AR060268A1 - Tiazolil - dihidro - indazoles - Google Patents
Tiazolil - dihidro - indazolesInfo
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- AR060268A1 AR060268A1 ARP070101386A ARP070101386A AR060268A1 AR 060268 A1 AR060268 A1 AR 060268A1 AR P070101386 A ARP070101386 A AR P070101386A AR P070101386 A ARP070101386 A AR P070101386A AR 060268 A1 AR060268 A1 AR 060268A1
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- Prior art keywords
- alkyl
- cycloalkyl
- aryl
- optionally substituted
- group
- Prior art date
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/04—Drugs for disorders of the respiratory system for throat disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/10—Anti-acne agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A61P27/16—Otologicals
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Otolaryngology (AREA)
- Physical Education & Sports Medicine (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Sus tautomeros, racematos, enantiomeros, diastereomeros y sus mezclas, así como eventualmente sus sales por adicion de ácidos, solvatos e hidratos farmacologicamente inocuos, así como procedimientos para la preparacion de estos tiazolil-dihidro- indazoles y su uso como medicamentos. Reivindicacion 1: Los compuestos de la formula general (1), en los que Ra hidrogeno o un radical eventualmente sustituido seleccionado del grupo compuesto por alquilo C1-8, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, cicloalquenilo C3-8, haloalquilo C1-6, arilo C6-14, aril C6-14-aIquilo C1-5, heteroarilo C5-10, cicloalquil C5-10-alquilo C1-4, cicloalquenil C3-8-alquilo C1-4, heteroaril C5-10-alquilo C1-4, espiro, heterocicloalquilo C3-8 y heterocicloalquil C3-8-alquilo C1-4, Rb hidrogeno o un radical eventualmente sustituido seleccionado del grupo compuesto por aIquilo C1-8, cicloalquilo C3-8, alquenilo C2-8, cicloalquenilo C3-8, haloalquilo C1-6, arilo C6-14, aril C6-14-alquilo C1- 5, heteroarilo C5-10, cicloalquil C3-8-alquilo C1-4, cicloalquenil C3-8-alquilo C1-4, heteroaril C5-10-alquilo C1-4, espiro, heterocicloalquilo C3-8, CONH2, aril C6-14-NH- y heterocicloalquil C3-8-NH-; R1 hidrogeno o un radical eventualmente sustituido seleccionado del grupo compuesto por alquilo C1-8, cicloalquilo C3-8, alquenilo C2-8, alquinilo C2-8 y aril C6-14-alquilo C1-5; R2 hidrogeno o un radical eventualmente sustituido seleccionado del grupo compuesto por alquilo C1-8, cicloalquilo C3-8, alquenilo C2-8, cicloalquenilo C3-8, haloalquilo C1-6, arilo C6-14, aril C6-14-alquilo C1-5, heteroarilo C5-10, cicloalquil C3-8-alquilo C1-4, cicloalquenil C3-8-alquilo C1-4, heteroaril C5-10-alquilo C1-6, espiro C9-13, heterocicloalquilo C3-8, heterocicloalquil C3-8-alquilo C1-6 y aril C6-14-alquilo C1-6 o R1 y R2 forman juntos un anillo eventualmente sustituido de cinco, seis o siete miembros compuesto por átomos de carbono y eventualmente 1 a 2 heteroátomos, seleccionados del grupo compuesto por oxigeno, azufre y nitrogeno o R1 y R2 forman juntos un anillo espirocíclico de 9 a 13 miembros eventualmente sustituido, o R2 un radical seleccionado del grupo compuesto por las formulas generales (A1) a (A18), en donde significan X e Y pueden estar unidos con el mismo o con distintos átomos de G, y X un enlace o un radical eventualmente sustituido seleccionado del grupo compuesto por alquileno C1-7, alquenileno C3-7 y alquinileno C3-7, o X forma junto con R1, R3 o R4 un puente de alquileno C1-7, Y un enlace o eventualmente sustituido alquileno C1-4, Q un radical eventualmente sustituido seleccionado del grupo compuesto por alquileno C1-7, alquenileno C3-7 y alquinileno C3-7, o Q forma junto con R1, R3 o R4 un puente de alquileno C1-7, R3, R4, R5 iguales o diferentes, hidrogeno o un radical eventualmente sustituido seleccionado del grupo compuesto por alquilo C1-8, cicloalquilo C3-8, haloalquilo C2-6, alquil C1-4-cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-4, NR7R8, NR7R8-alquilo C1-4-, alcoxi C1-4, alcoxi C1-4-alquilo C1-4, arilo C6-14 y heteroarilo C5-10, o dos de los sustituyentes R3, R4, R5 forman juntos un anillo eventualmente sustituido de cinco, seis o siete miembros, compuesto por átomos de carbono y eventualmente 1-2 heteroátomos, seleccionados del grupo compuesto por oxigeno, azufre y nitrogeno; G un sistema de anillos saturado, parcialmente saturado o insaturado de 3-10 átomos de C, en donde eventualmente hasta 6 átomos de C están reemplazados por heteroátomos seleccionados del grupo compuesto por nitrogeno, oxígeno y azufre; R6 igual o diferente, hidrogeno o un radical eventualmente sustituido, seleccionado del grupo compuesto por =O, alquilo C1-8, cicloalquilo C3-8, haloalquilo C2-8, arilo C6-14, heteroarilo C5-10, heterocicloalquilo C3-8, o un radical seleccionado del grupo compuesto por NR7R8, OR7, -CO-alquil C1-3-NR7R8, -O-alquil C1-3-NR7R8, CONR7R8, NR7COR8, -CO-alquil C1-3-NR7(CO)OR8, - O(CO)NR7R8, NR7(CO)NR8R9, NR7(CO)OR8, (CO)OR7, -O(CO)R7, COR7, (SO)R7, (SO2)R7, (SO2)NR7R8, NR7(SO2)R8, NR7(SO2)NR8R9, CN y halogeno; n 1, 2 o 3; R7, R8, R9 iguales o diferentes, hidrogeno o un radical eventualmente sustituido seleccionado del grupo compuesto por alquilo C1-8, cicloalquilo C3-8, haloalquilo C1-6, alquil C1-4-cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-3, arilo C6-14, alquil C1-4-arilo C6-14, aril C6-14-alquilo C1-4, heterocicloalquilo C3-8, alquil C1-5-heterocicloalquilo C3- 8, heterocicloalquil C3-8-alquilo C1-4, alquil C1-4(CO)- y alquil C1-4-O(CO)-; o dos de los sustituyentes R7, R8, R9 forman juntos un anillo eventualmente sustituido de cinco seis o siete miembros, compuesto por átomos de carbono y eventualmente 1-2 heteroátomos, seleccionados del grupo compuesto por oxigeno, azufre y nitrogeno; eventualmente en forma de sus tautomeros, sus racematos, sus enantiomeros, sus diastereoisomeros y sus mezclas, así como eventualmente sus sales por adicion de ácidos, solvatos e hidratos farmacologicamente inocuos, con la condicion de que se excluyan los siguientes compuestos: a) (1-fenil-4,5-dihidro-1H-pirazolo[3',4':3,4]benzo[1,2-d]tiazol-7-iI)-hidrazincarboxamida, b) 1-(2-dimetilamino-etil)-3-(1-fenil-4,5- dihidro-1H-pirazolo[3',4':3,4]benzo[1,2-d]tiazol-7-il)-urea, c) 1-(2-morfolin-4-il-etil)-3-(1-fenil-4,5-dihidro-1H-pirazolo[3',4':3,4]benzo[1,2-d]tiazol-7-il)-urea, d) 1-etil-3-(1-fenil-4,5-dihidro-1H-pirazolo[3',4':3,4]benzo[1,2-d]tiazol-7-iI)- urea, e) 1-metil-3-(1-fenil-4,5-dihidro-1H-pirazolo[3',4':3,4]benzo[1,2-d]tiazol-7-il)-urea, f) 1,1-dimetil-3-(1-fenil-4,5-dihidro-1H-pirazolo[3',4':3,4]benzo[1,2-d]tiazol-7-il)-urea, g) (1-fenil-4,5-dihidro-1H-pirazolo[3',4':3,4]benzo[1,2-d]tiazol- 7-iI)-amida del ácido morfolin-4-carboxílico, h) [1-(2-cloro-fenil)-3-isopropil-4,5-dihidro-1H-pirazolo[3',4:3,4]benzo[1,2-d]tiazol-7-il]-urea, i) N-(5,8-dihidro-4H-[1,3tiazolo[4,5-g]indol-2-il)-N'-etilurea, j) N-etil-N'-(8-metil-5,8-dihidro-4H- [1,3]tiazolo[4,5-g]indol-2-il)urea, k) éster terc butílico del ácido {4-[3-(1-fenil-4,5-dihidro-1H-pirazolo(3'4':3,4]benzo[1,2-d]tiazol-7-il)-ureido]-but-2-inil}-carbámico, l) 1-(4-amino-but-2-inil)-3-(1-fenil-4,5-dihidro-1H- pirazolo[3',4':3,4]benzo[1,2-d]tiazol-7-il)-urea, m) (1-fenil-4,5-dihidro-1H-pirazolo[3',4':3,4]benzo[1,2-d]tiazol-7-il)-urea.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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EP06112299 | 2006-04-06 |
Publications (1)
Publication Number | Publication Date |
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AR060268A1 true AR060268A1 (es) | 2008-06-04 |
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ID=36778288
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP070101386A AR060268A1 (es) | 2006-04-06 | 2007-04-03 | Tiazolil - dihidro - indazoles |
Country Status (15)
Country | Link |
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US (1) | US20070259855A1 (es) |
EP (1) | EP2018386A1 (es) |
JP (1) | JP2009532414A (es) |
KR (1) | KR20090006181A (es) |
CN (1) | CN101460507A (es) |
AR (1) | AR060268A1 (es) |
AU (1) | AU2007236044A1 (es) |
BR (1) | BRPI0710847A2 (es) |
CA (1) | CA2647434A1 (es) |
IL (1) | IL194492A0 (es) |
MX (1) | MX2008012332A (es) |
RU (1) | RU2008143552A (es) |
TW (1) | TW200806676A (es) |
WO (1) | WO2007115930A1 (es) |
ZA (1) | ZA200807580B (es) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
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MX2007004051A (es) * | 2004-10-07 | 2007-05-24 | Boehringer Ingelheim Int | Pi3-quinasas. |
US20070238746A1 (en) * | 2006-04-06 | 2007-10-11 | Trixi Brandl | Thiazolyl-dihydro-chinazoline |
US7691868B2 (en) | 2006-04-06 | 2010-04-06 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-quinazoline |
WO2008001883A1 (fr) * | 2006-06-29 | 2008-01-03 | Nissan Chemical Industries, Ltd. | DÉRIVÉ D'ACIDE α-AMINÉ ET PRODUIT PHARMACEUTIQUE QUI LE COMPREND EN TANT QUE MATIÈRE ACTIVE |
US20090325956A1 (en) * | 2006-10-13 | 2009-12-31 | Takahiko Taniguchi | Aromatic amine derivative and use thereof |
UY31700A (es) * | 2008-03-13 | 2009-11-10 | Boehringer Ingelheim Int | Tiazolil-dihidro-indazoles |
AU2009286604B2 (en) * | 2008-08-29 | 2015-05-28 | Onxeo Dk, Branch Of Onxeo S.A., France | Novel urea and thiourea derivatives |
EP2327704A4 (en) * | 2008-08-29 | 2012-05-09 | Shionogi & Co | RING-CONDENSED AZOL DERIVATIVE WITH PI3K-INHIBITING EFFECT |
UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
US8293753B2 (en) * | 2009-07-02 | 2012-10-23 | Novartis Ag | Substituted 2-carboxamide cycloamino ureas |
US8980878B2 (en) * | 2012-04-17 | 2015-03-17 | Gilead Sciences, Inc. | Compounds and methods for antiviral treatment |
US11633399B2 (en) | 2018-12-25 | 2023-04-25 | Sol-Gel Technologies Ltd. | Treatment of skin disorders with compositions comprising an EGFR inhibitor |
Family Cites Families (11)
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US5547975A (en) * | 1994-09-20 | 1996-08-20 | Talley; John J. | Benzopyranopyrazolyl derivatives for the treatment of inflammation |
KR20020084116A (ko) * | 2000-02-07 | 2002-11-04 | 애보트 게엠베하 운트 콤파니 카게 | 2-벤조티아졸릴 우레아 유도체 및 이의 단백질 키나제억제제로서의 용도 |
DE10344223A1 (de) * | 2003-09-24 | 2005-04-21 | Merck Patent Gmbh | 1,3-Benzoxazolylderivate als Kinase-Inhibitoren |
MX2007004051A (es) * | 2004-10-07 | 2007-05-24 | Boehringer Ingelheim Int | Pi3-quinasas. |
UY29149A1 (es) * | 2004-10-07 | 2006-05-31 | Boehringer Ingelheim Int | Tiazolil-dihidro-indazoles |
EP2007774B1 (de) * | 2006-04-06 | 2012-07-25 | Boehringer Ingelheim International GmbH | Thiazolyldihydroindazol-derivate als proteinkinase- inhibitoren |
US20070238746A1 (en) * | 2006-04-06 | 2007-10-11 | Trixi Brandl | Thiazolyl-dihydro-chinazoline |
US7691868B2 (en) * | 2006-04-06 | 2010-04-06 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-quinazoline |
JP2009532425A (ja) * | 2006-04-06 | 2009-09-10 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | チアゾリルジヒドロインダゾール |
US7517995B2 (en) * | 2006-04-06 | 2009-04-14 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-cyclopentapyrazole |
US20070238718A1 (en) * | 2006-04-06 | 2007-10-11 | Matthias Grauert | Thiazolyl-dihydro-indazole |
-
2007
- 2007-03-23 US US11/690,360 patent/US20070259855A1/en not_active Abandoned
- 2007-03-27 AU AU2007236044A patent/AU2007236044A1/en not_active Abandoned
- 2007-03-27 WO PCT/EP2007/052913 patent/WO2007115930A1/de active Application Filing
- 2007-03-27 CN CNA2007800208756A patent/CN101460507A/zh active Pending
- 2007-03-27 BR BRPI0710847-8A patent/BRPI0710847A2/pt not_active IP Right Cessation
- 2007-03-27 MX MX2008012332A patent/MX2008012332A/es not_active Application Discontinuation
- 2007-03-27 JP JP2009503533A patent/JP2009532414A/ja not_active Withdrawn
- 2007-03-27 CA CA002647434A patent/CA2647434A1/en not_active Abandoned
- 2007-03-27 RU RU2008143552/04A patent/RU2008143552A/ru not_active Application Discontinuation
- 2007-03-27 KR KR1020087027276A patent/KR20090006181A/ko not_active Application Discontinuation
- 2007-03-27 EP EP07727386A patent/EP2018386A1/de not_active Withdrawn
- 2007-04-03 AR ARP070101386A patent/AR060268A1/es not_active Application Discontinuation
- 2007-04-04 TW TW096111942A patent/TW200806676A/zh unknown
-
2008
- 2008-09-03 ZA ZA200807580A patent/ZA200807580B/xx unknown
- 2008-10-02 IL IL194492A patent/IL194492A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
TW200806676A (en) | 2008-02-01 |
AU2007236044A1 (en) | 2007-10-18 |
JP2009532414A (ja) | 2009-09-10 |
BRPI0710847A2 (pt) | 2011-08-23 |
CN101460507A (zh) | 2009-06-17 |
MX2008012332A (es) | 2008-10-09 |
IL194492A0 (en) | 2009-08-03 |
US20070259855A1 (en) | 2007-11-08 |
CA2647434A1 (en) | 2007-10-18 |
EP2018386A1 (de) | 2009-01-28 |
WO2007115930A1 (de) | 2007-10-18 |
RU2008143552A (ru) | 2010-05-20 |
ZA200807580B (en) | 2009-07-29 |
KR20090006181A (ko) | 2009-01-14 |
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