中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

99 records (took 0.025 seconds)

    71.
    发明专利
    未知

    公开(公告)号：AT139526T

    公开(公告)日：1996-07-15

    申请号：AT93101842

    申请日：1993-02-05

    Applicant: HOECHST AG

    Inventor： LANG HANS-JOCHEN DR ,  MANIA DIETER DR ,  WEICHERT ANDREAS DR ,  SCHOLZ WOLFGANG DR ,  ALBUS UDO DR ,  ENGLERT HEINRICH DR ,  LANG FLORIAN PROF DR

    IPC: A61K31/155 ,  A61K31/18 ,  A61K31/275 ,  A61P1/16 ,  A61P3/08 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P35/04 ,  C07C217/44 ,  C07C311/16 ,  C07C311/37 ,  C07C311/39 ,  C07C311/47 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65

    Abstract: There are described benzoylguanidines of the formula I where R(1) is equal to R(4)-SOm or R(5)R(6)N-SO2-, where R(4) and R(5) are equal to alk(en)yl, -CnH2n-R(7), and where R(7) is equal to cycloalkyl or phenyl, where R(5) also denotes H, R(6) is equal to H or C1-C4-alkyl, R(2) is hydrogen, halogen, alkyl, -O-(CH2)mCpF2p+1, -X-R(10), where X is equal to O, S, NR(11), R(10) is equal to H, (cyclo)alkyl(methyl), -CnH2n-R(12) where R(12) is equal to phenyl, R(3), inter alia, is defined as R(1), and their pharmaceutically tolerable salts. The compounds I are prepared by reaction of compounds of the formula II in which L represents a leaving group which can be easily substituted nucleophilically, with guanidine. Compounds I are outstandingly suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infract treatment and for the treatment of angina pectoris, where they also preventively inhibit or strongly decrease the pathophysiological processes during the formation of ischaemically induced damage. They are moreover distinguished by a strong inhibitory action on cell proliferation. They can therefore be used as antiatherosclerotics, agents against diabetic late complications, cancers, fibrotic disorders such as pulmonary fibrosis, fibrosis of the liver or fibrosis of the kidneys. They are effective inhibitors of the cellular sodium/protons antiporter (Na /H exchanger).

    ARYLCARBONYLAMINOALKYLDIHYDROOXOPYRIDINES, PROCESS OF THEIR PREPARATION AND THEIR USE
    73.
    发明专利
    ARYLCARBONYLAMINOALKYLDIHYDROOXOPYRIDINES, PROCESS OF THEIR PREPARATION AND THEIR USE 未知

    公开(公告)号：CZ403592A3

    公开(公告)日：1993-12-15

    申请号：CS403592

    申请日：1992-12-31

    Applicant: HOECHST AG

    Inventor： ENGLERT HEINRICH DR ,  MANIA DIETER DR ,  WETTLAUFER DAVID DR ,  KLAUS ERIK DR

    IPC: A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4425 ,  A61P9/00 ,  A61P21/00 ,  C07D213/64 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/89 ,  C07D401/12

    Abstract: Arylcarbonylaminoalkyl-dihydro-oxo-pyridines of Formula I are disclosed wherein aryl is an aromatic or heteroaromatic system, n is zero through 5; R and R(1), are hydrogen, or loweralkyl; W is hydrogen, (hetero)-(aryl)-loweralkyl; Z is hydrogen, CH2OR(2), CHO, (CO)OR(2), (CO)NR(2)2. Processes for the preparation of compound I are also disclosed. Compounds I are suitable for the treatment of disorders of the cardiovascular system, for example of hypertension, of cardiac insufficiency or of disturbances of blood flow in the coronary systems such as, for example, angina. Disturbances of cerebral and peripheral blood flow are likewise influenced beneficially. Furthermore, compounds I are able to influence smooth-muscle organs such as uterus, bronchi, intestines and biliary system, the urinary tract (ureter, bladder and urethra) in the sense of spasmolysis. They are therefore also suitable for the treatment of diseases associated with spasms of these organs, for example for the treatment of premature labor in pregnancy, of ureteral or biliary colic, of obstructive airway diseases such as asthma, of disturbances of intestinal motility such as, for example, of irritable colon or of bladder incontinence. Additionally, compounds of formula I can serve as anti-convulsants in the treatment of epilepsy and as hair growth inducers in the treatment of baldness.

    76.
    发明专利
    未知

    公开(公告)号：DE3208190A1

    公开(公告)日：1983-09-08

    申请号：DE3208190

    申请日：1982-03-06

    Applicant: HOECHST AG

    Inventor： ENGLERT HEINRICH DR ,  LANG HANS-JOCHEN DR ,  HROPOT MAX DR ,  KAISER JOACHIM DR

    IPC: A61K31/135 ,  A61K31/40 ,  A61K31/535 ,  A61K31/54 ,  A61P3/00 ,  A61P7/10 ,  A61P9/12 ,  C07C43/21 ,  C07C67/00 ,  C07C313/00 ,  C07C315/04 ,  C07C317/00 ,  C07C317/22 ,  C07C317/32 ,  C07C317/36 ,  C07D277/04 ,  C07D295/08 ,  C07D295/096 ,  C07D307/52 ,  C07C147/12 ,  C07C147/14 ,  C07C147/10

    Abstract: 1. Claims for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 2-Aminomethylphenols of the formula I see diagramm : EP0088346,P33,F2 in which R represents hydrogen or alkyl having 1 or 2 C atoms, R**1 represents alkyl having 1 to 8 C atoms, cycloalkyl having 3 to 12 C atoms and up to 8 ring members, alkenyl having 2 to 8 C atoms or cycloalkenyl having 5 to 12 C atoms and up to 8 ring members, it being possible for each of the aforementioned radicals to be substituted with 1 to 5 identical or different halogen atoms, R**2 and R**4 are identical or different and denote hydrogen, halogen, alkyl having 1 or 2 C atoms or alkoxy having 1 or 2 C atoms, R**3 denotes halogen, alkyl having 1 to 12 C atoms or cycloalkyl having 3 to 12 C atoms and up to 8 ring members, R**5 and R**6 are identical or different and represent hydrogen, alkyl having 1 to 6 C atoms, cycloalkyl having 3 to 10 C atoms and up to 8 ring members or the radical -[CH2 ]o -Ar, wherein o = 1 or 2, the -[CH2 ]o - chain can be substituted by 1 or 2 (C1 or C2 )-alkyl groups and Ar is a 5- or 6- membered aromatic or heteroaromatic system, which is optionally substituted by 1 to 3 identical or different radicals (C1 or C2 )-alkyl, (C1 or C2 )-alkoxy or halogen, and n is 1 or 2, it being possible for the radicals R**5 and R**6 and/or two of the radicals R**2 , R**3 and R**4 also to form a -[CH2 ]m - chain having m = 3 to 6, which can optionally be substituted by 1 or 2 methyl groups and, in the case of R**5 and R**6 , can also be interrupted by 1 or 2 oxygen atoms, sulfur atoms and/or imino groups, and their physiologically tolerated salts. 1. Claims for the Contracting State : AT A process for the preparation of the 2-aminomethylphenols of the formula I see diagramm : EP0088346,P35,F4 in which R represents hydrogen or alkyl having 1 or 2 C atoms, R**1 represents alkyl having 1 to 8 C atoms, cycloalkyl having 3 to 12 C atoms and up to 8 ring members, alkenyl having 2 to 8 C atoms or cycloalkenyl having 5 to 12 C atoms and up to 8 ring members, it being possible for each of the aforementioned radicals to be substituted with 1 to 5 identical or different halogen atoms, R**2 and R**4 are identical or different and denote hydrogen, halogen, alkyl having 1 or 2 C atoms or alkoxy having 1 or 2 C atoms, R**3 denotes halogen, alkyl having 1 to 12 C atoms or cycloalkyl having 3 to 12 C atoms and up to 8 ring members, R**5 and R**6 are identical or different and represent hydrogen, alkyl having 1 to 6 C atoms, cycloalkyl having 3 to 10 C atoms and up to 8 ring members or the radical -[CH2 ]o -Ar, wherein o = 1 or 2, the -[CH2 ]o - chain can be substituted by 1 or 2 (C1 or C2 )-alkyl groups and Ar is a 5- or 6-membered aromatic or heteroaromatic system, which is optionally substituted by 1 to 3 identical or different radicals (C1 or C2 )-alkyl, (C1 or C2 )-alkoxy or halogen, and n is 1 or 2, it being possible for the radicals R**5 and R**6 and/or two of the radicals R**2 , R**3 and R**4 also to form a -[CH2 ]m - chain having m = 3 to 6, which can optionally be substituted by 1 or 2 methyl groups and, in the case of R**5 and R**6 , can also be interrupted by 1 or 2 oxygen atoms, sulfur atoms and/or imino groups, and their physiologically tolerated salts, which comprises a) reacting a compound of the formula II see diagramm : EP0088346,P36,F1 wherein n, R**1 , R**2 , R**3 and R**4 have the abovementioned meanings, with an N-hydroxymethylcarboxamide of the general formula III see diagramm : EP0088346,P36,F2 in which R has the abovementioned meaning, R**5 denotes hydrogen or alkyl having 1 to 4 C atoms and R**7 represents hydrogen, optionally halogen-substituted alkyl having 1 to 4 C atoms or aryl having 6 to 10 C atoms, or in which R**5 and the radical COR**7 together represent the o-phthaloyl radical, to give a compound of the general formula IV see diagramm : EP0088346,P36,F3 and removing the acyl radical R**7 -CO by hydrolysis, b) reacting a compound of the formula II, in which the radicals R**1 to R**4 and n have the abovementioned meanings, in the presence of formaldehyde, with an amine of the general formula V see diagramm : EP0088346,P36,F4 in which R**5 and R**6 have the meanings mentioned in claim 1 with the exception of hydrogen, c) reacting a compound of the general formula VI see diagramm : EP0088346,P36,F5 in which n and R to R**4 have the abovementioned meanings and Z represents a leaving group, with an amine of the general formula H-N = Y, wherein Y represents an amine-protective group or the radicals R**5 and R**6 defined in claim 1, it being possible for R**6 also to be an amine-protective group, to give a compound of the general formula VII see diagramm : EP0088346,P37,F1 and, if appropriate, removing the amine-protective group by hydrolysis or hydrogenolysis, or d) reacting compounds of the general formula XIV see diagramm : EP0088346,P37,F2 in which n and R to R**4 have the abovementioned meanings, with an amine of the formula R**5 -NH2 , with R**5 having the abovementioned meaning, to give Schiff's bases of the formula XV see diagramm : EP0088346,P37,F3 in which n and R to R**5 have the abovementioned meanings, and reducing the latter to give a compound of the formula I, and optionally converting the compound of the formula I obtained according to one of the variants a) - d) into its physiologically tolerated salts.

Patent Agency Ranking