ECSP034710A - Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4 - Google Patents

Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4

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Publication number
ECSP034710A
ECSP034710A EC2003004710A ECSP034710A ECSP034710A EC SP034710 A ECSP034710 A EC SP034710A EC 2003004710 A EC2003004710 A EC 2003004710A EC SP034710 A ECSP034710 A EC SP034710A EC SP034710 A ECSP034710 A EC SP034710A
Authority
EC
Ecuador
Prior art keywords
optionally
carbon atom
alkyl
replaced
ring system
Prior art date
Application number
EC2003004710A
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English (en)
Inventor
Thomas Victor Magee
Anthony Marfat
Robert James Chambers
Original Assignee
Pfizer Prod Inc
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Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of ECSP034710A publication Critical patent/ECSP034710A/es

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    • C07D213/02—Heterocyclic 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
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    • C07D213/60—Heterocyclic 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
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  • Diabetes (AREA)
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Abstract

Compuestos de utilidad como inhibidores de PDE4 en el tratamiento de enfermedades reguladas por la activación y desgranulación de eosinófilos, especialmente asma, bronquitis crónica, y enfermedad pulmonar obstructiva crónica de fórmula: (gráfico). Donde j es 0 ó 1 con la condición de que cuando j es 0, n debe ser 2; k es 0 ó 1; m es 0, 1,, ó 2; n es 1 ó 2; W1 es -O-; o -S(=O)t-, donde t es 0,1 ó 2; o -N(R3)-; W2 es -O-CRARB-, o está ausente; y es =C(R1a)- o [N (O)k] -donde k es 0 ó 1; RA y RB son -H; -F; -CF3; alquilo C1-C4; cicloalqulo C3-C7; fenilo; 0 bencilo sustituido con 0 a 3 sustituyentes R10; o RA y RB se toman conjuntamente, pero únicamente en el caso en que m es 1, para formar un resto espiro; Re y RD tienen el mismo significado que RA y RB pero uno de ellos debe ser -H, R1 y R2 son -H; -F; -CI; -CH; -NO2; -alquilo C1-C4; - alquinilo C2-C4; -alquilo (C1-C3) fluorado; -OR16; y -C(=0)NR22a R22b; R3 es -H; -alquilo C1-C3; fenilo; bencilo; o- OR16; R4, R5 y R6 además de otros significados pueden tomarse conjuntamente para formar, por ejemplo Q1 es un sistema de anillos de carbono saturados o insaturados que es un monociclo de 3 a 7 miembros, o que es un policiclo condensado de 7 a 12 miembros; con la condición de que Q1 no es un resto biarilo discontinuo o restringido como se define en Q2; donde opcionalmente un átomo de carbono puede reemplazarse por un heterátomo seleccionado de N, O y S; donde opcionalmente un segundo átomo de carbono del mismo, y de forma adicional opcionalmente un tercer átomo de carbono del mismo pueden reemplazarse por N; Q2 es un resto blarilo discontinuo o restringido constituido por un sistema de anillo de carbono saturados o insaturados que es un monociclo de 3- a 7- miembros, o que es un policiclo condensado de 7 a 12 miembros; donde opcionalmente un átomo de carbono de dicho sistema de anillo de carbono puede reemplazarse por un heterátomo seleccionado de N,o y S, donde opcionalmente un segundo átomo de carbono del mismo y de forma adicional opcionalmente un tercer átomo de carbono del mismo pueden reemplazarse por N; Z se selecciona de: (gráfico)
EC2003004710A 2001-01-31 2003-07-31 Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4 ECSP034710A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26549201P 2001-01-31 2001-01-31

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ECSP034710A true ECSP034710A (es) 2003-09-24

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EC2003004709A ECSP034709A (es) 2001-01-31 2003-07-31 Derivados de eteres utiles como agentes inhibidores de las isozimas pde4
EC2003004710A ECSP034710A (es) 2001-01-31 2003-07-31 Derivados biarilicos nicotinamida de utilidad como inhibidores de isozimas pde4

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US (2) US6649633B2 (es)
EP (1) EP1355884A1 (es)
JP (1) JP2004520386A (es)
KR (1) KR20030074761A (es)
CN (1) CN1518542A (es)
BG (1) BG108038A (es)
BR (1) BR0116852A (es)
CA (1) CA2436535A1 (es)
CR (1) CR7025A (es)
CZ (1) CZ20031895A3 (es)
EA (1) EA200300621A1 (es)
EC (2) ECSP034709A (es)
EE (1) EE200300360A (es)
HU (1) HUP0400637A2 (es)
IL (1) IL156413A0 (es)
IS (1) IS6846A (es)
MA (1) MA26983A1 (es)
MX (1) MXPA03006887A (es)
NO (1) NO20033397L (es)
NZ (1) NZ526453A (es)
OA (1) OA12540A (es)
PL (1) PL364135A1 (es)
SK (1) SK8792003A3 (es)
WO (1) WO2002060875A1 (es)
ZA (1) ZA200304894B (es)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030055026A1 (en) 2001-04-17 2003-03-20 Dey L.P. Formoterol/steroid bronchodilating compositions and methods of use thereof
JP4510384B2 (ja) * 2001-05-23 2010-07-21 田辺三菱製薬株式会社 骨折治癒促進用組成物
EP1389467B1 (en) * 2001-05-23 2013-07-03 Mitsubishi Tanabe Pharma Corporation Therapeutic composition for the regenerative treatment of cartilage diseases
WO2003071870A1 (en) * 2002-02-26 2003-09-04 Schlesinger Stephen L Use of leukotriene receptor antagonist for treatment of scarring
EP1424101A3 (en) * 2002-11-29 2004-08-18 NOZAKI, Masako Use of a leukotriene C4 and D4 receptor antagonist for the preparation of a medicament for treating or preventing brain inflammation and sepsis
ATE457716T1 (de) 2002-12-30 2010-03-15 Angiotech Int Ag Wirkstofffreisetzung von schnell gelierender polymerzusammensetzung
US7153824B2 (en) * 2003-04-01 2006-12-26 Applied Research Systems Ars Holding N.V. Inhibitors of phosphodiesterases in infertility
GB0309781D0 (en) * 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
TWI359675B (en) 2003-07-10 2012-03-11 Dey L P Bronchodilating β-agonist compositions
GB0317482D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
GB0317516D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
US20050020587A1 (en) * 2003-07-25 2005-01-27 Pfizer Inc Nicotinamide derivatives useful as PDE4 inhibitors
US7153870B2 (en) 2003-07-25 2006-12-26 Pfizer Inc. Nicotinamide derivatives useful as PDE4 inhibitors
GB0317484D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
GB0317498D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Compounds
US7132435B2 (en) * 2003-07-25 2006-11-07 Pfizer Inc. Compounds
US7534894B2 (en) * 2003-09-25 2009-05-19 Wyeth Biphenyloxy-acids
US20050154006A1 (en) * 2004-01-09 2005-07-14 Boehringer Ingelheim International Gmbh Pharmaceutical compositions based on a scopineester and nicotinamide derivatives
US20090042951A1 (en) * 2004-02-20 2009-02-12 Robert Danziger Blood Pressure Reduction in Salt-Sensitive Hypertension
US20090253908A1 (en) * 2004-03-11 2009-10-08 Glaxo Group Limited Novel m3 muscarinic acetylchoine receptor antagonists
WO2005102388A1 (ja) * 2004-04-26 2005-11-03 Ono Pharmaceutical Co., Ltd. 新規なｂｌｔ２介在性疾患、ｂｌｔ２結合剤および化合物
US7704522B2 (en) * 2004-09-08 2010-04-27 Clyde Morgan Topical medicament
EP2410043A3 (en) 2004-12-29 2013-01-23 Hadasit Medical Research Services And Development Ltd. Stem cells culture systems
US8597947B2 (en) 2004-12-29 2013-12-03 Hadasit Medical Research Services & Development Limited Undifferentiated stem cell culture systems
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
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
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
EP2314289A1 (en) 2005-10-31 2011-04-27 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
AU2006311577B2 (en) 2005-11-09 2013-02-07 Zalicus Inc. Methods, compositions, and kits for the treatment of medical conditions
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
CA2651862A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. 5 ht receptor mediated neurogenesis
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
WO2008030651A1 (en) 2006-09-08 2008-03-13 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
JP2010516734A (ja) 2007-01-24 2010-05-20 グラクソ グループ リミテッド ３，５−ジアミノ−６−（２，３−ジクロロフェニル）−１，２，４−トリアジンまたはｒ（−）−２，４−ジアミノ−５−（２，３−ジクロロフェニル）−６−フルオロメチルピリミジンを含む医薬組成物
WO2008129554A1 (en) 2007-04-18 2008-10-30 Hadasit Medical Research Services & Development Limited Stem cell-derived retinal pigment epithelial cells
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
ES2707598T3 (es) 2009-05-12 2019-04-04 Koninklijke Philips Nv Fosfodiesterasa 4D7 como marcador para cáncer maligno de próstata sensible a hormonas
WO2010131195A1 (en) 2009-05-12 2010-11-18 Koninklijke Philips Electronics N.V. Phosphodiesterase 4d7 as prostate cancer marker
USRE46608E1 (en) 2009-09-01 2017-11-14 Catabasis Pharmaceuticals, Inc. Fatty acid niacin conjugates and their uses
US8304551B2 (en) 2009-09-01 2012-11-06 Catabasis Pharmaceuticals, Inc. Fatty acid niacin conjugates and their uses
WO2011044141A1 (en) * 2009-10-05 2011-04-14 Catabasis Pharmaceuticals, Inc. Fatty acid fibrate derivatives and their uses
WO2013106547A1 (en) 2012-01-10 2013-07-18 President And Fellows Of Harvard College Beta-cell replication promoting compounds and methods of their use
ES2784489T3 (es) 2013-06-27 2020-09-28 Lg Chemical Ltd Derivados de biarilo como agonistas de GPR120
US9630935B2 (en) * 2013-09-17 2017-04-25 Vectus Biosystems Limited Compositions for the treatment of hypertension and/or fibrosis
EP3916085A1 (en) 2014-12-30 2021-12-01 Cell Cure Neurosciences Ltd. Assessing retinal pigment epithelial cell populations
MX2017008737A (es) 2014-12-30 2018-01-25 Cell Cure Neurosciences Ltd Poblaciones de celulas rpe y metodos para generar las mismas.
EP3328995B1 (en) 2015-07-29 2021-03-31 Hadasit Medical Research Services And Development Large scale production of retinal pigment epithelial cells
DK3331994T3 (da) 2015-08-05 2022-11-21 Cell Cure Neurosciences Ltd Fremstilling af retinale pigmentepitelceller
EA201890442A1 (ru) 2015-08-05 2018-07-31 Селл Кьюр Нейросайансес Лтд. Получение фоторецепторов для лечения заболеваний сетчатки
CA3002919A1 (en) 2015-10-26 2017-05-04 Cell Cure Neurosciences Ltd. Preparation of retinal pigment epithelium cells
US9725406B1 (en) 2016-10-13 2017-08-08 Resolvex Pharmaceuticals Inc. Substituted hydroxystilbenes and their therapeutic applications
WO2018146679A2 (en) 2017-02-08 2018-08-16 Hadasit Medical Research Services And Development Ltd. Photoreceptor cells for the treatment of retinal diseases
KR20200031559A (ko) 2017-03-16 2020-03-24 리니지 셀 테라퓨틱스, 인크. 망막 질환 요법의 치료 효과를 측정하는 방법
KR20240161220A (ko) 2017-12-29 2024-11-12 셀 큐어 뉴로사이언시스 리미티드 망막 색소 상피 세포 조성물
KR20250107972A (ko) * 2018-05-04 2025-07-14 레미디 플랜, 인크. 암 줄기 세포를 표적화하는 암 치료
US20210353611A1 (en) 2018-09-20 2021-11-18 Yeda Research And Development Co. Ltd. Methods of treating amyotrophic lateral sclerosis
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections
CN111888349B (zh) * 2020-07-29 2021-10-22 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 印楝素在制备促进缺血超长随意皮瓣存活药物的作用
TWI853255B (zh) 2021-06-09 2024-08-21 美商譜系細胞治療公司 治療視網膜疾病及病況之方法及組成物
IL310156A (en) 2021-07-28 2024-03-01 Lineage Cell Therapeutics Inc Expansion of retinal pigment epithelial cells
EP4514949A1 (en) 2022-04-25 2025-03-05 Hadasit Medical Research Services&Development Ltd. Methods and compositions for treating vision loss

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2140772A5 (en) 1971-06-07 1973-01-19 Aries Robert Phenoxynicotinoylaminophenols - analgesics tranquillisers antipyretics, anti-inflammatories and antirheumatics
US4270946A (en) * 1979-10-01 1981-06-02 Stauffer Chemical Company N-Aryl,2-phenoxy nicotinamide compounds and the herbicidal use thereof
US4692185A (en) * 1986-01-13 1987-09-08 Stauffer Chemical Company N-(ortho-substituted) benzyl, 3-trifluoromethylphenoxy nicotinamides as herbicides
US4861891A (en) * 1988-08-31 1989-08-29 Pfizer Inc. Antidepressant N-substituted nicotinamide compounds
EP0500989B1 (en) 1991-02-27 1998-12-09 Lacer, S.A. N-(alpha-substituted-pyridinyl) carbonyl dipeptide antihypertensive agents
DE4200323A1 (de) 1992-01-09 1993-07-15 Bayer Ag Herbizide und pflanzennematizide mittel auf basis von mercaptonicotinsaeurederivaten
CA2133439C (en) 1992-04-02 2005-07-26 Siegfried Benjamin Christensen, Iv Compounds useful for treating allergic and inflammatory diseases
PT710109E (pt) 1993-06-18 2005-01-31 Smithkline Beecham Corp Metodo para identificar um inibidor de pde iv
JP3406689B2 (ja) 1994-03-15 2003-05-12 株式会社大塚製薬工場 ナフチリジン及びピリドピラジン誘導体
US5618027A (en) * 1994-07-20 1997-04-08 Nevrekar; Venkatesh R. Gate valve
JPH10511398A (ja) 1994-12-23 1998-11-04 スミスクライン・ビーチャム・コーポレイション ４，４−（二置換）シクロヘキサン−１−カルボキシレート単量体および関連する化合物
TW429148B (en) * 1995-10-27 2001-04-11 Pfizer Pharmaceutical agents for the treatment of acute and chronic inflammatory diseases
GB9622386D0 (en) 1996-10-28 1997-01-08 Sandoz Ltd Organic compounds
US5922557A (en) 1997-01-09 1999-07-13 Merck & Co., Inc. System for stably expressing a high-affinity camp phosphodiesterase and use thereof
TR199902432T2 (xx) 1997-04-04 2000-01-21 Prizer Products Inc. Nikotinamid t�revleri.
GB9715584D0 (en) * 1997-07-23 1997-10-01 Eisai Co Ltd Compounds
UA67753C2 (uk) 1997-10-10 2004-07-15 Смітклайн Бічам Корпорейшн Спосіб отримання заміщених 4-феніл-4-ціанциклогексанових кислот
AR015966A1 (es) 1997-10-17 2001-05-30 Smithkline Beecham Corp Uso de un compuesto inhibidor de pde4 para la preparacion de un medicamento util para el tratamiento de prurito
DZ2629A1 (fr) 1997-10-23 2003-03-08 Smithkline Beecham Corp Formes polymorphes nouvelles de cipamfylline procédé pour leur préparation et compositions les contenant.
PL357555A1 (en) * 2000-01-31 2004-07-26 Pfizer Products Inc. Pyrimidine carboxamides useful as inhibitors of pde4 isozymes
BR0107964A (pt) * 2000-01-31 2002-10-29 Pfizer Prod Inc Derivados de nicotinamida benzofundida com heterociclica úteis como inibidores seletivos de isozimas pde4

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