公开(公告)号：US07968547B2

公开(公告)日：2011-06-28

申请号：US12637719

申请日：2009-12-14

Applicant: Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu ,  Susan Ashwell ,  Gregory S. Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis

Inventor： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu ,  Susan Ashwell ,  Gregory S. Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis

IPC: C07D241/02 ,  A61K31/497

CPC classification number: A61K31/425 ,  A61K31/41 ,  A61K31/427 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/535 ,  A61K31/54 ,  C07D211/58 ,  C07D213/74 ,  C07D213/76 ,  C07D233/88 ,  C07D239/32 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/52 ,  C07D241/20 ,  C07D249/06 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/54 ,  C07D257/06 ,  C07D285/06 ,  C07D285/10 ,  C07D333/36 ,  C07D333/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  Y02A50/463 ,  A61K2300/00

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract translation: 公开了结合VLA-4的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。

公开(公告)号：US20100160343A1

公开(公告)日：2010-06-24

申请号：US12637719

申请日：2009-12-14

Applicant: Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Susan Ashwell ,  Gregory S. Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

Inventor： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Susan Ashwell ,  Gregory S. Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

IPC: A61K31/4965 ,  C07D241/20 ,  A61P19/02

CPC classification number: A61K31/425 ,  A61K31/41 ,  A61K31/427 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/50 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K31/535 ,  A61K31/54 ,  C07D211/58 ,  C07D213/74 ,  C07D213/76 ,  C07D233/88 ,  C07D239/32 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D239/52 ,  C07D241/20 ,  C07D249/06 ,  C07D251/18 ,  C07D251/48 ,  C07D251/50 ,  C07D251/52 ,  C07D251/54 ,  C07D257/06 ,  C07D285/06 ,  C07D285/10 ,  C07D333/36 ,  C07D333/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  Y02A50/463 ,  A61K2300/00

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：US07320960B2

公开(公告)日：2008-01-22

申请号：US10316205

申请日：2002-12-11

Applicant: Eugene D. Thorsett ,  Christopher M. Semko ,  Dimitrios Sarantakis ,  Michael A. Pleiss ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Darren B. Dressen ,  Susan Ashwell ,  Reinhardt Bernhard Baudy ,  Louis John Lombardo

Inventor： Eugene D. Thorsett ,  Christopher M. Semko ,  Dimitrios Sarantakis ,  Michael A. Pleiss ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Darren B. Dressen ,  Susan Ashwell ,  Reinhardt Bernhard Baudy ,  Louis John Lombardo

IPC: C07K5/06

CPC classification number: A61K31/397 ,  A61K31/4015 ,  A61K31/404 ,  A61K31/495 ,  A61K31/54 ,  A61K38/00 ,  C07K5/0215 ,  C07K5/06026 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract translation: 公开了结合VLA-4的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。

公开(公告)号：US07291645B2

公开(公告)日：2007-11-06

申请号：US10735499

申请日：2003-12-12

Applicant: Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Susan Ashwell ,  Gregory S. Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

Inventor： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Susan Ashwell ,  Gregory S. Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

IPC: A01N47/10 ,  A61K31/27 ,  A07C261/00 ,  A07C269/00 ,  A07C271/00

CPC classification number: C07D239/42

Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.

Abstract translation: 公开了一系列苯丙氨酸衍生物，含有它们的组合物，其制备方法及其在医药中的应用。

公开(公告)号：US07015216B2

公开(公告)日：2006-03-21

申请号：US09910431

申请日：2001-07-19

Applicant: Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Susan Ashwell ,  Gregory S. Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

Inventor： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett ,  Susan Ashwell ,  Gregory S. Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis ,  Darren B. Dressen ,  Francine S. Grant ,  Christopher Semko ,  Ying-Zi Xu

IPC: C07D213/02 ,  C07D213/30 ,  C07D403/06 ,  A61K31/44 ,  A61P19/02

CPC classification number: C07D213/81 ,  C07D251/46 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12

Abstract: Disclosed are a series of heteroaryl-β-alanine derivatives, compositions containing them, processes for their preparation and their use in medicine.

公开(公告)号：US20050192280A1

公开(公告)日：2005-09-01

申请号：US11107447

申请日：2005-04-14

Applicant: Andrei Konradi ,  Michael Pleiss ,  Eugene Thorsett ,  Susan Ashwell ,  Gregory Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis ,  Darren Dressen ,  Francine Grant ,  Christopher Semko ,  Ying-Zi Xu

Inventor： Andrei Konradi ,  Michael Pleiss ,  Eugene Thorsett ,  Susan Ashwell ,  Gregory Welmaker ,  Anthony Kreft ,  Dimitrios Sarantakis ,  Darren Dressen ,  Francine Grant ,  Christopher Semko ,  Ying-Zi Xu

IPC: A61P29/00 ,  C07D239/48 ,  C07D239/69 ,  C07D285/10 ,  C07D401/12 ,  A61K31/50 ,  A61K31/505 ,  C07D239/02

CPC classification number: C07D239/48 ,  C07D239/69 ,  C07D285/10 ,  C07D401/12

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract translation: 公开了结合VLA-4的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。

公开(公告)号：US06559127B1

公开(公告)日：2003-05-06

申请号：US09127533

申请日：1998-07-31

Applicant: Michael S. Dappen ,  Darren B. Dressen ,  Francine S. Grant ,  Michael A. Pleiss ,  Cynthia Y. Robinson ,  Dimitrios Sarantakis ,  Eugene D. Thorsett

Inventor： Michael S. Dappen ,  Darren B. Dressen ,  Francine S. Grant ,  Michael A. Pleiss ,  Cynthia Y. Robinson ,  Dimitrios Sarantakis ,  Eugene D. Thorsett

IPC: C07K506

CPC classification number: C07K5/06069 ,  A61K38/00 ,  C07K5/06026 ,  C07K5/06121

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：US5185340A

公开(公告)日：1993-02-09

申请号：US925713

申请日：1992-08-04

Applicant: Dimitrios Sarantakis

Inventor： Dimitrios Sarantakis

IPC: A61K31/505

CPC classification number: A61K31/505

Abstract: The compounds of this invention having Angiotensin II receptor binding properties and thus useful in the treatment of hypertension are of the formula: ##STR1## wherein: X.sup.1 =H, lower alkyl, phenyl or naphthyl;X.sup.2 is X.sup.1, perfluoroalkyl or halogen;X.sup.1 and X.sup.2 together are --(CH.sub.2).sub.n --where n is 3-6;X.sup.3 =H, lower alkyl, perfluoroalkyl, perchloroalkyl or halogen;X.sup.4 =5-tetrazolyl, carboxy or cyano;X.sup.5 =H, lower alkoxy or halogen;and the pharmaceutically acceptable salts thereof.

Abstract translation: 具有血管紧张素II受体结合特性并因此可用于治疗高血压的本发明化合物具有下式：其中：X1 = H，低级烷基，苯基或萘基; X2是X1，全氟烷基或卤素; X1和X2一起是 - （CH 2）n - ，其中n是3-6; X3 = H，低级烷基，全氟烷基，全氯烷基或卤素; X4 = 5-四唑基，羧基或氰基; X5 = H，低级烷氧基或卤素; 及其药学上可接受的盐。

公开(公告)号：US4282143A

公开(公告)日：1981-08-04

申请号：US159327

申请日：1980-06-13

Applicant: Dimitrios Sarantakis

Inventor： Dimitrios Sarantakis

IPC: A61K38/00 ,  C07K14/655 ,  C07C103/52 ,  C08L37/00

CPC classification number: C07K14/6555 ,  A61K38/00 ,  Y10S930/26

Abstract: Polypeptides of the formula: ##STR1## in which X.sub.1 is Phe, D-Phe or C.sub.6 H.sub.5 CH.sub.2 CH.sub.2 CO--;X.sub.2 is Phe, Tyr, Trp, Met or Leu;X.sub.3 is Trp or D-Trp;X.sub.4 is Thr, Val, .alpha.-Abu or Phe;andX.sub.5 is Phe, D-Phe or --NHCH.sub.2 CH.sub.2 C.sub.6 H.sub.5 ;the linear precursor intermediates thereof and pharmaceutically acceptable salts and amides thereof are selective inhibitors of growth hormone release without materially altering blood serum levels of glucagon or insulin. In addition, the above-described compounds are active growth hormone suppressants for periods as long as two hours.

Abstract translation: 其中X1是Phe，D-Phe或C6H5CH2CH2CO-的下式的多肽：; X2是Phe，Tyr，Trp，Met或Leu; X3是Trp或D-Trp; X4是Thr，Val，α-Abu或Phe; X5为Phe，D-Phe或-NHCH2CH2C6H5; 其线性前体中间体和其药学上可接受的盐和酰胺是生长激素释放的选择性抑制剂，而不会显着改变胰高血糖素或胰岛素的血清水平。 此外，上述化合物是活性生长激素抑制剂长达两个小时。

公开(公告)号：US4216127A

公开(公告)日：1980-08-05

申请号：US054549

申请日：1979-07-05

Applicant: Dimitrios Sarantakis

Inventor： Dimitrios Sarantakis

IPC: A61K38/00 ,  C07K14/70 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

CPC classification number: C07K14/702 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/28

Abstract: The polypeptides of the formula: ##STR1## in which R.sub.1 is hydrogen, methyl, allyl, cyclopropylmethyl, cyclobutylmethyl or Arg;R.sub.2 is hydrogen or methyl;X.sub.1 is D-Asn or D-Gln;R.sub.3 is hydrogen or methyl;X.sub.2 is D-Asn, D-Gln or D-Cys; andR.sub.4 is the hydroxyl group of the 1-carboxy substituent of the C-terminal amino acid moiety or a lower alkyl ester, amide or lower alkyl amide thereof or the --CH.sub.2 OH reduction product thereof;or a pharmaceutically acceptable salt thereof; exert an analgesic effect in warm blooded animals.

Abstract translation: 下式的多肽：其中R 1是氢，甲基，烯丙基，环丙基甲基，环丁基甲基或者Arg; R2是氢或甲基; X1为D-Asn或D-Gln; R3是氢或甲基; X2是D-Asn，D-Gln或D-Cys; 并且R 4是C末端氨基酸部分的1-羧基取代基或其低级烷基酯，酰胺或低级烷基酰胺或其-CH 2 OH还原产物的羟基; 或其药学上可接受的盐; 在温血动物中发挥镇痛作用。