）：其中环Y是6或7个成员的杂环; R4选自H，卤素，低级烷基，低级酰基等; R5和R6各自为H，低级烷基，低级酰基或低级烷基氨基甲酰基，或可形成所述组（II）的一部分。 1为0或1; m为1或2; n为0-5的整数。 （2-取代的氧苯基）烷酰胺衍生物或其盐具有优异的毛发生长和再生长促进作用，其可用于哺乳动物，特别是人的护发，改善或预防脱发。

公开(公告)号：US06204264B1

公开(公告)日：2001-03-20

申请号：US09398200

申请日：1999-09-17

申请人： Koji Kobayashi ,  Hirotada Fukunishi ,  Kenichi Umishio ,  Masahiro Tajima

发明人： Koji Kobayashi ,  Hirotada Fukunishi ,  Kenichi Umishio ,  Masahiro Tajima

IPC分类号： A61R31535

CPC分类号： C07D235/24 ,  A61K8/4946 ,  A61Q7/00 ,  C07D235/08

摘要： A benzimidazole derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is —(CH2)n—NR2R3; R2 and R3 individually represent H, lower alkyl, phenyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members, or —CONR5—(CH2)n—NR2R3 may be the following Group (W): wherein R2 is H, lower alkyl, phenyl or benzyl and ring E is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, cyano, trifluoromethyl, lower alkyl and etc.; R5 is H, lower alkyl, lower acyl or lower alkylcarbamoyl; m is 0 or 1; and n is an integer of 0-5. The benzimidazole derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.

摘要翻译： 由下式（I）表示的苯并咪唑衍生物或其盐：其中A和B中的一个是由R 1表示的C 10-30的烃基，而另一个是 - （CH 2）n -NR 2 R 3; R 2和R 3各自表示H，低级烷基，苯基或苄基，或-NR 2 R 3可以是具有3-7个成员的杂环，或-CONR 5 - （CH 2）n -NR 2 R 3可以是下列基团（W）：其中R 2是H 苯基或苄基，环E是6或7个成员的杂环; R4选自H，卤素，氰基，三氟甲基，低级烷基等; R5是H，低级烷基，低级酰基或低级烷基氨基甲酰基; m为0或1; n为0-5的整数。 苯并咪唑衍生物或其盐具有优异的毛发生长和再生长促进作用，其可用于哺乳动物，特别是人的护发，改善或预防脱发。

公开(公告)号：US6114325A

公开(公告)日：2000-09-05

申请号：US176947

申请日：1998-10-22

申请人： Hirotada Fukunishi ,  Kenichi Umishio ,  Masahiro Tajima ,  Koji Kobayashi

发明人： Hirotada Fukunishi ,  Kenichi Umishio ,  Masahiro Tajima ,  Koji Kobayashi

IPC分类号： A61K8/42 ,  A61K8/44 ,  A61K8/49 ,  A61Q5/00 ,  A61Q5/02 ,  A61Q7/00 ,  A61Q19/00 ,  C07C235/46 ,  C07C235/84 ,  C07C237/34 ,  C07C271/20 ,  C07C275/54 ,  C07C281/02 ,  C07D233/61 ,  C07D243/08 ,  C07D295/088 ,  C07D295/13 ,  C07D295/192 ,  C07D295/205 ,  C07D295/28 ,  A61K31/495 ,  A61K31/5513 ,  C07D241/04

CPC分类号： C07D295/32 ,  A61K8/42 ,  A61K8/44 ,  A61K8/49 ,  A61K8/4926 ,  A61K8/494 ,  A61Q7/00 ,  C07C235/46 ,  C07C235/84 ,  C07C237/34 ,  C07C271/20 ,  C07C275/54 ,  C07C281/02 ,  C07D243/08 ,  C07D295/088 ,  C07D295/13 ,  C07D295/192 ,  C07D295/205 ,  A61Q5/02

摘要： A 1,2-di-substituted benzene-carboxamide derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2)n-NR.sup.2 R.sup.3, wherein when A is R.sup.1, B is --(CH.sub.2)n-NR.sup.2 R.sup.3 and when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, B is R.sup.1 ; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.1 is a hydrocarbon group of C.sub.10-30 ; R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, or together represent a heterocyclic ring having 3-7 members; when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.2 may be a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, and R.sup.3 and R.sup.5 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; when --Z--B is --OCONR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 or --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.2 may be a hydrogen atom, a lower alkyl group, a phenyl group or a benzyl group, and R.sup.3 and R.sup.6 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; R.sup.4 is selected from the group consisting of a halogen atom, a lower alkyl group, a lower acyl group, a nitro group, a cyano group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a lower alkylamino group, a lower acylamino group, a lower alkoxy group and a lower acyloxy group; R.sup.5 is a hydrogen atom, a lower alkyl group, a lower acyl group or a lower alkylcarbamoyl group, or when A is --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.5 and R.sup.3 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; R.sup.6 is a hydrogen atom, a lower alkyl group, a lower acyl group or a lower alkylcarbamoyl group, or when --Z--B is --OCONR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 or --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3, R.sup.6 and R.sup.3 together may represent a heterocyclic ring of 6 or 7 members including two nitrogen atoms; l is an integer of 0-2; and n is an integer of 0-5. The 1,2-di-substituted benzene-carboxamide derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in humans.

公开(公告)号：US08592582B2

公开(公告)日：2013-11-26

申请号：US13520203

申请日：2011-01-05

申请人： Hirotada Fukunishi ,  Naoto Hanyu ,  Masaru Suetsugu ,  Takuya Hiruma

发明人： Hirotada Fukunishi ,  Naoto Hanyu ,  Masaru Suetsugu ,  Takuya Hiruma

IPC分类号： C07D403/04

CPC分类号： C07D403/04

摘要： The present invention provides a method for producing a pyrimidinylpyrazole compound (1), wherein aminoguanidine (2) or its salt is reacted with a β-diketone compound (3) to produce the pyrimidinylpyrazole compound: wherein R1 and R3 are each independently an alkyl group having 1 to 4 carbon atoms, and R2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. The method is excellent in the environmental compatibility and economic efficiency.

摘要翻译： 本发明提供一种制备嘧啶基吡唑化合物（1）的方法，其中氨基胍（2）或其盐与β-二酮化合物（3）反应以产生嘧啶基吡唑化合物：其中R 1和R 3各自独立地为烷基 具有1至4个碳原子，并且R 2是氢原子或具有1至4个碳原子的烷基。 该方法在环境兼容性和经济效益上优异。