Allergan, Inc.

Allergan Sales, Inc.

Citrix Systems, Inc.

Liming Wang

Ken Chow

Evelyn G Corpuz

Wenkui Ken Fang

Jayasree Vasudevan

Roshantha A Chandraratna

Michael E Garst

Wha-Bin Im

Santosh C Sinha

Alan T Johnson

John E Donello

Daniel W Gil

Wha Bin Im

Xiaoxia Liu

Mohammed I Dibas

Mohammad I Dibas

Dehua Huang

Ling Li

Janet A Takeuchi

Richard L Beard

Smita S Bhat

Kwok Yin Tsang

Thong Huy Vu

Kwok-Yin Tsang

Vidyasagar Pradeep Vuligonda

Mayssa Attar

Yang-Dar Yuan

Brandon D Swift

Tien T Duong

Haiqing Yuan

Rong Yang

Wenkiu K Fang

Roshantha S Chandraratna

Hao Chen

Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.

Alpha adrenergic receptor modulators

The present invention describes novel single drug entities, formed by direct linkage of an antibiotic to a steroidal drug. Upon topical application to the eye, the conjugate would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs. The antibiotic is coupled directly to the steroid drug.

Antibiotic conjugates directly linked with steroid drugs

The present invention describes Cyclosporine A/steroid hybrid analogs. These single drug entities are formed by connecting a steroid with Cyclosporine A. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.

Cyclosporine A steroid conjugates

The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

N&#x2014;(imidazolidin-2-ylidene)quinoline derivatives as modulators of alpha 2 adrenergic receptors

Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.

The present invention relates to novel N-(imidazolidin-2-ylidene) Heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

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The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Azetidine derivatives as sphingosine 1-phosphate (S1P) receptor modulators

The present invention relates to method of treating retinal diseases in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Ester pro-drugs of [3-(1-(1H-imidazol-4-YL)ethyl)-2-methylphenyl] methanol for treating retinal diseases

The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Oxadiazole derivatives as sphingosine 1-phosphate (S1P) receptor modulators

N-(imidazolidin-2-ylidene)quinoline derivatives as modulators of alpha 2 adrenergic receptors

The present invention relates to novel phenoxy derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Phenoxy derivatives as sphingosine 1-phosphate (S1P) receptor modulators

The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives as modulators of alpha 2 adrenergic receptors

The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Benzyl azetidine derivatives as sphingosine 1-phosphate (S1P) receptor modulators

The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and Rare defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.

The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

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Irvine, CA, United States of America

Liming Wang