公开(公告)号：US4737488A

公开(公告)日：1988-04-12

申请号：US676160

申请日：1984-11-29

Applicant: Oswald Lockhoff ,  Bernd-Wieland Kruger ,  Peter Stadler ,  Karl G. Metzger ,  Hans-Georg Opitz ,  Klaus Schaller ,  Klaus G. Stunkel ,  Hans-Joachim Zeiler

Inventor： Oswald Lockhoff ,  Bernd-Wieland Kruger ,  Peter Stadler ,  Karl G. Metzger ,  Hans-Georg Opitz ,  Klaus Schaller ,  Klaus G. Stunkel ,  Hans-Joachim Zeiler

IPC: C07H15/00 ,  C07H13/12 ,  C07H15/04 ,  A61K31/70 ,  C07H5/06

CPC classification number: C07H13/12 ,  C07H15/04

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, an optionally substituted aromatic hydrocarbon radical, an aralkyl radical or an optionally substituted aliphatic hydrocarbon radical having up to 45 C atoms,R.sup.2 is an optionally substituted aromatic hydrocarbon radical, an aralkyl radical or an optionally substituted aliphatic hydrocarbon radical having 5-50 C atoms,X is O, S, NH or NR, R being an alkyl radical having up to 20 C atoms, andZ is a glycosyl radical bonded via the anomeric carbon atom,or pharmaceutically acceptable salts thereof stimulate the immune system.

Abstract translation: 其中R 1是氢，任选取代的芳族烃基，芳烷基或具有至多45个C原子的任选取代的脂族烃基的式的化合物，R 2是任选取代的芳族烃基，芳烷基或 任选取代的具有5-50个碳原子的脂族烃基，X是O，S，NH或NR，R是具有至多20个C原子的烷基，Z是通过端基异碳键键合的糖基，或药学上可接受的 其盐刺激免疫系统。

公开(公告)号：US4699899A

公开(公告)日：1987-10-13

申请号：US832482

申请日：1986-02-21

Applicant: Bernd-Wieland Kruger ,  Yutaka Hayauchi ,  Oswald Lockhoff ,  Peter Stadler ,  Karl G. Metzger ,  Klaus G. Stunkel ,  Hans-Joachim Zeiler

Inventor： Bernd-Wieland Kruger ,  Yutaka Hayauchi ,  Oswald Lockhoff ,  Peter Stadler ,  Karl G. Metzger ,  Klaus G. Stunkel ,  Hans-Joachim Zeiler

IPC: C07H13/00 ,  A61K31/70 ,  A61K31/7024 ,  A61K31/7028 ,  A61P31/00 ,  A61P37/04 ,  C07H1/00 ,  C07H13/12 ,  C07H15/04 ,  C07H15/12

CPC classification number: C07H13/12 ,  C07H15/04 ,  Y10S514/885

Abstract: Novel compounds of the formula ##STR1## in which X is hydrogen or --CH.sub.2 --OR.sup.5,Z represents OR.sup.4, NH.sub.2 or ##STR2## R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or ##STR3## at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being ##STR4## Y and W each independently is oxygen, sulphur, NH or CH.sub.2, and R.sup.1, R.sup.6, R.sup.7 and R.sup.8 each independently is an optionally substituted hydrocarbon radical with up to 50 C atoms,stimulate the immune system.

Abstract translation: 式中，X为氢或-CH 2 OR 5的新颖化合物，Z为OR 4，NH 2或R 2，R 3，R 4和R 5各自独立地为氢或R 2，R 3， ，R 4和R 5是Y，W各自独立地是氧，硫，NH或CH 2，R 1，R 6，R 7和R 8各自独立地是具有至多50个C原子的任选取代的烃基，刺激免疫系统。

公开(公告)号：US4686208A

公开(公告)日：1987-08-11

申请号：US673811

申请日：1984-11-21

Applicant: Oswald Lockhoff ,  Bernd-Wieland Kruger ,  Peter Stadler ,  Arnold Paessens ,  Gert Streissle ,  Peter Taylor ,  Hans-Joachim Zeiler ,  Karl-Georg Metzger

Inventor： Oswald Lockhoff ,  Bernd-Wieland Kruger ,  Peter Stadler ,  Arnold Paessens ,  Gert Streissle ,  Peter Taylor ,  Hans-Joachim Zeiler ,  Karl-Georg Metzger

IPC: A61K31/70 ,  C07H13/06 ,  C07H13/12 ,  C07H5/06

CPC classification number: C07H13/06 ,  C07H13/12

Abstract: Compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted, straight-chain or branched, saturated, monounsaturated or polyunsaturated alkyl radical, an optionally substituted, saturated or one- or polyunsaturated cycloalkyl radical or an optionally substituted aryl radical or aralkyl radical,X represents CH.sub.2, O, S, NH or N-alkyl with up to 20 C atoms,R.sup.2 has the meaning of R.sup.1, and can represent hydrogen if X denotes CH.sub.2, the radicals R.sup.3 independently of one another represent hydrogen, an acyl radical or alkyl radical with in each case up to 20 C atoms, a silyl radical and/or a phosphoric acid or phosphoric acid ester radical andR.sup.4 denotes hydrogen, methyl or --CH.sub.2 --OR.sup.3, with the proviso that one of the radicals R.sup.3 always represents a phosphoric acid or phosphoric acid ester radical, which stimulate a patient's immune system and are thereby effective in combating viral disease and bacterial infection.

Abstract translation: 式“IMAGE”的化合物，其中R 1表示任选取代的直链或支链饱和的单不饱和或多不饱和烷基，任选取代的饱和或一或多不饱和环烷基或任选取代的芳基或芳烷基 X表示CH 2，O，S，NH或具有多达20个C原子的N-烷基，R 2具有R 1的含义，如果X表示CH 2，则可表示氢，基团R 3彼此独立地表示氢，酰基 或烷基，在每种情况下最多达20个C原子，甲硅烷基和/或磷酸或磷酸酯基，R4表示氢，甲基或-CH2-OR3，条件是基团R3之一总是表示 磷酸或磷酸酯基，其刺激患者的免疫系统，从而有效地对抗病毒性疾病和细菌感染。

公开(公告)号：US5859053A

公开(公告)日：1999-01-12

申请号：US945511

申请日：1997-10-24

Applicant: Eva Lesur ,  Dieter Neuser ,  Oswald Lockhoff ,  Elisabeth Perzborn ,  Peter Kurka ,  Johannes Peter Stasch

Inventor： Eva Lesur ,  Dieter Neuser ,  Oswald Lockhoff ,  Elisabeth Perzborn ,  Peter Kurka ,  Johannes Peter Stasch

IPC: C07C201/02 ,  C07C203/04 ,  C07C235/60 ,  C07D317/24 ,  A61K31/21 ,  C07C69/76 ,  C07C203/00 ,  C07C233/00

CPC classification number: C07C235/60 ,  C07C203/04 ,  C07D317/24

Abstract: The invention relates to new derivatives of acetylsalicylic acid (called ASA in the following), which contain an NO.sub.3 structure. They are therapeutically active either as the intact active compound molecule or after cleavage (NO release). The invention also relates to processes for their preparation and their use as medicaments, in particular for the alleviation of pain, inhibition of platelet aggregation, lowering of fever and for the prevention of cardiovascular disorders and oncoses.

Abstract translation: PCT No.PCT / EP96 / 01630 Sec。 371 1997年10月24日第 102（e）1997年10月24日PCT PCT 1996年4月19日PCT公布。 出版物WO96 / 34848 PCT 日期：1996年11月7日本发明涉及含有NO 3结构的乙酰水杨酸（以下称为ASA）的新衍生物。 它们作为完整的活性化合物分子或在裂解后（NO释放）是治疗活性的。 本发明还涉及其制备方法及其作为药物的用途，特别是用于缓解疼痛，抑制血小板聚集，降低发热和预防心血管疾病和肿瘤。

公开(公告)号：US4855283A

公开(公告)日：1989-08-08

申请号：US874983

申请日：1986-06-16

Applicant: Oswald Lockhoff ,  Yutaka Hayauchi ,  Peter Stadler ,  Klaus G. Stunkel ,  Gert Streissle ,  Arnold Paessens ,  Volker Klimetzek ,  Hans-Joachim Zeiler ,  Karl G. Metzger ,  Hein-Peter Kroll ,  Helmut Brunner ,  Klaus Schaller

Inventor： Oswald Lockhoff ,  Yutaka Hayauchi ,  Peter Stadler ,  Klaus G. Stunkel ,  Gert Streissle ,  Arnold Paessens ,  Volker Klimetzek ,  Hans-Joachim Zeiler ,  Karl G. Metzger ,  Hein-Peter Kroll ,  Helmut Brunner ,  Klaus Schaller

IPC: A61K31/70 ,  A61K31/7024 ,  A61K31/7028 ,  A61K39/39 ,  A61P1/16 ,  A61P11/00 ,  A61P27/16 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P37/00 ,  C07H13/04 ,  C07H13/06 ,  C07H13/12 ,  C07H15/04 ,  C07H15/12

CPC classification number: C07H13/04 ,  A61K39/39 ,  C07H13/12 ,  A61K2039/55511

Abstract: Compounds of the formula ##STR1## in which R.sup.1 denotes hydrogen or a saturated or singly or multiply unsaturated alkyl radical having up to 50 carbon atoms,X represents --CH.sub.2 --, --O-- or --NH--,R.sup.2 denotes hydrogen or a saturated or singly or multiply unsaturated alkyl radical having up to 50 carbon atoms,R.sup.3, R.sup.4 and R.sup.5, independently of one another, denotes hydrogen or acyl--CO--R.sup.6, R.sup.6 being an alkyl radical having up to 10 carbon atoms,R.sup.7 denotes hydrogen, C.sub.1 -C.sub.7 -alkyl-, hydroxymethyl, 1-hydroxyethyl, mercaptomethyl, 2-(methylthio)-ethyl, 3-aminopropyl, 3-ureidopropyl, 3-guanidyl-propyl, 4-aminobutyl, carboxymethyl, carbamylmethyl, 2-carboxyethyl, 2-carbamoylethyl, benzyl, 4-hydroxybenzyl, 3-indolylmethyl or 4-imidazolylmethyl, andR.sup.8 represents hydrogen or methyl, andR.sup.9 represents hydrogen, acetyl, benzoyl, trichloroacetyl, trifluoroacetyl, methoxycarbonyl, t-butyloxycarbonyl or benzyloxycarbonyl andR.sup.7 and R.sup.8 together can denote --CH.sub.2 --CH.sub.2 --CH.sub.2, and pharmaceutically acceptable salts thereof stimulate the immune system and can be used in conjuction with antibiotics and vaccines. New intermediates are also shown.

Abstract translation: 其中R 1表示氢或具有至多50个碳原子的饱和或单或多不饱和烷基的式“IMAGE”的化合物，X表示-CH 2 - ， - O-或-NH-，R 2表示氢或饱和或 具有多达50个碳原子的单或多不饱和烷基，R 3，R 4和R 5彼此独立地表示氢或酰基-CO-R 6，R 6是具有至多10个碳原子的烷基，R 7表示氢，C 1 C 1-7 - 烷基 - ，羟甲基，1-羟乙基，巯基甲基，2-（甲硫基） - 乙基，3-氨丙基，3-脲基丙基，3-氨基丙基 - 丙基，4-氨基丁基，羧甲基，氨基甲酰甲基，2-羧乙基， 乙酰基，苯甲酰基，三氯乙酰基，三氟乙酰基，甲氧基羰基，叔丁氧基羰基或苄氧基羰基，R7和R8一起可以表示（C 1 -C 6）烷基，苄基，4-羟基苄基，3-吲哚基甲基或4-咪唑基甲基，R 8表示氢或甲基， -CH 2 -CH 2 -CH 2，及其药学上可接受的盐 模拟免疫系统，并可与抗生素和疫苗结合使用。 还显示了新的中间体。

公开(公告)号：US4574122A

公开(公告)日：1986-03-04

申请号：US675690

申请日：1984-11-28

Applicant: Bernd-Wieland Kruger ,  Oswald Lockhoff ,  Peter Stadler ,  Karl G. Metzger ,  Hans-Georg Opitz ,  Klaus G. Stunkel ,  Hans-Joachim Zeiler

Inventor： Bernd-Wieland Kruger ,  Oswald Lockhoff ,  Peter Stadler ,  Karl G. Metzger ,  Hans-Georg Opitz ,  Klaus G. Stunkel ,  Hans-Joachim Zeiler

IPC: C07H15/12 ,  A61K31/70 ,  A61K31/7028 ,  A61P37/00 ,  C07H13/12 ,  C07H15/04 ,  C07H5/06

CPC classification number: C07H15/04 ,  Y10S514/885

Abstract: Compounds of the formula ##STR1## in which X is hydrogen or the radical --CH.sub.2 OR.sup.5,three of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or ##STR2## and the fourth is ##STR3## Z each independently is oxygen, sulphur, NH or CH.sub.2, and R.sup.1, R.sup.6 and R.sup.7 each independently is an optionally substituted hydrocarbon radical having up to 50 carbon atoms,stimulate the immune system's response and antibody production.

Abstract translation: 其中X是氢或基团-CH 2 OR 5，R 3，R 4，R 5和R 5中的三个各自独立地是氢或者“IMAGE”，而第四个是Z，Z各自独立地是氧，硫， NH或CH 2，并且R 1，R 6和R 7各自独立地为具有至多50个碳原子的任选取代的烃基，刺激免疫系统的应答和抗体产生。

公开(公告)号：US06034055A

公开(公告)日：2000-03-07

申请号：US255642

申请日：1999-02-22

Applicant: Oswald Lockhoff ,  Burkhard Mielke ,  Helmut Brunner ,  Klaus Schaller

Inventor： Oswald Lockhoff ,  Burkhard Mielke ,  Helmut Brunner ,  Klaus Schaller

IPC: C07H13/06 ,  A61K38/00 ,  A61P37/00 ,  A61P37/04 ,  C07H15/12 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K9/00 ,  A61K38/16 ,  A01N43/04

CPC classification number: C07H15/12 ,  C07K9/005 ,  A61K38/00 ,  Y10S514/885

Abstract: The present invention relates to (2-aminoacylamino-2-deoxy-glycosyl)-amides, which are substituted on the nitrogen atom of the amino acid, of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation and to their use in medicaments.

Abstract translation: 本发明涉及在通式（I）的氨基酸的氮原子上取代的（2-氨基酰基氨基-2-脱氧糖基） - 酰胺，其中取代基具有在说明书中给出的含义， 其制备过程及其在药物中的应用。

公开(公告)号：US5905071A

公开(公告)日：1999-05-18

申请号：US605031

申请日：1996-06-25

Applicant: Oswald Lockhoff ,  Burkhard Mielke ,  Helmut Brunner ,  Klaus Schaller

Inventor： Oswald Lockhoff ,  Burkhard Mielke ,  Helmut Brunner ,  Klaus Schaller

IPC: C07H13/06 ,  A61K38/00 ,  A61P37/00 ,  A61P37/04 ,  C07H15/12 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K9/00 ,  A61K31/70 ,  A01N43/04 ,  C07H15/00

CPC classification number: C07H15/12 ,  C07K9/005 ,  A61K38/00 ,  Y10S514/885

Abstract: The present invention relates to (2-aminoacylamino-2-deoxy-glycosyl)-amides, which are substituted on the nitrogen atom of the amino acid, of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation and to their use in medicaments.

Abstract translation: PCT No.PCT / EP94 / 02736 Sec。 371日期1996年6月25日第 102（e）1996年6月25日PCT PCT 1994年8月17日PCT公布。 出版物WO95 / 06654 日期：1995年3月9日本发明涉及在通式（I）的氨基酸的氮原子上被取代的（2-氨基酰基氨基-2-脱氧 - 糖基） - 酰胺，其中取代基具有 在描述中给出了它们的制备过程及其在药物中的用途。

公开(公告)号：US4716152A

公开(公告)日：1987-12-29

申请号：US675808

申请日：1984-11-28

Applicant: Bernd-Wieland Kruger ,  Oswald Lockhoff ,  Karl G. Metzger ,  Hans-Georg Opitz ,  Klaus Schaller ,  Klaus G. Stunkel ,  Hans-Joachim Zeiler

Inventor： Bernd-Wieland Kruger ,  Oswald Lockhoff ,  Karl G. Metzger ,  Hans-Georg Opitz ,  Klaus Schaller ,  Klaus G. Stunkel ,  Hans-Joachim Zeiler

IPC: A61K31/70 ,  A61K31/7028 ,  A61P37/00 ,  C07H15/04 ,  C07H15/10

CPC classification number: C07H15/04

Abstract: Compounds of the formula ##STR1## in which X is hydrogen or the radical CH.sub.2 OR.sup.5,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently is hydrogen or the radical ##STR2## Y is oxygen, sulphur, NH or CH.sub.2, and R.sup.1 and R.sup.6 each independently is an optionally substituted hydrocarbon radical having up to 50 carbon atoms, with the proviso that at least one of the radicals R.sup.1 and/or R.sup.6 contains between 9 to 50 carbon atoms,some of which are known, stimulate the immune system's response and antibody production.

Abstract translation: 其中X为氢或基团CH 2 OR 5，R 2，R 3，R 4和R 5各自独立地为氢或基团Y为氧，硫，NH或CH 2的式“IMAGE”的化合物，R 1和R 6各自独立地为 是具有至多50个碳原子的任选取代的烃基，条件是基团R 1和/或R 6中的至少一个含有9至50个碳原子，其中一些是已知的，刺激免疫系统的应答和抗体产生 。

公开(公告)号：US4710491A

公开(公告)日：1987-12-01

申请号：US681965

申请日：1984-12-14

Applicant: Oswald Lockhoff ,  Peter Stadler ,  Hans-Georg Opitz ,  Harald Horstmann ,  Bodo Junge ,  Bernhard Pelster

Inventor： Oswald Lockhoff ,  Peter Stadler ,  Hans-Georg Opitz ,  Harald Horstmann ,  Bodo Junge ,  Bernhard Pelster

IPC: A61K31/70 ,  A61K31/7008 ,  A61K31/7024 ,  A61K31/7028 ,  A61P29/00 ,  C07H5/06 ,  C07H13/04 ,  C07H13/06 ,  C07H15/04 ,  C07H15/12 ,  C07H15/18

CPC classification number: C07H13/04 ,  C07H13/06 ,  C07H15/04 ,  C07H15/18

Abstract: A method of combating rheumatic diseases which comprises administering to a patient afflicted therewith an amount effective to combat such disease of a compound of the formula ##STR1## in which Z is a glycosyl radical bonded via the anomeric carbon atom,R.sub.1 is hydrogen or an optionally substituted hydrocarbon radical with up to 30 C atoms, which hydrocarbon radical is optionally interrupted by O, N or S, andR.sub.2 is hydrogen or an alkyl or aralkyl radical with up to 30 C atoms, which is optionally interrupted by O, N or S or substituted by an oxygen-containing group or halogen,with the proviso that COR.sub.1 is not an acyl group with 1-5 C atoms if R.sub.2 is alkyl with 10-20 C atoms.

Abstract translation: 一种抗风湿性疾病的方法，其包括对患有其有效抗击下列化合物的疾病的患者施用：其中Z是通过端基异构体碳原子键合的糖基，R1是氢或任选的 具有多达30个C原子的取代的烃基，该烃基任选地被O，N或S间隔，并且R 2是氢或具有至多30个C原子的烷基或芳烷基，其任选地被O，N或S 或被含氧基团或卤素取代，条件是如果R2是具有10-20个C原子的烷基，则COR1不是具有1-5个C原子的酰基。