SK283263B6 - Fluóralkoxysubstituované benzamidy, spôsob ich výroby a ich použitie ako inhibítorov fosfodiesterázy cyklických nukleotidov - Google Patents

Fluóralkoxysubstituované benzamidy, spôsob ich výroby a ich použitie ako inhibítorov fosfodiesterázy cyklických nukleotidov Download PDF

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Publication number
SK283263B6
SK283263B6 SK1617-95A SK161795A SK283263B6 SK 283263 B6 SK283263 B6 SK 283263B6 SK 161795 A SK161795 A SK 161795A SK 283263 B6 SK283263 B6 SK 283263B6
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SK
Slovakia
Prior art keywords
alkyl
pyridyl
halogen
alkoxy
hydrogen
Prior art date
Application number
SK1617-95A
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English (en)
Slovak (sk)
Other versions
SK161795A3 (en
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.)
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Publication date
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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=SK283263(B6) "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 SK161795A3 publication Critical patent/SK161795A3/sk
Publication of SK283263B6 publication Critical patent/SK283263B6/sk

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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
SK1617-95A 1993-07-02 1994-07-02 Fluóralkoxysubstituované benzamidy, spôsob ich výroby a ich použitie ako inhibítorov fosfodiesterázy cyklických nukleotidov SK283263B6 (sk)

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 (2)

Publication Number Publication Date
SK161795A3 SK161795A3 (en) 1996-07-03
SK283263B6 true SK283263B6 (sk) 2003-04-01

Family

ID=4223466

Family Applications (1)

Application Number Title Priority Date Filing Date
SK1617-95A SK283263B6 (sk) 1993-07-02 1994-07-02 Fluóralkoxysubstituované benzamidy, spôsob ich výroby a ich použitie ako inhibítorov fosfodiesterázy cyklických nukleotidov

Country Status (28)

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

Families Citing this family (194)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
GB9311281D0 (en) * 1993-06-01 1993-07-21 Rhone Poulenc Rorer Ltd Novel composition of matter
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
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
US6331543B1 (en) 1996-11-01 2001-12-18 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
US5874437A (en) * 1996-11-01 1999-02-23 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitor compounds, compositions and their uses
EP0941086A4 (en) * 1996-11-01 2000-07-12 Nitromed Inc NITROSIZED AND NITROSYLATED PHOSPHODIESTERASE INHIBITING COMPOUNDS, COMPOSITIONS AND THEIR USE
IL130658A (en) 1997-02-17 2004-07-25 Altana Pharma Ag Preparations for the treatment of ARDS or IRDS containing 3 - (cyclopropylmethoxy) - N - (3, 5 - dichloro - 4 - pyridinyl) - 4 - (difluoromethoxy) benzamide and solvent for the lungs
US6472425B1 (en) 1997-10-31 2002-10-29 Nitromed, Inc. Methods for treating female sexual dysfunctions
US6118017A (en) * 1998-04-14 2000-09-12 Smithkline Beecham Corporation Substituted-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanocyclobutan-1-one
WO2000053182A2 (en) * 1999-03-10 2000-09-14 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
EP1176960B1 (en) * 1999-05-04 2004-09-29 ALTANA Pharma AG Synergistic combination comprising roflumilast and a pde-3 inhibitor
EP2193808A1 (en) * 1999-08-21 2010-06-09 Nycomed GmbH Synergistic combination
CA2407780A1 (en) * 2000-05-25 2001-11-29 Merck Frosst Canada & Co./Merck Frosst Canada & Cie Fluoroalkoxy-substituted benzamide dichloropyridinyl n-oxide pde4 inhibitor
DE10043074A1 (de) * 2000-09-01 2002-03-14 Aventis Cropscience Gmbh Herbizid wirksame Benzoylcyclohexandione
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
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
US6528527B2 (en) * 2000-11-07 2003-03-04 Merck & 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
US7153871B2 (en) * 2001-01-22 2006-12-26 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors, including aminoindazole and aminobenzofuran analogs
US7205320B2 (en) * 2001-01-22 2007-04-17 Memory Pharmaceuticals Corp. Phosphodiesterase 4 inhibitors
US6872382B1 (en) 2001-05-21 2005-03-29 Alcon, Inc. Use of selective PDE IV inhibitors to treat dry eye disorders
DE60205899T2 (de) 2001-05-24 2006-06-29 Merck Frosst Canada & Co, Kirkland 1-biaryl-1,8-naphthyridin-4-one als phosphodieseterase-inhibitoren
CA2457468A1 (en) * 2001-08-09 2003-02-27 Ono Pharmaceutical Co., Ltd. Carboxylic acid derivatives and pharmaceutical agent comprising the same as 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
US20050165041A1 (en) * 2002-05-07 2005-07-28 Altana Pharma Ag Combination for the treatment of airway disorders
CN1652822A (zh) * 2002-05-07 2005-08-10 奥坦纳医药公司 用于治疗气道病症的可逆质子泵抑制剂和气道治疗剂的新组合
US20040087653A1 (en) * 2002-05-16 2004-05-06 Manning Pamela T. Methods for the treatment of respiratory diseases and conditions with a selective iNOS inhibitor and a PDE inhibitor and compositions therefor
EP2020243B1 (en) * 2002-05-28 2018-08-15 AstraZeneca AB Topically applicable pharmaceutical preparation
EP1539697A1 (en) 2002-07-19 2005-06-15 Memory Pharmaceutical Corporation Phosphodiesterase 4 inhibitors, including n-substituted aniline and diphenylamine analogs
NZ537725A (en) * 2002-07-19 2006-08-31 Memory Pharm Corp 6-Amino-1H-indazole and 4-aminobenzofuran compounds as phosphodiesterase 4 inhibitors
WO2004022536A1 (en) * 2002-09-04 2004-03-18 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
US20060019932A1 (en) * 2002-09-06 2006-01-26 Mancini Joseph A Treatment of rheumatoid arthritis by inhibition of pde4
CN1684738A (zh) * 2002-09-20 2005-10-19 爱尔康公司 细胞因子合成抑制剂用于治疗干眼病的用途
US6822114B1 (en) 2002-10-08 2004-11-23 Albemarle Corporation Process for production of fluoroalkoxy-substituted benzamides and their intermediates
CA2503015A1 (en) 2002-10-23 2004-05-06 Glenmark Pharmaceuticals Ltd. Novel tricyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
JP2006508987A (ja) * 2002-11-19 2006-03-16 メモリー・ファーマシューティカルズ・コーポレイション ホスホジエステラーゼ4阻害剤
CN100346777C (zh) * 2002-11-27 2007-11-07 奥坦纳医药公司 包括罗氟斯特和福莫特罗的新的协同组合
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
DE602004023921D1 (de) 2003-03-10 2009-12-17 Nycomed Gmbh Neues verfahren zur herstellung vonroflumilast
BRPI0409229A (pt) 2003-04-01 2006-03-28 Applied Research Systems inibidores das fosfodiesterases na infertilidade
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
WO2004098598A1 (en) * 2003-05-12 2004-11-18 Altana Pharma Ag COMPOSITION COMPRISING ROFLUMILAST AND A TNFα ANTAGONIST
WO2004098596A1 (en) * 2003-05-12 2004-11-18 Altana Pharma Ag Composition comprising roflumilast and il-1 trap
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
JP2006528229A (ja) 2003-05-22 2006-12-14 アルタナ ファルマ アクチエンゲゼルシャフト Pde4阻害剤及びpde5阻害剤を含有する組成物
NZ543741A (en) * 2003-05-30 2009-10-30 Ranbaxy Lab Ltd Substituted pyrrole derivatives and their use as HMG-Co inhibitors
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
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
AU2004268847A1 (en) * 2003-08-29 2005-03-10 Ranbaxy Laboratories Limited Inhibitors of phosphodiesterase type-IV
MXPA06002521A (es) 2003-09-05 2006-06-20 Altana Pharma Ag Uso de inhibidores de pde4 para el tratamiento de diabetes mellitus.
WO2005026095A1 (en) * 2003-09-12 2005-03-24 Ranbaxy Laboratories Limited Process for the preparation of roflumilast
US20070117861A1 (en) * 2003-11-12 2007-05-24 University Of South Carolina Treatment or prevention of cardiovascular and respiratory disorders with novel substituted cyclic-amp specific phosphodiesterase inhibitors
ES2378374T3 (es) 2003-11-20 2012-04-11 Astellas Pharma Inc. Inhibidores de la PDE 4 para el tratamiento de la cistitis intersticial
WO2005051931A2 (en) * 2003-11-26 2005-06-09 Ranbaxy Laboratories Limited Phosphodiesterase inhibitors
MY141255A (en) * 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
SI1713471T1 (sl) * 2004-02-06 2012-07-31 Meda Pharma Gmbh & Co Kg Kombinacija antiholinergikov in inhibitorjev fosfodiesteraze tipa za zdravljenje respiratornih bolezni
WO2005074918A1 (en) * 2004-02-06 2005-08-18 Benzstrasse 1 D-61352 Bad Homburd The combination of anticholinergics and glucocorticoids for the long-term treatment of asthma and copd
CA2556086C (en) 2004-02-18 2014-04-01 Altana Pharma Ag Novel guanidinyl-substituted hydroxy-6-phenylphenenthridines 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
EP1775283A4 (en) * 2004-07-14 2008-12-10 Japan Tobacco Inc 3-AMINOBENZAMIDE COMPOUND AND INHIBITORS OF THE ACTIVITY OF VANILLOID RECEPTOR 1 (VR1)
EP2314585B1 (en) 2004-07-15 2012-09-12 Japan Tobacco, Inc. Condensed benzamide compounds as inhibitors of vanilloid receptor subtype 1 (VR1) activity
US20080009535A1 (en) * 2004-08-30 2008-01-10 Sarala Balachandran Inhibitors of phosphodiesterase type-IV
DE102004046236A1 (de) * 2004-09-22 2006-03-30 Altana Pharma Ag Arzneimittelzubereitung
DE102004046235A1 (de) 2004-09-22 2006-03-30 Altana Pharma Ag Arzneimittelzubereitung
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
WO2006041120A1 (ja) * 2004-10-13 2006-04-20 Kyowa Hakko Kogyo Co., Ltd. 医薬組成物
EP1810692A1 (en) * 2004-10-13 2007-07-25 Kyowa Hakko Kogyo Co., Ltd. Remedies/preventives for chronic skin disease
JP5122974B2 (ja) 2004-12-17 2013-01-16 グレンマーク・ファーマシューティカルズ・エスエー 炎症性障害およびアレルギー障害の治療に有用な新規な複素環式化合物
ES2417491T3 (es) 2004-12-17 2013-08-08 Glenmark Pharmaceuticals S.A. Novedosos compuestos heterocíclicos útiles para el tratamiento de trastornos inflamatorios y alérgicos
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
KR101302838B1 (ko) 2005-03-08 2013-09-03 다케다 게엠베하 진성 당뇨병 치료용 로플루밀라스트
SI1863476T1 (sl) * 2005-03-16 2016-05-31 Meda Pharma Gmbh & Co. Kg Kombinacija antiholinergikov in antagonistov receptorja levkotriena za zdravljenje respiratornih bolezni
EP2258350B1 (en) 2005-03-16 2014-12-24 Takeda GmbH Taste masked dosage form containing roflumilast
WO2006111495A1 (en) 2005-04-19 2006-10-26 Nycomed Gmbh Roflumilast for the treatment of pulmonary hypertension
EA200702358A1 (ru) * 2005-05-11 2008-04-28 Никомед Гмбх Комбинация ингибитора pde4 и производного тетрагидробиоптерина
KR20080029974A (ko) * 2005-06-09 2008-04-03 산텐 세이야꾸 가부시키가이샤 로플루밀라스트 점안액
EP2258357A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP1928437A2 (en) 2005-08-26 2008-06-11 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
AU2006304787A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
CA2625210A1 (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
AU2006329042B2 (en) 2005-12-21 2012-02-02 Meda Pharma Gmbh & Co Kg Combination of anticholinergics, glucocorticoids, beta2-agonists, PDE4 inhibitor and antileukotriene for the treatment of inflammatory diseases
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
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
CA2643199A1 (en) * 2006-03-08 2007-09-13 Braincells, Inc. Modulation of neurogenesis by nootropic agents
TW200744583A (en) * 2006-03-14 2007-12-16 Ranbaxy Lab Ltd Statin stabilizing dosage formulations
US7678808B2 (en) 2006-05-09 2010-03-16 Braincells, Inc. 5 HT receptor mediated neurogenesis
EP2377531A2 (en) 2006-05-09 2011-10-19 Braincells, Inc. Neurogenesis by modulating angiotensin
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
US20100069392A1 (en) 2006-07-05 2010-03-18 Nycomed Gmbh Combination of HMG-COA Reductase Inhibitors with Phosphodiesterase 4 Inhibitors for the Treatment of Inflammatory Pulmonary Disease
CL2007002044A1 (es) * 2006-07-14 2008-06-13 Ranbaxy Lab Ltd Polimorfo cristalino de la sal hemicalcica del acido (3r,5r)-7-[2-(4-fluorofenil)-5-isopropil-3-fenil-4-[(4-hidroximetilfenilamino)carbonil]-pirrol-1-il]-3,5-dihidroxiheptanoico; composicion farmaceutica; y uso para el tratamiento de la diabetes, enf
EP2058310A4 (en) 2006-09-01 2010-11-17 Kyorin Seiyaku Kk PYRAZOLOPYRIDINCARBOXYL ACID AMID DERIVATIVE AND THE DERIVATIVELY PHOSPHODIESTERASE (PDE) INHIBITOR
MX2009002496A (es) * 2006-09-08 2009-07-10 Braincells Inc Combinaciones que contienen un derivado de 4-acilaminopiridina.
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
WO2008036678A2 (en) * 2006-09-19 2008-03-27 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
WO2008035316A2 (en) * 2006-09-22 2008-03-27 Ranbaxy Laboratories Limited Phosphodiesterase inhibitors
WO2008110891A2 (en) * 2007-03-09 2008-09-18 Orchid Research Laboratories Limited, 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
KR101601284B1 (ko) 2007-05-16 2016-03-08 다케다 게엠베하 Pde4 억제제로서 피라졸론 유도체
EP2527360B1 (en) 2007-06-04 2015-10-28 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
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
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
AU2009256157B2 (en) 2008-06-04 2014-12-18 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
WO2010003084A2 (en) * 2008-07-02 2010-01-07 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors
CA2730603C (en) 2008-07-16 2019-09-24 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, 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
WO2011143106A1 (en) 2010-05-10 2011-11-17 Gilead Sciences, Inc. Bi - functional pyrazolopyridine compounds
NZ603136A (en) 2010-05-10 2014-11-28 Gilead Sciences Inc Bifunctional quinoline derivatives
EP3070091B1 (en) 2010-06-24 2019-04-17 Leo Pharma A/S Benzodioxole derivatives as phosphodiesterase inhibitors
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
CA3100941C (en) 2011-03-01 2024-03-05 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
RU2617401C2 (ru) * 2011-10-21 2017-04-25 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Производные 1-фенил 2-пиридинилалкиловых спиртов в качестве ингибиторов фосфодиэстеразы
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
US20150119399A1 (en) 2012-01-10 2015-04-30 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
ES2625417T3 (es) 2012-10-17 2017-07-19 Interquim, S.A. Procedimiento para preparar roflumilast
SG11201505835QA (en) * 2013-01-28 2015-08-28 Incozen Therapeutics Pvt Ltd Methods of treating autoimmune, respiratory and inflammatory disorders by inhalation of roflumilast n-oxide
EP2951161A1 (en) 2013-02-04 2015-12-09 Grünenthal GmbH 4-amino substituted condensed pyrimidine compounds as pde4 inhibitors
CA2899963A1 (en) 2013-02-04 2014-08-07 Grunenthal Gmbh Novel substituted condensed pyrimidine compounds
WO2014131024A2 (en) 2013-02-25 2014-08-28 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
JP2016514671A (ja) 2013-03-15 2016-05-23 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のアゴニストおよびその使用
TW201512189A (zh) 2013-04-16 2015-04-01 Gruenenthal Chemie 新型被取代之嘧啶縮合化合物
KR102272746B1 (ko) 2013-06-05 2021-07-08 보슈 헬스 아일랜드 리미티드 구아닐레이트 사이클라제 c의 초순수 작용제, 및 이의 제조 및 사용 방법
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
KR102456567B1 (ko) 2013-08-09 2022-10-19 알데릭스, 인코포레이티드 인산염 수송을 억제하기 위한 화합물 및 방법
WO2015018534A1 (en) 2013-08-09 2015-02-12 Grünenthal GmbH Novel substituted condensed pyrimidine compounds
US10357486B2 (en) 2013-08-16 2019-07-23 Universiteit Maastricht Treatment of cognitive impairment with PDE4 inhibitor
WO2015063669A1 (en) 2013-10-30 2015-05-07 Wockhardt Limited Pharmaceutical compositions comprising combination of roflumilast and acebrophylline or pharmaceutically acceptable salts thereof
WO2015173701A2 (en) 2014-05-12 2015-11-19 Glaxosmithkline Intellectual Property (No. 2) Limited Pharmaceutical compositions for treating infectious diseases
AR101198A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas como inhibidores de pde4b
AR101196A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos
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
US20210161870A1 (en) 2017-06-07 2021-06-03 Arcutis Biotherapeutics, Inc. Roflumilast formulations with an improved pharmacokinetic profile
US11129818B2 (en) 2017-06-07 2021-09-28 Arcutis Biotherapeutics, Inc. Topical roflumilast formulation having improved delivery and plasma half life
US9895359B1 (en) 2017-06-07 2018-02-20 Arcutis, Inc. Inhibition of crystal growth of roflumilast
US20200155524A1 (en) 2018-11-16 2020-05-21 Arcutis, Inc. Method for reducing side effects from administration of phosphodiesterase-4 inhibitors
US12042487B2 (en) 2018-11-16 2024-07-23 Arcutis Biotherapeutics, Inc. Method for reducing side effects from administration of phosphodiesterase-4 inhibitors
US12011437B1 (en) 2017-06-07 2024-06-18 Arcutis Biotherapeutics, Inc. Roflumilast formulations with an improved pharmacokinetic profile
US11534493B2 (en) 2017-09-22 2022-12-27 Arcutis Biotherapeutics, Inc. Pharmaceutical compositions of roflumilast in aqueous blends of water-miscible, pharmaceutically acceptable solvents
CN111278442B (zh) 2017-10-23 2023-06-06 勃林格殷格翰国际有限公司 用于治疗进行性纤维化间质性肺病(pf-ild)的活性剂的新组合
EP3801461A2 (en) 2018-06-04 2021-04-14 Arcutis, Inc. Method and formulation for improving roflumilast skin penetration lag time
CN114340631A (zh) 2019-05-21 2022-04-12 阿德利克斯股份有限公司 用于降低患者的血清磷酸盐的组合
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
US11707454B2 (en) 2020-12-04 2023-07-25 Arcutis Biotherapeutics, Inc. 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
MX2023009352A (es) 2021-02-10 2023-08-16 Iolyx Therapeutics Inc Metodos para la administracion oftalmica de roflumilast.
IL313866A (en) 2021-12-28 2024-08-01 Arcutis Biotherapeutics Inc Topical roflomilest spray foams
MX2024008196A (es) 2021-12-28 2024-09-25 Arcutis Biotherapeutics Inc Espumas topicas en aerosol.
WO2024058848A1 (en) 2022-09-15 2024-03-21 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
AU1574892A (en) * 1991-04-26 1992-12-21 Byk Gulden Lomberg Chemische Fabrik Gmbh Novel pyridazines
ES2102036T3 (es) * 1992-06-15 1997-07-16 Celltech Therapeutics Ltd Derivados con grupo fenilo trisustituido utilizados como inhibidores selectivos de la fosfodiesterasa iv.
GB9212693D0 (en) * 1992-06-15 1992-07-29 Celltech Ltd Chemical compounds
PT652868E (pt) * 1992-07-28 2005-01-31 Aventis Pharma Ltd Inibidores da fosfodiesterase do amp ciclico

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