SI0706513T1 - Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors - Google Patents

Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors

Info

Publication number
SI0706513T1
SI0706513T1 SI9430420T SI9430420T SI0706513T1 SI 0706513 T1 SI0706513 T1 SI 0706513T1 SI 9430420 T SI9430420 T SI 9430420T SI 9430420 T SI9430420 T SI 9430420T SI 0706513 T1 SI0706513 T1 SI 0706513T1
Authority
SI
Slovenia
Prior art keywords
stands
alkoxy
halogen
hydrogen
alkyl
Prior art date
Application number
SI9430420T
Other languages
English (en)
Slovenian (sl)
Inventor
Hermann Amschler
Dieter Flockerzi
Beate Gutterer
Armin Hatzelmann
Christian Schudt
Rolf Beume
Ulrich Kilian
Horst P. O. Wolf
Original Assignee
Altana Pharma Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=4223466&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SI0706513(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Altana Pharma Ag filed Critical Altana Pharma Ag
Publication of SI0706513T1 publication Critical patent/SI0706513T1/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/56Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
SI9430420T 1993-07-02 1994-07-02 Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors SI0706513T1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH199693 1993-07-02
PCT/EP1994/002169 WO1995001338A1 (de) 1993-07-02 1994-07-02 Fluoralkoxy substituierte benzamide und ihre verwendung als zyklisch-nukleotid phosphodiesterase-inhibitoren

Publications (1)

Publication Number Publication Date
SI0706513T1 true SI0706513T1 (en) 2002-10-31

Family

ID=4223466

Family Applications (1)

Application Number Title Priority Date Filing Date
SI9430420T SI0706513T1 (en) 1993-07-02 1994-07-02 Fluoroalkoxy-substituted benzamides and their use as cyclic nucleotide phosphodiesterase inhibitors

Country Status (28)

Country Link
US (1) US5712298A (xx)
EP (1) EP0706513B1 (xx)
JP (1) JP3093271B2 (xx)
KR (1) KR100331255B1 (xx)
CN (1) CN1046939C (xx)
AT (1) ATE217612T1 (xx)
AU (1) AU687087B2 (xx)
CA (1) CA2165192C (xx)
CY (2) CY2389B1 (xx)
CZ (1) CZ290266B6 (xx)
DE (2) DE59410119D1 (xx)
DK (1) DK0706513T3 (xx)
ES (1) ES2176252T3 (xx)
FI (1) FI112864B (xx)
FR (1) FR10C0052I2 (xx)
HK (1) HK1011690A1 (xx)
HU (1) HU220041B (xx)
LU (1) LU91709I2 (xx)
LV (1) LV13074B (xx)
NO (2) NO305598B1 (xx)
NZ (1) NZ271316A (xx)
PL (1) PL178314B1 (xx)
PT (1) PT706513E (xx)
RU (1) RU2137754C1 (xx)
SG (1) SG143011A1 (xx)
SI (1) SI0706513T1 (xx)
SK (1) SK283263B6 (xx)
WO (1) WO1995001338A1 (xx)

Families Citing this family (189)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9311281D0 (en) * 1993-06-01 1993-07-21 Rhone Poulenc Rorer Ltd Novel composition of matter
US5698711A (en) 1991-01-28 1997-12-16 Rhone-Poulenc Rorer Limited Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- or heteroatom-containing linking group
US6096768A (en) * 1992-01-28 2000-08-01 Rhone-Poulenc Rorer Limited Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- or heteroatom-containing linking group
AU6526896A (en) * 1995-07-22 1997-02-18 Rhone-Poulenc Rorer Limited Substituted aromatic compounds and their pharmaceutical use
JP4309475B2 (ja) * 1996-08-19 2009-08-05 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規のベンゾフラン―4―カルボキサミド
JP2001504457A (ja) * 1996-11-01 2001-04-03 ニトロメド インコーポレーテッド ニトロソ化およびニトロシル化ホスホジエステラーゼ阻害剤化合物、組成物及びその使用法
US5958926A (en) 1996-11-01 1999-09-28 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses
USRE37234E1 (en) * 1996-11-01 2001-06-19 Nitromed, Inc. Nitrosated and nitrosylated phosphodiestrase inhibitor compounds, compositions and their uses
US5874437A (en) * 1996-11-01 1999-02-23 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses
US6331543B1 (en) 1996-11-01 2001-12-18 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
KR100640025B1 (ko) 1997-02-17 2006-10-31 알타나 파마 아게 3-(시클로프로필메톡시)-n-(3,5-디클로로-4-피리디닐)-4-(디플루오로메톡시)벤즈아미드 및 폐 계면활성제를 포함하는 성인성호흡 곤란 증후군 및 영아 호흡 장애 증후군을 치료하기 위한 조성물
US6472425B1 (en) 1997-10-31 2002-10-29 Nitromed, Inc. Methods for treating female sexual dysfunctions
US6172118B1 (en) * 1998-04-14 2001-01-09 Smithkline Beecham Corporation Compounds
AU3284000A (en) * 1999-03-10 2000-09-28 Byk Gulden Lomberg Chemische Fabrik Gmbh 3-cyclopropylmethoxy-4-difluoromethoxy-n-(3,5-dichloropyrid- 4-yl)benzamide in the treatment of multiple sclerosis
US6653309B1 (en) 1999-04-26 2003-11-25 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme technical field of the invention
PT1176960E (pt) * 1999-05-04 2005-02-28 Altana Pharma Ag Combinacao sinergica compreendendo roflumilast e um inibidor de pde-3
DK1212089T3 (da) * 1999-08-21 2006-07-24 Altana Pharma Ag Synergistisk kombination af Roflumilast og Salmeterol
JP2003534328A (ja) 2000-05-25 2003-11-18 メルク フロスト カナダ アンド カンパニー フルオロアルコキシ置換ベンズアミドジクロロピリジニルn−オキシドpde4阻害剤
DE10043074A1 (de) * 2000-09-01 2002-03-14 Aventis Cropscience Gmbh Herbizid wirksame Benzoylcyclohexandione
EP1188438A1 (en) * 2000-09-15 2002-03-20 Warner-Lambert Company Pharmaceutical composition for preventing or treating a disease associated with an excess of Il-12 production
EP1199074A1 (en) * 2000-09-15 2002-04-24 Warner-Lambert Company Pharmaceutical composition for preventing or treating a disease associated with an excess of il-12 production
AU2002227123A1 (en) * 2000-11-07 2002-05-21 Merck And Co., Inc. Method of treatment with a combination of a pde4 inhibitor and a leukotriene antagonist
US20100310477A1 (en) * 2000-11-28 2010-12-09 Boehringer Ingelheim Pharma Gmbh & Co. Kg. Pharmaceutical compositions based on anticholingerics and additional active ingredients
US6699890B2 (en) 2000-12-22 2004-03-02 Memory Pharmaceuticals Corp. Phosphodiesterase 4 inhibitors
US7205320B2 (en) * 2001-01-22 2007-04-17 Memory Pharmaceuticals Corp. Phosphodiesterase 4 inhibitors
US7153871B2 (en) 2001-01-22 2006-12-26 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors, including aminoindazole and aminobenzofuran analogs
US6872382B1 (en) 2001-05-21 2005-03-29 Alcon, Inc. Use of selective PDE IV inhibitors to treat dry eye disorders
EP1397359B1 (en) 2001-05-24 2005-08-31 Merck Frosst Canada & Co. 1-biaryl-1,8-napthyridin-4-one phosphodiesterase-4 inhibitors
HUP0401963A3 (en) * 2001-08-09 2006-01-30 Ono Pharmaceutical Co Carboxylic acid derivative compounds and drugs comprising these compounds as the active ingredient
DE10207160A1 (de) * 2002-02-20 2003-12-18 Altana Pharma Ag Darreichungsform enthaltend PDE 4-Hemmer als Wirkstoff
MY140561A (en) 2002-02-20 2009-12-31 Nycomed Gmbh Dosage form containing pde 4 inhibitor as active ingredient
TWI347845B (en) * 2002-03-06 2011-09-01 Nycomed Gmbh Pharmaceutical compositions,combinations,and kits for the treatment of respiratory diseases and use of the same
WO2003094967A2 (en) * 2002-05-07 2003-11-20 Altana Pharma Ag New combination of reversible proton pump inhibitors and airway therapeutics for treating airway disorders
CA2484276A1 (en) * 2002-05-07 2003-11-20 Altana Pharma Ag Combination of a proton pump inhibitor and a respiratory agent for the treatment of respiratory diseases
AU2003232148A1 (en) * 2002-05-16 2003-12-02 Pharmacia Corporation A selective inos inhibitor and a pde inhibitor in combination for the treatment of respiratory diseases
DK2020243T3 (en) * 2002-05-28 2018-11-19 Astrazeneca Ab Pharmaceutical composition which can be applied topically
MXPA05000827A (es) 2002-07-19 2005-08-29 Memory Pharm Corp Inhibidores de fosfodiesterasa 4, incluyendo analogos de anilina y difenilamina n-sustituidos.
CN100381425C (zh) 2002-07-19 2008-04-16 记忆药物公司 作为磷酸二酯酶4抑制剂的6-氨基-1h-吲唑及其药物组合物和用途
AU2003263393A1 (en) * 2002-09-04 2004-03-29 Glenmark Pharmaceuticals Limited New heterocyclic amide compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
AU2003288901A1 (en) * 2002-09-06 2004-03-29 Merck And Co., Inc. Treatment of rheumatoid arthritis by inhibition of pde4
CA2497977A1 (en) 2002-09-20 2004-04-01 Alcon, Inc. Use of cytokine synthesis inhibitors for the treatment of dry eye disorders
US6822114B1 (en) 2002-10-08 2004-11-23 Albemarle Corporation Process for production of fluoroalkoxy-substituted benzamides and their intermediates
AP2021A (en) 2002-10-23 2009-08-03 Glenmark Pharmaceuticals Ltd Novel tricyclic compounds useful for the treatmentof inflammatory and allergic disorders: Process f or their preparation and pharmaceutical compositions containing them
DE60334243D1 (de) * 2002-11-19 2010-10-28 Memory Pharmaceutical Corp Pyridin-n-oxidverbindungen alsphosphodiesterase-4-inhibitoren
DE60321953D1 (de) * 2002-11-27 2008-08-14 Nycomed Gmbh Neue synergistische zusammensetzung enthaltend roflumilast und formoterol
WO2004067006A1 (en) * 2003-01-27 2004-08-12 Pharmacia Corporation Combination of a pde iv inhibitor and a tnf-alpha antagonist
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
EP1606261B1 (en) * 2003-03-10 2009-11-04 Nycomed GmbH Novel process for the preparation of roflumilast
EP1624893A2 (en) 2003-04-01 2006-02-15 Applied Research Systems ARS Holding N.V. Inhibitors of phosphodiesterases in infertility
CN1829711B (zh) 2003-04-11 2010-06-16 格兰马克药品股份有限公司 用于治疗炎性和过敏性病症的新杂环化合物、其制备方法和含有它们的药物组合物
DE10318610A1 (de) * 2003-04-24 2004-11-11 Elbion Ag 7-Azaindole und deren Verwendung als Therapeutika
WO2004098596A1 (en) * 2003-05-12 2004-11-18 Altana Pharma Ag Composition comprising roflumilast and il-1 trap
WO2004098598A1 (en) * 2003-05-12 2004-11-18 Altana Pharma Ag COMPOSITION COMPRISING ROFLUMILAST AND A TNFα ANTAGONIST
WO2004098595A1 (en) * 2003-05-12 2004-11-18 Altana Pharma Ag COMPOSITION COMPRISING ROFLUMILAST AND A TNFα ANTAGONIST
WO2004098597A1 (en) * 2003-05-12 2004-11-18 Altana Pharma Ag Composition comprising roflumilast and shuil-1r ii
EP1628682B1 (en) 2003-05-22 2013-09-25 Takeda GmbH Composition comprising a pde4 inhibitor and a pde5 inhibitor for the treatment of copd
US7923467B2 (en) * 2003-05-30 2011-04-12 Ranbaxy Laboratories, Inc. Substituted pyrrole derivatives and their use as HMG-CO inhibitors
US20050085430A1 (en) * 2003-07-31 2005-04-21 Robinson Cynthia B. Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with a PDE-4 inhibitor for treatment of asthma or chronic obstructive pulmonary disease
US20050026883A1 (en) * 2003-07-31 2005-02-03 Robinson Cynthia B. Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with a PDE-4 inhibitor for treatment of asthma or chronic obstructive pulmonary disease
US20090274676A1 (en) * 2003-07-31 2009-11-05 Robinson Cynthia B Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with a pde-4 inhibitor for treatment of asthma or chronic obstructive pulmonary disease
EP1663999A2 (en) * 2003-08-29 2006-06-07 Ranbaxy Laboratories, Ltd. Inhibitors of phosphodiesterase type-iv
CA2537230A1 (en) * 2003-09-05 2005-03-17 Altana Pharma Ag Use of pde4 inhibitors for the treatment of diabetes mellitus
WO2005026095A1 (en) * 2003-09-12 2005-03-24 Ranbaxy Laboratories Limited Process for the preparation of roflumilast
WO2005046676A1 (en) * 2003-11-12 2005-05-26 University Of South Carolina Treatment or prevention of cardiovascular and respiratory disorders with novel substituted cyclic amp-specific phosphodiesterase inhibitors
EP1685849B1 (en) 2003-11-20 2012-01-25 Astellas Pharma Inc. Pde 4 inhibitors for the treatment of interstitial cystitis
EP1694655A2 (en) * 2003-11-26 2006-08-30 Ranbaxy Laboratories Limited Phosphodiesterase inhibitors
MY141255A (en) * 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
JP4819699B2 (ja) * 2004-02-06 2011-11-24 メダ ファーマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディト ゲゼルシャフト 喘息及びcopdの長期間の治療のための抗コリン作用薬及びグルココルチコイドの組合せ剤
NZ548301A (en) * 2004-02-06 2010-07-30 Meda Pharma Gmbh & Co Kg Combination of anticholinergics and inhibitors of phosphodiesterase type 4 for the treatment of respiratory diseases
EP1720835B1 (en) 2004-02-18 2012-12-12 Nycomed GmbH Novel guanidinyl-substituted hydroxy-6-phenylphenanthridines as effective phosphodiesterase (pde) 4 inhibitors
US20070167496A1 (en) * 2004-02-27 2007-07-19 Attana Pharma Ag Roflumilast and glycopyrronium combination
ES2505473T3 (es) 2004-03-03 2014-10-10 Takeda Gmbh Nuevas hidroxi-6-heteroarilfenantridinas y su uso como inhibidores de la PDE4
WO2006006740A1 (ja) * 2004-07-14 2006-01-19 Japan Tobacco Inc. 3−アミノベンズアミド化合物及びバニロイド受容体1型(vr1)活性阻害剤
JP4018739B2 (ja) 2004-07-15 2007-12-05 日本たばこ産業株式会社 縮合ベンズアミド化合物及びバニロイド受容体1型(vr1)活性阻害剤
US20080009535A1 (en) * 2004-08-30 2008-01-10 Sarala Balachandran Inhibitors of phosphodiesterase type-IV
DE102004046235A1 (de) 2004-09-22 2006-03-30 Altana Pharma Ag Arzneimittelzubereitung
DE102004046236A1 (de) * 2004-09-22 2006-03-30 Altana Pharma Ag Arzneimittelzubereitung
US20080085858A1 (en) * 2004-10-13 2008-04-10 Kyowa Hakko Kogyo Co., Ltd. Pharmaceutical Composition
US20070287689A1 (en) * 2004-10-13 2007-12-13 Kyowa Hakko Kogyo Co., Ltd. Therapeutic And/Or Preventive Agents For Chronic Skin Diseases
CA2583497A1 (en) 2004-10-13 2006-04-20 Glenmark Pharmaceuticals S.A. Process for the preparation of n-(3,5-dichloropyrid-4-yl)-4difluoromethoxy-8-methanesulfonamido-dibenzo[b,d]furan-1-carboxamide
KR101317119B1 (ko) 2004-12-17 2013-10-11 그렌마크 파머수티칼스 에스. 아. 염증성 및 알레르기성 장애의 치료에 유용한 신규한헤테로사이클릭 화합물
SI1831227T1 (sl) 2004-12-17 2013-09-30 Glenmark Pharmaceuticals S.A. Nove heterociklične spojine uporabne za zdravljenje vnetnih in alergijskih motenj
WO2006094640A2 (en) * 2005-03-04 2006-09-14 F.Hoffmann-La Roche Ag Roflumilast and integrin inhibitor combination and method of treatment
WO2006094942A1 (en) * 2005-03-08 2006-09-14 Nycomed Gmbh Roflumilast for the treatment of diabetes mellitus
CN102600144A (zh) 2005-03-08 2012-07-25 奈科明有限责任公司 治疗糖尿病的罗氟司特
JP4991693B2 (ja) * 2005-03-16 2012-08-01 メダ ファーマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト 呼吸器疾患の治療のための抗コリン作用薬及びロイコトリエン受容体アンタゴニストの組み合わせ剤
JP5383183B2 (ja) 2005-03-16 2014-01-08 タケダ ゲゼルシャフト ミット ベシュレンクテル ハフツング ロフルミラストを含有する矯味された剤形
SI2366393T1 (sl) 2005-04-19 2013-12-31 Takeda Gmbh Roflumilast za zdravljenje pljučne hipertenzije
CA2607331A1 (en) * 2005-05-11 2006-11-16 Nycomed Gmbh Combination of the pde4 inhibitor roflumilast and a tetrahydrobiopterin derivative
WO2006132342A1 (ja) * 2005-06-09 2006-12-14 Santen Pharmaceutical Co., Ltd. ロフルミラスト点眼液
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス,インコーポレイティド ムスカリン性受容体調節による神経発生
JP2009512711A (ja) 2005-10-21 2009-03-26 ブレインセルス,インコーポレイティド Pde阻害による神経新生の調節
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
JP2009514851A (ja) * 2005-11-08 2009-04-09 ランバクシー ラボラトリーズ リミテッド (3r,5r)−7−[2−(4−フルオロフェニル)−5−イソプロピル−3−フェニル−4−[(4−ヒドロキシメチルフェニルアミノ)カルボニル]−ピロール−1−イル]−3,5−ジヒドロキシ−ヘプタン酸ヘミカルシウム塩の製法
RU2465915C2 (ru) 2005-12-21 2012-11-10 Меда Фарма Гмбх Унд Ко. Кг Комбинация и фармацевтический препарат для лечения воспалительных заболеваний
US7906508B2 (en) 2005-12-28 2011-03-15 Japan Tobacco Inc. 3,4-dihydrobenzoxazine compounds and inhibitors of vanilloid receptor subtype 1 (VRI) activity
US7863446B2 (en) * 2006-01-19 2011-01-04 Orchid Research Laboratories Limited Heterocycles
AU2007223036A1 (en) * 2006-03-08 2007-09-13 Braincells, Inc. Modulation of neurogenesis by nootropic agents
US20100216734A1 (en) * 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
CL2007000667A1 (es) * 2006-03-14 2008-03-14 Ranbaxi Lab Ltd Composicion farmaceutica que comprende al acido 7-[2-(4-fluorofenil)-5-isopropil-3-fenil-4-[(4-hidroximetilfenilamino)carbonil]pirrol-1-il]-3,5-dihidroxi-heptanoico o una sal y al menos un agente estabilizante; procedimiento de preparacion, util en e
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
US7678808B2 (en) 2006-05-09 2010-03-16 Braincells, Inc. 5 HT receptor mediated neurogenesis
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
MX2008016123A (es) 2006-07-05 2009-01-15 Nycomed Gmbh Combinacion de inhibidores de reductasa hmg-coa con inhibidores de fosfodiesterasa 4 para el tratamiento de enfermedades inflamatorias pulmonares.
RU2009105089A (ru) * 2006-07-14 2010-08-27 Ранбакси Лабораториз Лимитед (In) ПОЛИМОРФНЫЕ ФОРМЫ ГМГ-КоА-РЕДУКТАЗЫ И ИХ ПРИМЕНЕНИЕ
EP2058310A4 (en) 2006-09-01 2010-11-17 Kyorin Seiyaku Kk PYRAZOLOPYRIDINCARBOXYL ACID AMID DERIVATIVE AND THE DERIVATIVELY PHOSPHODIESTERASE (PDE) INHIBITOR
US7998971B2 (en) * 2006-09-08 2011-08-16 Braincells Inc. Combinations containing a 4-acylaminopyridine derivative
EP2066355A2 (en) * 2006-09-19 2009-06-10 Braincells, Inc. Combination comprising a peroxisome proliferator activated receptor agent and a second neurogenic agent for treating a nervous system disorder, increasing neurodifferentiation and increasing neurogenesis
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
WO2008035316A2 (en) * 2006-09-22 2008-03-27 Ranbaxy Laboratories Limited Phosphodiesterase inhibitors
US20080221103A1 (en) * 2007-03-09 2008-09-11 Orchid Research Laboratories Ltd. New heterocyclic compounds
KR100844125B1 (ko) * 2007-03-23 2008-07-04 한국화학연구원 7-(3′,4′-디알콕시페닐)-[1,2,4]트리아졸로[1,5-a]피리미딘 화합물, 이의 제조방법 및 이를 포함하는 천식 및만성폐쇄성 폐질환을 포함한 염증관련 질환, 관절염,아토피 피부염, 암 및 뇌질환의 치료 및 예방을 위한약제학적 조성물
BRPI0811214A2 (pt) 2007-05-16 2014-10-29 Nycomed Gmbh Derivados de pirazolona
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
CA3089569C (en) 2007-06-04 2023-12-05 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
JP5240205B2 (ja) 2008-01-11 2013-07-17 アステラス製薬株式会社 精巣の疼痛又は不快感行動及び頻尿併発モデル動物
CA2715069C (en) 2008-02-01 2016-06-07 Orchid Research Laboratories Limited Novel heterocycles
JP2011522828A (ja) 2008-06-04 2011-08-04 シナジー ファーマシューティカルズ インコーポレイテッド 胃腸障害、炎症、癌、およびその他の障害の治療のために有用なグアニル酸シクラーゼのアゴニスト
US20100029689A1 (en) * 2008-07-02 2010-02-04 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors
EP2321341B1 (en) 2008-07-16 2017-02-22 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
EP2216327A1 (en) * 2009-02-06 2010-08-11 CHIESI FARMACEUTICI S.p.A. Benzoic acid (1-phenyl-2-pyridin-4-yl)ethyl esters as phosphodiesterase inhibitors
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
AU2011253203A1 (en) 2010-05-10 2012-11-22 Gilead Sciences, Inc. Bifunctional quinoline derivatives
US8367829B2 (en) 2010-05-10 2013-02-05 Gilead Sciences, Inc. Bi-functional pyrazolopyridine compounds
TR201909709T4 (tr) * 2010-06-24 2019-07-22 Leo Pharma As Fosfordiesteraz inhibitörleri olarak benzodioksol türevleri.
CN102311382B (zh) * 2010-06-29 2014-05-21 大道隆达(北京)医药科技发展有限公司 罗氟司特的晶态及其制备方法
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
CN102093194B (zh) * 2010-12-24 2014-01-08 江苏先声药物研究有限公司 3-环丙基甲氧基-4-二氟甲氧基苯甲酸的合成方法
CN102617457A (zh) * 2011-01-28 2012-08-01 天津药物研究院 一种制备罗氟司特的新方法
CA2828346C (en) 2011-03-01 2021-01-26 Synergy Pharmaceuticals Inc. Process of preparing guanylate cyclase c agonists
CN102690194B (zh) * 2011-03-24 2014-06-25 上海通远生物科技有限公司 3-环丙基甲氧基-4-二氟甲氧基苯甲酸的制备方法
CN102775345A (zh) * 2011-05-13 2012-11-14 上海特化医药科技有限公司 制备罗氟司特的方法及中间体
CN102276522B (zh) * 2011-06-15 2013-04-17 无锡泓兴生物医药科技有限公司 一种制备罗氟司特的方法及其中间体
CN102336703B (zh) * 2011-07-20 2013-09-25 华润赛科药业有限责任公司 一种制备罗氟司特的方法
CN102351787B (zh) * 2011-08-18 2014-08-13 天津市汉康医药生物技术有限公司 高生物利用度的罗氟司特化合物
WO2013030789A1 (en) 2011-08-30 2013-03-07 Ranbaxy Laboratories Limited Pharmaceutical oral solid dosage form containing a poorly water soluble pde - iv inhibitor
CN102336704B (zh) * 2011-10-19 2013-04-17 丁克 一种制备罗氟司特的方法
KR20140078719A (ko) * 2011-10-21 2014-06-25 키에시 파르마슈티시 엣스. 피. 에이. 포스포디에스테라제 억제제로서 1-페닐-2-피리디닐 알킬 알코올의 유도체
CN102336705B (zh) * 2011-10-28 2013-03-27 成都苑东药业有限公司 一种制备n-(3,5-二氯吡啶-4-基)-3-环丙基甲氧基-4-二氟甲氧基苯甲酰胺的方法
CA2855021A1 (en) 2011-11-09 2013-05-23 Mylan Laboratories Ltd Process for the preparation of roflumilast
WO2013081565A1 (en) 2011-11-21 2013-06-06 Mahmut Bilgic Pharmaceutical compositions comprising roflumilast and terbutaline
WO2013077830A1 (en) 2011-11-25 2013-05-30 Mahmut Bilgic Synergistilly active combinations of roflumilast and carmoterol
WO2013084182A1 (en) 2011-12-08 2013-06-13 Glenmark Pharmaceuticals S.A. Pharmaceutical composition that includes a pde4 enzyme inhibitor and an analgesic agent
CN102603623A (zh) * 2011-12-26 2012-07-25 北京赛林泰医药技术有限公司 制备高纯度罗氟司特的方法
EP2804603A1 (en) 2012-01-10 2014-11-26 President and Fellows of Harvard College Beta-cell replication promoting compounds and methods of their use
WO2013131255A1 (en) 2012-03-07 2013-09-12 Scinopharm (Changshu) Pharmaceutical, Ltd. Preparation method of roflumilast
WO2014012954A1 (en) 2012-07-18 2014-01-23 Takeda Gmbh Treatment of partly controlled or uncontrolled severe asthma
CN103630613B (zh) * 2012-08-21 2015-08-05 北大方正集团有限公司 分离并检测罗氟司特及其中间体的方法
WO2014060464A1 (en) 2012-10-17 2014-04-24 Interquim, S.A. Process for preparing roflumilast
CN110464724A (zh) * 2013-01-28 2019-11-19 理森制药股份公司 通过吸入罗氟司特n-氧化物治疗自身免疫、呼吸和/或炎性病症的方法
JP6307525B2 (ja) 2013-02-04 2018-04-04 グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング 新規の置換縮合ピリミジン化合物
WO2014117947A1 (en) 2013-02-04 2014-08-07 Grünenthal GmbH 4-amino substituted condensed pyrimidine compounds as pde4 inhibitors
US9545446B2 (en) 2013-02-25 2017-01-17 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase and their uses
US9486494B2 (en) 2013-03-15 2016-11-08 Synergy Pharmaceuticals, Inc. Compositions useful for the treatment of gastrointestinal disorders
EP2970384A1 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
TW201512189A (zh) 2013-04-16 2015-04-01 Gruenenthal Chemie 新型被取代之嘧啶縮合化合物
JP6606491B2 (ja) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼcの超高純度アゴニスト、その作成および使用方法
CN103304475A (zh) * 2013-06-13 2013-09-18 湖南千金湘江药业股份有限公司 苯甲酰胺化合物及其制备方法和用途
KR20160042039A (ko) 2013-08-09 2016-04-18 알데릭스, 인코포레이티드 인산염 수송을 억제하기 위한 화합물 및 방법
ES2644367T3 (es) 2013-08-09 2017-11-28 Grünenthal GmbH Nuevos compuestos de pirimidina condensados sustituidos
ES2888074T3 (es) 2013-08-16 2021-12-30 Univ Maastricht Tratamiento del deterioro cognitivo con inhibidor de PDE4
WO2015063669A1 (en) 2013-10-30 2015-05-07 Wockhardt Limited Pharmaceutical compositions comprising combination of roflumilast and acebrophylline or pharmaceutically acceptable salts thereof
SG11201609276RA (en) 2014-05-12 2016-12-29 Glaxosmithkline Ip No 2 Ltd Pharmaceutical compositions comprising danirixin for treating infectious diseases
AR101196A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos
AR101198A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas como inhibidores de pde4b
AR101197A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas
CN104130116B (zh) * 2014-08-18 2015-11-11 朱丽平 一种制备罗氟司特中间体的方法
KR101878621B1 (ko) 2014-10-24 2018-07-13 히사미쓰 세이야꾸 가부시키가이샤 프로드러그
CN104447245B (zh) * 2014-10-29 2017-06-06 成都森科制药有限公司 罗氟司特中间体、中间体制备方法及罗氟司特的制备方法
KR20170034707A (ko) 2015-09-21 2017-03-29 한미약품 주식회사 로플루밀라스트 함유 경구용 고형제제 및 그 제조방법
EP3165224A1 (en) 2015-11-09 2017-05-10 Albert-Ludwigs-Universität Freiburg Use of pde4 inhibitors for the prophylaxis and/or therapy of dyslipoproteinaemia and related disorders
WO2017089347A1 (en) 2015-11-25 2017-06-01 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods and pharmaceutical compositions for the treatment of braf inhibitor resistant melanomas
CN105523954B (zh) * 2016-02-05 2017-07-18 徐江平 3‑环丙甲氧基‑4‑烷氧基苯甲酰胺类磷酸二酯酶4抑制剂
US9895359B1 (en) 2017-06-07 2018-02-20 Arcutis, Inc. Inhibition of crystal growth of roflumilast
US11129818B2 (en) 2017-06-07 2021-09-28 Arcutis Biotherapeutics, Inc. Topical roflumilast formulation having improved delivery and plasma half life
US11534493B2 (en) 2017-09-22 2022-12-27 Arcutis Biotherapeutics, Inc. Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents
CA3079299A1 (en) 2017-10-23 2019-05-02 Boehringer Ingelheim International Gmbh New combination of active agents for the treatment of progressive fibrosing interstitial lung diseases (pf-ild)
KR20210044191A (ko) 2018-06-04 2021-04-22 아큐티스, 인크. 로플루밀라스트 피부 침투 지연 시간의 개선 방법 및 제형
EP3972599A1 (en) 2019-05-21 2022-03-30 Ardelyx, Inc. Combination for lowering serum phosphate in a patient
BR112022015104A2 (pt) 2020-01-31 2022-09-27 Arcutis Biotherapeutics Inc Método para melhorar a distribuição e estender a meia-vida plasmática de uma composição de roflumilaste e uso de uma composição
US20230338345A1 (en) 2020-04-23 2023-10-26 Natural Medicine Institute Of Zhejiang Yangshengtang Co., Ltd. Drug combination and use thereof
CN111777550A (zh) * 2020-06-01 2020-10-16 山东希尔康泰药业有限公司 罗氟司特结晶性粉末原料药生产制备方法
WO2022120213A1 (en) 2020-12-04 2022-06-09 Berk David Reuben Topical roflumilast formulation having antifungal properties
WO2022156727A1 (zh) * 2021-01-21 2022-07-28 浙江养生堂天然药物研究所有限公司 治疗肿瘤的组合物及方法
WO2022169615A1 (en) 2021-02-05 2022-08-11 Arcutis Biotherapeutics, Inc. Roflumilast formulations with an improved pharmacokinetic profile
WO2023129892A1 (en) 2021-12-28 2023-07-06 Arcutis Biotherapeutics, Inc. Topical aerosol foams
WO2023129215A1 (en) 2021-12-28 2023-07-06 Arcutis Biotherapeutics, Inc. Topical roflumilast aerosol foams
US20240108609A1 (en) 2022-09-15 2024-04-04 Arcutis Biotherapeutics, Inc. Pharmaceutical compositions of roflumilast and solvents capable of dissolving high amounts of the drug

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3308239A1 (de) * 1983-03-09 1984-09-13 Basf Ag, 6700 Ludwigshafen N-acyl-anthranilsaeurederivate, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung unerwuenschten pflanzenwuchses
DK159431C (da) * 1984-05-10 1991-03-18 Byk Gulden Lomberg Chem Fab 6-phenyl-3(2h)-pyridazinoner, fremgangsmaade til fremstilling deraf, laegemidler indeholdende disse samt anvendelse af forbindelserne til fremstilling af laegemidler
JPS62158253A (ja) * 1985-12-28 1987-07-14 Kirin Brewery Co Ltd 4−アミノピリジンアミド誘導体
IE71647B1 (en) * 1991-01-28 1997-02-26 Rhone Poulenc Rorer Ltd Benzamide derivatives
US5449676A (en) * 1991-04-26 1995-09-12 Byk Gulden Lomberg Chemische Fabrik Gmbh Pyridazines
GB9212693D0 (en) * 1992-06-15 1992-07-29 Celltech Ltd Chemical compounds
DE69309030T2 (de) * 1992-06-15 1997-09-25 Celltech Therapeutics Ltd Trisubstituierte phenylderivate als selektive phosphodiesterase iv inhibitoren
HUT72656A (en) * 1992-07-28 1996-05-28 Rhone Poulenc Rorer Ltd Inhibitors of c-amp phosphodiesterase and tnf, their preparation pharmaceuticals contg. them and their use

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