公开(公告)号：EP0336356A3

公开(公告)日：1991-09-25

申请号：EP89105864.6

申请日：1989-04-04

Applicant: ABBOTT LABORATORIES

Inventor： Kerwin, James F. ,  Nadzan, Alex M.

IPC: C07D209/42 ,  C07D209/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D487/02 ,  A61K31/40 ,  A61K31/44 ,  A61K31/47 ,  A61K31/415 ,  A61K31/495

CPC classification number: C07D401/12 ,  C07D209/20 ,  C07D209/42 ,  C07D401/14 ,  C07D403/12 ,  C07D487/04 ,  C07K5/0202 ,  C07K5/06139

Abstract: A compound of the formula:
wherein R₁ and R₂ are independently selected from hydrogen, loweralkyl, cycloalkyl, loweralkenyl, adamantyl, aryl, substituted aryl, heterocyclic group, substituted alkyl, substituted amide, functionalized carbonyl, and nitrogen containing ring wherein R₁, R₂ and the adjacent nitrogen atom form a ring;
R₁₁ is hydrogen, loweralkyl, or loweralkenyl;
R₂₀ is hydrogen, loweralkyl, or loweralkenyl;
B is -(CH₂) m -, substituted alkenylene, -QCH₂- wherein Q is O, S, NH or substituted amino, -CH₂Q- wherein Q is as defined or B is NH;
Z is C=O, S(O)₂, or C=S;
Ar is a heterocyclic group, aryl or substituted aryl;
D is unsubstituted or substituted indol-3-yl, indolin-3-yl or oxindol-3-yl; and m is 0 to 4;
or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP0336356A2

公开(公告)日：1989-10-11

申请号：EP89105864.6

申请日：1989-04-04

Applicant: ABBOTT LABORATORIES

Inventor： Kerwin, James F. ,  Nadzan, Alex M.

IPC: C07D209/42 ,  C07D209/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D487/02 ,  A61K31/40 ,  A61K31/44 ,  A61K31/47 ,  A61K31/415 ,  A61K31/495

CPC classification number: C07D401/12 ,  C07D209/20 ,  C07D209/42 ,  C07D401/14 ,  C07D403/12 ,  C07D487/04 ,  C07K5/0202 ,  C07K5/06139

Abstract: A compound of the formula:
wherein R₁ and R₂ are independently selected from hydrogen, loweralkyl, cycloalkyl, loweralkenyl, adamantyl, aryl, substituted aryl, heterocyclic group, substituted alkyl, substituted amide, functionalized carbonyl, and nitrogen containing ring wherein R₁, R₂ and the adjacent nitrogen atom form a ring;
R₁₁ is hydrogen, loweralkyl, or loweralkenyl;
R₂₀ is hydrogen, loweralkyl, or loweralkenyl;
B is -(CH₂) m -, substituted alkenylene, -QCH₂- wherein Q is O, S, NH or substituted amino, -CH₂Q- wherein Q is as defined or B is NH;
Z is C=O, S(O)₂, or C=S;
Ar is a heterocyclic group, aryl or substituted aryl;
D is unsubstituted or substituted indol-3-yl, indolin-3-yl or oxindol-3-yl; and m is 0 to 4;
or a pharmaceutically acceptable salt thereof.

Abstract translation: 下式的化合物，其中R 1和R 2独立地选自氢，低级烷基，环烷基，低级烯基，金刚烷基，芳基，取代的芳基，杂环基，取代的烷基，取代的酰胺，官能化的羰基和含氮环，其中R1 R2和相邻的氮原子形成环; R11是氢，低级烷基或低级烯基; R 20是氢，低级烷基或低级烯基; B是 - （CH 2）m - ，取代的亚烯基，-Q CH 2 - 其中Q是O，S，NH或取代的氨基，-CH 2 Q-，其中Q定义或B是NH; Z为C = O，S（O）2或C = S; Ar是杂环基，芳基或取代的芳基; D是未取代或取代的吲哚-3-基，二氢吲哚-3-基或羟吲哚-3-基; m为0〜4; 或其药学上可接受的盐。

公开(公告)号：EP0308885A1

公开(公告)日：1989-03-29

申请号：EP88115462.9

申请日：1988-09-21

Applicant: ABBOTT LABORATORIES

Inventor： Nadzan, Alex M. ,  Lin, Chun Wel ,  Kerwin, James F., Jr.

IPC: C07D209/42 ,  C07D213/56 ,  C07D215/16 ,  C07D241/44 ,  C07D403/12 ,  A61K31/395

CPC classification number: C07D401/12 ,  C07C271/22 ,  C07C275/28 ,  C07D209/42 ,  C07D213/56 ,  C07D215/48 ,  C07D241/44 ,  C07K5/06104

Abstract: A compound of the formula:
wherein R₁ and R₂ are substituents; R₆ is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is a bond, an alkylene group, an alkenylene group, an alkadienylene group or a heteroatom containing linking group; D is a substituted acyl group or tetrazolyl; Z is CO, C(S) or S(O)₂; Ar is a heterocyclic group; and n is 1 to 3.
Also disclosed are a composition and a method for antagonizing CCK, a composition and method for treating or preventing gastrointestinal, central nervous, appetite regulating and pain regulating systems, a composition and method for treating or preventing hyperinsulinemia, methods of making the compounds and intermediates useful in making the compounds.

Abstract translation: 下式的化合物：其中R 1和R 2是取代基; R6是氢，低级烷基，环烷基，低级烯基，芳基烷基，（取代的芳基）烷基或（杂环）烷基; B是键，亚烷基，亚烯基，链二烯基或含杂原子的连接基团; D是取代的酰基或四唑基; Z是CO，C（S）或S（O）2; Ar是杂环基; 还公开了拮抗CCK的组合物和方法，治疗或预防胃肠，中枢神经，食欲调节和疼痛调节系统的组合物和方法，治疗或预防高胰岛素血症的组合物和方法，方法 使化合物和中间体可用于制备化合物。

公开(公告)号：EP0405506A1

公开(公告)日：1991-01-02

申请号：EP90112261.4

申请日：1990-06-27

Applicant: ABBOTT LABORATORIES

Inventor： Chung, John Y.-L. ,  Tufano, Michael D. ,  May, Paul D. ,  Shiosaki, Kazumi ,  Nadzan, Alex M. ,  Garvey, David S. ,  Shue, Youe-Kong ,  Brodie, Mark S. ,  Holladay, Mark W.

IPC: C07K5/00 ,  A61K37/02

CPC classification number: C07K5/1016 ,  A61K38/00 ,  C07K5/0207 ,  C07K5/0808 ,  C07K5/1024

Abstract: A tetrapeptide type-B CCK receptor ligand of the formula
A-B-C-D
or a pharmaceutically acceptable salt thereof, which is useful for treating central nervous system disorders, substance abuse, gastrointestinal disorders, endocrine disorders, eating-related disorders and treatment of shock, respiratory and cardiocirculatory insufficiencies.

Abstract translation: 用于治疗中枢神经系统疾病，药物滥用，胃肠道疾病，内分泌紊乱，进食相关疾病和休克，呼吸和心脏循环治疗的ABCD的四肽B型CCK受体配体或其药学上可接受的盐 不足。