ZA200804497B - (Indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines for treating rho kinase-mediated diseases and conditions - Google Patents
(Indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines for treating rho kinase-mediated diseases and conditionsInfo
- Publication number
- ZA200804497B ZA200804497B ZA200804497A ZA200804497A ZA200804497B ZA 200804497 B ZA200804497 B ZA 200804497B ZA 200804497 A ZA200804497 A ZA 200804497A ZA 200804497 A ZA200804497 A ZA 200804497A ZA 200804497 B ZA200804497 B ZA 200804497B
- Authority
- ZA
- South Africa
- Prior art keywords
- pyrazines
- indazol
- indol
- dihydro
- conditions
- Prior art date
Links
- UMRCHZNOQHLOGW-UHFFFAOYSA-N 1,3-dihydroindol-2-one;pyrazine Chemical class C1=CN=CC=N1.C1=CC=C2NC(=O)CC2=C1 UMRCHZNOQHLOGW-UHFFFAOYSA-N 0.000 title 1
- GTHRBGRAVFPOMM-UHFFFAOYSA-N 5-pyrazin-2-yl-1h-indazole Chemical class C1=C2C=NNC2=CC=C1C1=CN=CC=N1 GTHRBGRAVFPOMM-UHFFFAOYSA-N 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 230000001404 mediated effect Effects 0.000 title 1
- 102000000568 rho-Associated Kinases Human genes 0.000 title 1
- 108010041788 rho-Associated Kinases Proteins 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US75313605P | 2005-12-22 | 2005-12-22 |
Publications (1)
Publication Number | Publication Date |
---|---|
ZA200804497B true ZA200804497B (en) | 2009-10-28 |
Family
ID=37963712
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ZA200804497A ZA200804497B (en) | 2005-12-22 | 2006-12-19 | (Indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)-pyrazines for treating rho kinase-mediated diseases and conditions |
Country Status (14)
Country | Link |
---|---|
US (1) | US7655662B2 (xx) |
EP (1) | EP1962853A1 (xx) |
JP (1) | JP2009521494A (xx) |
KR (1) | KR20080077652A (xx) |
CN (1) | CN101340912A (xx) |
AR (1) | AR058618A1 (xx) |
BR (1) | BRPI0620463A2 (xx) |
CA (1) | CA2629342A1 (xx) |
MX (1) | MX2008008328A (xx) |
RU (1) | RU2008130111A (xx) |
TW (1) | TW200733964A (xx) |
UY (1) | UY30058A1 (xx) |
WO (1) | WO2007076360A1 (xx) |
ZA (1) | ZA200804497B (xx) |
Families Citing this family (52)
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ES2580108T3 (es) | 2005-07-11 | 2016-08-19 | Aerie Pharmaceuticals, Inc | Compuestos de isoquinolina |
WO2007008942A2 (en) * | 2005-07-11 | 2007-01-18 | Aerie Pharmaceuticals, Inc. | Phenylamino-acetic acid [1-(pyridin-4-yl)-methylidene]-hydrazide derivatives and related compounds as modulators of g protein-coupled receptor kinases for the treatment of eye diseases |
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KR101129868B1 (ko) * | 2006-10-04 | 2012-04-12 | 화이자 프로덕츠 인코포레이티드 | 칼슘 수용체 길항제로서의 피리도[4,3-d]피리미딘-4(3H)-온 유도체 |
US20100022517A1 (en) * | 2006-12-18 | 2010-01-28 | Richards Lori A | Ophthalmic formulation of rho kinase inhibitor compound |
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US8455514B2 (en) * | 2008-01-17 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-and 7-amino isoquinoline compounds and methods for making and using the same |
EP2299820A4 (en) * | 2008-06-18 | 2012-11-14 | Inspire Pharmaceuticals Inc | OPHTHALMOLOGICAL FORMULATION OF RHO KINASE INHIBITOR COMPOUND |
US8450344B2 (en) | 2008-07-25 | 2013-05-28 | Aerie Pharmaceuticals, Inc. | Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds |
RU2011123647A (ru) | 2008-11-10 | 2012-12-20 | Вертекс Фармасьютикалз Инкорпорейтед | Соединения, полезные в качестве ингибиторов atr киназы |
SG172248A1 (en) | 2008-12-19 | 2011-07-28 | Vertex Pharma | Pyrazine derivatives useful as inhibitors of atr kinase |
ES2834451T3 (es) | 2009-05-01 | 2021-06-17 | Aerie Pharmaceuticals Inc | Inhibidores de mecanismo doble para el tratamiento de enfermedades |
PT2516433E (pt) | 2009-12-21 | 2014-09-03 | Array Biopharma Inc | Compostos de n-(1h-indazol-4-il)imidazo[1,2- a]piridina-3 carboxamida substituída como inibidores de cfms |
EP2569287B1 (en) | 2010-05-12 | 2014-07-09 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
WO2011143419A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Pyrazines useful as inhibitors of atr kinase |
US9062008B2 (en) | 2010-05-12 | 2015-06-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP2569284B1 (en) | 2010-05-12 | 2015-07-08 | Vertex Pharmaceuticals Incorporated | 2-aminopyridine derivatives useful as inhibitors of atr kinase |
WO2011143399A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
CA2798763A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
NZ605627A (en) | 2010-06-23 | 2015-06-26 | Vertex Pharma | Pyrrolo-pyrazine derivatives useful as inhibitors of atr kinase |
WO2012138938A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
EP2723747A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
WO2012178125A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
CN103957917A (zh) | 2011-09-30 | 2014-07-30 | 沃泰克斯药物股份有限公司 | 用atr抑制剂治疗胰腺癌和非小细胞肺癌 |
US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP3878851A1 (en) | 2011-09-30 | 2021-09-15 | Vertex Pharmaceuticals Incorporated | Process for making compounds useful as inhibitors of atr kinase |
US8846686B2 (en) | 2011-09-30 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
WO2013071094A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
US8841337B2 (en) | 2011-11-09 | 2014-09-23 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
EP2776419B1 (en) | 2011-11-09 | 2016-05-11 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
PL2833973T3 (pl) | 2012-04-05 | 2018-02-28 | Vertex Pharmaceuticals Incorporated | Związki użyteczne jako inhibitory kinazy ATR i ich terapie skojarzone |
EP2904406B1 (en) | 2012-10-04 | 2018-03-21 | Vertex Pharmaceuticals Incorporated | Method for measuring atr inhibition mediated increases in dna damage |
WO2014062604A1 (en) | 2012-10-16 | 2014-04-24 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
BR112015012454B1 (pt) | 2012-12-07 | 2022-07-05 | Vertex Pharmaceuticals Incorporated | Compostos inibidores de atr quinase, seu uso e composição farmacêutica compreendendo os mesmos |
CN110396085A (zh) | 2013-03-15 | 2019-11-01 | 爱瑞制药公司 | 联合治疗 |
US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
US9328200B2 (en) * | 2013-07-17 | 2016-05-03 | Ultrasci Discovery Llp | Branched polymeric quaternary ammonium compounds and their uses |
SG11201604519PA (en) | 2013-12-06 | 2016-07-28 | Vertex Pharma | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
EP3152212B9 (en) | 2014-06-05 | 2020-05-27 | Vertex Pharmaceuticals Inc. | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
WO2015195740A1 (en) | 2014-06-17 | 2015-12-23 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of chk1 and atr inhibitors |
US11464774B2 (en) | 2015-09-30 | 2022-10-11 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
AU2015414743B2 (en) | 2015-11-17 | 2019-07-18 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
US9643927B1 (en) | 2015-11-17 | 2017-05-09 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
MX2019002396A (es) | 2016-08-31 | 2019-07-08 | Aerie Pharmaceuticals Inc | Composiciones oftalmicas. |
KR20190135027A (ko) | 2017-03-31 | 2019-12-05 | 에어리 파마슈티컬즈, 인코포레이티드 | 아릴 시클로프로필-아미노-이소퀴놀리닐 아미드 화합물 |
EP3849555A4 (en) | 2018-09-14 | 2022-05-04 | Aerie Pharmaceuticals, Inc. | ARYL CYCLOPROPYL AMINO ISOCHINOLINYL AMIDE COMPOUNDS |
TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
AU2021285850A1 (en) * | 2020-06-03 | 2023-02-09 | Glaukos Corporation | Rho kinase inhibitor releasing implants and related methods of use |
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EP0492903A1 (en) * | 1990-12-21 | 1992-07-01 | MERCK SHARP & DOHME LTD. | Substituted pyrazines, pyrimidines and pyridazines for use in the treatment of glaucoma |
ATE289815T1 (de) * | 1995-12-21 | 2005-03-15 | Alcon Lab Inc | Verwendung von substituierten isochinolinsulfonyl-verbindungen zur herstellung eines medikaments für die behandlung von glaukom und okularer ischämie |
US6586425B2 (en) * | 1996-02-21 | 2003-07-01 | Wisconsin Alumni Research Foundation | Cytoskeletal active agents for glaucoma therapy |
US5798380A (en) * | 1996-02-21 | 1998-08-25 | Wisconsin Alumni Research Foundation | Cytoskeletal active agents for glaucoma therapy |
SI0956865T2 (sl) * | 1996-08-12 | 2011-04-29 | Mitsubishi Pharma Corp | Zdravila, ki obsegajo inhibitor Rho-kinaze |
CA2214841A1 (en) | 1997-10-31 | 1999-04-30 | Lisa Mckerracher | Rho antagonists and their use to block inhibition of neurite outgrowth |
US6673812B1 (en) * | 1998-08-17 | 2004-01-06 | Senju Pharmaceutical Co., Ltd. | Preventives/remedies for glaucoma |
AU4144400A (en) * | 1999-04-27 | 2000-11-10 | Mitsubishi Pharma Corporation | Preventives/remedies for liver diseases |
JP3430254B2 (ja) | 2000-03-13 | 2003-07-28 | 独立行政法人産業技術総合研究所 | β−ジケトナートを有する金属錯体及びその製法、光電変換素子並びに、光化学電池 |
ATE327993T1 (de) | 2000-03-16 | 2006-06-15 | Mitsubishi Pharma Corp | Amid-verbindung und deren verwendung |
WO2001074391A1 (fr) * | 2000-03-31 | 2001-10-11 | Mitsubishi Pharma Corporation | Agent de prevention / remedes contre les maladies renales |
JPWO2002100833A1 (ja) | 2001-06-12 | 2004-09-24 | 住友製薬株式会社 | Rhoキナーゼ阻害剤 |
US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
DE60320933D1 (de) | 2002-01-10 | 2008-06-26 | Bayer Healthcare Ag | Rho-kinase inhibitoren |
JP4423043B2 (ja) | 2002-01-23 | 2010-03-03 | バイエル ファーマセチカル コーポレーション | Rho−キナーゼ阻害剤 |
GB0206860D0 (en) * | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
AU2003249369A1 (en) | 2002-06-21 | 2004-01-06 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
JPWO2004009555A1 (ja) | 2002-07-22 | 2005-11-17 | 旭化成ファーマ株式会社 | 5−置換イソキノリン誘導体 |
JPWO2004024717A1 (ja) | 2002-09-12 | 2006-01-05 | 麒麟麦酒株式会社 | キナーゼ阻害活性を有するイソキノリン誘導体およびそれを含む医薬 |
AU2004224392A1 (en) | 2003-03-24 | 2004-10-07 | Merck & Co., Inc. | Biaryl substituted 6-membered heterocyles as sodium channel blockers |
GB2400101A (en) | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
WO2005003101A2 (en) * | 2003-07-02 | 2005-01-13 | Biofocus Discovery Limited | Pyrazine and pyridine derivatives as rho kinase inhibitors |
US7390907B2 (en) * | 2003-09-30 | 2008-06-24 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
JP2008525453A (ja) | 2004-12-27 | 2008-07-17 | アルコン,インコーポレイティド | 緑内障と、rhoキナーゼを媒介とした他の疾患および症状を治療するためのアミノピラジン・アナログ |
-
2006
- 2006-12-19 CA CA002629342A patent/CA2629342A1/en not_active Abandoned
- 2006-12-19 EP EP06846689A patent/EP1962853A1/en not_active Withdrawn
- 2006-12-19 KR KR1020087015628A patent/KR20080077652A/ko not_active Application Discontinuation
- 2006-12-19 MX MX2008008328A patent/MX2008008328A/es active IP Right Grant
- 2006-12-19 US US11/612,894 patent/US7655662B2/en not_active Expired - Fee Related
- 2006-12-19 JP JP2008547727A patent/JP2009521494A/ja active Pending
- 2006-12-19 BR BRPI0620463-5A patent/BRPI0620463A2/pt not_active IP Right Cessation
- 2006-12-19 RU RU2008130111/04A patent/RU2008130111A/ru unknown
- 2006-12-19 ZA ZA200804497A patent/ZA200804497B/xx unknown
- 2006-12-19 WO PCT/US2006/062307 patent/WO2007076360A1/en active Application Filing
- 2006-12-19 CN CNA2006800482845A patent/CN101340912A/zh active Pending
- 2006-12-21 AR ARP060105725A patent/AR058618A1/es not_active Application Discontinuation
- 2006-12-21 UY UY30058A patent/UY30058A1/es not_active Application Discontinuation
- 2006-12-21 TW TW095148175A patent/TW200733964A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
US20070149548A1 (en) | 2007-06-28 |
EP1962853A1 (en) | 2008-09-03 |
TW200733964A (en) | 2007-09-16 |
US7655662B2 (en) | 2010-02-02 |
UY30058A1 (es) | 2007-03-30 |
MX2008008328A (es) | 2008-09-15 |
BRPI0620463A2 (pt) | 2011-11-16 |
WO2007076360A1 (en) | 2007-07-05 |
JP2009521494A (ja) | 2009-06-04 |
WO2007076360A8 (en) | 2007-12-06 |
RU2008130111A (ru) | 2010-01-27 |
CN101340912A (zh) | 2009-01-07 |
AR058618A1 (es) | 2008-02-13 |
CA2629342A1 (en) | 2007-07-05 |
KR20080077652A (ko) | 2008-08-25 |
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