CN100528835C - 结晶形式的β2肾上腺素能受体激动剂 - Google Patents

结晶形式的β2肾上腺素能受体激动剂 Download PDF

Info

Publication number
CN100528835C
CN100528835C CNB200480014438XA CN200480014438A CN100528835C CN 100528835 C CN100528835 C CN 100528835C CN B200480014438X A CNB200480014438X A CN B200480014438XA CN 200480014438 A CN200480014438 A CN 200480014438A CN 100528835 C CN100528835 C CN 100528835C
Authority
CN
China
Prior art keywords
compound
solution
hydroxyl
ethyl
crystalline
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CNB200480014438XA
Other languages
English (en)
Chinese (zh)
Other versions
CN1795169A (zh
Inventor
I·斯泰贾迪斯
E·约斯特
C·哈伯德
张纬江
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Theravance Biopharma R&D IP LLC
Original Assignee
Shiwan Pharmaceutical
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shiwan Pharmaceutical filed Critical Shiwan Pharmaceutical
Publication of CN1795169A publication Critical patent/CN1795169A/zh
Application granted granted Critical
Publication of CN100528835C publication Critical patent/CN100528835C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/24—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/25—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/43—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
CNB200480014438XA 2003-05-27 2004-05-26 结晶形式的β2肾上腺素能受体激动剂 Expired - Fee Related CN100528835C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US47342303P 2003-05-27 2003-05-27
US60/473,423 2003-05-27

Publications (2)

Publication Number Publication Date
CN1795169A CN1795169A (zh) 2006-06-28
CN100528835C true CN100528835C (zh) 2009-08-19

Family

ID=33490599

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB200480014438XA Expired - Fee Related CN100528835C (zh) 2003-05-27 2004-05-26 结晶形式的β2肾上腺素能受体激动剂

Country Status (19)

Country Link
US (3) US7557247B2 (https=)
EP (1) EP1641744A2 (https=)
JP (1) JP2007500233A (https=)
KR (1) KR20060017616A (https=)
CN (1) CN100528835C (https=)
AR (1) AR045317A1 (https=)
AU (1) AU2004243304A1 (https=)
BR (1) BRPI0410705A (https=)
CA (1) CA2525839A1 (https=)
CO (1) CO5650226A2 (https=)
IS (1) IS8111A (https=)
MA (1) MA27779A1 (https=)
MX (1) MXPA05012678A (https=)
NO (1) NO20056132L (https=)
NZ (1) NZ543355A (https=)
RU (1) RU2005140652A (https=)
TW (1) TW200510277A (https=)
WO (1) WO2004106279A2 (https=)
ZA (1) ZA200510104B (https=)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA73965C2 (en) * 1999-12-08 2005-10-17 Theravance Inc b2 ADRENERGIC RECEPTOR ANTAGONISTS
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
TW200510277A (en) * 2003-05-27 2005-03-16 Theravance Inc Crystalline form of β2-adrenergic receptor agonist
TW200526547A (en) * 2003-09-22 2005-08-16 Theravance Inc Amino-substituted ethylamino β2 adrenergic receptor agonists
TW200531692A (en) * 2004-01-12 2005-10-01 Theravance Inc Aryl aniline derivatives as β2 adrenergic receptor agonists
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
CA2561400A1 (en) * 2004-04-02 2005-10-13 Glaxo Group Limited Chemical process and new crystalline form
WO2006031556A2 (en) * 2004-09-10 2006-03-23 Theravance. Inc. Amidine substituted aryl aniline compounds
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
ES2265276B1 (es) 2005-05-20 2008-02-01 Laboratorios Almirall S.A. Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico.
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
EP2540725A1 (de) 2006-05-04 2013-01-02 Boehringer Ingelheim International GmbH Polymorphe von 1-((4-Methyl-chinazolin-2-yl)methyl)-3-methyl-7-(2-butin-1-yl)-8-(3-(R)-amino-piperidin-1-yl)xanthin
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
US8420286B2 (en) * 2008-03-27 2013-04-16 Xerox Corporation Toner process
US8367294B2 (en) * 2008-03-27 2013-02-05 Xerox Corporation Toner process
PE20091730A1 (es) 2008-04-03 2009-12-10 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
CN102149407A (zh) 2008-09-10 2011-08-10 贝林格尔.英格海姆国际有限公司 治疗糖尿病和相关病症的组合疗法
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
CN102256976A (zh) 2008-12-23 2011-11-23 贝林格尔.英格海姆国际有限公司 有机化合物的盐形式
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
EP2228368A1 (en) 2009-03-12 2010-09-15 Almirall, S.A. Process for manufacturing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one
KR20240090632A (ko) 2009-11-27 2024-06-21 베링거 인겔하임 인터내셔날 게엠베하 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료
CN102946875A (zh) 2010-05-05 2013-02-27 贝林格尔.英格海姆国际有限公司 组合疗法
WO2011161161A1 (en) 2010-06-24 2011-12-29 Boehringer Ingelheim International Gmbh Diabetes therapy
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
US8883800B2 (en) 2011-07-15 2014-11-11 Boehringer Ingelheim International Gmbh Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions
EP2578570A1 (en) 2011-10-07 2013-04-10 Almirall, S.A. Novel process for preparing 5-(2-{[6-(2,2-difluoro-2-phenylethoxy)hexyl]amino}-1(r)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one via novel intermediates of synthesis.
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
EP2641900A1 (en) 2012-03-20 2013-09-25 Almirall, S.A. Novel polymorphic Crystal forms of 5-(2-{[6-(2,2-difluoro-2-phenylethoxy) hexyl]amino}-1-(R)-hydroxyethyl)-8-hydroxyquinolin-2(1h)-one, heminapadisylate as agonist of the ß2 adrenergic receptor.
JP6218811B2 (ja) 2012-05-14 2017-10-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｓｉｒｓ及び／又は敗血症の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体
JP6224084B2 (ja) 2012-05-14 2017-11-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 糸球体上皮細胞関連障害及び／又はネフローゼ症候群の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
EP3110449B1 (en) 2014-02-28 2023-06-28 Boehringer Ingelheim International GmbH Medical use of a dpp-4 inhibitor
CN109310697A (zh) 2016-06-10 2019-02-05 勃林格殷格翰国际有限公司 利格列汀和二甲双胍的组合

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1402702A (zh) * 1999-12-08 2003-03-12 施万制药 β2肾上腺素能受体激动剂

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US676793A (en) * 1899-09-12 1901-06-18 A D Fenwick Machine Co Pasting-machine for collars, &c.
US654117A (en) * 1899-11-29 1900-07-17 Henry B Maddocks Coal-bucket.
US4064125A (en) * 1976-10-29 1977-12-20 E. R. Squibb And Sons, Inc. Substituted amides having antiinflammatory activity
IL63968A (en) * 1980-10-01 1985-10-31 Glaxo Group Ltd Form 2 ranitidine hydrochloride,its preparation and pharmaceutical compositions containing it
HU196775B (en) * 1986-08-05 1989-01-30 Richter Gedeon Vegyeszet Process for production of morfologically unique new modifications of famotidin and medical compositions containing such substances
US5290815A (en) 1989-09-07 1994-03-01 Glaxo Group Limited Treatment of inflammation and allergy
US5872126A (en) 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
GB9713819D0 (en) * 1997-06-30 1997-09-03 Glaxo Group Ltd Method of reducing the systemic effects of compounds
SE9704644D0 (sv) 1997-12-12 1997-12-12 Astra Ab New use
US6350738B1 (en) * 1998-03-06 2002-02-26 Brigham Young University Steroid derived antibiotics
US6541669B1 (en) * 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
US6683115B2 (en) * 1999-06-02 2004-01-27 Theravance, Inc. β2-adrenergic receptor agonists
UA73965C2 (en) 1999-12-08 2005-10-17 Theravance Inc b2 ADRENERGIC RECEPTOR ANTAGONISTS
US6759398B2 (en) * 2000-08-05 2004-07-06 Smithkline Beecham Corporation Anti-inflammatory androstane derivative
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
US7144908B2 (en) 2001-03-08 2006-12-05 Glaxo Group Limited Agonists of beta-adrenoceptors
ES2296923T3 (es) 2001-03-22 2008-05-01 Glaxo Group Limited Derivados formanilidas como agonistas del adrenorreceptor beta2.
UA77656C2 (en) * 2001-04-07 2007-01-15 Glaxo Group Ltd S-fluoromethyl ester of 6-alpha, 9-alpha-difluoro-17-alpha-[(2-furanylcarbonyl)oxy]-11-beta-hydroxy-16- alpha-methyl-3-oxoandrosta-1,4-dien-17-beta-carbothioacid as anti-inflammatory agent
KR20090057477A (ko) 2001-09-14 2009-06-05 글락소 그룹 리미티드 호흡기 질환 치료용 펜에탄올아민 유도체
TWI249515B (en) * 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
JP2005523920A (ja) 2002-04-25 2005-08-11 グラクソ　グループ　リミテッド フェネタノールアミン誘導体
AR040661A1 (es) 2002-07-26 2005-04-13 Theravance Inc Diclorhidrato cristalino de n-{2-[-((r)-2-hidroxi-2-feniletilamino)fenil]etil}-(r)-2hidroxi-2-(3-formamido-4-hidroxifenil)etilamina, agonista del receptor adrenergico beta 2
TW200510277A (en) * 2003-05-27 2005-03-16 Theravance Inc Crystalline form of β2-adrenergic receptor agonist
US8501994B2 (en) * 2007-08-28 2013-08-06 Sunovion Pharmaceuticals Inc. Acetamide stereoisomer

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1402702A (zh) * 1999-12-08 2003-03-12 施万制药 β2肾上腺素能受体激动剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Salt selection for basic drugs. Gould P L.International journal of pharmaceutics,Vol.33 No.1/3. 1986 *

Also Published As

Publication number Publication date
AR045317A1 (es) 2005-10-26
US7772434B2 (en) 2010-08-10
MXPA05012678A (es) 2006-02-22
NO20056132L (no) 2006-01-26
AU2004243304A1 (en) 2004-12-09
WO2004106279A2 (en) 2004-12-09
US20040248985A1 (en) 2004-12-09
RU2005140652A (ru) 2006-04-20
CA2525839A1 (en) 2004-12-09
WO2004106279A3 (en) 2005-02-03
NZ543355A (en) 2009-06-26
MA27779A1 (fr) 2006-02-01
EP1641744A2 (en) 2006-04-05
IS8111A (is) 2005-10-31
US7557247B2 (en) 2009-07-07
JP2007500233A (ja) 2007-01-11
CO5650226A2 (es) 2006-06-30
TW200510277A (en) 2005-03-16
BRPI0410705A (pt) 2006-06-13
CN1795169A (zh) 2006-06-28
US20070155990A1 (en) 2007-07-05
US20100125150A1 (en) 2010-05-20
KR20060017616A (ko) 2006-02-24
ZA200510104B (en) 2006-11-29

Similar Documents

Publication Publication Date Title
CN100528835C (zh) 结晶形式的β2肾上腺素能受体激动剂
US20050075271A1 (en) Crystalline beta2 adrenergic receptor agonist
CN1910137B (zh) 用作β2肾上腺素能受体激动剂的芳基苯胺衍生物
JP4143413B2 (ja) β２−アドレナリン受容体アゴニストとしてのホルムアニリド誘導体
CN100465158C (zh) 氨基取代的乙氨基β2－肾上腺素能受体激动剂
EP1641465B1 (en) Combinations of an aryl aniline beta-2 adrenergic receptor agonist and a corticosteroid
JP2005527618A (ja) アルコキシアリールβ２アドレナリン作動性レセプターアゴニスト
EP1622875B1 (en) Crystalline forms of an arylaniline beta-2 adrenergic receptor agonist
JP2006517939A (ja) 医薬化合物
US7772250B2 (en) Compounds
US20090227547A1 (en) Novel salt form of a Beta2-adrenergic agonist quinolin-2-one derivative

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
ASS Succession or assignment of patent right

Owner name: SCHWAN BIOPHARMA RESEARCH + DEVELOPMENT IP CO., LT

Free format text: FORMER OWNER: SCHWAN PHARMACY

Effective date: 20150316

C41 Transfer of patent application or patent right or utility model
TR01 Transfer of patent right

Effective date of registration: 20150316

Address after: California, USA

Patentee after: THERAVANCE BIOPHARMA R&D IP, LLC

Address before: American California

Patentee before: Shi Wanzhiyao

CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20090819

CF01 Termination of patent right due to non-payment of annual fee