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公开(公告)号：US20130189363A1
公开(公告)日：2013-07-25
申请号：US13814398
申请日：2010-08-05
IPC分类号： C07K7/54
摘要： β-Hairpin peptidomimetics of the general formula Cyclo (-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-), enantiomers and pharmaceutically acceptable salts thereof, with Xaa1-Xaa14 being amino acid residues of certain types which are defined in the description and the claims, have anti-infective activity, e.g. to selectively inhibit the growth of or to kill microorganisms such as Bacillus subtilis and/or Shigella boydii. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 通式为Xaa1（-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-）的β-发夹肽模拟物，其对映异构体和药学上可接受的盐， -Xaa14是在说明书和权利要求书中定义的某些类型的氨基酸残基，具有抗感染活性，例如， 选择性地抑制枯草芽孢杆菌和/或志贺氏志贺氏杆菌等生长或杀死微生物。 它们可用作治疗或预防感染的药物，或用作食品，化妆品，药物或其他含营养材料的消毒剂。 这些肽模拟物可以通过基于混合固相和溶液相合成策略的方法制造。
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公开(公告)号：US20130023483A1
公开(公告)日：2013-01-24
申请号：US13577153
申请日：2010-02-05
申请人： Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Christian Bisang , Christian Ludin
发明人： Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Christian Bisang , Christian Ludin
IPC分类号： A61K38/12 , A61P17/00 , A61P3/00 , A61P29/00 , A61P31/00 , A61P25/00 , A61P9/00 , A61P11/00 , A61P1/00 , A61P27/02 , A61P31/18 , A61P3/10 , A61P19/02 , A61P35/00 , A61P35/02 , C07K7/00
摘要： Specific template-fixed β-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.
摘要翻译： 通式（I）的具体的模板固定和平滑肽模拟物，其中单个元件T或P是从下一个连接的羰基（C = O）连接点连接到氮（N）的α-氨基酸残基 元件，并且其中所述元件取决于它们在链中的位置在描述中定义，并且权利要求具有作用于受体CXCR7的性质。 因此，这些β-螺旋肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经疾病，心血管疾病，呼吸系统疾病，胃肠疾病， 肠道疾病，泌尿科疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。
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公开(公告)号：US20100216809A1
公开(公告)日：2010-08-26
申请号：US12663009
申请日：2008-06-05
申请人： Jean-Pierre André Marc Bongartz , Lieven Meerpoel , Gustaaf Maria Boeckx , Guy Rosalia Eugeen Van Lommen , Christophe Francis Robert Buyck , Daniel Obrecht , Philipp Ermert , Anatol Luther
发明人： Jean-Pierre André Marc Bongartz , Lieven Meerpoel , Gustaaf Maria Boeckx , Guy Rosalia Eugeen Van Lommen , Christophe Francis Robert Buyck , Daniel Obrecht , Philipp Ermert , Anatol Luther
IPC分类号： A61K31/506 , A61K31/496 , A61K31/454 , C07D403/10 , C07D413/10 , C07D513/04 , C07D487/04 , C07D401/10 , A61P3/04 , A61P3/06 , A61P3/10 , A61P1/16
CPC分类号： C07D513/04 , C07D231/12 , C07D239/26 , C07D239/42 , C07D249/08 , C07D249/12 , C07D271/06 , C07D271/10 , C07D271/107 , C07D401/04 , C07D401/10 , C07D401/12 , C07D487/04
摘要： The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p-; C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
摘要翻译： 本发明还涉及式（I）的DGAT抑制剂，其包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-NR x -C（= O） - ; -Z-C（= O） - ; -Z-NRx-C（= O） - ; -S（= O）p-; C（═S） - ; -NR x -C（= S） - ; -Z-C（= S） - ; -Z-NRx-C（= S） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; R1表示含有至少2个杂原子的5元单环杂环; 6元芳族单环杂环; 或含有至少2个与苯基，环己基或5或6元杂环稠合的杂原子的5元杂环; 其中每个所述杂环可任选被取代; R2表示R3; R 3表示C 3-6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二氧杂环己烯基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或含1或2个N原子的6元芳族杂环，其中所述C3 6-环烷基，苯基，萘基，2,3-二氢-1,4-苯并二恶基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或6-元芳香杂环可以任选被取代; 其N-氧化物，其药学上可接受的盐或其溶剂合物。 本发明还涉及制备这些化合物的方法，包含所述化合物的药物组合物以及用作所述化合物的药物。
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公开(公告)号：US20050187145A1
公开(公告)日：2005-08-25
申请号：US10498468
申请日：2001-12-11
IPC分类号： C12N9/99 , A61K31/675 , A61K38/00 , A61K38/08 , A61K38/10 , A61K38/16 , A61P43/00 , C07K1/04 , C07K1/06 , C07K1/10 , C07K5/12 , C07K7/06 , C07K7/08 , C07K7/54 , C07K7/64
摘要： Template-fixed β-hairpin peptidomimetics of the general formulae (1), wherein Z is a template-fixed chain of 7 to 11 α-amino acid residues which, depending on their positions in the chain (counted starting formteh N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the aove formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 通式（1）的模板固定的β-发夹肽模拟物，其中Z是7至11个α-氨基酸残基的模板固定链，其取决于其在链中的位置（计数起始形式的N-末端氨基酸 ）是Gly或Pro，或某些类型，其作为酰基配方中的其余符号在说明书和权利要求书及其盐中定义，具有抑制蛋白酶，特别是丝氨酸蛋白酶的性质。 这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。
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公开(公告)号：US4929741A
公开(公告)日：1990-05-29
申请号：US169643
申请日：1988-03-17
IPC分类号： C07C45/29 , C07C45/45 , C07C45/51 , C07C45/67 , C07C49/794 , C07C49/796 , C07C49/813 , C07C49/835 , C07C49/84 , C07C49/86 , C07C59/66 , C07C59/68 , C07C323/22 , C07D317/54 , C07D317/60 , C07F7/18
CPC分类号： C07F7/1852 , C07C323/22 , C07C45/298 , C07C45/45 , C07C45/515 , C07C45/673 , C07C49/794 , C07C49/796 , C07C49/813 , C07C49/835 , C07C49/84 , C07C49/86 , C07C59/66 , C07C59/68 , C07C67/313 , C07C67/343 , C07C69/732 , C07C69/734 , C07C69/738 , C07D317/54 , C07D317/60
摘要： Propiolophenone derivatives of the formula ##STR1## wherein R.sup.6 is hydrogen, lower alkyl or a group of the formula ##STR2## as well as corresponding hydroxy compounds of the formula ##STR3## wherein R.sup.6' is hydrogen, lower alkyl, a group of formula (a), (b), (c), (d) or (e) or a group of the formula--C(R.sup.14)(R.sup.15)OR.sup.16' (f'):exhibit mucosa-protective and/or gastric acid secretion-inhibiting properties, such that they can be used for the control or prevention of illnesses of the gastrointestinal tract, especially against gastric ulcers and/or duodenal ulcers.
摘要翻译： 式（I）其中R 6为氢，低级烷基或式COOR 7基团，（a）CONR 8 R 9，（b）C（R 10）O，（C）C（R 11）（OR 12）2， （d）C（OR 13）3（e）或C（R 14）（R 15）OR 16; （f）以及相应的式II的羟基化合物，其中R 6'是氢，低级烷基，式（a），（b），（c），（d）或（e） 式-C（R 14）（R 15）OR 16'（f'）的基团表现出粘膜保护性和/或胃酸分泌抑制性质，使得它们可用于控制或预防胃肠道疾病 ，特别是针对胃溃疡和/或十二指肠溃疡。
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公开(公告)号：US09617308B2
公开(公告)日：2017-04-11
申请号：US14406108
申请日：2012-06-06
摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8 Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.
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公开(公告)号：US09521846B2
公开(公告)日：2016-12-20
申请号：US14074251
申请日：2013-11-07
申请人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。
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公开(公告)号：US09512139B2
公开(公告)日：2016-12-06
申请号：US13508531
申请日：2010-08-03
申请人： Daniel Obrecht , Philipp Ermert , Said Oumouch , Franck Lach , Anatol Luther , Karsten Marx , Kerstin Möhle
发明人： Daniel Obrecht , Philipp Ermert , Said Oumouch , Franck Lach , Anatol Luther , Karsten Marx , Kerstin Möhle
IPC分类号： C07D273/02 , A61K31/407 , C07D273/00 , A61K31/4985 , A61K31/437 , A61P1/00 , A61P25/06 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P19/00 , C07D498/04 , C07D497/18 , C07D498/18
CPC分类号： C07D498/04 , A61K31/407 , A61K31/437 , A61K31/4985 , C07D497/18 , C07D498/18
摘要： Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the β-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.
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公开(公告)号：US20140187472A1
公开(公告)日：2014-07-03
申请号：US14175193
申请日：2014-02-07
申请人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections.These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
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公开(公告)号：US20130225506A1
公开(公告)日：2013-08-29
申请号：US13577143
申请日：2011-02-04
申请人： Frank Otto Gombert , Alexander Lederer , Ralf Löwe , Daniel Obrecht , Barbara Romagnoli , Johann Zimmermann , Kalpana Patel
发明人： Frank Otto Gombert , Alexander Lederer , Ralf Löwe , Daniel Obrecht , Barbara Romagnoli , Johann Zimmermann , Kalpana Patel
IPC分类号： C07K7/64
CPC分类号： C07K7/64 , A61K38/00 , A61K38/17 , A61K38/177 , A61K38/1793 , C07K14/705 , C07K14/715 , C07K14/7158
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.
摘要翻译： 通式（I）的新型模板固定β-发夹肽模拟物，其中单个元件T或P是从下述的羰基（C = O）连接点连接到氮（N）的α-氨基酸残基 元件，并且其中所述元件取决于它们在链中的位置在描述中定义，并且权利要求具有作用于受体CXCR7的性质。 因此，这些β-发夹肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经系统疾病，心血管疾病，呼吸系统疾病，胃肠道疾病或疾病 泌尿系疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。
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