公开(公告)号：KR1020110028050A

公开(公告)日：2011-03-17

申请号：KR1020090085954

申请日：2009-09-11

Applicant: 한국화학연구원

Inventor： 허정녕 ,  배명애 ,  김낙정 ,  장성연 ,  강남숙 ,  유성은 ,  황은숙

IPC: C07D265/33 ,  C07D265/32 ,  A61K31/4965 ,  A61P19/10

CPC classification number: C07D213/50 ,  C07D213/89 ,  C07D239/26 ,  C07D241/12 ,  C07D295/088 ,  C07D333/22

Abstract: PURPOSE: A pharmaceutical composition containing indenone derivative for preventing or treating bone diseases is provided to suppress bone absorption of osteoclast. CONSTITUTION: An indenone derivative is denoted by chemical formula 1. In chemical formula 1, R1 is 5-10 cyclic heteroaryl of C6-C10 aryl, Y is CH, N, N+(-C1-C6alkyl) or N+(-O-). A pharmaceutical composition for preventing and treating bone diseases contains the indenone derivative and physiologically acceptable salt as an active ingredient. The bone diseases is osteoporosis, fracture, periodontal diseases, bone metastatic cancer, or rheumatoid arthritis.

Abstract translation: 目的：提供含有用于预防或治疗骨病的茚酮酮衍生物的药物组合物，以抑制破骨细胞的骨吸收。 在化学式1中，R1是C6-C10芳基的5-10个环状杂芳基，Y是CH，N，N +（ - C1-C6烷基）或N +（ - O-） 。 用于预防和治疗骨疾病的药物组合物含有茚酮酮衍生物和生理学上可接受的盐作为活性成分。 骨病是骨质疏松症，骨折，牙周病，骨转移性癌症或类风湿性关节炎。

公开(公告)号：KR1020100094337A

公开(公告)日：2010-08-26

申请号：KR1020097017134

申请日：2008-01-16

Applicant: (주) 카이노스메드 ,  한국화학연구원 ,  영진약품 주식회사

Inventor： 김성수 ,  안진희 ,  천혜경 ,  이상달 ,  강남숙 ,  김기영 ,  강승규 ,  정원훈 ,  김성규 ,  김선영 ,  권재홍 ,  손상권 ,  신민기 ,  하니나

IPC: C07D277/22 ,  C07D417/12 ,  A61K31/427 ,  A61P19/10

CPC classification number: C07D277/06 ,  C07D417/12 ,  Y02P20/55

Abstract: PURPOSE: A dipeptidyl peptidase(DPP-IV) inhibitor is provided to use in treating DPP-IV-mediated disease. CONSTITUTION: A 2-carbonyl-3-acyl-1,3-thiazolidine of salt or prodrug form has a beta-amino group on acyl chain. A method for preparing the 2-carbonyl-3-acyl-1,3-thiazolidine derivative comprises: a step of condensing an amino acid of chemical formula Q-2 with a 2-cabonyl-1,3-thiazolidine compounds of chemical formula Q-3 to form a compound of chemical formula Q-4; and a step of deprotecting the compound of chemical formula Q-4 to obtain 2-carbonyl-3-acyl-1,3-thiazolidine derivative of chemical formula Q-1a. A pharmaceutical composition contains the 2-carbonyl-3-acyl-1,3-thiazolidine, pharmaceutically acceptable diluents, or carrier. The pharmaceutical composition is used for preventing or treating dipeptidyl peptidase IV(DPP-IV)-mediated disease.

Abstract translation: 目的：提供二肽基肽酶（DPP-IV）抑制剂用于治疗DPP-IV介导的疾病。 构成：盐或前药形式的2-羰基-3-酰基-1,3-噻唑烷在酰基链上具有β-氨基。 制备2-羰基-3-酰基-1,3-噻唑烷衍生物的方法包括：将化学式Q-2的氨基酸与化学式Q的2-缩水甘油基-1,3-噻唑烷化合物缩合的步骤 -3以形成化学式Q-4的化合物; 以及使化学式Q-4的化合物脱保护，得到化学式Q-1a的2-羰基-3-酰基-1,3-噻唑烷衍生物的工序。 药物组合物含有2-羰基-3-酰基-1,3-噻唑烷，药学上可接受的稀释剂或载体。 该药物组合物用于预防或治疗二肽基肽酶IV（DPP-IV）介导的疾病。

公开(公告)号：KR100848491B1

公开(公告)日：2008-07-28

申请号：KR1020070004577

申请日：2007-01-16

Applicant: 영진약품 주식회사 ,  한국화학연구원

Inventor： 김성수 ,  천혜경 ,  이상달 ,  안진희 ,  김기영 ,  강남숙 ,  강승규 ,  정원훈 ,  김성규 ,  김선영 ,  권재홍 ,  손상권 ,  신민기 ,  하니나

IPC: C07D277/06 ,  C07D417/06 ,  A61P3/08 ,  A61P3/04

CPC classification number: C07D277/06 ,  C07D417/12 ,  Y02P20/55

Abstract: 2-Thiazolidine derivatives having beta-amino group are provided to inhibit activity of DPP-IV(dipeptidyl peptidase-IV) associated with activity regulation of various hormones, so that the compounds are useful for treating diseases mediated by DPP-IV including type 2 diabetes mellitus. The 2-thiazolidine derivatives having beta-amino group represented by the formula(1) are prepared by reacting an amino acid represented by the formula(2) with 2-thiazolidine compounds represented by the formula(3) to prepare compounds represented by the formula(4), and deprotecting the compounds represented by the formula(4), wherein BOC is a protecting group; A is -NR^e(CH2)nR2 or -OR^b; R^a is hydrogen, C1-6 alkyl, C1-6 alkoxy, -OCF3, halogen, -CN or -CF3; R^b is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, isopropyl, t-butyl, -CH2CH2OH, -CH2CH2NH2, -CH2CH2N(CH2CH2)2O, -CH2CH2N(CH2CH3)2 or -CH2CH2NHCOCH3; R^c is hydrogen, C1-6 alkyl, C3-6 cycloalkyl, benzyl, isopropyl or t-butyl; R^d and R^e are each independently hydrogen, C1-6 alkyl or C3-6 cycloalkyl; Y is carbon, oxygen, sulfur or nitrogen; Z is hydrogen, C1-6 alkyl, C3-6 cycloalkyl or -CO2R^b; and n is an integer of 0, 1 or 2.

Abstract translation: 提供具有β-氨基的2-噻唑烷衍生物以抑制与各种激素的活性调节相关的DPP-IV（二肽基肽酶-IV）的活性，使得该化合物可用于治疗包括2型糖尿病的DPP-IV介导的疾病 糖尿病。 由式（1）表示的具有β-氨基的2-噻唑烷衍生物通过使由式（2）表示的氨基酸与由式（3）表示的2-噻唑烷化合物反应来制备由式 （4）表示的化合物，并使由式（4）表示的化合物脱保护，其中BOC为保护基; A是-NR e（CH 2）n R 2或-OR b; R a a是氢，C 1-6烷基，C 1-6烷氧基，-OCF 3，卤素，-CN或-CF 3; 异丙基，叔丁基，-CH 2 CH 2 OH，-CH 2 CH 2 NH 2，-CH 2 CH 2 N（CH 2 CH 2）2 O，-CH 2 CH 2 N（CH 2 CH 3）2或-CH 2 CH 2 NHCOCH 3; R c是氢，C 1-6烷基，C 3-6环烷基，苄基，异丙基或叔丁基; R d和R e e各自独立地为氢，C 1-6烷基或C 3-6环烷基; Y是碳，氧，硫或氮; Z是氢，C 1-6烷基，C 3-6环烷基或-CO 2 R b; 且n为0,1或2的整数。

公开(公告)号：KR1020080007764A

公开(公告)日：2008-01-23

申请号：KR1020060066812

申请日：2006-07-18

Applicant: 한국화학연구원 ,  영진약품 주식회사

Inventor： 김성수 ,  천혜경 ,  이상달 ,  안진희 ,  김기영 ,  강남숙 ,  강승규 ,  정원훈 ,  김성규 ,  김선영 ,  권재홍 ,  손상권 ,  신민기

IPC: C07D255/02 ,  A61P3/00

Abstract: A 1,2,5-triazepane derivative showing excellent DPP-IV inhibitory activity is provided to be effectively used for preventing or treating diseases mediated by DPP-IV such as insulin-dependent, insulin non-dependent diabetes, arthritis, obesity, osteoporosis, and damaged glucose resistance. A 1,2,5-triazepane derivative having a beta-amino group is represented by the formula(1), wherein R1 is a group represented by the structural formula(1-1) or (1-2); R2 is H, C1-6 alkyl, or a group represented by the structural formula(1-3); R3 is H, C1-6 alkyl, C3-6 cycloalkyl, CH2CO2R^b, COCO2R^b, pyrazine, and a group represented by the structural formula(1-4), (1-5) or (1-6); R^a is independently H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, OCF3, halogen, CN, CF3, COOR^b or NR^bR^c; each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl; R^d is C1-6 alkyl, trifluoromethyl, and a group represented by the structural formula(1-1), (1-7), (1-8), or (1-9); R^e is C1-6 alkyl, C3-6 cycloalkyl, and a group represented by the structural formula(1) or (2); R^f is H, halogen, NR^bR^c, tetrazole, proline, and a group represented by the structural formula(1-10), (1-11), (1-12), or (1-13); A is CH, N, O or S; B is H, C1-6 alkyl, C3-6 cycloalkyl, benzyl or CO2R^d; X is O or S; and n is 0 or 1. A method for preparing the 1,2,5-triazepane derivative comprises the steps of: (a) subjecting an amino acid represented by the formula(2) and 1,2,5-triazepane to a condensation reaction to prepare a compound represented by the formula(4); (b) reacting the compound of the formula(4) with an electrophilic compound substituted with R2 to prepare a compound represented by the formula(5); and (c) deprotecting the compound of the formula(5). A pharmaceutical composition for preventing or treating diseases mediated by DPP-IV comprises an effective amount of the 1,2,5-triazepane derivative or a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.

Abstract translation: 提供了显示优异的DPP-IV抑制活性的1,2,5-三氮丙平衍生物，其有效用于预防或治疗由DPP-IV介导的疾病，例如胰岛素依赖性，胰岛素非依赖型糖尿病，关节炎，肥胖症，骨质疏松症， 并损害葡萄糖耐量。 具有β-氨基的1,2,5-三氮杂环庚烷衍生物由式（1）表示，其中R1是由结构式（1-1）或（1-2）表示的基团。 R2是H，C1-6烷基或由结构式（1-3）表示的基团; R 3是H，C 1-6烷基，C 3-6环烷基，CH 2 CO 2 R b，COCO 2 R b，吡嗪和由结构式（1-4），（1-5）或（1-6）表示的基团。 R a a独立地为H，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，OCF 3，卤素，CN，CF 3，COOR b或NR b R c; 每个R b和R c独立地是H，C 1-6烷基或C 3-6环烷基; R 1-6是C1-6烷基，三氟甲基和由结构式（1-1），（1-7），（1-8）或（1-9）表示的基团。 R 1-6是C 1-6烷基，C 3-6环烷基和由结构式（1）或（2）表示的基团。 （1-10），（1-11），（1-12）或（1-13）表示的基团，其中R为氢，卤素，NR 4 b R c，四唑，脯氨酸和由结构式 ; A是CH，N，O或S; B是H，C 1-6烷基，C 3-6环烷基，苄基或CO 2 R d; X是O或S; 并且n为0或1.制备1,2,5-三氮杂环庚烷衍生物的方法包括以下步骤：（a）使由式（2）表示的氨基酸和1,2,5-三氮杂环庚烷进行缩合 反应制备式（4）表示的化合物; （b）使式（4）的化合物与被R 2取代的亲电子化合物反应，制备由式（5）表示的化合物。 和（c）使式（5）的化合物脱保护。 用于预防或治疗由DPP-IV介导的疾病的药物组合物包含有效量的1,2,5-三氮丙烯衍生物或其药学上可接受的盐和药学上可接受的载体。

公开(公告)号：KR100792275B1

公开(公告)日：2008-01-08

申请号：KR1020060017372

申请日：2006-02-22

Applicant: 영진약품 주식회사 ,  한국화학연구원

Inventor： 김성수 ,  천혜경 ,  이상달 ,  안진희 ,  강남숙 ,  김기영 ,  강승규 ,  정원훈 ,  김성규 ,  김선영 ,  권재홍 ,  손상권

IPC: C07D231/04 ,  C07D237/04

CPC classification number: Y02P20/55

Abstract: 하기 화학식 1로 표시되는, 베타아미노기를 갖는 고리화된 히드라자이드 유도체 또는 이의 약학적으로 허용 가능한 염이 제공된다. 이 고리화된 히드라자이드 유도체는 DPP-IV의 활성을 억제하여, DPP-IV에 의해 매개되는 각종 질환을 치료하는데 유용하다.
[화학식 1]

상기 식에서, R
1 , R
2 및 n은 명세서에 정의되는 바와 같다.
고리화된 히드라자이드 유도체, DPP-IV, 제조 방법, 약학 조성물

公开(公告)号：KR1020120111347A

公开(公告)日：2012-10-10

申请号：KR1020110029772

申请日：2011-03-31

Applicant: 한국화학연구원

Inventor： 김기영 ,  안진희 ,  강승규 ,  이상달 ,  배명애 ,  안성훈 ,  김희연 ,  정원훈 ,  강남숙

IPC: C07C311/43 ,  C07C311/41 ,  A61K31/18 ,  A61P3/10

Abstract: PURPOSE: An arylsulfoneamide derivative comprising a cyclopropyl group is provided to have excellent 11B-HSD1 restraining activity and to treat or prevent diseases like hardening of the arteries, osteoporosis, damaged glucose resistance, etc which are carried by 11B-HSD1. CONSTITUTION: An arylsulfoneamide derivative comprising a cyclopropyl group or a pharmaceutically acceptable salt thereof is represented by chemical formula 1. In chemical formula 1, if R^1 and R^2 is cyclopropyl then R^3 is methyl, if R^3 is cyclopropyl then R^1 and R^2 is respectively hydrogen, Ar is a functional group in chemical formula 1-a, a functional group in chemical formula 1-b, a functional group in chemical formula 1-c or naphthyl, R^a is respectively and independently methyl, isopropyl, t-butyl, C1-6 alkyl, methoxy, OCF3, halogen or CF3, and R^b and R^c is respectively and independently hydrogen, methyl, halogen or CF3.

Abstract translation: 目的：提供包含环丙基的芳基砜酰胺衍生物，以具有优异的11B-HSD1抑制活性，并治疗或预防由11B-HSD1携带的动脉硬化，骨质疏松症，损伤的葡萄糖耐药性等疾病。 构成：包含环丙基的芳基磺酰胺衍生物或其药学上可接受的盐由化学式1表示。在化学式1中，如果R 1和R 2是环丙基，则R 3是甲基，如果R 3是环丙基 那么R 1和R 2分别是氢，Ar是化学式1-a中的官能团，化学式1-b中的官能团，化学式1-c中的官能团或萘基，R 1 a 分别独立地为甲基，异丙基，叔丁基，C 1-6烷基，甲氧基，OCF 3，卤素或CF 3，R 1b和R cc分别独立地为氢，甲基，卤素或CF 3。

公开(公告)号：KR101117128B1

公开(公告)日：2012-03-14

申请号：KR1020090121291

申请日：2009-12-08

Applicant: 한국화학연구원

Inventor： 김낙정 ,  배명애 ,  유성은 ,  강남숙 ,  허정녕 ,  이규양 ,  서지희 ,  장성연 ,  황은숙 ,  홍정호

IPC: C07D487/04 ,  A61K31/437 ,  A61P19/08 ,  A61P3/04

Abstract: 본 발명은 페닐테트라졸 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 골다공증, 비만, 당뇨 또는 고지혈증의 예방 또는 치료용 약학적 조성물에 관한 것으로서, 상기 유도체는 TAZ 단백질을 조절하므로, 골다공증, 비만, 당뇨 또는 고지혈증의 예방 또는 치료에 유용하게 사용될 수 있다.
페닐테트라졸 유도체, TAZ, 골다공증, 비만, 당뇨, 고지혈증

公开(公告)号：KR1020100130027A

公开(公告)日：2010-12-10

申请号：KR1020090048675

申请日：2009-06-02

Applicant: 한국화학연구원

Inventor： 김낙정 ,  배명애 ,  유성은 ,  강남숙 ,  허정녕 ,  이규양 ,  서지희 ,  임채조 ,  황은숙 ,  홍정호

IPC: C07D257/04 ,  C07D403/08 ,  A61P19/10

Abstract: PURPOSE: A pharmaceutical composition containing imidazo phenyltetrazole derivative for preventing and treating osteoporosis, obesity, diabetes or hyperlipidemia is provided. CONSTITUTION: A pharmaceutical composition for preventing or treating osteroporosis contaisn imidazo phenyltetrazole derivative of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for preventing or treating obesity, diabetes or hyperlipidemia contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient.

Abstract translation: 目的：提供含有咪唑并噻唑衍生物的预防和治疗骨质疏松症，肥胖症，糖尿病或高脂血症的药物组合物。 构成：用于预防或治疗化学式1的咪唑并苯并噻唑衍生物或其药学上可接受的盐作为有效成分的药物组合物。 用于预防或治疗肥胖症，糖尿病或高脂血症的药物组合物含有化学式1的化合物或其药学上可接受的盐作为活性成分。

公开(公告)号：KR1020080065722A

公开(公告)日：2008-07-15

申请号：KR1020070002715

申请日：2007-01-10

Applicant: 한국화학연구원

Inventor： 전동주 ,  노재성 ,  송종환 ,  이계형 ,  김익연 ,  박창민 ,  소원영 ,  이지선 ,  김은주 ,  강남숙 ,  천혜경 ,  조영식 ,  송진숙 ,  배명애 ,  김지현 ,  조중명 ,  노성구 ,  현영란 ,  이철순 ,  이재일 ,  유성은

IPC: C07D231/12 ,  C07D401/04 ,  C07D403/10 ,  C07D413/04

Abstract: A novel compound is provided to show excellent activity on PDE-4 enzymes and high selectivity on other PDE enzymes, thereby being used as a therapeutic agent of inflammation related diseases, arthritis, atopic dermatitis, leukemia, various cancers and degenerative brain diseases with little side effects. A 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole compound is represented by a formula(1) and is prepared by reacting a halo-benzyl compound represented by a formula(2) with a pyrazole compound represented by a formula(3). In the formula(1), each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, aryl or heteroaryl, ar(C1-5)alkyl, or ar(C1-5)alkoxy, or the R1 and R2 may be linked to each other by C1-3 alkylene; each R3, R4 and R5 is independently H, phenyl, pyridinyl, N-oxypyridinyl, linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, halogen, cyano, nitro, amino, mono- or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, C3-7 cycloalkylamino, 3 to 7-membered saturated or unsaturated hetero-ring including O, N or S, guanidinyl, ureido, benzyl, benzyloxy, formyl, C1-7 alkanoyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, hydroxy(C1-7)alkyl, carboxyl, or (C1-7)alkoxycarbonyl; R6 is linear or branched saturated and unsaturated C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, phenyl, phenoxy, benzyl, benzyloxy, C1-7 alkoxy, or (C1-7)alkoxy(C1-7)alkyl. A pharmaceutical composition for treating or preventing diseases related to airway inflammation, arthritis, atopic dermatitis, leukemia, cancer or degenerative brain diseases comprises the 1-[1-(3,4-dialkoxyphenyl)-alkyl]-1H-pyrazole derivative as an effective ingredient.

Abstract translation: 提供了一种新型化合物，以显示对PDE-4酶的优异活性和对其他PDE酶的高选择性，从而被用作炎症相关疾病，关节炎，特应性皮炎，白血病，各种癌症和退行性脑病的治疗剂 效果。 1-（1-（3,4-二烷氧基苯基） - 烷基] -1H-吡唑化合物由式（1）表示，通过式（2）表示的卤代苄基化合物与吡唑化合物 由公式（3）表示。 在式（1）中，每个R 1和R 2独立地为H，可被卤素取代或未取代的直链或支链饱和或不饱和C 1-7烷基，C 3-7环烷基，（C 3-7）环烷基（C 1-7） 烷基，芳基或杂芳基，芳（C 1-5）烷基或芳（C 1-5）烷氧基，或者R 1和R 2可以被C 1-3亚烷基相互连接; 每个R 3，R 4和R 5独立地为H，苯基，吡啶基，N-氧代吡啶基，直链或支链饱和和不饱和C 1-7烷基，C 3-7环烷基，（C 3-10）环烷基（C 1-7）烷基，卤素，氰基 ，硝基，氨基，单或二（C1-7）烷基氨基，单或二（C1-7）烷基氨基羰基，C3-7环烷基氨基，3至7元饱和或不饱和杂环，包括O，N或S，胍基 （C 1-7）烷基，羟基（C 1-7）烷基，羧基或（C 1-7）烷氧基羰基;（C 1-7）烷氧基， R6是直链或支链饱和和不饱和的C1-7烷基，C3-7环烷基，（C3-10）环烷基（C1-7）烷基，苯基，苯氧基，苄基，苄氧基，C1-7烷氧基或（C1-7） 烷氧基（C 1-7）烷基。 用于治疗或预防与气道炎症，关节炎，特应性皮炎，白血病，癌症或退行性脑疾病相关的疾病的药物组合物包括1- [1-（3,4-二烷氧基苯基） - 烷基] -1H-吡唑衍生物作为有效的 成分。

公开(公告)号：KR100753017B1

公开(公告)日：2007-08-30

申请号：KR1020060046860

申请日：2006-05-25

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  이계형 ,  박창민 ,  소원영 ,  강남숙 ,  홍석주 ,  천혜경 ,  조영식 ,  김기영 ,  배명애 ,  송진숙 ,  노성구 ,  현영란 ,  이운영 ,  김용은 ,  강봉균 ,  이혜련 ,  유성은

IPC: A61K31/437 ,  A61P35/00

Abstract: A pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprising 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds is provided to inhibit activity of PDE-4(phosphodiesterase-4) and reduce side effects such as vomiting by reducing HARBS(high-affinity rolipram binding sites) affinity. The pharmaceutical composition for treating or preventing arthritis, atopic dermatitis, tumor and degenerative brain diseases comprises 7-(3,4-Dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidine compounds represented by the formula(1), wherein R1 and R2 are independently hydrogen atom, linear or branched saturated or unsaturated (C1-C7)alkyl, linear or branched saturated or unsaturated (C1-C7)alkyl containing halogen atom, (C3-C7)cycloalkyl, 3-membered to 7-membered heterocycloalkyl containing oxygen, nitrogen or sulfur in a hetero aromatic ring, (C4-C10)cycloalkyl(C1-C7)alkyl, 3-membered to 7-membered heterocycloalkyl(C1-C7)alkyl containing oxygen, nitrogen or sulfur in a hetero ring, phenyl, benzyl or allyl group; R3 is hydrogen atom, halogen atom, formyl, linear or branched and saturated or unsaturated (C1-C7)alkyl, (C1-C7)alkylketone, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl group, carboxylic acid, carboxyl(C1-C7)alkylester, carboxyl(C1-C7)alkylamide, amino, or mono or di(C1-C7)alkylaminocarbonyl; and R4 is hydrogen atom, formyl, linear or branched saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C1-C7)alkoxy, (C1-C7)alkoxy (C1-C7)alkyl, hydroxy(C1-C7)alkyl ketone, (C1-C10)alkylcarboxylic acid, carboxyl(C1-C10)alkylester, carboxyl(C1-C10)alkylamide, amino, mono or di(C1-C7)alkylamino, mono or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamine, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide or aryl group.

Abstract translation: 用于治疗或预防关节炎，特应性皮炎，肿瘤和退行性脑疾病，其包括7-（3,4-二烷氧基） - 吡唑并提供[1,5-a]嘧啶化合物抑制PDE-4的活性（phosphodiesterase-的药物组合物 4）并通过减少HARBS（高亲和力咯利普兰结合位点）亲和力来减少副作用，例如呕吐。 用于治疗或预防关节炎，特应性皮炎，肿瘤和退行性脑疾病的药物组合物包含7-（3,4-二烷氧基） - 吡唑并[1,5-a]嘧啶化合物由式（1）表示，其中R1和R2 （C 1 -C 7）烷基，含有卤素原子的直链或支链饱和或不饱和（C 1 -C 7）烷基，（C 3 -C 7）环烷基，含有3至7元杂环烷基的3元至7元杂环烷基 （C4-C10）环烷基（C1-C7）烷基，在杂环中含有氧，氮或硫的3元至7元杂环烷基（C1-C7）烷基，苯基 ，苄基或烯丙基; （C 1 -C 7）烷基，（C 1 -C 7）烷氧基，（C 1 -C 7）烷氧基（C 1 -C 7）烷基，（C 1 -C 7）烷氧基， （C 1 -C 7）烷基，羧酸，羧基（C 1 -C 7）烷基酯，羧基（C 1 -C 7）烷基酰胺，氨基或单或二（C 1 -C 7）烷基氨基羰基; （C 1 -C 7）烷基，（C 3 -C 7）环烷基，（C 1 -C 7）烷氧基，（C 1 -C 7）烷氧基（C 1 -C 7）烷基，羟基（C 1 -C 7）烷基， C1-C7）烷基酮，（C1-C10）烷基羧酸，羧基（C1-C10）烷基酯，羧基（C1-C10）烷基酰胺，氨基，单或二（C1-C7）烷基氨基，单或二（C1-C7 ）烷基氨基羰基，（C3-C7）环烷基胺，吗啉，氧化吗啉，哌啶，哌嗪，哌嗪氧化物或芳基。