公开(公告)号：US3549652A

公开(公告)日：1970-12-22

申请号：US3549652D

申请日：1968-02-19

Applicant: SANDOZ AG

Inventor： SIMPSON WILLIAM R J

IPC: C07D263/52 ,  C07D85/48

CPC classification number: C07D263/52 ,  Y10S514/869

公开(公告)号：US3929884A

公开(公告)日：1975-12-30

申请号：US45601774

申请日：1974-03-29

Applicant: SANDOZ AG

Inventor： SIMPSON WILLIAM R J

IPC: C07D243/08 ,  C07D401/04 ,  C07C123/00

CPC classification number: C07D401/04 ,  C07D243/08 ,  Y10S514/866 ,  Y10S514/909

Abstract: Compounds of the formula

WHEREIN R is alkyl of 1 to 6 carbon atoms, EACH X is independently alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or halo, and M IS 0, 1 OR 2, AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, ARE USEFUL AS ANTI-OBESITY AND ANTI-DIABETIC AGENTS. They are synthesized by reacting a 2-alkyl-5-arylisoxazolium salt with ethylene diamine to obtain a compound of the formula

or a tautomer thereof, wherein R, X and m are as defined above, which is then cyclized with a strong acid.

Abstract translation: 式WHEREIN R的化合物是具有1至6个碳原子的烷基，每个X独立地是1至4个碳原子的烷基，1至4个碳原子的烷氧基或卤素，M IS 0，1 OR 2和药物可接受的酸 其添加量为有用的抗生素和抗糖尿病药物。 它们通过2-烷基-5-芳基异恶唑鎓盐与乙二胺反应得到式OH化合物：H 2 N-CH 2 CH 2 -NH-C-CH = C PARALLEL N 2，R或其互变异构体，其中R， X和m如上所定义，然后用强酸环化。

公开(公告)号：US3637701A

公开(公告)日：1972-01-25

申请号：US3637701D

申请日：1969-06-26

Applicant: SANDOZ AG

Inventor： GABEL LLOYD P ,  SIMPSON WILLIAM R J

IPC: C07D491/04 ,  C07D51/48

CPC classification number: C07D491/04 ,  Y10S514/929

Abstract: THE INVENTION DISCLOSED COMPOUNDS OF THE CLASS WHICH ARE NITRATES OF 4-SUBSTITUTED-AMINO-QUINAZOLINES, E.G., 4(2-HYDROXYETHYL)AMINO-6,7-DIMETHOXYQUINAZOLINE NITRATE, HAVING PHARMACOLOGICAL ACTIVITY IN ANIMALS AND USEFUL, FOR EXAMPLE, AS HYPOTENSIVE AND ANTI-ANGINAL AGENTS. ALSO DISCLOSED ARE THE HYDROXY INTERMEDIATES USEFUL IN PREPARATION OF SAID NITRATES.

公开(公告)号：US3637700A

公开(公告)日：1972-01-25

申请号：US3637700D

申请日：1970-11-13

Applicant: SANDOZ AG

Inventor： GABEL LLOYD P ,  SIMPSON WILLIAM R J

IPC: C07D239/94 ,  C07D403/04 ,  C07D31/48

CPC classification number: C07D403/04 ,  C07D239/94 ,  Y10S514/929

Abstract: DISCLOSED ARE COMPOUNDS OF THE CLASS OF QUINAZOLINES SUBSTITUTED IN THE BENZENE RING PORTION OF THE QUINAZOLINE BY TRIALKOXY AND FURTHER SUBSTITUTED AT THE 4-POSITION BY AN AMINO FUNCTION BEARING A HYDROXYALKYL NITRATE MOIETY, E.G., 4-(5-HYDROXYPENTYL) AMINO-6,7,8-TRIMETHOXYQUINAZOLINE NITRATE. THE COMPOUNDS HAVE PHARMACOLOGICAL ACTIVITY IN ANIMALS AND ARE USEFUL, FOR EXAMPLE, AS HYPOTENSIVE, CORONARY DILATORS AND ANTIANGINAL AGENTS. ALSO DISCLOSED ARE THE CORRESPONDING HYDROXY INTERMEDIATES USEFUL IN PREPARATION OF THE NITRATES.

公开(公告)号：US3892758A

公开(公告)日：1975-07-01

申请号：US44852574

申请日：1974-03-06

Applicant: SANDOZ AG

Inventor： SIMPSON WILLIAM R J

IPC: C07D519/00 ,  C07D63/18

CPC classification number: C07D519/00 ,  Y10S514/866 ,  Y10S514/909

Abstract: WHEREIN N IS 1 TO 6, M IS 0 OR 1, P IS 0 OR 1, R* is hydrogen, halo, alkyl or alkoxy, and R'', R and R1 are hydrogen or alkyl, e.g., 1,3-Bis(1-(4-thieno(3,2-c)pyridinyl)-4-piperidyl)propane.
ANTI-OBESITY agents of the formula:

Abstract translation: 抗体药剂的配方：

公开(公告)号：US3637699A

公开(公告)日：1972-01-25

申请号：US3637699D

申请日：1970-02-24

Applicant: SANDOZ AG

Inventor： GABEL LLOYD P ,  SIMPSON WILLIAM R J

IPC: C07D491/04 ,  C07D51/48

CPC classification number: C07D491/04 ,  Y10S514/929

Abstract: DISCLOSED ARE COMPOUNDS OF THE CLASS OF QUINAZOLINES SUBSTITUTED IN THE BENZENE RING PORTION OF THE QUINAZOLINE BY LOWER ALKYL AND FURTHER SUBSTITUTED AT THE 4-POSITION BY AN AMINO FUNCTION BEARING A HYDROXYALKYL NITRATE MOIETY, E.G., 4-(5-HYDROXYPENTYL)AMINO-7,8 - DIMETHYLQUINAZOLINE NITRATE. THE COMPOUDNS HAVE PHARMACOLOGICAL ACTIVITY IN ANIMALS AND ARE USEFUL, FOR EXAMPLE, AS HYPOTENSIVE AND CORONARY DILATING AGENTS. ALSO DISCLOSED ARE THE CORRESPONDING HYDROXY INTERMEDIATES USEFUL IN PREPARATION OF THE NIRATES.