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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- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- 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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- A—HUMAN NECESSITIES
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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
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- 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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- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- 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)
Applications Claiming Priority (2)
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| US24938609P | 2009-10-07 | 2009-10-07 | |
| US61/249,386 | 2009-10-07 |
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| KR20120093859A true KR20120093859A (ko) | 2012-08-23 |
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Country Status (15)
Families Citing this family (19)
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| AU2011285928B9 (en) * | 2010-08-03 | 2018-08-02 | B3Ar Therapeutics, Inc. | Combinations of beta - 3 adrenergic receptor agonists and muscarinic receptor antagonists for treating overactive bladder |
| US9522129B2 (en) | 2010-08-03 | 2016-12-20 | Velicept Therapeutics, Inc. | Pharmaceutical Combination |
| US9907767B2 (en) | 2010-08-03 | 2018-03-06 | Velicept Therapeutics, Inc. | Pharmaceutical compositions and the treatment of overactive bladder |
| EP2706997B1 (en) * | 2011-05-10 | 2019-03-27 | TheraVida, Inc. | Combinations of solifenacin and pilocarpine for the treatment of overactive bladder |
| 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 |
| US9809536B2 (en) | 2011-10-27 | 2017-11-07 | Merck Sharp & Dohme Corp. | Process for making beta 3 agonists and intermediates |
| SG11201404776PA (en) * | 2012-02-09 | 2014-09-26 | Altherx Inc | Combination of muscarinic receptor antagonists and beta- 3 adrenoceptor agonists for treating overactive bladder |
| HUE045260T2 (hu) | 2013-03-15 | 2019-12-30 | Merck Sharp & Dohme | Eljárás béta 3 antagonisták és köztitermékeik elõállítására |
| AU2014293141A1 (en) * | 2013-07-23 | 2016-02-18 | Serenity Pharmaceuticals Llc | Methods and compositions comprising desmopressin in combination with a beta-3 adrenergic receptor agonist |
| 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 |
| PT3365321T (pt) | 2015-10-23 | 2024-01-12 | B3Ar Therapeutics Inc | Zwiterião de solabegron e suas utilizações |
| WO2018039159A1 (en) * | 2016-08-22 | 2018-03-01 | Chase Pharmaceuticals Corporation | Muscarinic m2-antagonist combination |
| US12102638B2 (en) | 2017-06-06 | 2024-10-01 | Urovant Sciences Gmbh | Use of vibegron to treat overactive bladder |
| KR20250095747A (ko) * | 2017-06-06 | 2025-06-26 | 유로반트 사이언시즈 게엠베하 | 과민성 방광의 치료를 위한 비베그론의 투약 |
| CN111556753A (zh) * | 2017-12-21 | 2020-08-18 | 杏林制药株式会社 | 用于夜间尿频的治疗剂 |
| BR112021010856A2 (pt) | 2018-12-05 | 2021-11-16 | Urovant Sciences Gmbh | Vibegron para o tratamento de sintomas de bexiga hiperativa |
| 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 |
| TWI295669B (en) * | 2002-10-30 | 2008-04-11 | Theravance Inc | Substituted 4-amino-1-(pyridylmethyl) piperidine and related compounds |
| 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 |
| AU2008233232A1 (en) * | 2007-03-29 | 2008-10-09 | Merck Sharp & Dohme Corp. | 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 US US13/500,574 patent/US20120202819A1/en not_active Abandoned
- 2010-09-27 WO PCT/US2010/050328 patent/WO2011043942A1/en not_active Ceased
- 2010-09-27 EP EP10822429.6A patent/EP2485595A4/en not_active Withdrawn
- 2010-09-27 IN IN2782DEN2012 patent/IN2012DN02782A/en unknown
- 2010-09-27 JP JP2012533204A patent/JP5738871B2/ja active Active
- 2010-09-27 CA CA2774992A patent/CA2774992A1/en not_active Abandoned
- 2010-09-27 KR KR1020127008961A patent/KR20120093859A/ko not_active Withdrawn
- 2010-09-27 NZ NZ599233A patent/NZ599233A/xx not_active IP Right Cessation
- 2010-09-27 RU RU2012118668/13A patent/RU2012118668A/ru not_active Application Discontinuation
- 2010-09-27 CN CN2010800550891A patent/CN102638987A/zh active Pending
- 2010-09-27 MX MX2012004134A patent/MX2012004134A/es not_active Application Discontinuation
- 2010-09-27 AU AU2010303811A patent/AU2010303811B2/en not_active Ceased
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2012
- 2012-03-20 IL IL218756A patent/IL218756A0/en unknown
- 2012-04-05 ZA ZA2012/02520A patent/ZA201202520B/en unknown
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| EP2485595A4 (en) | 2014-03-12 |
| IN2012DN02782A (cg-RX-API-DMAC7.html) | 2015-09-18 |
| ZA201202520B (en) | 2012-12-27 |
| US20120202819A1 (en) | 2012-08-09 |
| BR112012007829A2 (pt) | 2015-09-22 |
| JP2013507363A (ja) | 2013-03-04 |
| RU2012118668A (ru) | 2013-11-20 |
| JP5738871B2 (ja) | 2015-06-24 |
| IL218756A0 (en) | 2012-06-28 |
| CA2774992A1 (en) | 2011-04-14 |
| NZ599233A (en) | 2013-04-26 |
| EP2485595A1 (en) | 2012-08-15 |
| AU2010303811A1 (en) | 2012-04-19 |
| CN102638987A (zh) | 2012-08-15 |
| AU2010303811B2 (en) | 2013-01-24 |
| WO2011043942A1 (en) | 2011-04-14 |
| MX2012004134A (es) | 2012-05-08 |
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