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WO/2015/185649A9 |
The invention relates to novel compounds which are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof. M...
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WO/2016/203112A1 |
The present invention provides novel spiro[cyclobutane-1,3'-indolin]-2'- derivatives of formula (I) in which Cy R1, R2, R4, L and 'm' are have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The com...
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WO/2016/201096A1 |
The present invention relates to novel aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of ot7-nAChR, and methods of preparing these compounds and compositions, ...
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WO/2016/193241A1 |
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations w...
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WO/2016/193240A1 |
The invention relates to novel compounds which are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
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WO/2016/162878A1 |
The present invention discloses the process for preparation of 1- ¬Azoniabicyclo[2.2.2]octane,3-[(hydroxydi-2-thienylacety1)o
xy]-1-(3¬iphenoxypropy1)-, bromide, (3R)- and its novel crystalline form-I
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WO/2016/156836A1 |
A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-
1- azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2- dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R) yl meth...
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WO/2016/159268A1 |
Provided is a novel non-deliquescent acid addition salt of 3-aminoquinuclidine, which is a compound industrially useful as an intermediate for a medicine and the like. An acid addition salt of 3-aminoquinuclidine selected from the group ...
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WO/2016/140136A1 |
Provided is a new agent for treating chronic obstructive pulmonary disease. The present invention provides quinuclidine derivatives represented by general formula (1), and a pharmaceutical containing the same. (In the formula, R1 indicat...
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WO/2016/131789A1 |
The present invention relates to benzopyrrolidone derivatives and/or pharmaceutically acceptable salts thereof for the use in the treatment of infectious diseases or cancer, and pharmaceutical compositions containing at least one of said...
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WO/2016/128456A1 |
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations w...
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WO/2016/124125A1 |
The present invention relates to a new crystalline form of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxa
mide hydrochloride and a preparation method for the new crystalline form. The crystalline form has advantageous prope...
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WO/2016/073294A1 |
Disclosed are nonlimiting embodiments comprising novel methods for treating underactive bladder in a subject, including administering an effective amount of a pharmaceutical composition comprising an Ml -selective muscarinic agonist to t...
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WO/2015/062560A9 |
An efficient and industrially applicable process for preparing aclidinium bromide of formula I, comprising the following steps a) preparation of the quinuclidinyl ester by transestenfication of methyl di(2-thienly)giycolate with R-(-)-3-...
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WO/2016/051187A1 |
There are provided compounds of formula I, wherein R1A to R1E, R2 to R4, R5a, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: th...
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WO/2016/046390A1 |
The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respirato...
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WO/2016/039048A1 |
The present invention provides a compound which is represented by formula (I-1) (wherein R4 represents a hydrogen atom, a C1-6 alkyl group or the like; Ar1 represents a C6-10 aryl group, a 3-6 membered heterocyclyl group or the like; A r...
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WO/2016/031987A1 |
A compound represented by any of formulas (Ia)-(Ic) or formula (II), or a pharmaceutically acceptable salt thereof. (In the formulas, R1, R2, R3, R4a, R4c, R5, R15, ring A, X1, and X2 are as defined in the specification.)
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WO/2016/023787A1 |
The present invention relates to a process for the preparation of a compound of formula (I) wherein A1 and A2 are C-H, or one of A1 and A2 is C-H and the other is N; R1 is C1-C4alkyl, C1-C4haloalkyl or C3-C6cycloalkyl; each R2 is indepen...
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WO/2016/010538A1 |
Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the com...
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WO/2016/007630A1 |
Provided are substituted quinuclidine compounds, pharmaceutical compositions comprising such compounds, and methods of modulating α7 nicotinic acetylcholine receptors and treating neurological disorders using such compounds.
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WO/2015/185128A1 |
The invention relates to novel 3,5-dichloro,4-(3,4-(cyclo-) alkoxyphenyl)-2-carbonyloxy)ethyl)pyridine compounds which are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of prepar...
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WO/2015/185130A1 |
The invention relates to novel 3,5-dichloro,4-(3,4-(cyclo-) alkoxyphenyl)--2-carbonyloxy)ethyl)pyridine compounds which are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing ...
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WO/2015/185650A1 |
The invention relates to novel compounds which are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof. (...
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WO/2015/185780A1 |
The invention relates to symmetrical polar compounds of bispyridinium, bisquinuclidinium and bisquinolinium with a linker derived from 1,2-bis(p-tolyloxy)ethane, which are inhibitors of choline kinase. The invention also relates to the s...
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WO/2015/162452A1 |
The present invention relates to compounds of formula 1, or isotopic forms, stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, S-oxides or N-oxides thereof, and processes for their preparation. T...
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WO/2015/163427A1 |
The present invention provides: a novel disubstituted 1, 2, 4-triazine compound that has an aldosterone synthase inhibitory activity and is useful in the prevention and/or treatment of various diseases or symptoms involving aldosterone, ...
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WO/2015/144101A1 |
New forms of aclidinium chloride of formula I. The process for preparing the crystalline aclidinium chloride consists in reaction of the quinuclidinyl ester of formula V with 3-phenoxypropyl chloride in acetonitrile.
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WO/2015/130110A1 |
Provided are: a solid dispersion composition containing solifenacin or a pharmaceutically acceptable salt thereof, wherein the active ingredient thereof comprises only an amorphous form of solifenacin or a pharmaceutically acceptable sal...
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WO/2015/129630A1 |
[Problem] To provide a novel method for producing (S)-2-(5-chloro-2-nitrophenyl)-4-cyclopropyl-1,1,1-trifluoro
but-3-yne-2-ol. [Solution] An alkynyl ketone represented by belowmentioned formula (1) is reacted with (trifluoromethyl) trime...
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WO/2015/087291A1 |
A novel method for obtaining 3-carboxy-4-(R)-phenylpyrrolidine-2-one from 3-carboxy-4- (R,S)-phenylpyrrolidine-2-one in which the racemic mixture is separated using 3-(S)- benzoyloxyquinuclidine.
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WO/2015/071824A1 |
The present invention relates to process for the preparation of aclidiunium or intermediates thereof. More particularly, it relates to the preparation of aclidinium bromide.
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WO/2015/057629A1 |
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, ...
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WO/2015/057626A1 |
The present invention comprises compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease...
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WO/2015/019325A1 |
The present invention relates to benzimidazolyl-methyl urea derivatives of formula (I), wherein n, D, E, R1, R2, R3, R4, R6, R7, R8 and R9 are as defined in the description, their preparation and their use as pharmaceutically active comp...
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WO/2015/007073A1 |
Disclosed in the present invention are quinine compounds, and pharmaceutically acceptable salts, solvates, precursors and optical isomers thereof. Also disclosed in the present invention are that the above compounds have a selective bloc...
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WO/2014/184328A1 |
The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or...
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WO/2014/151291A1 |
The invention relates to a method of preparing inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy,...
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WO/2014/152215A1 |
The present invention relates to novel salt forms of (S)-Quinuclidin-3-yl (2-(2-(4-fluorophenyl)thiazol-4-yl)propan-2-yl)carbamate useful as an inhibitor of glucosylceramide synthase (GCS) and for the treatment metabolic diseases, such a...
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WO/2014/140091A1 |
This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same a...
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WO/2014/140318A1 |
The present invention relates to a novel process for the preparation of esters like Aclidinium, Atropin, Glycopyrroniunn, Tiotropium, Trospium and their respective precursors and derivatives, based on direct acyl transfer reactions.
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WO/2014/110491A1 |
Prodrugs of treprostinil are provided which can be used in the treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable...
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WO/2014/095920A1 |
The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respirato...
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WO/2014/086924A1 |
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations w...
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WO/2014/086855A1 |
The invention relates to novel compounds which are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use the...
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WO/2014/086927A1 |
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations w...
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WO/2014/086849A1 |
The invention relates to novel compounds which are both inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use the...
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WO/2014/086852A1 |
The invention relates to novel compounds which are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
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WO/2014/078454A1 |
Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of...
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WO/2014/077401A1 |
Provided is a compound that has cholinergic muscarinic M1 receptor positive allosteric modulator activity and that is useful in the prevention and treatment of conditions such as Alzheimer's disease, schizophrenia, pain, and sleep disord...
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