公开(公告)号：US20070213372A1

公开(公告)日：2007-09-13

申请号：US11607262

申请日：2006-12-01

Applicant: Ulrich Rosentreter ,  Thomas Kramer ,  Andrea Vaupel ,  Walter Hubsch ,  Nicole Diedrichs ,  Thomas Krahn ,  Klaus Dembowsky ,  Johannes-Peter Stasch

Inventor： Ulrich Rosentreter ,  Thomas Kramer ,  Andrea Vaupel ,  Walter Hubsch ,  Nicole Diedrichs ,  Thomas Krahn ,  Klaus Dembowsky ,  Johannes-Peter Stasch

IPC: A61K31/44 ,  C07D213/02

CPC classification number: C07D401/12 ,  C07D213/85 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/14

Abstract: The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) wherein the definitions of substituent groups R1-R7 are as provided in the specification and claims, to a pharmaceutical composition containing such a compound, to a process for preparation of such materials, and to their use as medicaments for the treatment of cardiovascular disorders and diabetes.

Abstract translation: 本发明涉及式（I）的取代的2,6-二氨基-3,5-二氰基-4-芳基吡啶，其中取代基R 1〜R 7的定义< SUP>如说明书和权利要求书中所述，涉及含有这种化合物的药物组合物，其制备方法和用作治疗心血管疾病和糖尿病的药物。

公开(公告)号：US20060264432A1

公开(公告)日：2006-11-23

申请号：US11359927

申请日：2006-02-21

Applicant: Ulrich Rosentreter ,  Rolf Henning ,  Marcus Bauser ,  Thomas Kramer ,  Andrea Vaupel ,  Walter Hubsch ,  Klaus Dembowsky ,  Olga Salcher-Schraufstatter ,  Johannes-Peter Stasch ,  Thomas Krahn ,  Elisabeth Perzborn

Inventor： Ulrich Rosentreter ,  Rolf Henning ,  Marcus Bauser ,  Thomas Kramer ,  Andrea Vaupel ,  Walter Hubsch ,  Klaus Dembowsky ,  Olga Salcher-Schraufstatter ,  Johannes-Peter Stasch ,  Thomas Krahn ,  Elisabeth Perzborn

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/4439 ,  C07D413/02 ,  C07D403/02 ,  C07D401/02

CPC classification number: C07D401/12 ,  C07D213/85 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The invention relates to compounds of general formula (I), a method for the production thereof and the use thereof as pharmacologically effective substances for a broad medical indication spectrum. Furthermore, selective adenosine receptor ligands, preferably selective adenosine A1-, adenosine A2a- and/or adenosine A2b-receptor ligands are provided for the prophylaxis and/or the treatment of diseases, especially cardiovascular diseases, diseases of the urogenital region, diseases of the respiratory tract, inflammatory and neuroinflammatory diseases, diabetes, especially pancreatic diabetes, neurodegenerative diseases, pain states, cancer as well as liver fibrosis and liver cirrhosis.

公开(公告)号：US07135486B1

公开(公告)日：2006-11-14

申请号：US10110284

申请日：2000-09-19

Applicant: Ulrich Rosentreter ,  Rolf Henning ,  Marcus Bauser ,  Thomas Krämer ,  Andrea Vaupel ,  Walter Hübsch ,  Klaus Dembowsky ,  Olga Salcher-Schraufstätter ,  Johannes-Peter Stasch ,  Thomas Krahn ,  Elisabeth Perzborn

Inventor： Ulrich Rosentreter ,  Rolf Henning ,  Marcus Bauser ,  Thomas Krämer ,  Andrea Vaupel ,  Walter Hübsch ,  Klaus Dembowsky ,  Olga Salcher-Schraufstätter ,  Johannes-Peter Stasch ,  Thomas Krahn ,  Elisabeth Perzborn

IPC: C07D213/85 ,  A61K31/44

CPC classification number: C07D401/12 ,  C07D213/85 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: This application relates to compounds of formula (I), wherein R1, R2, R3, and R4 are defined as recited in the claims, or a tautomer, salt, hydrate, or alkoxide thereof. A process for preparing such materials, pharmaceutical compositions containing them, and methods of treating a cardiovascular disorder by administering them to a patient are also disclosed and claimed.

Abstract translation: 本申请涉及式（I）化合物，其中R 1，R 2，R 3和R 4， SUP>如权利要求中所定义，或其互变异构体，盐，水合物或醇盐。 还公开并要求保护制备这种材料的方法，含有它们的药物组合物，以及通过将它们给予患者来治疗心血管疾病的方法。

公开(公告)号：US20060100207A1

公开(公告)日：2006-05-11

申请号：US10525608

申请日：2003-08-18

Applicant: Heike Gielen-Haertwig ,  Volkhart Li ,  Ulrich Rosentreter ,  Karl-Heinz Schlemmer ,  Swen Allerheiligen ,  Leila Telan ,  Lars Barfacker ,  Jorg Keldenich ,  Mary Fitzgerald ,  Kevin Nash ,  Barbara Albrecht ,  Dirk Meurer

Inventor： Heike Gielen-Haertwig ,  Volkhart Li ,  Ulrich Rosentreter ,  Karl-Heinz Schlemmer ,  Swen Allerheiligen ,  Leila Telan ,  Lars Barfacker ,  Jorg Keldenich ,  Mary Fitzgerald ,  Kevin Nash ,  Barbara Albrecht ,  Dirk Meurer

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/4545 ,  C07D413/02 ,  C07D403/02 ,  C07D401/02

CPC classification number: C07D401/04 ,  C07D211/90 ,  C07D405/04 ,  C07F7/1804

Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.

Abstract translation: 本发明涉及新的二氢吡啶酮衍生物，其制备方法及其在药物中的用途，特别是用于治疗慢性阻塞性肺疾病，急性冠状动脉综合征，急性心肌梗塞和心力衰竭发展。

公开(公告)号：US20050165014A1

公开(公告)日：2005-07-28

申请号：US10498967

申请日：2002-12-09

Applicant: Heike Gielen -Haertwig ,  Volkhart Li ,  Ulrich Rosentreter ,  Karl-Heinz Schlemmer ,  Swen Allerheiligen ,  Kevin Nash ,  Mary Fitzgerald

Inventor： Heike Gielen -Haertwig ,  Volkhart Li ,  Ulrich Rosentreter ,  Karl-Heinz Schlemmer ,  Swen Allerheiligen ,  Kevin Nash ,  Mary Fitzgerald

IPC: A61K31/4422 ,  A61K31/444 ,  A61P11/00 ,  A61P29/00 ,  C07D211/90 ,  C07D401/04 ,  A61K31/5377 ,  A61K31/496 ,  C07D413/02 ,  C07D43/14

CPC classification number: C07D401/04 ,  C07D211/90

Abstract: The invention relates to novel 1,4-dihydro-1,4-diphenylpyridine derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases.

Abstract translation: 本发明涉及新的1,4-二氢-1,4-二苯基吡啶衍生物，其制备方法及其在药物中的应用，特别是用于治疗慢性阻塞性肺疾病。

公开(公告)号：US5204374A

公开(公告)日：1993-04-20

申请号：US679710

申请日：1991-04-03

Applicant: Ulrich E. Muller ,  Ulrich Rosentreter ,  Ulrich Niewohner ,  Elisabeth Perzborn ,  Erwin Bischoff ,  Hans-Georg Dellweg ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis

Inventor： Ulrich E. Muller ,  Ulrich Rosentreter ,  Ulrich Niewohner ,  Elisabeth Perzborn ,  Erwin Bischoff ,  Hans-Georg Dellweg ,  Peter Norman ,  Nigel J. Cuthbert ,  Hilary P. Francis

IPC: A61K31/40 ,  A61K31/403 ,  A61P7/02 ,  A61P11/00 ,  A61P37/08 ,  C07D209/86 ,  C07D209/94 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12

CPC classification number: C07D401/12 ,  C07D409/12 ,  C07D417/12

Abstract: New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different andrepresent hydrogen, nitro, cyano, halogen, trifluoromethyl, carboxyl, hydroxyl or trifluoromethoxy, orrepresent a group of the formula --S(O).sub.w R.sup.5, in whichR.sup.5 denotes alkyl or optionally substituted aryl,w denotes the number 0, 1 or 2, orrepresents alkoxy or alkoxycarbonyl, or benzyloxy, orrepresents a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 are identical or different anddenote hydrogen, alkyl or acyl ordenote aryl, ordenote a group of the formula --S(O).sub.w R.sup.5, in which R.sup.5 and w have the abovementioned meaning,represent cycloalkyl orrepresent optionally substituted alkyl or alkenyl,m represents the number 1, 2, 3 or 4,n represents the number 0, 1 or 2,z represents the number 1, 2, 3 or 4,A represents a bond or the --NH group,X represents an optionally substituted heterocycle,Y represents hydroxyl, alkoxy, phenoxy or a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 have the abovementioned meaning, an isomeric form thereof or salts thereof are useful to treat thromboembolisms, ischaemias, asthma and allergies. Processes of making and chemical intermediates are also disclosed.

公开(公告)号：US5132419A

公开(公告)日：1992-07-21

申请号：US589304

申请日：1990-09-27

Applicant: Joachim Lanz ,  Paul Naab ,  Ulrich Rosentreter

Inventor： Joachim Lanz ,  Paul Naab ,  Ulrich Rosentreter

IPC: C07D205/095 ,  C07D501/00 ,  C07D501/04 ,  C07D501/08 ,  C07D501/18 ,  C07D501/22

CPC classification number: C07D205/095 ,  C07D501/00

Abstract: (7-APCA) having the formula (I) ##STR1## which is an important synthesis intermediate in the preparation of cephalosporin-like antibiotics, is prepared by treating a compound of the formula (II) ##STR2## in which R.sub.1 and R.sub.2 represent alkyl, aryl and aralkyl radicals, with a strong protonic acid or with a Lewis acid. Compound (II) is prepared by adding triphenylphosphine and alkali metal iodide to a compound of the formula (VI) ##STR3## then reacting with acetaldehyde in base. Compound (VI) is prepared by treating a compound of the formula (VII) ##STR4## with a base in a polar solvent at -70.degree. C. to 0.degree. C. Compound (VII) is prepared by treating a compound of the formula (VIII) ##STR5## with a chlorinating agent in an organic solvent.

Abstract translation: 通过将式（II）化合物（II）化合物制备，其具有式（I）的化合物（I）作为制备头孢菌素样抗生素的重要的合成中间体， 其中R 1和R 2表示烷基，芳基和芳烷基，具有强质子酸或路易斯酸。 通过将三苯基膦和碱金属碘化物加入到式（VI）化合物（VI）中，然后与乙醛在碱中反应来制备化合物（II）。 通过在极性溶剂中在-70℃至0℃下用碱处理式（VII）的化合物（VII）制备化合物（VI）。化合物（VII）通过将化合物 （VIII）的化合物（VIII）与有机溶剂中的氯化剂反应。

公开(公告)号：US4965258A

公开(公告)日：1990-10-23

申请号：US442043

申请日：1989-11-28

Applicant: Horst Boshagen ,  Ulrich Rosentreter ,  Folker Lieb ,  Hermann Oediger ,  Friedel Seuter ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler

Inventor： Horst Boshagen ,  Ulrich Rosentreter ,  Folker Lieb ,  Hermann Oediger ,  Friedel Seuter ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler

IPC: A61K31/40 ,  A61K31/403 ,  A61P7/02 ,  A61P11/00 ,  A61P37/08 ,  C07D209/80 ,  C07D209/86 ,  C07D209/88 ,  C07D209/94 ,  C07D491/10

CPC classification number: C07D209/80 ,  C07D209/86 ,  C07D209/88 ,  C07D491/10

Abstract: Cycloalkano[1,2-b]indole-sulphonamides of the formula ##STR1## where appropriate in an isomeric form, and their salts are disclosed. These compounds are useful to inhibit platelet aggregation and to antoganize thromboxane A.sub.2.

公开(公告)号：US4886898A

公开(公告)日：1989-12-12

申请号：US352522

申请日：1989-05-16

Applicant: Ulrich Niewohner ,  Franz-Peter Hoever ,  Folker Lieb ,  Ulrich Rosentreter ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler ,  Friedel Seuter

Inventor： Ulrich Niewohner ,  Franz-Peter Hoever ,  Folker Lieb ,  Ulrich Rosentreter ,  Elisabeth Perzborn ,  Volker-Bernd Fiedler ,  Friedel Seuter

IPC: C07C49/747 ,  A61K31/18 ,  A61K31/19 ,  A61K31/215 ,  A61K31/22 ,  A61P7/02 ,  A61P9/10 ,  C07C45/00 ,  C07C67/00 ,  C07C69/675 ,  C07C213/00 ,  C07C217/74 ,  C07C231/00 ,  C07C231/12 ,  C07C235/20 ,  C07C253/00 ,  C07C255/47 ,  C07C307/02 ,  C07C311/17 ,  C07C311/21

CPC classification number: A61K31/215 ,  A61K31/18 ,  C07C307/02

Abstract: Certain intermediate aminomethyl-5,6,7,8-tetrahydronaphthyl-oxyacetic acid derivatives of the formula ##STR1## in which R.sup.2 is hydroxyl, alkoxy, phenoxy, benzoxy or NR.sup.4 R.sup.5, andR.sup.4 and R.sup.5 each independently is hydrogen or alkyl, or one of the radicals R.sup.4 or R.sup.5 is benzyl,which are useful in preparing the corresponding aryl-sulfonamides which in-turn have antithrombotic, antiatherosclerotic and antiischaemic properties.

Abstract translation: 其中R 2是羟基，烷氧基，苯氧基，苯氧基或NR 4 R 5，以及R 4和R 5各自独立地是氢或烷基，或一个或多个的一个中间氨基甲基-5,6,7,8-四氢萘基 - 氧乙酸衍生物 基团R 4或R 5为苄基，其可用于制备相应的芳基 - 磺酰胺，其依次具有抗血栓形成，抗动脉粥样硬化和抗静电特性。

公开(公告)号：US4707479A

公开(公告)日：1987-11-17

申请号：US806057

申请日：1985-12-05

Applicant: Horst Meyer ,  Gerhard Franckowiak ,  Ulrich Rosentreter ,  Rainer Gross ,  Gunter Thomas ,  Matthias Schramm ,  Michael Kayser ,  Friedel Seuter ,  Elisabeth Perzborn ,  Martin Bechem

Inventor： Horst Meyer ,  Gerhard Franckowiak ,  Ulrich Rosentreter ,  Rainer Gross ,  Gunter Thomas ,  Matthias Schramm ,  Michael Kayser ,  Friedel Seuter ,  Elisabeth Perzborn ,  Martin Bechem

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/50 ,  A61P3/08 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  C07D211/90 ,  C07D237/00 ,  C07D237/04 ,  C07D333/00 ,  C07D335/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  C07D401/06

CPC classification number: C07D401/12 ,  C07D211/90 ,  C07D237/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/04

Abstract: 1,4-Dihyropyridinecarboxamides of the formula ##STR1## and salts thereof, are effective for treating cardiac insufficiency, thromboses, thromboembolisms and ischaemias, for influencing the blood-sugar level and the circulation and as coronary therapeutic agents and anti-arrhythmic agents.

Abstract translation: 具有式“IMAGE”及其盐的1,4-二氢吡啶甲酰胺及其盐对于治疗心功能不全，血栓形成，血栓栓塞和间皮瘤有效，用于影响血糖水平和循环以及作为冠状动脉治疗剂和抗心律不齐剂。