KR20120093859A - 베타 ３ 아드레날린 수용체 효능제 및 항무스카린제를 사용하는 조합 요법 - Google Patents
베타 ３ 아드레날린 수용체 효능제 및 항무스카린제를 사용하는 조합 요법 Download PDFInfo
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- KR20120093859A KR20120093859A KR1020127008961A KR20127008961A KR20120093859A KR 20120093859 A KR20120093859 A KR 20120093859A KR 1020127008961 A KR1020127008961 A KR 1020127008961A KR 20127008961 A KR20127008961 A KR 20127008961A KR 20120093859 A KR20120093859 A KR 20120093859A
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- Prior art keywords
- mmol
- methyl
- tert
- phenyl
- butyl
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- 206010020853 Hypertonic bladder Diseases 0.000 claims abstract description 15
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims abstract description 15
- 208000020629 overactive bladder Diseases 0.000 claims abstract description 14
- 238000011282 treatment Methods 0.000 claims abstract description 13
- 239000000556 agonist Substances 0.000 claims description 74
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- 229960005434 oxybutynin Drugs 0.000 claims description 32
- OOGJQPCLVADCPB-HXUWFJFHSA-N tolterodine Chemical compound C1([C@@H](CCN(C(C)C)C(C)C)C=2C(=CC=C(C)C=2)O)=CC=CC=C1 OOGJQPCLVADCPB-HXUWFJFHSA-N 0.000 claims description 31
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- -1 pesoterodine Chemical compound 0.000 claims description 28
- FUZBPOHHSBDTJQ-CFOQQKEYSA-L disodium;5-[(2r)-2-[[(2r)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylate Chemical compound [Na+].[Na+].C1([C@@H](O)CN[C@@H](CC=2C=C3OC(OC3=CC=2)(C([O-])=O)C([O-])=O)C)=CC=CC(Cl)=C1 FUZBPOHHSBDTJQ-CFOQQKEYSA-L 0.000 claims description 10
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- 150000001875 compounds Chemical class 0.000 description 65
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- 125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 24
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- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 20
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 20
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- HMVYYTRDXNKRBQ-UHFFFAOYSA-N 1,3-thiazole-4-carboxylic acid Chemical compound OC(=O)C1=CSC=N1 HMVYYTRDXNKRBQ-UHFFFAOYSA-N 0.000 description 13
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- 230000008569 process Effects 0.000 description 13
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- 230000008602 contraction Effects 0.000 description 12
- 239000003480 eluent Substances 0.000 description 12
- YCWRFIYBUQBHJI-UHFFFAOYSA-N 2-(4-aminophenyl)acetonitrile Chemical group NC1=CC=C(CC#N)C=C1 YCWRFIYBUQBHJI-UHFFFAOYSA-N 0.000 description 11
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- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 10
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 10
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 10
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 description 9
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- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 9
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
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- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/221—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
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| US24938609P | 2009-10-07 | 2009-10-07 | |
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| KR20120093859A true KR20120093859A (ko) | 2012-08-23 |
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| US9907767B2 (en) | 2010-08-03 | 2018-03-06 | Velicept Therapeutics, Inc. | Pharmaceutical compositions and the treatment of overactive bladder |
| US9522129B2 (en) | 2010-08-03 | 2016-12-20 | Velicept Therapeutics, Inc. | Pharmaceutical Combination |
| KR20180008918A (ko) * | 2010-08-03 | 2018-01-24 | 앨씨알엑스, 인크. | 과민성 방광 치료를 위한 베타-3 아드레날린 수용체 작용제 및 무스카린 수용체 길항제의 약학적 배합제 |
| BR112013028755A2 (pt) * | 2011-05-10 | 2017-01-31 | Theravida Inc | combinações de solifenacina e estimulantes salivares para o tratamento de bexiga hiperativa |
| JP6063948B2 (ja) | 2011-10-27 | 2017-01-18 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ベータ３アゴニストおよび中間体を製造するプロセス |
| WO2013062878A1 (en) | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Process for making beta 3 angonists and intermediates |
| KR20150020160A (ko) * | 2012-02-09 | 2015-02-25 | 앨씨알엑스, 인크. | 과민성 방광의 치료를 위한 무스카린 수용체 길항제 및 베타―3 아드레날린 수용체 작용제의 조합물 |
| LT2968269T (lt) | 2013-03-15 | 2019-10-25 | Merck Sharp & Dohme | Beta 3 agonistų ir tarpinių junginių gamybos būdas |
| CN105579057A (zh) * | 2013-07-23 | 2016-05-11 | 阿勒根公司 | 包含与β-3-肾上腺素能受体激动剂组合的去氨加压素的方法和组合物 |
| JP2017535567A (ja) | 2014-11-20 | 2017-11-30 | アラーガン、インコーポレイテッドＡｌｌｅｒｇａｎ，Ｉｎｃｏｒｐｏｒａｔｅｄ | アルファ−アドレナリン受容体拮抗薬と組み合わせたデスモプレシンを含む方法及び組成物 |
| CN107205964A (zh) | 2014-12-03 | 2017-09-26 | 威力塞帕特治疗股份有限公司 | 使用调节释放索拉贝隆用于下尿路症状的组合物和方法 |
| WO2017015349A1 (en) * | 2015-07-20 | 2017-01-26 | Chase Pharmaceuticals Corporation | Muscarinic combination of a selective m2-antagonist and a peripheral non-selective antagonist for treating hypocholinergic disorders |
| WO2017070689A2 (en) | 2015-10-23 | 2017-04-27 | Velicept Therapeutics, Inc. | Solabegron zwitterion and uses thereof |
| WO2018039159A1 (en) * | 2016-08-22 | 2018-03-01 | Chase Pharmaceuticals Corporation | Muscarinic m2-antagonist combination |
| EP4410295A3 (en) | 2017-06-06 | 2024-10-16 | Urovant Sciences GmbH | Use of vibegron to treat overactive bladder |
| KR20200012939A (ko) * | 2017-06-06 | 2020-02-05 | 유로반트 사이언시즈 게엠베하 | 과민성 방광의 치료를 위한 비베그론의 투약 |
| MY201379A (en) * | 2017-12-21 | 2024-02-21 | Kyorin Seiyaku Kk | An agent for treating nocturnal pollakiuria |
| NZ774649A (en) | 2018-12-05 | 2025-07-25 | Urovant Sciences Gmbh | Vibegron for the treatment of overactive bladder symptoms |
| CN115850286B (zh) * | 2022-12-05 | 2023-08-22 | 奥锐特药业(天津)有限公司 | 一种维贝格龙中间体及其制备方法 |
Family Cites Families (8)
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| FR2789076B1 (fr) * | 1999-02-02 | 2001-03-02 | Synthelabo | Derives de alpha-azacyclomethyl quinoleine, leur preparation et leur application en therapeutique |
| GB2356197A (en) * | 1999-10-12 | 2001-05-16 | Merck & Co Inc | Amide derivatives as beta 3 agonists |
| WO2003024483A1 (fr) * | 2001-09-11 | 2003-03-27 | Fujisawa Pharmaceutical Co., Ltd. | Potentialisateur d'effets inhibiteurs sur la frequence des mictions et l'incontinence urinaire |
| TW200800953A (en) * | 2002-10-30 | 2008-01-01 | Theravance Inc | Intermediates for preparing substituted 4-amino-1-(pyridylmethyl) piperidine |
| US20040248979A1 (en) * | 2003-06-03 | 2004-12-09 | Dynogen Pharmaceuticals, Inc. | Method of treating lower urinary tract disorders |
| EP1804778A1 (de) * | 2004-10-18 | 2007-07-11 | Boehringer Ingelheim International GmbH | Verwendung eines beta-3-agonisten zur behandlung von beschwerden der prostata und des unteren urogenitaltrakts |
| WO2008121268A1 (en) * | 2007-03-29 | 2008-10-09 | Merck & Co., Inc. | Combination therapy for the treatment-of lower urinary tract symptoms |
| PE20091825A1 (es) * | 2008-04-04 | 2009-12-04 | Merck & Co Inc | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 |
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2010
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- 2010-09-27 CN CN2010800550891A patent/CN102638987A/zh active Pending
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2012
- 2012-03-20 IL IL218756A patent/IL218756A0/en unknown
- 2012-04-05 ZA ZA2012/02520A patent/ZA201202520B/en unknown
Also Published As
| Publication number | Publication date |
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| EP2485595A1 (en) | 2012-08-15 |
| AU2010303811A1 (en) | 2012-04-19 |
| RU2012118668A (ru) | 2013-11-20 |
| JP2013507363A (ja) | 2013-03-04 |
| CA2774992A1 (en) | 2011-04-14 |
| IN2012DN02782A (enExample) | 2015-09-18 |
| ZA201202520B (en) | 2012-12-27 |
| JP5738871B2 (ja) | 2015-06-24 |
| NZ599233A (en) | 2013-04-26 |
| WO2011043942A1 (en) | 2011-04-14 |
| IL218756A0 (en) | 2012-06-28 |
| BR112012007829A2 (pt) | 2015-09-22 |
| AU2010303811B2 (en) | 2013-01-24 |
| EP2485595A4 (en) | 2014-03-12 |
| CN102638987A (zh) | 2012-08-15 |
| MX2012004134A (es) | 2012-05-08 |
| US20120202819A1 (en) | 2012-08-09 |
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