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1. 发明申请

US20100216809A1 PIPERIDINE/PIPERAZINE DERIVATIVES 有权
标题翻译：哌啶/哌嗪衍生物
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。

2. 发明授权

US08835437B2 Piperidine/piperazine derivatives 有权
标题翻译：哌啶/哌嗪衍生物
公开(公告)号：US08835437B2
公开(公告)日：2014-09-16
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 Nestor 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 Nestor Buyck , Daniel Obrecht , Philipp Ermert , Anatol Luther
IPC分类号： A61K31/496 , C07D487/04 , C07D513/04 , C07D239/42 , C07D239/26 , A61K31/506 , A61K31/454 , C07D231/12 , C07D249/08 , C07D249/12 , C07D271/06 , C07D401/10
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。

3. 发明授权

US07612064B2 Sulfopyrroles 有权
标题翻译：硫磺吡咯
公开(公告)号：US07612064B2
公开(公告)日：2009-11-03
申请号：US10557664
申请日：2004-05-24
申请人： Martin Eberle , Philipp Ermert , Daniel Obrecht , Frank Lach , Anatol Luther , Felix Bachmann , Allessandro Strebel
发明人： Martin Eberle , Philipp Ermert , Daniel Obrecht , Frank Lach , Anatol Luther , Felix Bachmann , Allessandro Strebel
IPC分类号： C07D233/00 , C07D249/08 , C07D413/00 , A61K31/535 , A01N43/50 , A01N43/64
CPC分类号： C07D401/04 , C07D207/48 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The invention relates to compounds of formula (I) wherein R1 represents aryl, aralkyl or heteroaryl, R2 is aryl or heteroaryl and R3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
摘要翻译：本发明涉及式（I）化合物，其中R 1表示芳基，芳烷基或杂芳基，R 2为芳基或杂芳基，R 3为芳基，杂芳基或任选取代的氨基甲基，合成这些化合物的方法为含有式（I）化合物用于制备用于治疗肿瘤和自身免疫性疾病的药物组合物的式（I）化合物的使用，以及使用式（I）或式（I）化合物治疗肿瘤和自身免疫性疾病的方法，含有该组合物的药物组合物。

4. 发明授权

US09512139B2 Conformationally constrained, fully synthetic macrocyclic compounds 有权
标题翻译：构象约束的全合成大环化合物
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.

5. 发明申请

US20120270881A1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权
标题翻译：一致的约束，全合成大环化合物
公开(公告)号：US20120270881A1
公开(公告)日：2012-10-25
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 , C07D273/00 , A61K31/4985 , A61K31/437 , A61P1/00 , A61P19/00 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61K31/407 , A61P25/06
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.
摘要翻译：构型限制，式Ia和Ib的空间限定的12-30元大环环系由三个不同的分子部分构成：模板A，构象调节剂B和桥C.这些大环Ia和Ib容易通过平行合成或组合化学溶液或固相。它们被设计为与多种特异性生物靶标类型相互作用，其实例是对G蛋白偶联受体（GPCR），离子通道和信号转导通路的激动或拮抗活性。特别地，这些大环化合物作为拮抗剂作为拮抗剂，作为5-HT2B亚型的5-羟色胺受体的调节剂作为电压门控钾通道Kv1.3的阻断剂，作为抑制剂，作为拮抗剂受体，FP受体和嘌呤能受体P2Y1 连接蛋白依赖的规范Wnt通路。因此，它们作为各种疾病的药物具有巨大的潜力。

6. 发明授权

US09695191B2 Conformationally constrained, fully synthetic macrocyclic compounds 有权
公开(公告)号：US09695191B2
公开(公告)日：2017-07-04
申请号：US13388891
申请日：2009-08-05
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 , 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 type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.

7. 发明申请

US20120202821A1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权
标题翻译：一致的约束，全合成大环化合物
公开(公告)号：US20120202821A1
公开(公告)日：2012-08-09
申请号：US13388891
申请日：2009-08-05
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： A61K31/407 , A61K31/4985 , A61K31/4745 , A61P1/00 , A61P15/06 , A61P25/06 , A61P25/18 , A61P25/24 , A61P27/02 , A61P27/06 , C07D498/04 , A61P25/00
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 type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
摘要翻译：构形限制的（I）型的空间定义的12-30元大环环体系由描述和权利要求书中详细描述的三个不同的构成单元构成：芳族模板a，构象调节剂b和间隔子部分c。类型（I）的大环化合物容易通过平行合成或组合化学制备。它们旨在与具体的生物目标相互作用。特别地，它们表现出对胃动素受体（MR受体），5-HT2B（5-HT2B受体）5型血清素受体和前列腺素F2受体（FP受体）的激动作用或拮抗作用。因此，它们可用于治疗胃肠道的运动障碍，如糖尿病性胃轻瘫和便秘型肠易激综合征; CNS相关疾病如偏头痛，精神分裂症，精神病或抑郁症; 的高眼压症如青光眼和早产。

8. 发明申请

US20070060570A1 Sulfopyrroles 有权
标题翻译：硫磺吡咯
公开(公告)号：US20070060570A1
公开(公告)日：2007-03-15
申请号：US10557664
申请日：2004-05-24
申请人： Martin Eberle , Daniel Obrecht , Philipp Ermert , Franck Lach , Anatol Luther , Felix Bachmann , Alessandro Strebel
发明人： Martin Eberle , Daniel Obrecht , Philipp Ermert , Franck Lach , Anatol Luther , Felix Bachmann , Alessandro Strebel
IPC分类号： A61K31/55 , A61K31/454 , A61K31/4015 , A61K31/4025 , C07D403/02
CPC分类号： C07D401/04 , C07D207/48 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14
摘要： The invention relates to compounds of formula (I) wherein R1 represents aryl, aralkyl or heteroaryl, R2 is aryl or heteroaryl and R3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
摘要翻译：本发明涉及其中R 1表示芳基，芳烷基或杂芳基，R 2是芳基或杂芳基和R 3'的式（I）化合物，是将芳族，杂芳基或任选取代的氨基甲基与合成式（I）化合物的药物组合物的合成方法，涉及式（I）化合物用于制备用于治疗肿瘤和自身免疫疾病，以及使用式（I）化合物或含有其的药物组合物治疗肿瘤和自身免疫性疾病的方法。

9. 发明授权

US08895499B2 β-hairpin peptidomimetics 有权
标题翻译：＆bgr; -hairpin肽模拟物
公开(公告)号：US08895499B2
公开(公告)日：2014-11-25
申请号：US13814398
申请日：2010-08-05
申请人： Daniel Obrecht , Frank Otto Gombert , John Anthony Robinson , Krystyna Patora-Komisarska
发明人： Daniel Obrecht , Frank Otto Gombert , John Anthony Robinson , Krystyna Patora-Komisarska
IPC分类号： A61K38/00 , C07K7/54 , A01N47/44 , C07K7/64
CPC分类号： C07K7/54 , A01N47/44 , C07K7/64
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-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-）的通式肽模拟物，其对映异构体和药学上可接受的盐与作为在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa1-Xaa14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。

10. 发明授权

US08865656B2 Beta-hairpin peptidomimetics having CXCR4 antagonizing activity 有权
标题翻译：具有CXCR4拮抗活性的β-发夹肽模拟物
公开(公告)号：US08865656B2
公开(公告)日：2014-10-21
申请号：US13319052
申请日：2009-05-07
申请人： Daniel Obrecht , Frank Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
发明人： Daniel Obrecht , Frank Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
IPC分类号： A61K38/00 , C07K7/54 , A61P35/00 , C07K7/08 , C07K7/02
CPC分类号： C07K7/08 , C07K1/061 , C07K7/02
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa1, Xaa2, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa12, Xaa13, Xaa14, Xaa15 and Xaa16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing 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 peptides 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-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物，Cys4之间的二硫键和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa1，Xaa2，Xaa3，Xaa5，Xaa6，Xaa7，Xaa8，Xaa12，Xaa13，Xaa14，Xaa15和Xaa16，具有CXCR4拮抗特性，可用于预防健康个体中的HIV感染，或用于减缓和阻止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员以调节组织修复的试剂。这些肽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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