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    Lipase Variants for Pharmaceutical Use
    1.
    发明申请
    Lipase Variants for Pharmaceutical Use 有权
    药用脂肪酶变体

    公开(公告)号：US20100034797A1

    公开(公告)日：2010-02-11

    申请号：US12519868

    申请日：2007-12-12

    申请人： Allan Svendsen ,  Michael Skjoet ,  Deborah Yaver ,  Lars Lehman Hylling Christensen ,  Signe Eskildsen Larsen ,  Nina Lundin ,  Michael Lamsa ,  Peter Colin Gregory

    发明人： Allan Svendsen ,  Michael Skjoet ,  Deborah Yaver ,  Lars Lehman Hylling Christensen ,  Signe Eskildsen Larsen ,  Nina Lundin ,  Michael Lamsa ,  Peter Colin Gregory

    IPC分类号： A61K38/54 ,  C12N9/20 ,  C12Q1/34 ,  A61K38/46

    CPC分类号： A61K38/465 ,  A61K38/47 ,  A61K38/48 ,  C12N9/20

    摘要： The pharmaceutical use of lipases related to the Thermomyces lanuginosus (Humicola lanuginosa) lipase comprising amino acids 1-269 of SEQ ID NO: 2, optionally in combination with a protease and/or an amylase. Examples of medical indications are: Treatment of digestive disorders, pancreatic exocrine insufficiency (PEI), pancreatitis, cystic fibrosis, diabetes type I, and/or diabetes type II. The lipases of the invention have, e.g., an improved digestion performance in vitro, an improved activity at a pH in the neutral range, an improved stability at low pH, an are stable against protease-degradation, and/or are stable in the presence of pepsin and bile salts. The invention also relates to methods of determining digestion performance in vitro of lipases, as well as to certain novel variants of the lipase of T. lanuginosus.

    摘要翻译： 与包含SEQ ID NO：2的氨基酸1-269的Thermomyces lanuginosus（Humicola lanuginosa）脂肪酶相关的脂肪酶的药物用途，任选地与蛋白酶和/或淀粉酶组合。 医学适应症的例子有：消化系统疾病，胰腺外分泌功能不全（PEI），胰腺炎，囊性纤维化，I型糖尿病和/或II型糖尿病的治疗。 本发明的脂肪酶具有例如体外改进的消化性能，在中性范围内的pH值改善的活性，在低pH下的改进的稳定性，对蛋白酶降解是稳定的，和/或在存在时是稳定的 的胃蛋白酶和胆汁盐。 本发明还涉及确定脂肪酶的体外消化性能的方法以及T.lanuginosus的脂肪酶的某些新颖变体。

    Lipases for Pharmaceutical Use
    2.
    发明申请
    Lipases for Pharmaceutical Use 审中-公开
    药物用脂肪酶

    公开(公告)号：US20090047266A1

    公开(公告)日：2009-02-19

    申请号：US11917584

    申请日：2006-06-16

    申请人： Allan Svendsen ,  Peter Colin Gregory ,  Kim Borch

    发明人： Allan Svendsen ,  Peter Colin Gregory ,  Kim Borch

    IPC分类号： A61K38/54 ,  A61K38/46 ,  A61P3/10 ,  A61P11/00 ,  A61P1/00

    CPC分类号： C12N9/20

    摘要： The pharmaceutical use of lipases related to a variant of the Thermomyces lanuginosus (Humicola lanuginosa) lipase comprising amino acids 1-269 of SEQ ID NO: 1, optionally in combination with a protease and/or an amylase. Examples of medical indications are: Treatment of digestive disorders, pancreatic exocrine insufficiency (PEI), pancreatitis, cystic fibrosis, diabetes type I, and/or diabetes type II. The lipases of the invention have an improved efficacy in vivo, are stable against protease-degradation, and/or are stable in the presence of bile salts.

    摘要翻译： 与包含SEQ ID NO：1的氨基酸1-269的Thermomyces lanuginosus（Humicola lanuginosa）脂肪酶的变体相关的脂肪酶的药物用途，任选地与蛋白酶和/或淀粉酶组合。 医学适应症的例子有：消化系统疾病，胰腺外分泌功能不全（PEI），胰腺炎，囊性纤维化，I型糖尿病和/或II型糖尿病的治疗。 本发明的脂肪酶在体内具有改善的功效，对蛋白酶降解是稳定的，和/或在胆汁盐存在下是稳定的。

    NOVEL MEDICAL USES OF 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1- ANTAGONISTIC ACTIVITY
    4.
    发明申请
    NOVEL MEDICAL USES OF 4,5-DIHYDRO-1H-PYRAZOLE DERIVATIVES HAVING CB1- ANTAGONISTIC ACTIVITY 审中-公开
    具有CB1-拮抗活性的4,5-二氢-1H-吡唑衍生物的新医学用途

    公开(公告)号：US20050239859A2

    公开(公告)日：2005-10-27

    申请号：US10929377

    申请日：2004-08-31

    申请人： Jochen Antel ,  Gunter Krause ,  Josephus Lange ,  Cornelis Kruse ,  Peter-Colin Gregory ,  Cathaline Den Besten

    发明人： Jochen Antel ,  Gunter Krause ,  Josephus Lange ,  Cornelis Kruse ,  Peter-Colin Gregory ,  Cathaline Den Besten

    IPC分类号： A61K31/415

    CPC分类号： A61K31/415

    摘要： Abstract of the DisclosureThe present invention relates to a novel medical use of 4,5-dihydro-1H-pyrazole compounds which are potent antagonists of the cannabis CB1-receptor. Said compounds are particularly suitable in the manufacture of medicaments for the treatment and/or prophylaxis of CB1 receptor related diseases in juvenile patients and/or for the treatment and/or prophylaxis of drug induced obesity in juvenile as well as in adolescent patients. The compounds have the general formula (I) wherein the group Bb represents sulfonyl or carbonyl, and the substituents R, R1, R2 and R3, and the group Aa are defined as shown in the description.

    摘要翻译： 本发明摘要本发明涉及作为大麻CB 1受体的有效拮抗剂的4,5-二氢-1H-吡唑化合物的新型医疗用途。 所述化合物特别适用于制备用于治疗和/或预防少年患者中CB 1受体相关疾病的药物和/或用于治疗和/或预防未成年人药物诱导的肥胖的药物 就像青少年患者一样。 化合物具有通式（I），其中基团Bb表示磺酰基或羰基，取代基R 1，R 1，R 2和R 3， SUB>，并且组Aa如说明书所示定义。

    Pharmaceutical compositions comprising CB1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions
    7.
    发明授权
    Pharmaceutical compositions comprising CB1 cannabinoid receptor antagonists and potassium channel openers for the treatment of obesity and related conditions 有权
    包含CB1大麻素受体拮抗剂和用于治疗肥胖症和相关病症的钾通道开放剂的药物组合物

    公开(公告)号：US08058264B2

    公开(公告)日：2011-11-15

    申请号：US11257056

    申请日：2005-10-25

    申请人： Michael Firnges ,  Peter-Colin Gregory ,  Jochen Antel ,  Josephus Hubertus Maria Lange ,  Harald Waldeck

    发明人： Michael Firnges ,  Peter-Colin Gregory ,  Jochen Antel ,  Josephus Hubertus Maria Lange ,  Harald Waldeck

    IPC分类号： A01N33/26 ,  A61K31/535

    CPC分类号： A61K31/00 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4152 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/655 ,  A61K45/06 ,  G01N33/6872 ,  G01N33/948 ,  G01N2500/00 ,  G01N2800/042 ,  G01N2800/044 ,  A61K2300/00

    摘要： Described is a novel combination therapy for diabetes mellitus type I and/or for obesity and its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, by administering a combination of at least one KATP channel opener as a first active agent and at least one CB1 cannabinoid receptor antagonist as a second active agent. The invention is further directed to such novel combination therapy wherein a dually acting compound with combined KATP channel opening and CB1 antagonistic properties is used. The invention also relates to novel pharmaceutical compositions comprising KATP channel openers and CB1 antagonists and the use of said pharmaceutical compositions in the treatment, delayed progression, delayed onset of and/or inhibition of diabetes mellitus type 1, and the prophylaxis and treatment, of obesity as well as the prophylaxis, treatment, delayed onset and/or inhbition of its concomitant and/or secondary diseases or conditions, in particular the metabolic syndrome and/or syndrome X, and/or diabetes mellitus type II, in mammals and humans. The invention is further directed to such novel pharmaceutical compositions comprising a dually acting compound with combined KATP channel opening and CB1 antagonistic properties.

    摘要翻译： 描述了通过施用组合来描述I型糖尿病和/或用于肥胖及其伴随和/或继发疾病或病症，特别是代谢综合征和/或综合征X和/或II型糖尿病的新型联合治疗 的至少一种KATP通道开放剂作为第一活性剂和至少一种CB1大麻素受体拮抗剂作为第二活性剂。 本发明进一步涉及这种新型联合治疗，其中使用具有组合的KATP通道开放和CB1拮抗性质的双作用化合物。 本发明还涉及包含KATP通道开放剂和CB1拮抗剂的新型药物组合物，以及所述药物组合物在治疗，延迟进展，延迟发作和/或抑制1型糖尿病以及预防和治疗肥胖症中的用途 以及其伴随和/或继发疾病或病症，特别是哺乳动物和人类的代谢综合征和/或综合征X和/或II型糖尿病的预防，治疗，延迟发作和/或吸收。 本发明还涉及这种新型药物组合物，其包含具有组合的KATP通道开口和CB1拮抗性质的双作用化合物。

    Proteases for Pharmaceutical Use
    8.
    发明申请
    Proteases for Pharmaceutical Use 审中-公开
    药用蛋白酶

    公开(公告)号：US20110110910A1

    公开(公告)日：2011-05-12

    申请号：US13009078

    申请日：2011-01-19

    申请人： Allan Svendsen ,  Claus Crone Fuglsang ,  Peter Colin Gregory

    发明人： Allan Svendsen ,  Claus Crone Fuglsang ,  Peter Colin Gregory

    IPC分类号： A61K38/54 ,  C12N9/56 ,  A61K38/48 ,  A61P1/00 ,  A61P3/10 ,  A61P3/00 ,  A61P29/00

    CPC分类号： C12N9/54

    摘要： The pharmaceutical use of proteases related to amino acids 1-274 of SEQ ID NO: 2, the serine protease derived from Bacillus licheniformis, which is also designated subtilisin Carlsberg, optionally in combination with a lipase and/or an amylase. Examples of medical indications are: Treatment of digestive disorders, pancreatic exocrine insufficiency (PEI), pancreatitis, cystic fibrosis, diabetes type I, and/or diabetes type II.

    摘要翻译： 与SEQ ID NO：2的氨基酸1-274相关的蛋白酶的药物用途，来自地衣芽孢杆菌的丝氨酸蛋白酶，其也被指定为枯草杆菌蛋白酶卡尔斯伯格，任选与脂肪酶和/或淀粉酶组合。 医学适应症的例子有：消化系统疾病，胰腺外分泌功能不全（PEI），胰腺炎，囊性纤维化，I型糖尿病和/或II型糖尿病的治疗。