公开(公告)号：US20030069300A1

公开(公告)日：2003-04-10

申请号：US10229982

申请日：2002-08-28

Applicant: SmithKline Beecham, plc

Inventor： Andrew Parsons ,  Mervyn Thompson ,  Neil Upton ,  John Morris Evans

IPC: A61K031/381

CPC classification number: A61K31/353

Abstract: Benzopyran derivatives and analogs are disclosed as useful for the treatment and/or prophylaxis of degenerative diseases such as Huntingdon's chorea, schizophrenia, neurological deficits associated with AIDS, sleep disorders (including circadian rhythm disorders, insomnia and narcolepsy), tics (e.g. Giles de la Tourette's syndrome), traumatic brain injury, tinnitus, neuralgia, especially trigeminal neuralgia, neuropathic pain, dental pain, cancer pain, inappropriate neuronal activity resulting in neurodysthesias in diseases such as diabetes, MS and motor neurone disease, ataxias, muscular rigidity (spasticity), temporomandibular joint dysfunction.

公开(公告)号：US20020137772A1

公开(公告)日：2002-09-26

申请号：US10099161

申请日：2002-03-13

Applicant: SmithKline Beecham plc

Inventor： Stephen Alistair Smith

IPC: A61K031/4439 ,  A61K031/155

CPC classification number: A61K31/44 ,  A61K2300/00

Abstract: A method for the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof, in a mammal which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitiser and a biguanidine antihyperglycaemic agent, to a mammal in need thereof and a pharmaceutical composition comprising an insulin sensitiser and a biguanide antihyperglycaemic agent.

Abstract translation: 一种用于治疗和/或预防糖尿病的方法，与糖尿病有关的病症及其某些并发症的方法，所述方法包括给予有效的无毒和药学上可接受量的胰岛素敏化剂和双胍类抗高血糖药， 需要其的哺乳动物和包含胰岛素敏化剂和双胍抗高血糖药的药物组合物。

公开(公告)号：US20020128172A1

公开(公告)日：2002-09-12

申请号：US09969408

申请日：2001-10-02

Applicant: SmithKline Beecham PLC

Inventor： Gareth John Sanger ,  Kay Alison Wardle

IPC: A61K031/00

CPC classification number: A61K31/215 ,  A61K31/00 ,  A61K31/245 ,  A61K31/40 ,  A61K31/435 ,  A61K31/44 ,  A61K31/445

Abstract: A compound which acts as an antagonist at 5-HT4 receptors is of potential use in the treatment of conditions associated with bladder hypersensitivity, such as urinary incontinence, which is often associated with irritable bowel syndrome (IBS) and a compound which acts as an agonist at 5-HT4 receptors is of potential use in the treatment of conditions associated with a poorly functioning bladder, such as urinary bladder hypoactivity following prostectomy.

Abstract translation: 作为5-HT4受体拮抗剂的化合物在治疗与膀胱过敏有关的病症中是潜在的，例如尿失禁，其通常与肠易激综合征（IBS）和作为激动剂的化合物相关 在5-HT4受体可能用于治疗与功能低下的膀胱相关的病症，例如前列腺切除术后尿膀胱低反应性。

公开(公告)号：US20020123514A1

公开(公告)日：2002-09-05

申请号：US10091008

申请日：2002-03-05

Applicant: SmithKline Beecham plc

Inventor： Stephen Alistair Smith

IPC: A61K031/4439

CPC classification number: A61K31/702 ,  A61K31/44 ,  A61K31/445 ,  A61K45/06 ,  A61K2300/00

Abstract: A method for the treatment of diabetes mellitus and conditions associated with diabetes mellitus in a mammal, which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitizer and an alpha-glucosidase inhibitor antihyperglycaemic agent, to a mammal in need thereof.

Abstract translation: 一种用于治疗哺乳动物的糖尿病和与糖尿病有关的病症的方法，该方法包括向有需要的哺乳动物施用有效的无毒和可药用量的胰岛素敏化剂和α-葡糖苷酶抑制剂抗高血糖药物 。

公开(公告)号：US20020032220A1

公开(公告)日：2002-03-14

申请号：US09925354

申请日：2001-08-09

Applicant: SmithKline Beecham plc

Inventor： Ahmad Khalaf Al-Deeb Al-Ghazawi ,  Graham Stanley Leonard

IPC: A61K009/48 ,  A61K031/4525

CPC classification number: A61K31/4525 ,  A61K9/4858 ,  A61K9/4866 ,  A61K9/4891

Abstract: Pharmaceutical formulations of paroxetine are provided in which the paroxetine is in solution in a solid, semi-solid or liquid carrier. The solutions are used to fill capsules, or self-supporting solid solutions are shaped into solid dosage forms such as tablets or pellets. Also disclosed are novel liquid formulations in which a solubilising agent is used to solubilise paroxetine in oils and/or lipids, and methods of avoiding other paroxetine forms converting to the hemihydrate, by use of anhydrous or hydrophobic carriers or excipients.

Abstract translation: 提供帕罗西汀的药物制剂，其中帕罗西汀在固体，半固体或液体载体中的溶液中。 溶液用于填充胶囊，或将自支撑固体溶液成形为固体剂型，例如片剂或丸剂。 还公开了新的液体制剂，其中使用增溶剂来溶解油和/或脂质中的帕罗西汀，以及通过使用无水或疏水性载体或赋形剂避免其他帕罗西汀形式转化为半水合物的方法。

公开(公告)号：US20010023252A1

公开(公告)日：2001-09-20

申请号：US09803798

申请日：2001-03-12

Applicant: SmithKline Beecham Plc

Inventor： Ahmad Khalaf Al-Deeb Al-Ghazawi ,  Andrew Simon Craig ,  David Philip Elder ,  Victor Witold Jacewicz ,  David Alan Jones ,  Deirdre O'Keeffe ,  Padma Meneaud Patel ,  Michael Urquhart ,  Neal Ward

IPC: A61K031/4525

CPC classification number: A61K31/452 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2059 ,  A61K31/7012 ,  A61K31/715

Abstract: Invented are pharmaceutical compositions containing paroxetine methanesulfonate.

Abstract translation: 发明的是含有帕罗西汀甲磺酸盐的药物组合物

公开(公告)号：US20040005356A1

公开(公告)日：2004-01-08

申请号：US10615322

申请日：2003-07-08

Applicant: Smithkline Beecham plc

Inventor： Ram Dutta Pathak ,  David George Doughty

IPC: A61K009/20 ,  B27N003/00

CPC classification number: A61K31/445 ,  A61K9/2095

Abstract: Paroxetine which is formulated into tablets using a formulation process in which water is absent.

Abstract translation: 使用其中不存在水的制剂方法将帕曲西汀制成片剂。

公开(公告)号：US20030187030A1

公开(公告)日：2003-10-02

申请号：US10394858

申请日：2003-03-21

Applicant: SmithKline Beecham plc ,  Smith Kline Beecham Corporation

Inventor： Jeffrey Roger Granett ,  Hamish Ross ,  Jaikrishna Patel ,  Robin Kevin John Price ,  Paul Nigel Wray

IPC: A61K031/4439

CPC classification number: A61K31/4439

Abstract: A pharmaceutical composition comprising Compound (I), characterised in that the composition comprises 2 to 12 mg of Compound (I) in a pharmaceutically acceptable form and optionally a pharmaceutically acceptable carrier therefor, the use of such a composition in medicine, processes for the preparation of such a composition and intermediate composition useful in such a process.

Abstract translation: 包含化合物（I）的药物组合物，其特征在于所述组合物包含2至12mg药学上可接受的形式的化合物（I）和任选的药学上可接受的载体，在药物中使用这种组合物，制备方法 的这样的组合物和中间体组合物。

公开(公告)号：US20030114684A1

公开(公告)日：2003-06-19

申请号：US10354865

申请日：2003-01-30

Applicant: SmithKline Beecham plc

Inventor： Michael Fedouloff ,  John Bryce Strachan

IPC: C07D209/18

CPC classification number: C07D209/42

Abstract: A process for the preparation of methyl 2-(3-chloropropoxy)-indole-3-carboxylate, which comprises reacting a 3-chloro-3-carboxylate indole compound with 3-chloropropanol in the presence of an acid having a pKa of from 0 to 2.

公开(公告)号：US20030109553A1

公开(公告)日：2003-06-12

申请号：US10340426

申请日：2003-01-10

Applicant: SmithKline Beecham plc

Inventor： Stephen Alistair Smith

IPC: A61K031/4439 ,  A61K031/426 ,  A61K031/155

CPC classification number: A61K31/44 ,  A61K2300/00

Abstract: A method for the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof, in a mammal which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitiser and a biguanide antihyperglycaemic agent, to a mammal in need thereof and a pharmaceutical composition comprising an insulin sensitiser and a biguanide antihyperglycaemic agent.

Abstract translation: 一种用于治疗和/或预防糖尿病的方法，与糖尿病有关的病症及其某些并发症的方法，所述方法包括向所述哺乳动物施用有效的无毒和药学上可接受量的胰岛素敏化剂和双胍类抗高血糖药， 需要其的哺乳动物和包含胰岛素敏化剂和双胍抗高血糖药的药物组合物。