CN103038232B - 单独的和与PDE5抑制剂相组合的sGC刺激剂、sGC活化剂用于治疗系统性硬化症(SSc)的用途 - Google Patents

单独的和与PDE5抑制剂相组合的sGC刺激剂、sGC活化剂用于治疗系统性硬化症(SSc)的用途 Download PDF

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CN103038232B
CN103038232B CN201180036565.XA CN201180036565A CN103038232B CN 103038232 B CN103038232 B CN 103038232B CN 201180036565 A CN201180036565 A CN 201180036565A CN 103038232 B CN103038232 B CN 103038232B
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systemic sclerosis
ssc
compound
fibrosis
treatment
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CN103038232A (zh
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C.希尔特-迪特里希
P.桑德纳
J-P.施塔施
A.克诺尔
G.冯德根费尔德
M.哈恩
M.福尔曼
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Adfolio Pharmaceutical LLC
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Adfolio Pharmaceutical LLC
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CN201180036565.XA 2010-05-26 2011-05-24 单独的和与PDE5抑制剂相组合的sGC刺激剂、sGC活化剂用于治疗系统性硬化症(SSc)的用途 Expired - Fee Related CN103038232B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE102010021637.2 2010-05-26
DE102010021637A DE102010021637A1 (de) 2010-05-26 2010-05-26 Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
EP10170413.8 2010-07-22
EP10170413 2010-07-22
PCT/EP2011/058433 WO2011147810A1 (en) 2010-05-26 2011-05-24 THE USE OF sGC STIMULATORS, sGC ACTIVATORS, ALONE AND COMBINATIONS WITH PDE5 INHIBITORS FOR THE TREATMENT OF SYSTEMIC SCLEROSIS (SSc).

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CN103038232B true CN103038232B (zh) 2016-01-20

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Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2576548T1 (sl) 2010-05-26 2015-11-30 Adverio Pharma Gmbh Uporaba sGC stimulatorjev, sGC aktivatorjev, samih in v kombinacijah s PDE5 inhibitorji za zdravljenje sistemske skleroze
DE102010021637A1 (de) * 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
EP2637659B1 (en) 2010-11-09 2016-05-18 Ironwood Pharmaceuticals, Inc. Sgc stimulators
EP2594270A3 (en) * 2011-11-18 2013-07-31 BIP Patents The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc)
CN102491974B (zh) * 2011-12-12 2013-08-07 南京药石药物研发有限公司 1-(2-氟苄基)-1H-吡唑并[3,4-b]吡啶-3-甲脒盐酸盐的合成方法
CN106117194A (zh) 2011-12-27 2016-11-16 铁木医药有限公司 可用作sgc刺激剂的2‑苄基、3‑(嘧啶‑2‑基)取代的吡唑类
ES2644781T3 (es) * 2012-03-06 2017-11-30 Bayer Intellectual Property Gmbh Azabiciclos sustituidos y su uso
ES2748798T3 (es) * 2012-09-07 2020-03-18 Boehringer Ingelheim Int Alcoxi pirazoles como activadores de la guanilato ciclasa soluble
US9487508B2 (en) 2012-09-19 2016-11-08 Ironwood Pharmaceuticals, Inc. SGC stimulators
CN105102457A (zh) 2013-02-21 2015-11-25 阿德弗里奥药品有限责任公司 {4,6-二氨基-2-[1-(2-氟苄基)-1H-吡唑并[3,4-b]吡啶-3-基]嘧啶-5-基}甲基氨基甲酸甲酯的形式
ES2900815T3 (es) * 2013-03-15 2022-03-18 Scripps Research Inst Compuestos y métodos para inducir la condrogénesis
EP3024455A1 (en) 2013-07-25 2016-06-01 Bayer Pharma Aktiengesellschaft Sgc stimulators or sgc activators and pde5 inhibitors in combination with additional treatment for the therapy of cystic fibrosis
WO2015056663A1 (ja) * 2013-10-15 2015-04-23 トーアエイヨー株式会社 4-アミノメチル安息香酸誘導体
WO2015106268A1 (en) 2014-01-13 2015-07-16 Ironwood Pharmaceuticals, Inc. USE OF sGC STIMULATORS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
JP6557684B2 (ja) 2014-06-13 2019-08-07 インベンティバ 線維性疾患の治療に用いられるppar化合物
TW201625584A (zh) 2014-07-02 2016-07-16 諾華公司 茚滿及吲哚啉衍生物及其作為可溶性鳥苷酸環化酶活化劑之用途
EP3172202B1 (en) 2014-07-22 2020-01-29 Boehringer Ingelheim International GmbH Heterocyclic carboxylic acids as activators of soluble guanylate cyclase
CN107580495A (zh) 2015-05-06 2018-01-12 拜耳制药股份公司 单独和与PDE5抑制剂组合的sGC刺激剂、sGC活化剂用于治疗伴随系统性硬化症(SSc)的指溃疡(DU)的用途
WO2017013010A1 (de) * 2015-07-23 2017-01-26 Bayer Pharma Aktiengesellschaft Stimulatoren und/oder aktivatoren der löslichen guanylatzyklase (sgc) in kombination mit einem inhibitor der neutralen endopeptidase (nep inhibitor) und/oder einem angiotensin aii-antagonisten und ihre verwendung
KR102317700B1 (ko) * 2015-10-07 2021-10-26 아이비바 바이오파마, 인크. 피부 섬유성 장애를 치료하는 조성물 및 방법
AU2016371762A1 (en) 2015-12-14 2018-06-21 Cyclerion Therapeutics, Inc. Use of sGC stimulators for the treatment of gastrointestinal sphincter dysfunction
JP2018537488A (ja) 2015-12-18 2018-12-20 ノバルティス アーゲー インダン誘導体、ならびに可溶性グアニル酸シクラーゼ活性化剤としてのその使用
BR112018015718A2 (pt) 2016-02-01 2019-01-08 Ironwood Pharmaceuticals Inc utilização de estimuladores de sgc para o tratamento de esteato-hepatite não alcoólica (nash)
WO2018111795A2 (en) 2016-12-13 2018-06-21 Ironwood Pharmaceuticals, Inc. Use of sgc stimulators for the treatment of esophageal motility disorders
US20190388407A1 (en) 2017-02-12 2019-12-26 Aiviva Biopharma, Inc. Multikinase inhibitors of vegf and tfg beta and uses thereof
JP7090639B2 (ja) 2017-04-11 2022-06-24 サンシャイン・レイク・ファーマ・カンパニー・リミテッド フッ素置換されたインダゾール化合物及びその使用
CN108690016B (zh) * 2017-04-11 2022-08-12 广东东阳光药业有限公司 吡唑并吡啶类化合物及其用途
EP3574905A1 (en) 2018-05-30 2019-12-04 Adverio Pharma GmbH Method of identifying a subgroup of patients suffering from dcssc which benefits from a treatment with sgc stimulators and sgc activators in a higher degree than a control group
KR20210031931A (ko) 2018-07-11 2021-03-23 사이클리온 테라퓨틱스, 인크. 미토콘드리아 장애의 치료를 위한 sGC 자극제의 용도
AU2019321429B2 (en) 2018-08-15 2022-12-08 Aiviva Biopharma, Inc. Multi-kinase inhibitors of VEGF and TGF beta and uses thereof
CN111638329B (zh) * 2020-06-09 2021-06-01 南方医科大学 一种用于检测布鲁氏菌病elispot检测试剂盒及其应用
EP3925953A1 (en) * 2020-06-16 2021-12-22 Adverio Pharma GmbH Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate
CN115160312B (zh) * 2022-06-29 2023-12-26 常州制药厂有限公司 一种维立西呱关键中间体及其制备方法
KR102831482B1 (ko) * 2022-11-04 2025-07-07 한국타이어앤테크놀로지 주식회사 차량용 타이어의 젖은 노면 제동성능 측정방법
WO2024097316A1 (en) 2022-11-04 2024-05-10 Boehringer Ingelheim International Gmbh Soluble guanylate cyclase activators for treating systemic sclerosis
CN117462685A (zh) * 2023-04-14 2024-01-30 北京悦康科创医药科技股份有限公司 Pde5抑制剂或其组合物在制备用于治疗泌尿系统疾病药物中的用途

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998016223A1 (de) * 1996-10-14 1998-04-23 Bayer Aktiengesellschaft Verwendung von 1-benzyl-3-(substituiertes-hetaryl)-kondensierten pyrazol-derivaten zur belandlung von speziellen erkrankungen des herz-kreislaufsystems und des zentralnervensystems
WO2000002851A1 (en) * 1998-07-08 2000-01-20 Aventis Pharma Deutschland Gmbh Sulfur substituted sulfonylaminocarboxylic acid n-arylamides, their preparation, their use and pharmaceutical preparations comprising them
WO2000006569A1 (de) * 1998-07-29 2000-02-10 Bayer Aktiengesellschaft Mit sechsgliedrigen heterocyclischen ringen kondensierte substituierte pyrazolderivate
DE19943635A1 (de) * 1999-09-13 2001-03-15 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
WO2002042301A1 (de) * 2000-11-22 2002-05-30 Bayer Aktiengesellschaft Neue pyridin-substituierte pyrazolopyridinderivate
WO2003095451A1 (de) * 2002-05-08 2003-11-20 Bayer Healthcare Ag Carbamat-substituierte pyrazolopyridine
WO2009032249A1 (en) * 2007-09-06 2009-03-12 Merck & Co., Inc. Soluble guanylate cyclase activators
WO2009068652A1 (en) * 2007-11-30 2009-06-04 Smithkline Beecham Corporation 2, 6-disubstituted pyridines and 2, 4-disubstituted pyrimidines as soluble guanylate cyclase activators
WO2009071504A1 (en) * 2007-12-03 2009-06-11 Smithkline Beecham Corporation 2,6-disubstituted pyridines as soluble guanylate cyclase activators
WO2009123316A1 (ja) * 2008-04-04 2009-10-08 武田薬品工業株式会社 複素環誘導体及びその用途

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5380945A (en) 1989-06-21 1995-01-10 Abbott Laboratories Guanidino compounds as regulators of nitric oxide synthase
US6331543B1 (en) 1996-11-01 2001-12-18 Nitromed, Inc. Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
DE19834047A1 (de) 1998-07-29 2000-02-03 Bayer Ag Substituierte Pyrazolderivate
DE19943636A1 (de) 1999-09-13 2001-03-15 Bayer Ag Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE19943634A1 (de) 1999-09-13 2001-04-12 Bayer Ag Neuartige Dicarbonsäurederivate mit pharmazeutischen Eigenschaften
US6538023B1 (en) 2000-09-15 2003-03-25 Tsuyoshi Ohnishi Therapeutic uses of green tea polyphenols for sickle cell disease
DE10054278A1 (de) * 2000-11-02 2002-05-08 Bayer Ag Verwendung von Stimulatoren der löslichen Guanylatcyclase zur Behandlung von Osteoporose
EP1355645A4 (en) * 2000-12-29 2005-02-23 Alteon Inc METHOD FOR THE TREATMENT OF FIBROUS OR OTHER IIIC INDICATIONS
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
DE10110749A1 (de) 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
GB0202254D0 (en) 2002-01-31 2002-03-20 Pfizer Ltd Prevention of scarring
US20050267032A1 (en) 2004-05-21 2005-12-01 Icagen, Inc. Sulfone-containing prodrugs
DE102004038328A1 (de) * 2004-08-06 2006-03-16 Bayer Healthcare Ag Neue Verwendungen von 2-Phenyl-substituierten Imidazotriazinon-Derivaten
DE102005016345A1 (de) 2005-04-09 2006-10-12 Bayer Healthcare Ag Neue Verwendung von 2-Phenyl-substituierten Imidazotriazinon-Derivaten
DE102005047945A1 (de) * 2005-07-16 2007-01-18 Bayer Healthcare Ag Verwendung von Aktivatoren der löslichen Guanylatzyklase zur Behandlung von Raynaud Phänomenen
BRPI0614001A2 (pt) 2005-07-18 2011-03-01 Bayer Healthcare Ag uso de ativadores e estimuladores de guanilato ciclase solúvel para a prevenção ou tratamento de distúrbios renais
WO2008138483A1 (en) 2007-05-12 2008-11-20 Bayer Schering Pharma Aktiengesellschaft sGC STIMULATORS, sGC ACTIVATORS AND COMBINATIONS FOR THE TREATMENT OF UROLOGICAL DISORDERS
DE102007026392A1 (de) 2007-06-06 2008-12-11 Bayer Healthcare Ag Lösungen für die Perfusion und Konservierung von Organen und Geweben
WO2009143018A2 (en) * 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US8633318B2 (en) 2008-09-16 2014-01-21 Proximagen Ltd Compounds for treatment or prevention of inflammation, an inflammatory disease, or an immune or an autoimmune disorder
AU2009322836B2 (en) 2008-11-25 2013-04-04 Merck Sharp & Dohme Corp. Soluble guanylate cyclase activators
EP2387404B1 (en) 2009-01-17 2014-06-25 Bayer Intellectual Property GmbH Sgc stimulators and activators in combination with pde5 inhbitors for the treatment of erectile dysfunction
DK2421519T3 (en) 2009-04-23 2017-02-06 Univ Zuerich NMDA RECEPTOR BLOCKERS FOR THE TREATMENT OF SEAL CELL ANAEMS
AU2010330813B2 (en) * 2009-12-18 2016-04-28 Exodos Life Sciences Limited Partnership Methods and compositions for treating peripheral vascular disease
SI2531187T1 (sl) 2010-02-05 2016-01-29 Adverio Pharma Gmbh Stimulatorji sGC ali aktivatorji sGC sami in v kombinaciji z inhibitorji PDE5 za zdravljenje cistične fibroze
SI2576548T1 (sl) 2010-05-26 2015-11-30 Adverio Pharma Gmbh Uporaba sGC stimulatorjev, sGC aktivatorjev, samih in v kombinacijah s PDE5 inhibitorji za zdravljenje sistemske skleroze

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998016223A1 (de) * 1996-10-14 1998-04-23 Bayer Aktiengesellschaft Verwendung von 1-benzyl-3-(substituiertes-hetaryl)-kondensierten pyrazol-derivaten zur belandlung von speziellen erkrankungen des herz-kreislaufsystems und des zentralnervensystems
WO2000002851A1 (en) * 1998-07-08 2000-01-20 Aventis Pharma Deutschland Gmbh Sulfur substituted sulfonylaminocarboxylic acid n-arylamides, their preparation, their use and pharmaceutical preparations comprising them
WO2000006569A1 (de) * 1998-07-29 2000-02-10 Bayer Aktiengesellschaft Mit sechsgliedrigen heterocyclischen ringen kondensierte substituierte pyrazolderivate
DE19943635A1 (de) * 1999-09-13 2001-03-15 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
WO2001019780A3 (de) * 1999-09-13 2001-09-07 Bayer Ag Neuartige aminodicarbonsäurederivate mit pharmazeutischen eigenschaften
WO2002042301A1 (de) * 2000-11-22 2002-05-30 Bayer Aktiengesellschaft Neue pyridin-substituierte pyrazolopyridinderivate
WO2003095451A1 (de) * 2002-05-08 2003-11-20 Bayer Healthcare Ag Carbamat-substituierte pyrazolopyridine
WO2009032249A1 (en) * 2007-09-06 2009-03-12 Merck & Co., Inc. Soluble guanylate cyclase activators
WO2009068652A1 (en) * 2007-11-30 2009-06-04 Smithkline Beecham Corporation 2, 6-disubstituted pyridines and 2, 4-disubstituted pyrimidines as soluble guanylate cyclase activators
WO2009071504A1 (en) * 2007-12-03 2009-06-11 Smithkline Beecham Corporation 2,6-disubstituted pyridines as soluble guanylate cyclase activators
WO2009123316A1 (ja) * 2008-04-04 2009-10-08 武田薬品工業株式会社 複素環誘導体及びその用途

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