公开(公告)号：KR100844125B1

公开(公告)日：2008-07-04

申请号：KR1020070028620

申请日：2007-03-23

Applicant: 한국화학연구원

Inventor： 전동주 ,  노재성 ,  송종환 ,  이계형 ,  김익연 ,  박창민 ,  천혜경 ,  조영식 ,  송진숙 ,  배명애 ,  유성은

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: A 7-(3',4'-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compound is provided to show excellent activity on PDE-4 enzymes and high selectivity on other PDE enzymes and improve vomiting related side effects, which is one most serious problem of the PDE-4 inhibitors, thereby being used as a therapeutic agent of asthma and chronic obstructive pulmonary diseases, arthritis, atopic dermatitis, leukemia, cancer and brain diseases. A 7-(3',4'-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compound is represented by a formula(1) and is prepared by reacting 3-amino-triazole compound represented by a formula(4) with 3-(dimethylamino)-1-(3,4-dialkoxyphenyl)prophenone compound represented by a formula(5) or 3-(3,4-dialkoxyphenyl)3-oxopropionealdehyde compound represented by a formula(6) in the presence of acetic acid. In the formulae, each R1 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl, linear or branched saturated or unsaturated C1-7 alkyl including O, N or S, C3-7 cycloalkyl, C3-7 cycloalkyl including O, N or S, (C3-7)cycloalkyl(C1-7)alkyl, 3 to 7-membered saturated or unsaturated heterocycloalkyl including O, N, or S in a heterocycle, phenyl or benzyl, or R1 and R2 may be linked to each other by C1-3 alkylene or C1-3 alkylene including halogen; R3 is aryl selected from groups(1) to (4). A pharmaceutical composition for treating or preventing diseases related to bronchial inflammation such as asthma and chronic obstructive pulmonary disease, arthritis, atopic dermatitis, leukemia, cancer and brain diseases such as Alzheimer's disease, depression and memory decrease comprises the 7-(3',4'-dialkoxyphenyl)-[1,2,4]-triazolo[1,5-a]pyrimidine compound or a pharmaceutically acceptable carrier as an effective ingredient.

Abstract translation: 提供7-（3'，4'-二烷氧基苯基） - [1,2,4] - 三唑并[1,5-a]嘧啶化合物以显示对PDE-4酶的优异活性和对其它PDE酶的高选择性， 改善呕吐相关的副作用，这是PDE-4抑制剂的一个最严重的问题，从而被用作哮喘和慢性阻塞性肺疾病，关节炎，特应性皮炎，白血病，癌症和脑疾病的治疗剂。 7-（3'，4'-二烷氧基苯基） - [1,2,4] - 三唑并[1,5-a]嘧啶化合物由式（1）表示，并通过3-氨基 - 三唑化合物 由式（4）与由式（5）表示的3-（二甲基氨基）-1-（3,4-二烷氧基苯基）丙烯酮化合物或由式（5）表示的3-（3,4-二烷氧基苯基）3-氧代丙醛化合物 （6）在乙酸存在下。 在该式中，每个R 1和R 2独立地为H，直链或支链饱和或不饱和的C 1-7烷基，包括O，N或S，C 3-7环烷基，C 3-7环烷基的直链或支链饱和或不饱和C 1-7烷基，包括 O，N或S，（C 3-7）环烷基（C 1-7）烷基，在杂环中包括O，N或S的3至7元饱和或不饱和杂环烷基，苯基或苄基，或R 1和R 2可以相连 通过C1-3亚烷基或包括卤素的C1-3亚烷基; R3是选自（1）〜（4）的芳基。 用于治疗或预防与哮喘和慢性阻塞性肺病，关节炎，特应性皮炎，白血病，癌症和脑疾病如阿尔茨海默病，抑郁和记忆减退等支气管炎有关的疾病的药物组合物包括7-（3'，4 '二烷氧基苯基） - [1,2,4] - 三唑并[1,5-a]嘧啶化合物或药学上可接受的载体作为有效成分。

公开(公告)号：KR100820246B1

公开(公告)日：2008-04-07

申请号：KR1020060098670

申请日：2006-10-10

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  정준원 ,  박창민 ,  소원영 ,  강남숙 ,  서지희 ,  김낙정 ,  박순찬 ,  천혜경 ,  조영식 ,  배명애 ,  김기영 ,  송진숙 ,  현영란 ,  김용은 ,  노성구 ,  이태규 ,  조중명 ,  유성은

IPC: C07D231/12 ,  C07D401/04

Abstract: A novel pyrazole compound is provided to show excellent inhibitory activity on PDE-4 enzyme, thereby being used in order to prevent and treat asthma, chronic obstructive pulmonary disease, arthritis, atopic dermatitis, tumor and degenerative brain diseases. A 1-(3,4-dialkoxybenzyl)-1H-pyrazole compound is represented by the formula(1), wherein each R1 and R2 is independently H, linear or branched C1-7 alkyl, linear or branched C1-7 C1-7 alkyl including halogen, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, 3- to 7-membered heterocycloalkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkyl including O, N or S in a hetero-cycle, phenyl, benzyl or allyl, or R1 and R2 may be linked to each other with C1-3 alkylene or C1-3 alkylene including halogen; R3 is H, formyl, halogen, linear or branched C1-10 alkyl, C1-10 alkoxy, C3-7 cycloalkyl, (C1-7)alkoxy(C1-7)alkyl, C1-7 alkyl ketone, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, (C1-10)alkylcarboxylic acid, carboxyl(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl; (C3-7)cycloalkylamino, morpholine, morpholine oxide, piperidine, piperazine, piperazine oxide, cyano, nitro, carboxylic acid guanidine, urea, phenoxy, benzyloxy, or an Aryl represented by the group(I); each R4 and R5 is independently H, halogen, formyl, linear or branched C1-10 alkyl, C1-10 alkoxy, (C1-10)alkoxy(C1-10)alkyl, C1-7 alkylketone, hydroxy(C1-10)alkyl, C3-7 cycloalkyl, (C3-7)cycloalkyl(C1-7)alkyl, (C3-7)cycloalkyl(C1-7)alkoxy, carboxylic acid, carboxyl(C1-10)alkylester, carboxyl(C1-10)alkylamide, amino, mono or di(C1-7)alkylamino, mono or di(C1-7)alkylaminocarbonyl, phenyl, phenoxy, benzyl, benzyloxy, 3- to 7-membered heterocycloalkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkyl including O, N or S in a hetero-cycle, 3- to 7-membered heterocycloalkyl(C1-7)alkoxy including O, N or S in a hetero-cycle, cyano, nitro, (C3-7)cycloalkylamino, guanidine, or urea. A method for preparing the compound of the formula(1) comprises a step of reacting a halobenzyl compound represented by the formula(3) with a pyrazole compound represented by the formula(4), each R1, R2, R3, R4, and R5 are same as defined above, and X is halogen. A pharmaceutical composition for preventing and treating inflammation related diseases such as asthma and chronic obstructive pulmonary diseases comprises the compound of the formula(1) as an effective ingredient.

Abstract translation: 提供了一种新的吡唑化合物，以显示对PDE-4酶的优异抑制活性，从而用于预防和治疗哮喘，慢性阻塞性肺病，关节炎，特应性皮炎，肿瘤和退行性脑疾病。 1-（3,4-二烷氧基苄基）-1H-吡唑化合物由式（1）表示，其中每个R 1和R 2独立地为H，直链或支链C 1-7烷基，直链或支链C 1-7 C1-7 烷基，包括卤素，C 3-7环烷基，（C 3-7）环烷基（C 1-7）烷基，在杂环中包括O，N或S的3-至7-元杂环烷基，3-至7-元杂环烷基 -7）烷基，包括异环周期中的O，N或S，苯基，苄基或烯丙基，或者R 1和R 2可以与C 1-3亚烷基或包括卤素的C 1-3亚烷基彼此连接; R 3为H，甲酰基，卤素，直链或支链C 1-10烷基，C 1-10烷氧基，C 3-7环烷基，（C 1-7）烷氧基（C 1-7）烷基，C 1-7烷基酮，（C 3-7） 环烷基（C1-7）烷基，（C3-7）环烷基（C1-7）烷氧基，（C1-10）烷基羧酸，羧基（C1-10）烷基酯，羧基（C1-10）烷基酰胺，氨基，单或二 （C 1-7）烷基氨基，单或二（C 1-7）烷基氨基羰基; （C3-7）环烷基氨基，吗啉，吗啉氧化物，哌啶，哌嗪，哌嗪氧化物，氰基，硝基，羧酸胍，脲，苯氧基，苄氧基或由基团（I）表示的芳基。 每个R 4和R 5独立地为H，卤素，甲酰基，直链或支链C 1-10烷基，C 1-10烷氧基，（C 1-10）烷氧基（C 1-10）烷基，C 1-7烷基酮，羟基（C 1-10）烷基 ，C3-7环烷基，（C3-7）环烷基（C1-7）烷基，（C3-7）环烷基（C1-7）烷氧基，羧酸，羧基（C1-10）烷基酯，羧基（C1-10）烷基酰胺 ，氨基，单或二（C1-7）烷基氨基，单或二（C1-7）烷基氨基羰基，苯基，苯氧基，苄基，苄氧基，包含异质周期中的O，N或S的3-至7-元杂环烷基， 包含杂环中的O，N或S的3-至7-元杂环烷基（C 1-7）烷基，异异环中包括O，N或S的3-至7-元杂环烷基（C 1-7）烷氧基， 氰基，硝基，（C 3-7）环烷基氨基，胍或脲。 制备式（1）化合物的方法包括使由式（3）表示的卤苄基化合物与式（4）表示的吡唑化合物反应，每个R 1，R 2，R 3，R 4和R 5 与上述相同，X为卤素。 用于预防和治疗炎症相关疾病如哮喘和慢性阻塞性肺疾病的药物组合物包含式（1）化合物作为有效成分。

公开(公告)号：KR100617992B1

公开(公告)日：2006-08-31

申请号：KR1020040101458

申请日：2004-12-03

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  이계형 ,  정준원 ,  박창민 ,  정순민 ,  장규환 ,  강남숙 ,  홍석주 ,  천혜경 ,  남지연 ,  장범수 ,  곽현정 ,  송진숙 ,  허준영 ,  양승돈 ,  전영호 ,  노성구 ,  이태규 ,  현영란 ,  유성은 ,  조중명 ,  허용석 ,  윤정민

IPC: C07D487/04

Abstract: 본 발명은 화학식 1로 표시되는 신규한 2-아릴-7-(3′,4′-디알콕시페닐)-피라졸로[1,5-а]피리미딘 화합물 또는 그의 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효성분으로 함유하는 것을 특징으로 하는 천식 및 만성폐쇄성 폐질환(Chronic Obstructive Pulmonary Disease)을 포함한 염증관련 질환의 치료를 위한 약제학적 조성물에 관한 것이다.
[화학식1]

公开(公告)号：KR100850969B1

公开(公告)日：2008-08-12

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: 본 발명은 하기의 화학식 1로 표시되는 신규한 1-[1-(3,4-디알콕시페닐)-알킬]-1
H -피라졸 화합물 또는 그의 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효성분으로 함유하는 것을 특징으로 하는 천식 및 만성폐쇄성 폐질환(Chronic Obstructive Pulmonary Disease)을 포함한 염증관련 질환의 치료 및 관절염, 아토피피부염, 백혈병과 각종 암 및 알쯔하이머 등의 퇴행성뇌질환의 예방 및 치료용 또는 기억력증진용 약제학적 조성물에 관한 것이다.
[화학식 1]

1-[1-(3,4-디알콕시페닐)-알킬]-1H-피라졸 화합물, PDE-4, 천식, 만성폐쇄성 폐질환, 염증관련 질환, 관절염, 아토피피부염, 백혈병, 암, 중추신경계 질환, 알쯔하이머.

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。

公开(公告)号：KR100689961B1

公开(公告)日：2007-03-08

申请号：KR1020050018325

申请日：2005-03-04

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  이계형 ,  정준원 ,  박창민 ,  정순민 ,  김지영 ,  강남숙 ,  홍석주 ,  천혜경 ,  남지연 ,  장범수 ,  곽현정 ,  송진숙 ,  허준영 ,  양승돈 ,  전영호 ,  노성구 ,  이태규 ,  현영란 ,  조중명 ,  허용석 ,  윤정민 ,  유성은

IPC: C07D277/42 ,  A61P11/06 ,  A61P25/28

Abstract: 본 발명은 하기의 화학식 1로 표시되는 신규한 4-(3,4-디알콕시페닐)-2-아미노티아졸 화합물 또는 그의 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효성분으로 함유하는 것을 특징으로 하는 천식 및 만성폐쇄성 폐질환(Chronic Obstructive Pulmonary Disease)을 포함한 염증관련 질환의 치료 및 알쯔하이머를 포함한 중추신경계통 질환의 치료, 예방을 위한 약제학적 조성물에 관한 것이다.
[화학식 1]

4-(3,4-디알콕시페닐)-2-아미노티아졸, PDE-4, 천식, 만성폐쇄성 폐질환, 염증관련 질환, 중추신경계 질환, 알쯔하이머.

公开(公告)号：KR100833799B1

公开(公告)日：2008-05-30

申请号：KR1020070002725

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: C07D401/06 ,  C07D413/14

Abstract: 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds are provided to inhibit activity of PDE-4(phosphodiesterase-4) with high activity and selectivity without side effects, so that the compounds are useful for treating inflammation diseases, neurodegenerative disease and cancers. 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds represented by the formula(1) are provided, wherein A is N or CH; R1 is linear or branched, saturated or unsaturated (C1-C7)alkyl or halogen-substituted linear or branched, saturated or unsaturated (C1-C7)alkyl; R2 is hydrogen atom, (C3-C7)cycloalkyl or (C3-C8)cycloalkylmethyl; R3, R4 and R5 are each independently hydrogen atom, phenyl, pyridinyl, N-oxypyridinyl, linear or branched, saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C3-C10)cycloalkyl(C1-C7)alkyl, halogen atom, cyano, nitro, amino, mono- or di(C1-C7)alkylamino, mono- or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamino, 3- to 7-membered saturated or unsaturated hetero ring containing oxygen, nitrogen or sulfur in hetero ring, guanidinyl, ureido, benzyl, benzyloxy, formyl, (C1-C7)alkanoyl, (C1-C7)alkoxy, (C1-C7)alkoxy(C1-C7)alkyl, hydroxy(C1-C7)alkyl, carboxyl or (C1-C7)alkoxycarbonyl; and R6 is pyridinyl or N-oxypyridinyl group.

Abstract translation: 提供1- [1-（3,4-二烷氧基芳基） - 吡啶基甲基] -1H-吡唑化合物以抑制具有高活性和选择性的PDE-4（磷酸二酯酶-4）的活性而没有副作用，使得该化合物可用于 治疗炎症疾病，神经退行性疾病和癌症。 提供由式（1）表示的1- [1-（3,4-二烷氧基芳基） - 吡啶基甲基] -1H-吡唑化合物，其中A是N或CH; R1是直链或支链饱和或不饱和（C1-C7）烷基或卤素取代的直链或支链饱和或不饱和（C1-C7）烷基; R2是氢原子，（C3-C7）环烷基或（C3-C8）环烷基甲基; R 3，R 4和R 5各自独立地为氢原子，苯基，吡啶基，N-氧代吡啶基，直链或支链，饱和或不饱和的（C1-C7）烷基，（C3-C7）环烷基，（C3-C10）环烷基 ）（C 1 -C 7）烷基氨基羰基，（C 3 -C 7）环烷基氨基，3至7元饱和或不饱和的（C 1 -C 7）烷基氨基， 杂环中含氧，氮或硫的杂环，胍基，脲基，苄基，苄氧基，甲酰基，（C1-C7）烷酰基，（C1-C7）烷氧基，（C1-C7）烷氧基（C1-C7） （C 1 -C 7）烷基，羧基或（C 1 -C 7）烷氧基羰基; R6是吡啶基或N-氧代吡啶基。

公开(公告)号：KR1020060097242A

公开(公告)日：2006-09-14

申请号：KR1020050018325

申请日：2005-03-04

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  이계형 ,  정준원 ,  박창민 ,  정순민 ,  김지영 ,  강남숙 ,  홍석주 ,  천혜경 ,  남지연 ,  장범수 ,  곽현정 ,  송진숙 ,  허준영 ,  양승돈 ,  전영호 ,  노성구 ,  이태규 ,  현영란 ,  조중명 ,  허용석 ,  윤정민 ,  유성은

IPC: C07D277/42 ,  A61P11/06 ,  A61P25/28

Abstract: 본 발명은 하기의 화학식 1로 표시되는 신규한 4-(3,4-디알콕시페닐)-2-아미노티아졸 화합물 또는 그의 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효성분으로 함유하는 것을 특징으로 하는 천식 및 만성폐쇄성 폐질환(Chronic Obstructive Pulmonary Disease)을 포함한 염증관련 질환의 치료 및 알쯔하이머를 포함한 중추신경계통 질환의 치료, 예방을 위한 약제학적 조성물에 관한 것이다.
[화학식 1]

4-(3,4-디알콕시페닐)-2-아미노티아졸, PDE-4, 천식, 만성폐쇄성 폐질환, 염증관련 질환, 중추신경계 질환, 알쯔하이머.

公开(公告)号：KR1020060062581A

公开(公告)日：2006-06-12

申请号：KR1020040101458

申请日：2004-12-03

Applicant: 한국화학연구원

Inventor： 노재성 ,  전동주 ,  송종환 ,  이계형 ,  정준원 ,  박창민 ,  정순민 ,  장규환 ,  강남숙 ,  홍석주 ,  천혜경 ,  남지연 ,  장범수 ,  곽현정 ,  송진숙 ,  허준영 ,  양승돈 ,  전영호 ,  노성구 ,  이태규 ,  현영란 ,  유성은 ,  조중명 ,  허용석 ,  윤정민

IPC: C07D487/04

Abstract: 본 발명은 화학식 1로 표시되는 신규한 2-아릴-7-(3′,4′-디알콕시페닐)-피라졸로[1,5-а]피리미딘 화합물 또는 그의 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효성분으로 함유하는 것을 특징으로 하는 천식 및 만성폐쇄성 폐질환(Chronic Obstructive Pulmonary Disease)을 포함한 염증관련 질환의 치료를 위한 약제학적 조성물에 관한 것이다.
[화학식1]