公开(公告)号：US3658845A

公开(公告)日：1972-04-25

申请号：US3658845D

申请日：1970-03-10

Applicant: DEGUSSA

Inventor： POSSELT KLAUS ,  THIELE KURT

IPC: C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D209/12 ,  C07D209/14 ,  C07D213/38 ,  C07D213/50 ,  C07D215/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D277/22 ,  C07D277/24 ,  C07D277/28 ,  C07D277/34 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/54 ,  C07D317/58 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  C07D333/58 ,  C07D63/22

CPC classification number: C07D207/335 ,  C07D207/34 ,  C07D209/12 ,  C07D209/14 ,  C07D213/38 ,  C07D213/50 ,  C07D215/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D277/24 ,  C07D277/28 ,  C07D277/34 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/54 ,  C07D317/58 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  C07D333/58

Abstract: X(-R1)(-R2)(-R3)-R4

THEIR SALTS AND QUATERNARY AMMONIUM COMPOUNDS, AS WELL AS THEIR OPTICALLY ACTIVE ISOMERS OR DIASTEREOMERS WHEREIN R1 TO R4 REPRESENT HYDROGEN, HALOGEN, LOWER ALKYL, ARALKYL, PHENYL, HYDROXYL, LOWER ALKOXY, NITRO OR LOWER CARBOALKOXY, R5 AND R6 ARE HYDROGEN OR METHYL, R7 AND R8 ARE HYDROGEN, HALOGEN OR LOWER ALKOXY, X IS A HETEROCYCLIC RING SYSTEM, MONO- OR CONDENSED BICYCLIC, WITH 1-4 HETERO ATOMS, IN WHICH THE INDIVIDUAL RINGS HAVE 5 TO 6 MEMBERS AND CAN ALSO CONTAIN 1 OR MORE CARBONYL GROUPS, Y IS -CO- OR -CH(OH)-. THESE COMPOUNDS HAVE PHARMACOLOGICAL ACTIVITY IN THAT THEY INCREASE THE CORONARY BLOOD FLOW BY SIMULTANEOUSLY CAUSING DILATION OF THE CORONARIES AND AN INCREASE IN CONTRACTION STRENGTH.

(R7,R8-PHENYL)-CH(-OH)-CH(-R6)-NH-CH2-CH(-R5)-Y-
COMPOUNDS OF THE FORMULA

公开(公告)号：US3631055A

公开(公告)日：1971-12-28

申请号：US3631055D

申请日：1970-03-10

Applicant: DEGUSSA

Inventor： POSSELT KLAUS ,  THIELE KURT

IPC: C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D209/12 ,  C07D209/14 ,  C07D213/38 ,  C07D213/50 ,  C07D215/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D277/22 ,  C07D277/24 ,  C07D277/28 ,  C07D277/34 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/54 ,  C07D317/58 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  C07D333/58 ,  C07D31/42

CPC classification number: C07D207/335 ,  C07D207/34 ,  C07D209/12 ,  C07D209/14 ,  C07D213/38 ,  C07D213/50 ,  C07D215/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D277/24 ,  C07D277/28 ,  C07D277/34 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/54 ,  C07D317/58 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  C07D333/58

Abstract: COMPOUNDS OF THE FORMULA

(R7,R8-PHENYL)-CH(-OH)-CH(-R6)-NH-CH2-CH(-R5)-Y-X(-R1)

(-R2)(-R3)(-R4)

THEIR SALTS AND QUARTENARY AMMONIUM COMPOUNDS, AS WELL AS THEIR OPTICALLY ACTIVE ISOMERS OR DIASTEREOMERS WHEREIN R1 TO R4 REPRESEN HYDROGEN, HALOGEN, LOWER ALKYL, ARALKYL, PHENYL, HYDROXYL, LOWER ALKOXY, NITRO OR LOWER CARBOALKOXY, R5 AND R6 ARE HYDROGEN OR METHYL, R7 AND R8 ARE HYDROGEN, HALOGEN OR LOWER ALKOXY, X IS A HETEROCYCLIC RING SYSTEM, MONO- OR CONDENSED BYCYCLIC, WITH 1-4 HETERO ATOMS, IN WHICH THE INDIVIDUAL RINGS HAVE 5 TO 6 MEMBERS AND CAN ALSO CONTAIN 1 OR MORE CRBONYL GROUPS, Y IS -CO- OR -CH(OH)-. THESE COMPOUNDS HAVE PHARMACOLOGICAL ACTIVITY IN THAT THEY INCREASE THE CORONARY BLOOD FLOW BY SIMULTANEOUSLY CAUSING DILATION OF THE CORONARIES AND AN INCREASE IN CONTRACTION STRENGTH.

公开(公告)号：US3859305A

公开(公告)日：1975-01-07

申请号：US13757571

申请日：1971-04-26

Applicant: DEGUSSA

Inventor： POSSELT KLAUS ,  THIELE KURT

IPC: C07D207/34 ,  C07D209/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/58 ,  C07D319/18 ,  C07D319/20 ,  C07D333/22 ,  C07D333/28 ,  C07D27/56

CPC classification number: C07D307/81 ,  C07D207/34 ,  C07D209/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D307/52 ,  C07D307/73 ,  C07D317/58 ,  C07D319/18 ,  C07D319/20 ,  C07D333/22 ,  C07D333/28

Abstract: THEIR SALTS AND QUATERNARY AMMONIUM COMPOUNDS, AS WELL AS THEIR OPTICALLY ACTIVE ISOMERS OR DIASTEREOMERS WHEREIN R1 to R4 represent hydrogen, halogen, lower alkyl, aralkyl, phenyl, hydroxyl, lower alkoxy, nitro or lower carboalkoxy, R5 and R6 are hydrogen or methyl, R7 and R8 are hydrogen, halogen or lower alkoxy, X is a heterocyclic ring system, mono- or condensed bicyclic, with 1 - 4 hetero atoms, in which the individual rings have 5 to 6 members and can also contain 1 or more carbonyl groups, Y is -CO-or -CH(OH)-. These compounds have pharmacological activity in that they increase the coronary blood flow by simultaneously causing dilation of the coronaries and an increase in contraction strength.

Compounds of the formula

公开(公告)号：US3514465A

公开(公告)日：1970-05-26

申请号：US3514465D

申请日：1967-12-26

Applicant: DEGUSSA

Inventor： POSSELT KLAUS ,  THIELE KURT

IPC: C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D209/12 ,  C07D209/14 ,  C07D213/38 ,  C07D213/50 ,  C07D215/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D277/22 ,  C07D277/24 ,  C07D277/28 ,  C07D277/34 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/54 ,  C07D317/58 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  C07D333/58 ,  C07D31/42 ,  C07D91/32

CPC classification number: C07D207/335 ,  C07D207/34 ,  C07D209/12 ,  C07D209/14 ,  C07D213/38 ,  C07D213/50 ,  C07D215/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D277/24 ,  C07D277/28 ,  C07D277/34 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/54 ,  C07D317/58 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  C07D333/58

公开(公告)号：US3686206A

公开(公告)日：1972-08-22

申请号：US3686206D

申请日：1970-03-13

Applicant: DEGUSSA

Inventor： POSSELT KLAUS ,  ENKHEIM BERGEN ,  THIELE KURT

IPC: C07D207/32 ,  C07D207/335 ,  C07D207/34 ,  C07D209/12 ,  C07D209/14 ,  C07D213/38 ,  C07D213/50 ,  C07D215/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D277/22 ,  C07D277/24 ,  C07D277/28 ,  C07D277/34 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/54 ,  C07D317/58 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  C07D333/58 ,  C07D49/18

CPC classification number: C07D207/335 ,  C07D207/34 ,  C07D209/12 ,  C07D209/14 ,  C07D213/38 ,  C07D213/50 ,  C07D215/14 ,  C07D217/16 ,  C07D217/24 ,  C07D231/12 ,  C07D231/22 ,  C07D231/26 ,  C07D231/28 ,  C07D277/24 ,  C07D277/28 ,  C07D277/34 ,  C07D307/52 ,  C07D307/73 ,  C07D307/81 ,  C07D317/54 ,  C07D317/58 ,  C07D319/08 ,  C07D319/18 ,  C07D319/20 ,  C07D333/16 ,  C07D333/20 ,  C07D333/22 ,  C07D333/28 ,  C07D333/58

Abstract: COMPOUNDS OF THE FORMULA

(R7,R8-PHENYL)-CH(-OH)-CH(-R6)-NH-CH2-CH(-R5)-Y-X(-R1)

(-R2)(-R3)-R4

THEIR SALTS AND QUATERNARY AMMONIUM COMPOUNDS, AS WELL AS THEIR OPTICALLY ACTIVE ISOMERS OR DIASTEREOMERS WHERIN R1 TO R4 REPRESENT HYDROGEN, HALOGEN, LOWER ALKYL, ARALKYL, PHENYL, HYDROXYL, LOWER ALKOXY, NITRO OR LOWER CARBOALKOXY, R5 AND R6 ARE HYDROGEN OR METHYL, R7 AND R8 ARE HYDROGEN, HALOGEN OR LOWER ALKOXY, X IS A HETEROCYCLIC RING SYSTEM, MONO- OR CONDENSED BICYCLIC, WITH 1-4 HETERO ATOMS, IN WHICH THE INDIVIDUAL RINGS HAVE 5 TO 6 MEMBERS AND CAN ALSO CONTAIN 1 OR MORE CARBONYL GROUPS, Y IS -CO- OR -CH(OH)-. THESE COMPOUNDS HAVE PHARMACOLOGICAL ACTIVITY IN THAT THEY INCREASE THE CORONARY BLOOD FLOW BY SIMULTANEOUSLY CAUSING DILATION OF THE CORONARIES AND AN INCREASE IN CONTRACTION STRENGTH. THE PYRAZOLES AND PYRAZOLONES HAVE ANTIPHLOGISTIC ACTION.

公开(公告)号：US3591593A

公开(公告)日：1971-07-06

申请号：US3591593D

申请日：1968-07-09

Applicant: DEGUSSA

Inventor： THIELE KURT ,  BEBENBURG WALTER VON ,  POSSELT KLAUS

IPC: C07D211/02 ,  C07D211/52 ,  C07D29/20

CPC classification number: C07D211/52 ,  C07D211/02

Abstract: SUBSTITUTED PIPERIDINES OF THE FORMULA

1-((R5,R6-PHENYL)-ALK-),3-((R3,R4-PHENYL)-CO-),4-HO,

4-(R1,R2-PHENYL)-PIPERIDINE

WHEREIN HAL IS CL OR BR WITH ONE MOL OF A COMPOUND OF THE FORMULA IV OR REACTING 2 MOL OF A COMPOUND OF THE FORMULA VII WITH 1 MOL OF A COMPOUND OF THE FORMULA V IN THE PRESENCE OF AN ACID ACCEPTOR. (C) REACTING 2 MOL OF A COMPOUND OF THE FORMULA

(R1,R2-PHENYL)-CO-CH3

WITH ONE MOL OF A COMPOUND OF THE FORMULA V AND FORMALDEHYDE OR A FORMALDEHYDE YIELDING SUBSTANCE AND, IF DESIRED, FORMING THE ACID ADDITION OR QUATERNARY AMMONIUM SALTS OF THE COMPOUND PRODUCED.

(R1,R2-PHENYL)-CO-CH2-CH2-HAL

IN AN INERT MEDIUM. (B) REACTING ONE MOL OF A COMPOUND OF THE FORMULA

R1,R2,((R5,R6-PHENYL)-ALK-NH-CH2-CH2-CO-)BENZENE

OR HEATING A COMPOUND OF THE FORMULA

(R5,R6-PHENYL)-ALK-NH2

OR REACTING 2 MOL OF A COMPOUND OF THE FORMULA II OR THE FORMULA III WITH ONE MOL OF A COMPOUND OF THE FORMULA

R3,R4,((R5,R6-PHENYL)-ALK-NH-CH2-CH2-CO-)BENZENE

WHEREIN R7 AND R8 ARE LOWER ALKYL WITH ONE MOL OF A COMPOUND OF THE FORMULA

(R1,R2-PHENYL)-CO-CH2-CH2-N(-R7)-R8

OR THE CORRESPONDING MANNICH COMPOUND OF THE FORMULA

(R1,R2-PHENYL)-CO-CH=CH2

AND THEIR ACID ADDITION SALTS AND THEIR QUATERNARY AMMONIUM SALTS AND THEIR DIASTEROMERS AND OPTICALLY ACITVE ISOMERS HAVING PHARMACEUTICAL ACTIVITY FOR TREATMENT OF HEART AND CIRVULATORY CONDITIONS AND ESPECIALLY FOR INCREASING THE CONONARY BLOOD FLOW PARTLY IN COMBINATION WITH AN IMPROVEMENT OF THE HEART FUNCTION WHEREIN: ALK IS A STRAIGHT OR BRANCH CHAINED SATURATED ALKPHATIC HYDROCARBON OR HYDROXY SUBSTITUTED HYDROCARBON CHAIN OF 2-4 CARBON ATOMS; EACH OF R1-R6 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALOGEN, NITRO, HYDROXY, LOWER ALKOXY, LOWER ALKYL OR LOWER TRIFLUOUOALKYL AND EACH PAIR OF R1 AND R2, R3 AND R4 AND R5 AND R6 ON THE PHENYL RINGS WHEN TAKEN TOGETHER CAN BE LOWER ALKYLENE DIOXY, WHICH ARE PREPARED BY (A) REACTING ONE MOL OF A COMPOUND OF THE FORMULA

公开(公告)号：US3426034A

公开(公告)日：1969-02-04

申请号：US3426034D

申请日：1966-03-24

Applicant: DEGUSSA

Inventor： THIELE KURT ,  POSSELT KLAUS

IPC: C07D213/38 ,  C07D31/42

CPC classification number: C07D213/38

公开(公告)号：FI70205C

公开(公告)日：1986-09-15

申请号：FI791188

申请日：1979-04-11

Applicant: DEGUSSA

Inventor： ENGEL JURGEN ,  KLEEMANN AXEL ,  POSSELT KLAUS ,  STROMAN FRITZ ,  THIEMER KLAUS

IPC: A61K31/135 ,  A61K20060101 ,  A61K31/13 ,  A61K31/137 ,  A61K31/43 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P29/00 ,  C07C20060101 ,  C07C67/00 ,  C07C213/00 ,  C07C213/02 ,  C07C213/08 ,  C07C215/30 ,  C07C215/60 ,  C07C221/00 ,  C07C225/06 ,  C07C225/10 ,  C07C225/14 ,  C07C97/10

Abstract: There are prepared compounds of the formula: wherein X is the group >C=O or >CH(OH), Y is the group R2 is hydrogen or C1 to C6 alkyl, R3 is hydrogen or a hydroxy group and R1 is the adamantyl group or a saturated or single unsaturated C3 to C16 cycloalkyl group where the C3 to C16 cycloalkyl group can be substituted by a C1-C4 alkyl group or a halogen atom and their salts. The compounds are useful in dilating the peripheral blood vessels and in lowering blood pressure.

公开(公告)号：CA1123826A

公开(公告)日：1982-05-18

申请号：CA327735

申请日：1979-05-16

Applicant: DEGUSSA

Inventor： ENGEL JUERGEN ,  KLEEMANN AXEL ,  POSSELT KLAUS ,  STROMAN FRITZ ,  THIEMER KLAUS

IPC: A61K31/135 ,  A61K20060101 ,  A61K31/13 ,  A61K31/137 ,  A61K31/43 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P29/00 ,  C07C20060101 ,  C07C67/00 ,  C07C213/00 ,  C07C213/02 ,  C07C213/08 ,  C07C215/30 ,  C07C215/60 ,  C07C221/00 ,  C07C225/06 ,  C07C225/10 ,  C07C225/14 ,  C07C91/23 ,  C07C97/10

Abstract: The present invention proviaes a compound having the formula I wherein X represents the group >CO or >CH(OH), R2 represents hydrogen or a C1 to C6 alkyl group, R3 represents hydrogen or a hydroxy group and R1 represents the adamantyl radical or a saturated or mono-unsaturated C3 to C16 -cycloalkyl radical which cycloalkyl radical may be substituted by a C1 to C4 alkyl group or a halogen atom, or a pharmaceutically acceptable salt thereof. Such compounds are pharmacodynamically active and cause, for example, a decrease of blood pressure and an improvement of cerebral or peripheral blood flow. Moreover, they have an antiphlogistic effect and are distinguished by good resorption.

公开(公告)号：FI773814A

公开(公告)日：1978-06-18

申请号：FI773814

申请日：1977-12-16

Applicant: DEGUSSA

Inventor： ISAAC OTTO ,  POSSELT KLAUS ,  UTHEMANN HORST ,  THIEMER KLAUS

IPC: C07J17/00 ,  A61K31/585 ,  A61K31/704 ,  A61P9/04 ,  C07J19/00 ,  C07J41/00 ,  C07J43/00 ,  C07J