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1. 发明授权

US06429288B1 Peptides containing an arginine mimetic for the treatment of bone metabolic disorders, their production, and drugs containing these compounds 失效
标题翻译：含有精氨酸模拟物的肽用于治疗骨代谢紊乱，其生产和含有这些化合物的药物
公开(公告)号：US06429288B1
公开(公告)日：2002-08-06
申请号：US09486679
申请日：2000-03-31
申请人： Angelika Esswein , Eike Hoffmann , Lothar Kling , Silvia Konetschny-Rapp
发明人： Angelika Esswein , Eike Hoffmann , Lothar Kling , Silvia Konetschny-Rapp
IPC分类号： C07K508
CPC分类号： C07D403/12 , A61K38/00 , C07D207/20 , C07K5/0205 , C07K5/0207 , C07K5/1024 , C07K14/635
摘要： Arginine mimetic peptides according to Formula I of this application have a stimulating effect on bone formation and are useful for the treatment of bone metabolic disorders.
摘要翻译：根据本申请式I的精氨酸模拟肽对骨形成具有刺激作用，并且可用于治疗骨代谢紊乱。

2. 发明授权

US06911553B1 Osteoblast-specific mitogens and drugs containing such compounds 失效
标题翻译：成骨细胞特异性有丝分裂原和含有此类化合物的药物
公开(公告)号：US06911553B1
公开(公告)日：2005-06-28
申请号：US09675943
申请日：2000-09-29
申请人： Angelika Esswein , Lothar Kling
发明人： Angelika Esswein , Lothar Kling
IPC分类号： C07F9/09 , C07F9/06
CPC分类号： C07F9/091
摘要： The invention is directed to compounds of formula (I) wherein R1 alkyl, alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; and the physiologically safe salts, esters, optically active forms, racemates and derivatives thereof which can be metabolized in vivo to yield compounds of general formula (I), methods of preparing same, and drugs containing said compounds, for treating bone metabolic disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 2，R 2， n = 0-12; X =氧或NH; 以及其可在体内代谢产生通式（I）的化合物，其制备方法和含有所述化合物的药物用于治疗骨代谢紊乱的生理上安全的盐，酯，光学活性形式，外消旋体及其衍生物。

3. 发明授权

US06444832B1 Amino alcohol derivatives, method of producing said derivatives and medicaments containing them 失效
标题翻译：氨基醇衍生物，所述衍生物的制造方法和含有它们的药物
公开(公告)号：US06444832B1
公开(公告)日：2002-09-03
申请号：US09407981
申请日：1999-09-29
申请人： Angelika Esswein , Lothar Kling , Ulrike Leser , Walter-Gunar Friebe
发明人： Angelika Esswein , Lothar Kling , Ulrike Leser , Walter-Gunar Friebe
IPC分类号： C07C23100
CPC分类号： C07C233/18 , C07C233/20
摘要： Compounds of formula I in which R1 denotes hydrogen or methyl R2 denotes lower straight-chained or branched alkyl with 1 to 10 carbon atoms R3 denotes hydrogen or lower alkyl n denotes 0-12 R4 denotes alkyl, alkenyl or alkinyl with 6 to 24 carbon atoms, processes for the production thereof as well as pharmaceutical agents containing these compounds for the treatment of osteoporosis.
摘要翻译： R1表示氢或甲基R2的式Iin化合物表示具有1至10个碳原子的较低直链或支链烷基R 3表示氢或低级烷基，表示0-12R 4表示具有6至24个碳原子的烷基，烯基或炔基，其制备方法以及含有这些化合物用于治疗骨质疏松症的药剂。

4. 发明申请

US20050014723A1 Osteoblast-specific mitogens and drugs containing such compounds 审中-公开
标题翻译：成骨细胞特异性有丝分裂原和含有此类化合物的药物
公开(公告)号：US20050014723A1
公开(公告)日：2005-01-20
申请号：US10893426
申请日：2004-07-16
申请人： Angelika Esswein , Lothar Kling
发明人： Angelika Esswein , Lothar Kling
IPC分类号： C07F9/09 , A61K31/685 , A61K31/66
CPC分类号： C07F9/091
摘要： Osteoblast-specific mitogens and drugs containing such compounds can be used for treating metabolic bone diseases. Novel compounds for this treatment include lysophosphatidylic acid derivatives selected from the group consisting of compounds of formula: wherein R1=alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen; the compounds (all-cis-5,8,11,14)-eicosatetraenoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9, cis-12-octadecadienoic acid 2-hydroxy-3-phosphonooxypropyl ester; (all-cis-9,12,15)-octadecatrienoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9-octadecenoic acid 2-hydroxy-3-phosphonooxypropyl ester; and erucic acid 2-hydroxy-3-phosphonooxypropylester being excluded, and the physiologically tolerable salts, esters, optically active forms, and racemates of said compounds.
摘要翻译：成骨细胞特异性有丝分裂原和含有此类化合物的药物可用于治疗代谢性骨病。用于该处理的新型化合物包括选自下式的化合物的溶血磷脂酰衍生物：其中R 1 =具有6至24个碳原子的链烯基或炔基; n = 0-12; X =氧; 化合物（全顺式-5,8,11,14） - 二十碳四烯酸2-羟基-3-膦酰氧丙基酯; 顺式-9，顺式-12-十八碳二烯酸2-羟基-3-膦酰氧基丙基酯; （全顺式-9,12,15） - 十八碳三烯酸2-羟基-3-膦酰氧丙基酯; 顺-9-十八碳烯酸2-羟基-3-膦酰氧基丙酯; 和芥酸2-羟基-3-膦酰氧基丙基酯，以及所述化合物的生理上可耐受的盐，酯，旋光形式和外消旋体。

5. 发明授权

US06197759B1 Osteoblast-specific mitogens and drugs containing such compounds 有权
标题翻译：成骨细胞特异性有丝分裂原和含有此类化合物的药物
公开(公告)号：US06197759B1
公开(公告)日：2001-03-06
申请号：US09508714
申请日：2000-04-11
申请人： Angelika Esswein , Lothar Kling
发明人： Angelika Esswein , Lothar Kling
IPC分类号： A61K31661
CPC分类号： C07F9/091
摘要： Osteoblast-specific mitogens and drugs containing such compounds can be used for treating metabolic bone diseases. These compounds include lysophosphatidylic acid derivatives selected from the group consisting of compounds of formula: wherein R1=alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; the compounds (all-cis-5,8,11,14)-eicosatetraenoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9, cis-12-octadecadienoic acid 2-hydroxy-3-phosphonooxypropyl ester; (all-cis-9,12,15)-octadecatrienoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9-octadecenoic acid 2-hydroxy-3-phosphonooxypropyl ester; and erucic acid 2-hydroxy-3-phosphonooxypropylester being excluded, and the physiologically tolerable salts, esters, optically active forms, and racemates of said compounds, and derivatives of said compounds, salts, esters, optically active forms and racemates which can be metabolized in vivo to yield the corresponding compound of formula (I).
摘要翻译：成骨细胞特异性有丝分裂原和含有此类化合物的药物可用于治疗代谢性骨病。这些化合物包括选自下式的化合物的溶血磷脂酰衍生物：其中R1 =具有6至24个碳原子的烯基或炔基; n = 0-12; X =氧或NH;化合物（全顺式-5， 8,11,14） - 二十碳四烯酸2-羟基-3-膦酰氧基丙基酯; 顺式-9，顺式-12-十八碳二烯酸2-羟基-3-膦酰氧基丙基酯; （全顺式-9,12,15） - 十八碳三烯酸2-羟基-3-膦酰氧丙基酯; 顺-9-十八碳烯酸2-羟基-3-膦酰氧基丙酯; 和芥酸2-羟基-3-膦酰氧基丙基酯，以及所述化合物的生理上可耐受的盐，酯，旋光形式和外消旋物，以及所述化合物的衍生物，盐，酯，旋光活性物质和可被代谢的外消旋体在体内产生相应的式（I）化合物。

6. 发明授权

US06673816B1 Rhodanine carboxylic acid derivatives for the treatment and prevention of metabolic bone disorders 失效
标题翻译：用于治疗和预防代谢性骨骼疾病的罗丹明羧酸衍生物
公开(公告)号：US06673816B1
公开(公告)日：2004-01-06
申请号：US09787917
申请日：2001-06-21
申请人： Angelika Esswein , Wolfgang Schaefer , Christos Tsaklakidis , Konrad Honold , Klaus Kaluza
发明人： Angelika Esswein , Wolfgang Schaefer , Christos Tsaklakidis , Konrad Honold , Klaus Kaluza
IPC分类号： A61K31426
CPC分类号： C07D277/20 , C07D277/36 , C07D417/06 , C07D417/12 , C07D493/04
摘要： Compounds of general formula (I), in which m is 0-8, q is a 0-8, a is 0-4, A signifies a single or double bond, R1, R2 signify hydrogen or lower alkyl and, when m signifies 2-8, R1 and R2 in the group CR1═CR2 can have various significances within the following sequence, R3 signifies hydrogen or lower alkyl, X signifies hydrogen or —(CH2)b—COR4 with b=0-4, Y signifies hydrogen, —COR4, phenyl or indolyl residue R4 signifies hydroxyl, lower alkoxy or the NR1R2 residue, W signifies an optionally mono- or polysubstituted saturated or unsaturated mono-, bi- or tricycle which can contain hetero atoms, as well physiologically compatible salts, esters, optically active forms, racemates, tautomers, and derivatives which can be metabolized in vivo to compounds of general formula (I).
摘要翻译：通式（I）的化合物，其中m为0-8，q为0-8，a为0-4，A表示单键或双键，R1，R2表示氢或低级烷基，当m表示 2-8中，基团CR1 = CR2中的R1和R2可以在以下序列中具有各种含义，R3表示氢或低级烷基，X表示氢或 - （CH2）b-COR4，其中b = 0-4，Y表示氢，-COR 4，苯基或吲哚基残基R 4表示羟基，低级烷氧基或NR 1 R 2残基，W表示可以含有杂原子的任选的单取代或多取代的饱和或不饱和单 - ，二 - 或三环，以及生理上相容的盐，酯，光学活性形式，外消旋体，互变异构体和衍生物，其可以在体内被代谢为通式（I）的化合物。

7. 发明授权

US5698541A 2,4-diphosphonoglutaric acid derivatives, processes for their production and pharmaceutical agents containing these compounds 失效
标题翻译： 2,4-二膦酸葡萄糖酸衍生物，其制备方法和含有这些化合物的药剂
公开(公告)号：US5698541A
公开(公告)日：1997-12-16
申请号：US714076
申请日：1996-09-25
申请人： Gerd Zimmermann , Angelika Esswein , Christos Tsaklakidis , Frieder Bauss
发明人： Gerd Zimmermann , Angelika Esswein , Christos Tsaklakidis , Frieder Bauss
IPC分类号： A61K31/66 , A61P3/00 , C07F9/38 , C07F9/547 , C07F9/572 , C07F9/40
CPC分类号： C07F9/3869 , C07F9/3873 , C07F9/5721
摘要： The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring and R.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl, their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.
摘要翻译： PCT No.PCT / EP95 / 01062 Sec。 371日期1996年9月25日 102（e）日期1996年9月25日PCT提交1995年3月22日PCT公布。公开号WO95 / 26358 日期1995年10月5日本发明涉及通式Ⅰ（I）的化合物，其中R表示可以被羟基，烷氧基，氨基，二烷基氨基，烷基巯基，烷基亚磺酰基，烷基磺酰基，环烷基，芳基或杂环，或者表示低级烯基，环烷基，环烯基，芳基或杂环，并且R 1和R 2可以彼此独立地为氢，低级烷基，环烷基，芳基或芳甲基，它们的光学活性盐作为其药理学上可接受的盐，其生产方法以及含有这些化合物用于治疗钙代谢疾病的药剂。此外，本发明涉及式II化合物作为制备式I化合物的中间产物。

8. 发明申请

US20070191274A1 Active hedgehog protein conjugate 审中-公开
标题翻译：活性刺猬蛋白结合物
公开(公告)号：US20070191274A1
公开(公告)日：2007-08-16
申请号：US11645014
申请日：2006-12-22
申请人： Angelika Esswein , Kurt Lang , Petra Rueger , Tilman Seytter
发明人： Angelika Esswein , Kurt Lang , Petra Rueger , Tilman Seytter
IPC分类号： A61K38/17 , C07K14/47 , A61K31/727 , A61K31/185
CPC分类号： A61K31/185 , A61K31/727 , A61K38/00 , C07K14/47
摘要： A hedgehog conjugate which is characterized in that it contains: a) a polypeptide composed of 10 to 30 hydrophobic amino acids and/or amino acids which form transmembrane helices and are positively charged, b) 1 to 4 aliphatic, saturated or unsaturated hydrocarbon residues with a chain length of 10 to 24 C atoms and with a hydrophobic action or c) a hydrophobic thio compound covalently bound to a hedgehog protein and which has a several-fold increased activity and is suitable as a pharmaceutical agent.
摘要翻译：一种刺猬蛋白缀合物，其特征在于其包含：a）由10至30个疏水氨基酸和/或氨基酸组成的多肽，其形成跨膜螺旋并带正电荷，b）1至4个脂族，饱和或不饱和的烃残基，链长为10至24个C原子并具有疏水作用，或c）与猬蛋白共价结合的疏水性硫代化合物，并且其具有几倍增加的活性并且适于作为药剂。

9. 发明授权

US5627170A Phosphonic acid compound containing heterocyclic substituents, pharmaceutical composition contains same and a method of treating calcium metabolism disturbance 失效
标题翻译：含有杂环取代基的膦酸化合物，药物组合物含有相同的治疗钙代谢紊乱的方法
公开(公告)号：US5627170A
公开(公告)日：1997-05-06
申请号：US465360
申请日：1995-06-05
申请人： Christos Tsaklakidis , Elmar Bosies , Angelika Esswein , Frieder Bauss
发明人： Christos Tsaklakidis , Elmar Bosies , Angelika Esswein , Frieder Bauss
IPC分类号： A61K31/66 , A61K31/662 , A61K31/675 , A61P3/00 , A61P3/14 , C07F9/38 , C07F9/40 , C07F9/553 , C07F9/572 , C07F9/58 , C07F9/6506 , C07F9/6509 , A61K31/40 , C07D203/08 , C07D205/04 , C07D207/06
CPC分类号： C07F9/65062 , C07F9/3808 , C07F9/4006 , C07F9/5532 , C07F9/5721 , C07F9/5722 , C07F9/582 , C07F9/65061
摘要： Compounds of the formula I ##STR1## in which R signifies a possibly substituted amino group of the general formula --NR.sup.1 R.sup.2, whereby, independently of one another, R.sup.1 and R.sup.2 each signify hydrogen, lower alkyl, lower alkenyl or lower alkynyl or R represents a saturated, unsaturated or aromatic heterocyclic ring which can possibly be substituted once or twice by lower alkyl or halogen, alk signifies a valency bond, a methylene, a saturated or unsaturated, straight-chained or branched alkylene chain with 2-6 carbon atoms and R.sup.3, R.sup.4 and R.sup.5, in each case independently of one another, signify hydrogen, lower alkyl or benzyl, as well as their pharmacologically acceptable salts and enantiomers, whereby, for the case that R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3 and alk signifies a valency bond, R cannot be the dimethylamino group, processes for their preparation and medicaments which contain these compounds for the treatment of calcium metabolism diseases.
摘要翻译：其中R表示通式-NR1R2的可能取代的氨基的式I化合物（I），其中R 1和R 2各自独立地表示氢，低级烷基，低级烯基或低级炔基或 R表示可以被低级烷基或卤素取代一次或两次的饱和，不饱和或芳族杂环，alk表示具有2-6碳的价键，亚甲基，饱和或不饱和的直链或支链亚烷基链原子和R 3，R 4和R 5在每种情况下彼此独立地表示氢，低级烷基或苄基，以及它们的药理学上可接受的盐和对映异构体，其中在R3 = R4 = R5 = CH3且alk表示化合键，R不能是二甲基氨基，其制备方法和含有这些化合物用于治疗钙代谢疾病的药物。

10. 发明授权

US06468978B1 Active hedgehog protein conjugate 失效
标题翻译：活性刺猬蛋白结合物
公开(公告)号：US06468978B1
公开(公告)日：2002-10-22
申请号：US09301199
申请日：1999-04-28
申请人： Angelika Esswein , Kurt Lang , Petra Rueger , Tilman Seytter
发明人： Angelika Esswein , Kurt Lang , Petra Rueger , Tilman Seytter
IPC分类号： A61K3817
CPC分类号： A61K31/185 , A61K31/727 , A61K38/00 , C07K14/47
摘要： A hedgehog conjugate which is characterized in that it contains: a) a polypeptide composed of 10 to 30 hydrophobic amino acids and/or amino acids which form transmembrane helices and are positively charged, b) 1 to 4 aliphatic, saturated or unsaturated hydrocarbon residues with a chain length of 10 to 24 C atoms and with a hydrophobic action or c) a hydrophobic thio compound covalently bound to a hedgehog protein and which has a several-fold increased activity and is suitable as a pharmaceutical agent.
摘要翻译：一种刺猬蛋白缀合物，其特征在于其包含：a）由10至30个疏水氨基酸和/或氨基酸组成的多肽，其形成跨膜螺旋并带正电荷，b）1至4个脂族，饱和或不饱和的烃残基，链长为10至24个C原子并具有疏水作用，或c）与猬蛋白共价结合的疏水性硫代化合物，并且其具有几倍增加的活性并且适于作为药剂。

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